WorldWideScience

Sample records for tc-99m-labeled antibody an experimental

  1. Imaging endocarditis with Tc-99m-labeled antibody--an experimental study: concise communication

    Energy Technology Data Exchange (ETDEWEB)

    Wong, D.W.; Dhawan, V.K.; Tanaka, T.; Mishkin, F.S.; Reese, I.C.; Thadepalli, H.

    1982-03-01

    The sensitivity and specificity of Tc-99m-labeled antibacterial antibody (Tc-99m Ab) for detecting bacterial endocarditis were evaluated in an experimental model. Rabbit-produced antistaphylococcal antibody was extracted using Rivanol and chemically labeled with Tc-99m. This Tc-99m Ab was injected intravenously in New Zealand rabbits 24 hr after producing Staphylococcus aureus endocarditis of the aortic valve. Imaging and tissue analyses were performed on the following day. All 11 animals developed S. aureus aortic-valve vegetations and showed increased uptake of Tc-99m Ab at the aortic valve, 118 times higher than at the uninfected tricuspid valve. Although high hepatic radioactivity and anatomic uncertainties interfered with in vivo delineation of these lesions, images of the excised hearts showed all affected valves. Two rabbits inoculated with Escherichia coli did not develop endocarditis and had little uptake of Tc-99m Ab, while six rabbits with enterococcal endocarditis had no uptake of the Tc-99m Ab in their vegetations. The findings suggest potential value of Tc-99m Ab on the rapid diagnosis of endocarditis.

  2. Imaging endocarditis with Tc-99m-labeled antibody--an experimental study: concise communication

    International Nuclear Information System (INIS)

    Wong, D.W.; Dhawan, V.K.; Tanaka, T.; Mishkin, F.S.; Reese, I.C.; Thadepalli, H.

    1982-01-01

    The sensitivity and specificity of Tc-99m-labeled antibacterial antibody (Tc-99m Ab) for detecting bacterial endocarditis were evaluated in an experimental model. Rabbit-produced antistaphylococcal antibody was extracted using Rivanol and chemically labeled with Tc-99m. This Tc-99m Ab was injected intravenously in New Zealand rabbits 24 hr after producing Staphylococcus aureus endocarditis of the aortic valve. Imaging and tissue analyses were performed on the following day. All 11 animals developed S. aureus aortic-valve vegetations and showed increased uptake of Tc-99m Ab at the aortic valve, 118 times higher than at the uninfected tricuspid valve. Although high hepatic radioactivity and anatomic uncertainties interfered with in vivo delineation of these lesions, images of the excised hearts showed all affected valves. Two rabbits inoculated with Escherichia coli did not develop endocarditis and had little uptake of Tc-99m Ab, while six rabbits with enterococcal endocarditis had no uptake of the Tc-99m Ab in their vegetations. The findings suggest potential value of Tc-99m Ab on the rapid diagnosis of endocarditis

  3. 99mTC-dextran-antibody conjugates. Labelling procedures

    International Nuclear Information System (INIS)

    Marquez, M.; Westlin, J.E.; Nilsson, S.; Holmberg, A.R.

    1996-01-01

    Dextran forms stable chelates with 99m Tc, a radionuclide with ideal properties for planar scintigraphic and tomographic imaging. This study investigates some of the factors of importance to the formation of 99m Tc-dextran. The complex was used for the technetium labelling of a monoclonal antibody. Two radiolabelling methods were studied: Direct dextran labelling with the reductant dissolved in HCl and labelling via a weak 'transfer' chelator (tartaric acid) with the reductant dissolved in ethanol. Different conditions during the labelling reaction were studied. Finally, dextran was coupled to a monoclonal anticytokeratin antibody and the conjugate was subsequently radiolabelled with 99m Tc. Gel filtration (GFR) and thin layer chromatography (TLC) were compared as methods for estimation of the labelling efficiency. When using 10-500 μM of ligand, 5-100 μM SnC1 2 with 10-500 MBq of technetium at pH7 incubated for 10-15 min, the radiolabelling seemed optimal (70-75% labelling efficiency). It was found that 100 μM tartaric acid used as a weak intermediate chelator with SnCl 2 dissolved in ethanol improved the reproducibility of the labelling. The labelling efficiency was not affected by either the presence of oxygen or the addition of an oxygen scavenger during the labelling incubation. In general, TLC showed higher labelling efficiencies than GFR, indicating inadequate separation of the different moieties. (orig.)

  4. Direct labelling of monomeric antibody fragments Fab' with 99mTc

    International Nuclear Information System (INIS)

    Li Jun; Wang Shizhen; Yang Ziyi

    1994-01-01

    Direct labelling method and conditions of monomeric antibody Fab' with 99m Tc were investigated. Polyclonal antibody IgG was digested with ficin to produce dimeric fragments F(ab') 2 , which was subsequently reduced to monomeric fragments Fab' with 2-mercaptoethylamine. Finally, Fab' was incubated with sodium gluconate (Sn(II)) kit solution and 99m TcO 4 - eluted at room temperature to form 99m Tc-Fab'. The labelling efficiency was 85%-95%. The stability of labelled products was satisfactory and the elimination rate was faster than 99m Tc-IgG

  5. Labeling and stability of radiolabeled antibody fragments by a direct 99mTc-labeling method

    International Nuclear Information System (INIS)

    Pak, K.Y.; Nedelman, M.A.; Tam, S.H.; Wilson, E.; Daddona, P.E.

    1992-01-01

    The in vitro labeling and stability of 99m Tc-labeled antibody Fab' fragments prepared by a direct labeling technique were evaluated. Eight antibody fragments derived from murine IgG1 (N = 5), IgG2a (N = 2) and IgG3 (N = 1) isotypes were labeled with a preformed 99m Tc-D-glucarate complex. No loss of radioactivity incorporation was observed for all the 99m Tc-labeled antibody fragments after 24 h incubation at 37 o C. 99m Tc-labeled antibody fragments (IgG1, N = 2; IgG2a, n = 2; IgG3, N = 1) were stable upon challenge with DTPA, EDTA or acidic pH. Using the affinity chromatography technique, two of the 99m Tc-labeled antibody fragments displayed no loss of immunoreactivity after prolonged incubation in phosphate buffer up to 24 h at 37 o C. Bonding between 99m Tc and antibody fragments was elucidated by challenging with a diamide ditholate (N 2 S 2 ) compound. The Fab' with IgG2a isotype displayed tighter binding to 99m Tc in comparison to Fab' from IgG1 and IgG3 isotype in N 2 S 2 challenge and incubation with human plasma. The in vivo biodistribution of five 99m Tc-labeled fragments were evaluated in normal mice. (Author)

  6. Direct 99mTc labeling of monoclonal antibodies: radiolabeling and in vitro stability

    International Nuclear Information System (INIS)

    Garron, J.Y.; Moinereau, M.; Pasqualini, R.; Saccavini, J.C.

    1991-01-01

    Direct labeling involves 99m Tc binding to different donor groups on the protein, giving multiple binding sites of various affinities resulting in an in vivo instability. The stability has been considerably improved by activating the antibody using a controlled reduction reaction (using 2-aminoethanethiol). This reaction generates sulfhydryl groups, which are known to strongly bind 99m Tc. The direct 99m Tc antibody labeling method was explored using whole antibodies and fragments. Analytical methods were developed for routine evaluation of radiolabeling yield and in vitro stability. Stable direct antibody labeling with 99m Tc requires the generation of sulfhydryl groups, which show high affinity binding sites for 99m Tc. Such groups are obtained with 2-aminoethanethiol (AET), which induces the reduction of the intrachain or interchain disulfide bond, with no structural deterioration or any loss of immunobiological activity of the antibody. The development of fast, reliable analytical methods has made possible the qualitative and quantitative assessment of technetium species generated by the radiolabeling process. Labeling stability is determined by competition of the 99m Tc-antibody bond with three ligands, Chelex 100 (a metal chelate-type resin), free DTPA solution and 1% HSA solution. Very good 99m Tc-antibody stability is obtained with activated IgG (IgGa) and Fab' fragment, which makes these substances possible candidates for immunoscintigraphy use. (author)

  7. Detection of experimental infections with 99mTc-labeled monoclonal antibodies against TNF-α and interleukin-8

    International Nuclear Information System (INIS)

    Welling, Mick; Feitsma, Hans I.J.; Calame, Wim; Pauwels, Ernest K.J.

    1997-01-01

    This study was designed to assess monoclonal antibodies (MAbs) directed against tumor necrosis factor-α (TNF-α) (anti-TNF) or interleukin-8 (anti-IL-8) as radioactive agents for the detection of Staphylococcus aureus- or Klebsiella pneumoniae-infected thighs in mice. At 5 min (acute infection) or 20 h (established) post-infection, 20 μg of the 99m Tc-labeled MAbs were injected. At various time intervals, the accumulation of the radiotracer in the infected thighs was assessed and expressed as a target-to-nontarget (T/NT) ratio. The binding of 99m Tc-labeled MAbs to circulating mononuclear cells and granulocytes was quantitated 20 h after injection. The pharmacokinetics of the MAbs, in relation to the control agents 99m Tc-labeled polyclonal human immunoglobulin (IgG) and a 99m Tc-labeled nonspecific IgG1 MAb, were also studied. In acute infections, 99m Tc-anti-TNF accumulated to a higher extent (p 99m Tc-IgG and was higher at 0.25 h in K. pneumoniae-infected mice (p 99m Tc-IgG. In established S. aureus and K. pneumoniae infections, 99m Tc-anti-IL-8 detected the infection more intensely than 99m Tc-IgG until 1 h after injection. In both S. aureus and K. pneumoniae infections, localization of sites of infection correlates (p 99m Tc-labeled MAbs to granulocytes and mononuclear cells in both acute and established infections. It was concluded that 99m Tc-labeled MAbs, directed against TNF-α and IL-8, accumulate in bacterial infections in mice to a higher extent than does 99m Tc-IgG after infection and is related to the binding of the antibodies to blood leukocytes. With these 99m Tc-labeled MAbs, information might be gained about the development of an infection

  8. 99mTc-HMPAO labeled leucocyte, 99mTc-labeled antigranulocyte antibody and 67Ga scintigraphy in the evaluation of painful hip and knee prosthetic replacements

    International Nuclear Information System (INIS)

    Oliveira, S.; Pereira, L.; Joao, F.; Lima, J.

    2003-01-01

    Full text: Objective: To evaluate the utility of 99mTc-HMPAO labeled leucocyte, 99mTc-labeled anti-granulocyte antibody and 67Ga scintigraphy in patients suspected to have infected hip and knee replacements, from March/1998 to March/ 2002. Methods: Retrospective study of 33 patients (12 male, 21 female) with an average age of 61,1 ± 7,3 years. Nineteen had hip replacements and 14 were submitted to knee replacements. 99mTc-HMPAO labeled leucocyte scintigraphy was performed in 17 patients, 99mTc-labeled anti-granulocyte antibody scintigraphy in 13 patients and 67Ga scintigraphy in 3 patients. Twenty-six patients were also submitted to 3-phase 99mTc-MDP bone scintigraphy. Results were compared to those from studies with infection/inflammation agents. Concordant positive studies were considered to be a positive result for infection. A second study using 67Ga was also performed in 3 patients. Results: Diagnosis was based on surgical findings in 14 patients, pathologic study of biopsy specimen in 1 case and clinical/ imaging follow-up in 18 patients. Infection was detected in 22 cases and absent in 11. The conjoined evaluation of scintigraphic studies considered infection to be present in 20 cases and absent in 13. With infection/inflammation agents, 20 cases were positive (+) and 13 cases were negative (-). Using 99mTc-HMPAO labeled leucocytes, 12 cases were (+) and 5 cases were (-). With 99mTc-labeled anti-granulocyte antibodies, 8 cases were (+) and 5 were (-). With 67Ga, all 3 cases were (-). In patients with (+) studies using infection/ inflammation agents, a false positive case with 99mTc-HMPAO labeled leucocytes was reported. Two false negative cases were detected, both with 99mTc-labeled antigranulocyte antibodies, in patients with (-) studies. Regarding the studies with 99mTc-MDP, 24 were (+) and 2 were (-). Eighteen of these (+) cases were also (+) in studies with infection/inflammation agents, but 6 were (-) with these agents. Negative cases were also (-) in

  9. In vivo instability of reduction-mediated 99mTc-labeled monoclonal antibody

    International Nuclear Information System (INIS)

    Sakahara, Harumi; Saga, Tsuneo; Endo, Keigo

    1993-01-01

    A murine monoclonal antibody that reacts with human osteogenic sarcoma (OST7) was reduced and directly labelled with 99m Tc without any loss of immunoreactivity. No fragmentation of the antibody was detected by high performance liquid chromatography after the labelling. However, SDS-PAGE analysis of the labelled antibody demonstrated the presence of low molecular weight species. Although more than 95% of the radioactivity remained bound at the antibody after incubation with human serum for 24 h, 99m Tc-labelled OST7 was cleared faster from the circulation than 125 I-labelled OST7 or 111 In-labelled OST7 in mice. (author)

  10. sup(99m)Tc-labeled antibacterial antibody scan for the diagnosis of infective endocarditis (in rabbit)

    Energy Technology Data Exchange (ETDEWEB)

    Huang, J T; Tanaka, T; Wong, D W; Mishkin, F; Thadepalli, H [University of Southern California, Los Angeles (USA)

    1978-01-01

    The mortality of infective endocarditis is high and the results of blood cultures and clinical manifestations may be unreliable in its diagnosis. A technique has been developed using the specific antigen-antibody reaction against sup(99m)Tc-labelled antibacterial antibody. The antibody, tagged by an electrolytic method, remained very active and was not denatured since 99% of the sup(99m)Tc-antibody was able to react with antigen. The labelled antibody was injected intravenously into rabbits with experimental aortic endocarditis. The radioactivity of the infected aortic valves was about four times greater than that in the uninfected valves. A scintillation scan was able to detect the infected valves in vivo.

  11. sup(99m)Tc-labeled antibacterial antibody scan for the diagnosis of infective endocarditis (in rabbit)

    International Nuclear Information System (INIS)

    Huang, J.T.; Tanaka, T.; Wong, D.W.; Mishkin, F.; Thadepalli, H.

    1978-01-01

    The mortality of infective endocarditis is high and the results of blood cultures and clinical manifestations may be unreliable in its diagnosis. A technique has been developed using the specific antigen-antibody reaction against sup(99m)Tc-labelled antibacterial antibody. The antibody, tagged by an electrolytic method, remained very active and was not denatured since 99% of the sup(99m)Tc-antibody was able to react with antigen. The labelled antibody was injected intravenously into rabbits with experimental aortic endocarditis. The radioactivity of the infected aortic valves was about four times greater than that in the uninfected valves. A scintillation scan was able to detect the infected valves in vivo. (U.K.)

  12. Kinetic data of in-vivo labeled granulocytes in humans with a murine Tc-99m-labelled monoclonal antibody

    International Nuclear Information System (INIS)

    Becker, W.; Boerner, W.; Borst, U.; Schaefer, R.; Fischbach, W.; Pasurka, B.

    1989-01-01

    Twenty-five patients were examined in vivo with 99m Tc labelled monoclonal antibodies; 15 with suspected infections with an antigranulocyte antibody (BW 250/183), 10 with suspected recurrence of a colorectal carcinoma with an anti CEA antibody (BW 431/26). Both antibodies were IgG1 isotypes. In the patients with suspected infections no change of the peripheral leukocyte count could be observed after the antibody injection (1 mg, n=9; 0.05 mg, n=1; 0.25 mg, n=6). In 2 patients examined with the anti CEA antibody (2 mg), a significant decrease of the peripheral leukocyte count could be observed. The recovery rate of the 99m Tc antibody labelled granulocytes was calculated to be about 10%. The increase of the antibody-antigen binding was calculated to be 0.2%/min. In vivo the organ distribution curves demonstrated an increase of 99m Tc activity over spleen and bone marrow of 1.1%/min, which was interpreted as antigen-antibody reactivity. The organ distribution curves of the anti granulocyte antibody over spleen and bone marrow showed typical binding characteristics to the local granulocyte epitopes. The curves over other organs showed a simple perfusion pattern. The curves of the anti CEA antibody showed a perfusion pattern over all the examined organs. A sham dialysis model in one patient with renal insufficiency undergoing regular dialysis treatment demonstrated the viability of 99m Tc antibody labelled granulocytes in vivo. The kinetic patterns of the 99m Tc antibody in patients with Crohn's disease were interpreted as CEA binding of the antibody in the bowel wall. (orig.)

  13. Studies of monoclonal antibodies IOR-CEA-1 and IOR-EGF/R3 labelled with 99mTc

    International Nuclear Information System (INIS)

    Dias, Carla Roberta de Barros Rodrigues

    2005-01-01

    Nuclear Medicine is a speciality that uses radioisotopes for the diagnosis or treatment of diseases and it is considered one of the best tools among the diagnostic modalities for detection of cancer. 99m Tc is one of the main isotopes for labelling antibodies and in Nuclear Medicine in general, due to its adequate physical properties, availability and low cost. Labelled monoclonal antibodies have shown promising results for diagnosis and therapy of cancer and their use has brought great experimental and clinical advances in the field of oncology. The main clinical applications of immunoscintigraphy with monoclonal antibodies are staging and evaluation of tumoral reappearance. The antibodies employed in this work were: OIR-CEA-1, a murine monoclonal antibody that acts directly against CEA expressed in several neoplasia in particular those from the gastrointestinal tract (colorectal cancer) and IOR-EGF/R3, a murine monoclonal antibody that binds to the external domain of EGF-R and it has been used in the diagnosis of tumors of epithelial origin. The objectives of this work were the development and optimization of the reduction and purification processes, the radiolabelling techniques and quality control procedures (radiochemical, immunoreactivity and cystein challenge) and imaging studies of monoclonal antibodies OIR-CEA-1 and IOR-EGF/R3, using the simple, fast and efficient method of direct labelling of the antibody with 99m Tc. The final results was the definition of the best conditions for the preparation of lyophilized reactive kits of OIR-CEA-1 and IOR- EGF/R3 for an efficient diagnostic application in Nuclear Medicine. The most adequate conditions for the labelling of the antibodies were: 1.0 mg Ab, 29 μL MDP, 3.0 μg Sn 2+ , 1 mL of 99m Tc and 30 min. reaction time. With these conditions the labelling yield was always higher than 95% and the maximum activity of 99m Tc was about 2220 MBq (60 mCi). The evidences of the efficiency and quality of the methods here

  14. 99mTc-Labeling of Monoclonal Antibody to Carcinoembryonic Antigen and Biodistribution

    International Nuclear Information System (INIS)

    Moon, Dae Hyuk; Chung, June Key; Lee, Myu ng Chul; Koh, Chang Soon; Chung, Hong Keun; Park, Jae Gahb

    1992-01-01

    This study was designed to evaluate a direct method of 99m Tc labeling using β-mercaptoethanol as a reducing agent, and to investigate whether 99m Tc labeled specific monoclonal antibody against carcinoembryonic antigen (CEA-92) can be used for the scintigraphic localization of human colon cancer xenograft. Purified CEA-92 IgG was fragmented into F(ab') 2 and then labeled with 99m Tc by transchelation method using glucarate as a chelator. Labeling efficiency, immunological reactivity and in vitro stability of 99m Tc CEA-92 F(ab') 2 were measured and then injected intravenously into nude mice bearing human colon cancer (SNU-C4). Scintigrams were obtained at 24 hour after injection. Then nude mice were sacrificed and the radioactivity was measured. Labeling efficiency of injected 99m Tc CEA-92 F(ab') 2 , immunoreactive fraction and in vitro stability at 24 hour of injected 99m Tc CEA-92 F(ab') 2 was 45.2%, 32.8% and 57.4%, respectively. At 24 hour after injection, %ID/g in kidney (46.77) showed high uptake, but %ID/g in tumor (1.65) was significantly higher than spleen (0.69), muscle (0.16), intestine (0.45), stomach (0.75), heart (0.48) and blood(0.45). There was no significant difference between tumor and liver (1.81). Tumor contrast as quantitated by tumor to blood ratio of 99m Tc CEA-92 F(ab') 2 was increased significantly (p 131 I-CEA-92 F(ab') 2 . The scintigram demonstrated localization of radioactivity over transplanted tumor, but significant background radioactivity was also noted over kidney and abdomen. It is concluded that CEA-92 F(ab') 2 can be labeled with 99m Tc by a direct transchelation method using β-mercaptoethanol as a reducing agent and 99m Tc labeled CEA-92 F(ab') 2 can be used for the scintigraphic localization of human colon cancer xenograft in nude mice model.

  15. Monoclonal anti-elastin antibody labelled with technetium-99m

    International Nuclear Information System (INIS)

    Oliveira, Marcia B.N. de; Silva, Claudia R. da; Araujo, Adriano C. de; Bernardo Filho, Mario; Porto, Luis Cristovao M.S.; Gutfilen, Bianca; Souza, J.E.Q.; Frier, Malcolm

    1999-01-01

    Technetium-99m ( 99m Tc) is widely employed in nuclear medicine due to its desirable physical, chemical and biological properties. Moreover, it is easily available and normally is inexpensive. A reducing agent is necessary to label cells and molecules with 99m Tc and stannous chloride (Sn C L 2 ) is usually employed. Elastin is the functional protein component of the elastic fiber and it is related with some diseases such as arteriosclerosis, pulmonary emphysema and others. The present study refers to the preparation of the 99m Tc labeled monoclonal anti-elastin antibody. The monoclonal antibody was incubated with an excess of 2-iminothiolane. The free thiol groups created, were capable of binding with the reduced technetium. Labeling was an exchange reaction with 99m Tc-glucoheptonate. The labeled preparation was left at 4 deg C for one hour. Then, it was passed through a Sephadex G50 column. Various fractions were collected and counted. A peak corresponding to the radiolabeled antibody was obtained. Stability studies of the labelled anti-elastin were performed at 0,3 6, 24 hours, at both 4 deg C or room temperature. The biodistribution pattern of the 99m Tc-anti-elastin was studied in healthy male Swiss mice. The immunoreactivity was also determined. An useful labeled-anti-elastin was obtained to future immunoscintigraphic investigations. (author)

  16. Detection of thrombi using a Tc-99m labelled antifibrin monoclonal antibody (MoAb)

    International Nuclear Information System (INIS)

    Wasser, M.N.J.M.

    1989-01-01

    This thesis presents an investigation into the possibility of immunoscintigraphic detection of thrombi using an antifibrin monoclonal antibody, and fragments of the latter. The antifibrin antibody and tis fragments were labelled with Ec-99m, which has excellent characteristics for imaging with a gamma camera. The characterization of the antifibrin antibody and its fragments, the assessment of quality of labelling with Tc-99m, and results of experiments in vitro and in animals, which show the potential of immunoscintigraphic detection, are described. (author). 142 refs.; 44 figs.; 5 tabs

  17. Application of 99mTc-labeled chimeric Fab fragments of monoclonal antibody A7 for radioimmunoscintigraphy of pancreatic cancer

    International Nuclear Information System (INIS)

    Matsumura, Hiroomi

    1999-01-01

    Pancreatic cancer is one of the most lethal diseases and its prognosis is still poor. To improve the survival rate, it is essential to develop new technologies for early and definitive diagnosis. In this study, chimeric Fab fragments of monoclonal antibody A7 were successfully radio-labeled with 99m Tc, preventing depression of the antigen-binding activity. 99m Tc-labeled monoclonal antibody A7, 99m Tc-labeled chimeric Fab fragments of monoclonal antibody A7, 99m Tc-labeled normal mouse IgG and 99m Tc-labeled Fab fragments of normal mouse IgG were injected intravenously into nude mice bearing human pancreatic cancer xenografts and the radioactivity was subsequently measured. The tumor accumulation was significantly higher with labeled monoclonal antibody A7 than with normal mouse IgG, and higher with chimeric Fab fragments of monoclonal antibody A7 than with Fab fragments of normal mouse IgG. The tumor/blood ratio of radioactivity increased rapidly over time with chimeric Fab fragments of monoclonal antibody A7. These results suggest that chimeric Fab fragments of monoclonal antibody A7 may be useful for diagnosing pancreatic cancer by means of radioimmunoscintigraphy. (author)

  18. Targeting osteomyelitis with complete [99mTc]besilesomab and fragmented [99mTc]sulesomab antibodies: kinetic evaluations

    International Nuclear Information System (INIS)

    GRATZ, Stefan; KEMKE, Bendix; KEIZE, Patrik; KAMPEN, Wim U.; LUSTER, Markus; HÖFFKEN, Helmut

    2016-01-01

    The aim of this retrospective study was to compare the targeting of “pure” osteomyelitis (i.e., without surrounding soft tissue infection) by directly 99mTc-labelled complete immunoglobulin G (IgG) monoclonal antibody (MAb) ([99mTc]besilesomab) and by directly 99mTc-labelled fragment antigen-binding (FAb) MAb ([99mTc]sulesomab) in relation to their kinetic fate. A total of 73 patients with “pure” osteomyelitis were examined with [99mTc]besilesomab, (Scintimun®, IBA/CIS bio international, Saclay, France; N.=38) and [99mTc]sulesomab (LeukoScan®, Immunomedics Inc., Morris Plains, NJ, USA; N.=35). Kinetic data were deduced from whole-body and single-photon emission computed tomographic scans, performed 10 minutes to 24 hour p.i. (region-of-interest technique [ROI]). In targeting “pure” osteomyelitis, sensitivities at 1-4 hours were found to be higher for [99mTc]sulesomab (44% and 80% for [99mTc]besilesomab and [99mTc]sulesomab, respectively) but at significantly lower target/background (T/B) ratios than with [99mTc]besilesomab (1.8±0.3 versus 1.4±0.5 for [99mTc]besilesomab and [99mTc]sulesomab respectively; P<0.01). With [99mTc]besilesomab, there was a continuous osteomyelitis uptake over 24 hours, whereas with [99mTc]sulesomab, the maximal uptake occurred mostly within 1-4 hours, with subsequent clearance being slower for antigen-bound activity than for nonspecific background. Hence, diagnosis was possible mostly after 4h with [99mTc]sulesomab but often not before 24 hours with [99mTc]besilesomab, the later increasing significantly (P<0.01) in sensitivity (87% and 84% for [99mTc]besilesomab and [99mTc]sulesomab, respectively). These results show that the higher sensitivity of [99mTc]sulesomab in osteomyelitis targeting at earlier p.i. times does not rely on an increased antibody uptake but on a more rapid clearance of nonspecific background activity due to faster metabolism and excretion. Intact [99mTc]besilesomab show a slow, continuous uptake

  19. The biodistribution study of 99mTc labelled anti-CEA monoclonal antibody in tumor bearing nude mice

    International Nuclear Information System (INIS)

    Lou Zongxin

    1992-01-01

    The author report the optimal condition of 99m Tc labelling with anti-CEA monoclonal antibody using chelating of 99m Tc with dimethylformamide. The labelling rate of this method is 60%-80%, the radiochemical purity of labelling antibody over 90% and maintain its better immuno activity. The biodistribution of the tumor bearing nude mice demonstrates that as compared with the control group, 24 hours after the intraperitoneal injection the injected labelled antibody has its specific concentration in tumor tissue

  20. 99mTc labeling of carbon nanomaterials

    International Nuclear Information System (INIS)

    Chu Ying; Li Qingnuan; Li Wenxin; Li Yufeng; Zhang Xiaoyong

    2008-01-01

    The effects of experimental conditions on preparation of 99m Tc-labeled carbon nanotubes and nanocarbon blacks by SnCl 2 were investigated. At given conditions the labeling yields were over 90%. In a culture medium, the radiochemical purity of the labeling compounds kept (86 ± 4)% within 2.5 h. The 99m Tc-labeled MWNTs and NCBs obtained in this work meet satisfactory experimental demands for study of cellular uptake and toxicity. The experiments showed that labeling process was based on physical adsorption of low valent technetium resulted from reduction reaction on the surface of the carbon nanomaterials. (authors)

  1. Technetium-99m labeling anti-amastigote polyclonal antibodies of Leishmania amazonensis

    International Nuclear Information System (INIS)

    Araujo, J.G.V.C.; Toledo, V.P.C.P.; Guimaraes, T.M.P.D.; Bernardo-Filho, M.; Simal, C.J.R.; Mota, L.G.; Diniz, S.O.F.; Cardoso, V.N.

    2002-01-01

    Anti-amastigote polyclonal antibody (IgG) was incubated with solutions of stannous chloride and sodium borohidride. After that, 3.7 MBq of technetium-99m ( 99m Tc) was added. A labeling yield of the antibody about 84% was obtained. After filtration of 99m Tc-IgG, the radiochemical purity increased from 84 to 95%. The labeling of IgG with 99m Tc did not modify the immunoreactivity of the antibody, since it was able to identify in vitro and in vivo the specific antigen of Leishmania amazonensis

  2. /sup 99m/Tc labeling of antibodies to cardiac myosin Fab and to human fibrinogen

    International Nuclear Information System (INIS)

    Khaw, B.A.; Strauss, H.W.; Carvalho, A.; Locke, E.; Gold, H.K.; Haber, E.

    1982-01-01

    We have developed a method of labeling biologically active labile macromolecules, such as human fibrinogen (HF) and anticardiac-myosin Fab (AM-Fab), with /sup 99m/Tc at neutral pH. This method uses dithionite reduction of pertechnetate and subsequent labeling, to test the method with acid-labile macromolecules. Complexes of diethylene triamine pentaacetic acid with macromolecules such as human fibrinogen (D-HF) and anticardiac-myosin Fab (D-AM-Fab) were labeled and utilized in in vitro and in vivo studies. In biodistribution studies, the /sup 99m/Tc D-HF had a two-component blood clearance (half-times 1 hr and 15 hr) and was 80--88% coagulable. The /sup 99m/Tc AM-Fab retained its immunoreactivity as tested by affinity chromatography; also during in vivo localization in experimental myocardial infarction. This labeling technique provides an easy and efficient approach to the /sup 99m/Tc labeling of other biologically active and acid-labile macromolecules

  3. The clinical application of radioimmunoimaging with 99mTc labeled anti-CEA monoclonal antibody C50

    International Nuclear Information System (INIS)

    Jiang Ningyi; Sha Xiaozhen; Zhang Hua

    1996-01-01

    To evaluate the clinical value of the radioimmunoimaging (RII) for the diagnosis of tumor with 99m Tc labeled anti-CEA monoclonal antibody C50, C50 was labeled with 99m Tc using modified 2-mercaptoethanol method. 99m Tc-C50 RII was performed in 70 patients with tumor. All were pathologically proved after operation. The sensitivity of 99m Tc-C50 RII for tumor was 82.9%, the specificity was 86.2%, the false negative rate was 17.1%, and the false positive rate was 13.8%. The positive predictive value was 89.5%, the negative predictive value was 78.1%. The coincidence rates was 82.4%, 84.6% and 80.0% for the ovarial intestinal and lung tumor respectively. 99m Tc-C50 RII was useful in clinical diagnosis of tumor

  4. 99mTc-HMPAO Labelled WBC Scan in Experimental Abscess by Labelling Autologous Leukocytes with In-House-Synthesized HMPAO

    International Nuclear Information System (INIS)

    Lee, Dong Soo; Shin, Hyung Sik; Ahn, Curie; Chung, June Key; Lee, Myung Chul; Choi, Kang Won; Koh, Chang Soon; Jung, Jae Min; Chung, Eun Ju

    1991-01-01

    With HMPAO we have synthesized in our laboratory, we labelled 99m Tc to canine leukocytes. Experimental abscess made by subcutaneous injection with Staphylococcus aureus was imaged with these 99m Tc labelled leukocytes. Labelling efficiency of HMPAO with 99m Tc was 66.2% ± 14.6% (N=9). Labelling efficiency of leukocytes with 99m Tc-HMPAO was 54% ± 7.79 (N=7). Cell bound radio activity in 99m Tc-HMPAO labelled leukocytes was around 80%. when these cells were incubated in plasma in vitro at 37 .deg. C for 5 hours. In vivo cell bound activity was over 80% at 24 hours after injection. One day and four days after inoculation, uptake at the inflammatory focus was found with 99m Tc labelled leukocytes. Uptake showed up in 4 hour image, and the uptake at the lesion was most prominent in 24 hour image. These findings show that in-house-synthesized HMPAO could be used for labelling leukocytes with 99m Tc, and that 99m Tc-HMPAO-labelled leukocytes were so stable and viable that inflammatory focus could be visualized with these 99m Tc-labelled leukocytes.

  5. Studies of monoclonal antibodies IOR-CEA-1 and IOR-EGF/R3 labelled with {sup 99m}Tc; Estudo de marcacao dos anticorpos monoclonais IOR-CEA-1 e IOR-EGF/R3 com {sup 99m}Tc

    Energy Technology Data Exchange (ETDEWEB)

    Dias, Carla Roberta de Barros Rodrigues

    2005-07-01

    Nuclear Medicine is a speciality that uses radioisotopes for the diagnosis or treatment of diseases and it is considered one of the best tools among the diagnostic modalities for detection of cancer. {sup 99m}Tc is one of the main isotopes for labelling antibodies and in Nuclear Medicine in general, due to its adequate physical properties, availability and low cost. Labelled monoclonal antibodies have shown promising results for diagnosis and therapy of cancer and their use has brought great experimental and clinical advances in the field of oncology. The main clinical applications of immunoscintigraphy with monoclonal antibodies are staging and evaluation of tumoral reappearance. The antibodies employed in this work were: OIR-CEA-1, a murine monoclonal antibody that acts directly against CEA expressed in several neoplasia in particular those from the gastrointestinal tract (colorectal cancer) and IOR-EGF/R3, a murine monoclonal antibody that binds to the external domain of EGF-R and it has been used in the diagnosis of tumors of epithelial origin. The objectives of this work were the development and optimization of the reduction and purification processes, the radiolabelling techniques and quality control procedures (radiochemical, immunoreactivity and cystein challenge) and imaging studies of monoclonal antibodies OIR-CEA-1 and IOR-EGF/R3, using the simple, fast and efficient method of direct labelling of the antibody with {sup 99m}Tc. The final results was the definition of the best conditions for the preparation of lyophilized reactive kits of OIR-CEA-1 and IOR- EGF/R3 for an efficient diagnostic application in Nuclear Medicine. The most adequate conditions for the labelling of the antibodies were: 1.0 mg Ab, 29 {mu}L MDP, 3.0 {mu}g Sn{sup 2+}, 1 mL of {sup 99m}Tc and 30 min. reaction time. With these conditions the labelling yield was always higher than 95% and the maximum activity of {sup 99m}Tc was about 2220 MBq (60 mCi). The evidences of the efficiency and

  6. Labeling of human immune gamma globulin with sup(99m)Tc

    International Nuclear Information System (INIS)

    Wong, D.W.; Huang, J.T.

    1977-01-01

    Human immune serum gamma globulin and rabbit anti-Stap. aureus antibody have been successfully labeled with sup(99m)Tc at pH 7.4 with an average binding efficiency of 86 and 82%, respectively. The labeled proteins behave similarly to unlabeled gamma-globulin fraction in the normal human serum as demonstrated by protein electrophoresis. The biological half-time of sup(99m)Tc-gamma-globulin in dog has been determined to be 54 min for the fast component and 14.7 hr for a slower component. Immunological assays demonstrate no significant change in antibody activity after labeling process. (author)

  7. 99mTc-HYNIC-derivatized ternary ligand complexes for 99mTc-labeled polypeptides with low in vivo protein binding

    International Nuclear Information System (INIS)

    Ono, Masahiro; Arano, Yasushi; Mukai, Takahiro; Fujioka, Yasushi; Ogawa, Kazuma; Uehara, Tomoya; Saga, Tsuneo; Konishi, Junji; Saji, Hideo

    2001-01-01

    6-Hydrazinopyridine-3-carboxylic acid (HYNIC) is a representative agent used to prepare technetium-99m ( 99m Tc)-labeled polypeptides with tricine as a coligand. However, 99m Tc-HYNIC-labeled polypeptides show delayed elimination rates of the radioactivity not only from the blood but also from nontarget tissues such as the liver and kidney. In this study, a preformed chelate of tetrafluorophenol (TFP) active ester of [ 99m Tc](HYNIC)(tricine)(benzoylpyridine: BP) ternary complex was synthesized to prepare 99m Tc-labeled polypeptides with higher stability against exchange reactions with proteins in plasma and lysosomes using the Fab fragment of a monoclonal antibody and galactosyl-neoglycoalbumin (NGA) as model polypeptides. When incubated in plasma, [ 99m Tc](HYNIC-Fab)(tricine)(BP) showed significant reduction of the radioactivity in high molecular weight fractions compared with [ 99m Tc](HYNIC-Fab)(tricine) 2. When injected into mice, [ 99m Tc](HYNIC-NGA)(tricine)(BP) was metabolized to [ 99m Tc](HYNIC-lysine)(tricine)(BP) in the liver with no radioactivity detected in protein-bound fractions in contrast to the observations with [ 99m Tc](HYNIC-NGA)(tricine) 2. In addition, [ 99m Tc](HYNIC-NGA)(tricine)(BP) showed significantly faster elimination rates of the radioactivity from the liver as compared with [ 99m Tc](HYNIC-NGA)(tricine) 2. Similar results were observed with 99m Tc-labeled Fab fragments where [ 99m Tc](HYNIC-Fab)(tricine)(BP) exhibited significantly faster elimination rates of the radioactivity not only from the blood but also from the kidney. These findings indicated that conjugation of [ 99m Tc](HYNIC)(tricine)(BP) ternary ligand complex to polypeptides accelerated elimination rates of the radioactivity from the blood and nontarget tissues due to low binding of the [ 99m Tc](HYNIC)(tricine)(BP) complex with proteins in the blood and in the lysosomes. Such characteristics would render the TFP active ester of [ 99m Tc](HYNIC)(tricine)(BP) complex

  8. New insights into the development of technetium-99m labelling kits based on monoclonal antibodies

    Energy Technology Data Exchange (ETDEWEB)

    Haase, B. [Hoechst AG, Werk Kalle-Albert, Wiesbaden (Germany)

    1995-09-01

    Two-vial antibody kits for tumour scintigraphy, detection of inflammation and scintigraphy of the bone marrow are freeze-dried preparation ready for labelling with {sup 99m}Tc according to the instructions for use. Experiences about possible influences of antibody structure, in vitro analytical methods (TLC and HPLC), different types of eluate ({sup 99}Tc : {sup 99m}Tc ratios), sampling times, activity range, ratio between protein amount and activity as well as tin(II) amounts on radiochemical purity are described or discussed on an experimental basis. In a special case, {sup 99m}Tc Mab BW 250/183 suffered from an In vitro effect during quality control (only TLC) which gave false increased values for {sup 99m}Tc- pertechnetate. 3 refs., 3 tabs., 1 fig.

  9. {sup 99m}Tc-labeled chimeric anti-NCA 95 antigranulocyte monoclonal antibody for bone marrow imaging

    Energy Technology Data Exchange (ETDEWEB)

    Sarwar, M.; Higuchi, Tetsuya; Tomiyoshi, Katsumi [Gunma Univ., Maebashi (Japan). School of Medicine] [and others

    1998-09-01

    Chimeric mouse-human antigranulocyte monoclonal antibody (ch MAb) against non-specific cross-reacting antigen (NCA-95) was labeled with {sup 99m}Tc (using a direct method) and {sup 125}I (using the chloramine T method), and its binding to human granulocytes and LS-180 colorectal carcinoma cells expressing carcinoembryonic antigen on their surfaces, cross-reactive with anti-NCA-95 chimeric monoclonal antibody, increased in proportion to the number of cells added and reached more than 80% and 90%, respectively. In biodistribution studies, {sup 99m}Tc and {sup 125}I-labeled ch anti-NCA-95 MAb revealed high tumor uptake, and the tumor-to-blood ratio was 2.9 after 24 hours. The tumor-to-normal-organ ratio was also more than 3.0 in all organs except for the tumor-to-kidney ratio. Scintigrams of athymic nude mice confirmed the results of biodistribution studies that showed higher radioactivity in tumor and kidney of the mice administered with {sup 99m}Tc-labeled ch MAb. A normal volunteer injected with {sup 99m}Tc-labeled ch anti-NCA-95 antigranulocyte MAb showed clear bone marrow images, and a patient with aplastic anemia revealed irregular uptake in his lumbar spine, suggesting its utility for bone marrow scintigraphy and for the detection of hematological disorders, infections, and bone metastasis. (author)

  10. Radioimmunoscintigraphy of experimental arterial and venous thrombi in animals with 99Tcm labelled monoclonal antibody against thrombus elements

    International Nuclear Information System (INIS)

    Ji Shundong; Liu Xiaojian; Zhang Rongjun; Wan Weixing; Jin Jian; Yuan Changgeng

    2000-01-01

    Object: To evaluate the use of 99 Tc m labelled anti P-Selection monoclonal antibody (McAb)SZ-51 and anti-fibrin McAb SZ-63 in detection of experimental thrombi in rabbits and dogs. Method: The McAb SZ-51 and SZ-63 were labelled by using the method of 2-imino-thiolane modification and 99 Tc m -glucoheptonate (GH) trans-chelation. The experimental femoral arterial and venous thrombosis were prepared, then 99 Tc m -McAb was injected into ear-edge vein, finally imaged by SPECT. 99 Tc m -labelled murine IgG was used as a negative control. Results: The fresh arterial and venous thrombi in dogs were clearly imaged 0.5 to 2 h and 2 to 4 h after injection of 99 Tc m -SZ-51/63 and 99 Tc m -SZ-51, respectively. The old arterial and venous thrombi in rabbits were clearly imaged 2 to 4 h after injection of 99 Tc m -SZ-63. Conclusion: the monoclonal antibody SZ-51 and SZ-63 would be a potential agent for imaging diagnosis of thrombotic disease

  11. Tumor affinity of technetium-99m labeled radiopharmaceuticals. II. Sup(99m)Tc-Sn-diphosphonate (sup(99m)Tc-EHDP), sup(99m)Tc-Sn-dimercaptosuccinic acid (sup(99m)Tc-DMSA), sup(99m)Tc-Sn-diethyl stilbestrol diphosphate (sup(99m)Tc-DSDP)

    Energy Technology Data Exchange (ETDEWEB)

    Itoh, K; Kobayashi, S; Hisada, K; Tonami, N [Kanazawa Univ. (Japan). School of Medicine; Ando, A

    1976-10-01

    The authors have examined the tumor affinity of various sup(99m)Tc-labelled radiopharmaceuticals to Ehrlich's tumor for the purpose of delineating human malignant neoplasm positively. The biologic distributions of sup(99m)Tc-Sn-diphosphonate (sup(99m)Tc-EHDP), sup(99m)Tc-Sn-dimercaptosuccinic acid (sup(99m)Tc-DMSA) and sup(99m)Tc-Sn-diethyl stilbestrol diphosphate (sup(99m)Tc-DSDP, sup(99m)Tc-Honvan) are included as the second report on the tumor affinity of Ehrlich-bearing mice. Tumor concentration of sup(99m)Tc-EHDP was lowest and the positive delineation of implanted tumor with sup(99m)Tc-EHDP was poorest in sequential images, though active accumulation in some soft tissues malignant neoplasms, breast cancer, and thyroid cancer, has been reported. Tumor concentration and the tumor-to-blood ratio of sup(99m)Tc-DMSA were not so high, contrary to our expectation that /sup 197/Hg-DMSA might show high tumor concentration and high tumor-to-blood ratio the same as /sup 197/Hg chlormerodrin of the renal scanning radiopharmaceuticals. Tumor concentration of sup(99m)Tc-DSDP was highest. The tumor-to-blood concentration ratio was lower than that of the above mentioned radiopharmaceuticals but the tumor-to-liver ratio and/or tumor-to-lung ratio was over 1.0 at the earlier time. Biologic distribution of sup(99m)Tc-DSDP was similar to that of /sup 32/P labeled DSDP. It is presumed that sup(99m)Tc is labeled at the phosphate ester of DSDP which is dephospholytated immediately by phospholylase in vivo following intravenous injection. Although it is not known precisely it may be assumed that the mechanism of accumulating sup(99m)Tc-DSDP in Ehrlich's tumor is related to the phospholylase activity in neoplasms.

  12. /sup 99m/Tc labelled ulcer avid agents

    International Nuclear Information System (INIS)

    Scopinaro, F.; Linari, G.; Baldieri, M.; Liberatore, M.; Corti, E.; Signori, C.

    1986-01-01

    Sulfated oligosaccharides have some interesting pharmacological properties: they are anticoagulants and protect the ulcerative areas of epithelia by precipitating over ulcers together with exudative proteins. Some sucralfate labelling methods using /sup 75/Se, /sup 111/In, /sup 99m/Tc-albumin and /sup 99m/Tc-DTPA have been reported. Only the /sup 99m/Tc-sucralfate has, at present, the requisites to be used as an ulcer-seeking agent. The aim of this study were: (a) to introduce a simple and easy-to-repeat method for the labelling of sucralfate with /sup 99m/Tc-DTPA; (b) to demonstrate that it is possible to label the sucrose octasulfate directly with /sup 99m/Tc without the aid of other ligands (e.g. DTPA)

  13. Biodistribution of immunoliposome labeled with Tc-99m in tumor xenografted mice

    International Nuclear Information System (INIS)

    Kitamura, Naoto; Shigematsu, Naoyuki; Nakahara, Tadaki; Kanoh, Momoe; Hashimoto, Jun; Kunieda, Etsuo; Kubo, Atsushi

    2009-01-01

    Immunoliposome (PEG, GAH, liposome; PGL), consisting of F(ab') 2 fragment of monoclonal antibody, GAH and polyethyleneglycol-coated (PEGylated) liposome was provided. Immunoliposome, PGL was labeled with technetium-99m (Tc-99m) by two methods: labeling F(ab') 2 fragment with Tc-99m; Tc-99m-PGL, and entrapping Tc-99m into liposome; PGL[Tc-99m]. The objective of this study was to compare the biodistribution of Tc-99m-PGL and PGL[Tc-99m] in human gastric cancer xenografted mice. Tc-99m-PGL, PGL[Tc-99m], and Tc-99m-entrapped liposome; Lipo[Tc-99m] were prepared. They were injected into human gastric cancer, MKN45, xenografted mice via the tail vein, and their biodistribution was studied. No marked accumulation of either PGL[Tc-99m] or Lipo[Tc-99m] was observed in the stomach. The uptake of Tc-99m-PGL by the liver, spleen, and lung was higher than that by the tumor. On the other hand, the uptake of PGL[Tc-99m] by the lung and spleen was markedly lower as compared with that of Tc-99m-PGL; the accumulation of PGL[Tc-99m] was lower in the lung and higher in the spleen as compared with that of the tumor. Although the liver uptake of PGL[Tc-99m] was markedly decreased as compared with that of Tc-99m-PGL, it was higher than the uptake of the tumor. The Tc-99m-PGL was strongly taken up by the tumor, with a high level of incorporation also seen in the stomach. These findings suggest the need for further study of the labeling stability. PGL[Tc-99m] appears to show promise for high tumor uptake and retention. This is an important implication for the potential application of immunoliposomes entrapped with Re-186, instead of Tc-99m, in internal radiotherapy. (author)

  14. In vitro and in vivo comparison of binding of 99m-Tc-labeled anti-CEA MAb F33-104 with 99m-Tc-labeled anti-CEA MAb BW431/26

    International Nuclear Information System (INIS)

    Watanabe, N.; Gunma Univ. School of Medicine; Oriuchi, N.; Inoue, T.; Sugiyama, S.; Kuroki, M.; Matsuoka, Y.; Tanada, S.; Murata, H.; Sasaki, Y.

    1999-01-01

    Aim: The purpose of this study was to assess the potential for radioimmunodetection (RAID) of murine anti-carcinoembryonic antigen (CEA) monoclonal antibody (MAb) F33-104 labeled with technetium-99m (99m-Tc) by a reduction-mediated labeling method. Methods: The binding capacity of 99m-Tc-labeled anti-CEA MAb F33-104 with CEA by means of in vitro procedures such as immunoradiometric assay and cell binding assay and the biodistribution of 99m-Tc-labeled anti-CEA MAb F33-104 in normal nude mice and nude mice bearing human colon adenocarcinoma LS180 tumor were investigated and compared with 99m-Tc-labeled anti-CEA MAb BW431/26. Results: The in vitro binding rate of 99m-Tc-labeled anti-CEA MAb F33-104 with CEA in solution and attached to the cell membrane was significantly higher than 99m-Tc-labeled anti-CEA MAb BW431/261 (31.4 ± 0.95% vs. 11.9 ± 0.55% at 100 ng/mL of soluble CEA, 83.5 ± 2.84% vs. 54.0 ± 2.54% at 10 7 of LS 180 cells). In vivo, accumulation of 99m-Tc-labeled anti-CEA MAb F33-104 was higher at 18 h postinjection than 99m-Tc-labeled anti-CEA MAb BW431/26 (20.1 ± 3.50% ID/g vs. 14.4 ± 3.30% ID/g). 99m-Tc-activity in the kidneys of nude mice bearing tumor was higher at 18 h postinjection than at 3 h (12.8 ± 2.10% ID/g vs. 8.01 ± 2.40% ID/g of 99m-Tc-labeled anti-CEA MAb F33-104, 10.7 ± 1.70% ID/g vs. 8.10 ± 1.75% ID/g of 99m-Tc-labeled anti-CEA MAb BW431/26). Conclusion: 99m-Tc-labeled anti-CEA MAb F33-104 is a potential novel agent for RAID of recurrent colorectal cancer. (orig.) [de

  15. Radioimmunoimaging of 99mTc-OC125 on experimental research and clinical application of ovarian cancer

    International Nuclear Information System (INIS)

    Zhang Hong; Xu Huimin; Wu Jinchang

    2000-03-01

    The objective of research is to investigate radioimmunoimaging (RII) on ovarian tumor by labelling anti-ovarian cancer monoclonal antibody (OC125) with 99m Tc. the nude mice models were produced by injection ovarian serous cyst adenocarcinoma cell HO8910. Experimental group was injected with 99m Tc-OC125 as tracer and control groups were injected normal mice IgG labelled with 99m Tc and anti-HO8910 antibody labelled with 99m Tc. RII using 99m Tc-OC125 McAb was also performed on 4 nude mice model of glioma (control group). Imaging positive rate, negative rate and tumor/non-tumor ratio were calculated. Results show positive rate of imaging of tumor was 100%. The most distinct pictures were gained between 4 to 6 h after injection of tracer. T/NT ratios of experimental group were higher than that of control groups (P 99m Tc on the nude mice models was sensitive and specific. 16 ovarian neoplasm patients were received RII 6 h after intravenous injected OC125 McAb labelled with 99m Tc. Four patients of malignant tumor repeated RII after operation and chemotherapy. The result of RII was accorded perfectly with operation. RII also can find micro recurrence focus of post-operation. The sensitivity and specificity was more excellent than the radioimmunoassay of CA125. RII is useful for defining character of ovarian tumor, especially for detecting early recurrence focus of post-operation patients

  16. Direct {sup 99m}Tc labeling of Herceptin (trastuzumab) by {sup 99m}Tc(I) tricarbonyl ion

    Energy Technology Data Exchange (ETDEWEB)

    Chen, W.-J.; Yen, C.-L.; Lo, S.-T.; Chen, K.-T. [Department of Biomedical Engineering and Environmental Sciences, National Tsing Hua University, Hsinchu 30013, Taiwan (China); Lo, J.-M. [Department of Biomedical Engineering and Environmental Sciences, National Tsing Hua University, Hsinchu 30013, Taiwan (China)], E-mail: jmlo@mx.nthu.edu.tw

    2008-03-15

    By simply incubating Herceptin (trastuzumab) with [{sup 99m}Tc(CO){sub 3}(OH{sub 2}){sub 3}]{sup +} ion in saline, a significant yield of {sup 99m}Tc-labeled trastuzumab was found to be achievable. The effective labeling may be based on that trastuzumab is inherent with endogenous histidine group to which {sup 99m}Tc(I) tricarbonyl ion can be strongly bound. For practical {sup 99m}Tc labeling processing, trastuzumab was purified beforehand from the commercial product, Herceptin (Genentech) via size exclusion chromatography to remove the excipient, {alpha}-histidine and a high-labeled yield could be obtained by incubating the purified trastuzumab with [{sup 99m}Tc(CO){sub 3}(OH{sub 2}){sub 3}]{sup +}. Retention of bioactivity of the {sup 99m}Tc(I)-labeled trastuzumab was validated using a cell binding test.

  17. Preparation of a pure 99mTc-F(ab')2 radioimmunoconjugate by direct labeling methods

    International Nuclear Information System (INIS)

    Griffiths, G.L.; Jones, A.L.; Hansen, H.J.; Goldenberg, D.M.

    1994-01-01

    Intact IgG and Fab' can be labeled directly with 99m Tc to give quantitative incorporation of radioactivity into the protein. With F(ab') 2 the reductive conditions yield a mixture of 99m Tc-F(ab') 2 and 99m Tc-Fab'. We now report a direct labeling method to produce only 99m Tc-F(ab') 2 in quantitative yield and contaminated with 99m Tc-Fab'. The properties, stability and biodistribution of the 99m Tc-F(ab') 2 have been compared to 99m Tc-Fab'. This new technology will allow us to compare technetium direct-labeled IgG, F(ab') 2 and Fab' derivatives of the same antibody for radioimmunodetection. (author)

  18. Sup(99m)Tc(Sn)-sucralfate; development of an instant labelling kit

    International Nuclear Information System (INIS)

    Grouls, R.J.E.; Ackerman, E.W.; Weegh, G. op de

    1988-01-01

    An instant labelling kit for the preparation of 99m Tc(Sn)-sucralfate has been developed containing 500 mg sucralfate and 1 mg SnCl 2 · 2 H 2 O. The labelling yield, in vitro stability and biodistribution indicate (bio)equivalence of 99m Tc(Sn)-sucralfate and 99m Tc(HSA)-sucralfate. The percentages of labelling obtained with the kit during a period of 8 months always exceeded 95%. The preparation kit is inexpensive and the labelling procedure fast and easy. (author)

  19. Electrolytic 99mTcO4- reduction: a different pathway to obtain 99mTc-labelled compounds

    International Nuclear Information System (INIS)

    Savio, E.; Kremer, C.; Gambino, D.; Kremer, E.; Leon, A.

    1991-01-01

    Electrolytic reduction of 99m TcO 4 - at inert electrodes to obtain 99m Tc cationic complexes and in vitro stability of labelled compounds were studied. Amines were used as neutral N-donor ligands and a systematic analysis of various parameters involved in the reduction process was performed. Usefulness of electrolytic reduction was proved as an alternative 99m Tc-labelling method. Its most important advantages are: production of complexes with a high radiochemical purity, negligible presence of red-hyd- 99m Tc, lack of foreign materials, simplicity of development and possibility of further applications. (author)

  20. sup 99m Tc-labelled anti NCA-95 antibodies in prosthetic heart valve endocarditis

    Energy Technology Data Exchange (ETDEWEB)

    Bair, H J; Becker, W; Wolf, F [Dept. of Nuclear Medicine, Univ. Erlangen-Nuernberg, Erlangen (Germany); Volkholz, H J [Dept. of Internal Medicine 1, Univ. of Erlangen-Nuernberg, Erlangen (Germany)

    1991-08-01

    A 54-y old women with earlier replacement of the mitral and aortic valves and clinical signs of localized endocarditis was studied with {sup 99m}Tc-labelled anti NCA-95 antibody. Whereas echocardiographic findings were negative, increased radionuclide uptake was observed left parasternal over the mitral valve as a sign of prosthetic valve endocarditis. This result could be confirmed by a similar study with leukocytes labelled in vitro with {sup 111}In-oxine. (orig.).

  1. Tumor scintigraphy by the method for subtracting the initial image with technetium-99m labeled antibody

    International Nuclear Information System (INIS)

    Karube, Yoshiharu; Katsuno, Kentaro; Ito, Sanae; Matsunaga, Kazuhisa; Takata, Jiro; Kuroki, Masahide; Murakami, Masaaki; Matsuoka, Yuji

    1999-01-01

    The method for subtracting the initial image from the localization image was evaluated for radioimmunoscintigraphy of tumors with technetium-99m (Tc-99m) labeled antibodies. Monoclonal antibodies were parental mouse and mouse-human chimeric antibodies to carcinoembryonic antigen (CEA), designated F11-39 and ChF11-39, respectively, both of which have been found to discriminate CEA in tumor tissues from the CEA-related antigens. After reduction of the intrinsic disulfide bonds, these antibodies were labeled with Tc-99m. In vivo studies were performed on athymic nude mice bearing the human CEA-producing gastric carcinoma xenografts. Though biodistribution results showed selective and progressive accumulation of Tc-99m labeled antibodies at the tumor site, high radioactivity in blood was inappropriate for scintigraphic visualization of the tumors within a few hours. We examined the subtraction of the initial Tc-99m image from the Tc-99m localization image after a few hours. Subtracted images of the same count reflected the in vivo behavior of the Tc-99m radioactivity. The subtracted scintigrams revealed excellent tumor images with no significant extrarenal background. Visualization of the tumor site was dependent on antigen-specific binding and nonspecific exudation. These results demonstrate that a method of subtraction of the initial image may serve as a potentially useful diagnostic method for an abnormal site for agents with a low pharmacokinetic value. (author)

  2. Somatostatin analogues labelled with 99mTc

    International Nuclear Information System (INIS)

    Obenaus, E.; Crudo, J.; Edreira, M.; Viaggi, M.; De Castiglia, S.G.

    2001-01-01

    The aim of the present work was to study the biological and radiochemical behaviour of two somatostatin analogues, the RC-160 and Tyr3Octreotide(TOC) peptides when labelling with 99m Tc by two methods: direct and indirect using S-benzoyl- mercaptoacetyl triglycine (MAG-3) and hydrazinonicotinamide (HYNIC) as chelating agents. RC-160 was labelled with 125I (30% labelling yield) in order to examine its receptor specificity and to study the biodistribution in normal animals. A total binding of 30% and a non specific binding lower than 10% was obtained. On the other hand, the RC-160 was labelled with 99m Tc by a direct method (70% labelling yield), using sodium ascorbate and dithionite in order to reduce the peptide and 99m Tc, respectively. The synthesis of RC-160 with S-benzoyl MAG-3 and TOC with HYNIC, for labelling with 99m Tc are also described. The conjugates were prepared on a small scale and labelled with the radionuclide using tricine as co-ligands for HYNIC conjugates. Chromatographic studies were performed using HPLC system and radiochemical purities higher than 75% and 95% were obtained respectively. Biodistributions studies in normal Wistar rats were performed and results were correlated with chromatographic and protein binding properties. Lower lipophilicity of the labelled conjugates resulted in a higher renal excretion. HYNIC-TOC complex showed promising results when labelling with 99m Tc using tricine as co-ligand although higher stability should be found for ternary co-ligands compared to tricine. (author)

  3. Labelling and quality control of 99mTc labelled somatostatin analogues

    International Nuclear Information System (INIS)

    Poramatikul, N.; Sangsuriyan, J.; Kongpeth, P.; Ngamprayad, T.; Laloknam, S.; Permtermsin, C.; Madsomboon, N.

    2001-01-01

    To standardize interlaboratory reproducibility, iodination of RC-160 with 125 I and direct labelling of RC-160 with 99m Tc, quality control and binding assay were performed. Two conjugated peptides, HYNIC-RC-160 and MAG-3-RC-160, were synthesized. The conjugated peptides were radiolabelled with 99m Tc via co-ligands; 99m Tc-MAG-3-RC-160 via glucoheptonate, 99m Tc-HYNIC-RC-160 via EDDA and tricine. Conditions for labelling were optimized. Analytical and purification methods for the labelled products were developed. Radiochemical purity test of 99m Tc labelled peptides was performed by HPLC with gradient elution of 0.1%TFA/water and acetonitrile, or by ITLC-SG in saline and in 50% acetonitrile. The contaminants in 99m Tc radiolabelled product were separated by elution from SEPPAK C-18 cartridge by 0.1% acetic acid and the pure product was eluted out of SEPPAK column by 50% acetonitrile with about 68% recovery. Stability of the purified 99m Tc-MAG3-RC-160 stored at -20 deg. C was more than 72 h. 99m Tc-MAG-3-RC-160 showed a high equilibrium dissociation constant with K D of 26 pmole/mg protein and B max of 7.9 mM. (author)

  4. Labelling, biodistribution and compartmental analysis of N-acetylcysteine labelled with Tc-99m. Comparative investigation with with 99m Tc-MIBI in an in vivo tumoral model

    International Nuclear Information System (INIS)

    Faintuch, Bluma Linkowski

    1997-01-01

    Labelling and biodistribution studies were done with two different ligands, respectively Methoxy isobutyl isonitrile (MIBI) and N-acetylcysteine (NAC), employing Tc-99m as a tracer. The main objective was to assess the pharmacokinetic properties of the second substance, aiming at its possible application in cancer diagnosis. To this purpose an in vivo investigation was done using healthy and tumor-bearing rats with experimental cancer. Images of tumor-bearing rats registered in a scintillation camera indicated that with 99m Tc-MIBI none of the two selected times was adequate for visualization of the cancer mass. In contrast, 99m Tc-NAC permitted clear identification of the humor, four hours after injection. The results have demonstrated that 99m Tc-NAC is a radiopharmaceutical with affinity for cancer tissue and promising for further investigation concerning imaging diagnosis of tumors. (author)

  5. Efficient one-step direct labelling of recombinant antibodies with technetium-99m

    International Nuclear Information System (INIS)

    Liberatore, M.; Neri, D.; Neri, G.; Pini, A.; Lurilli, A.P.; Ponzo, F.; Spampinato, G.; Padula, F.; Pala, A.; Colella, A.C.

    1995-01-01

    High-affinity bacterially expressed antibody fragments can nowadays be cloned from established hybridomas or, more conveniently, isolated directly from antibody libraries displayed on filamentous phage. Such antibodies can be tagged with C-terminal peptide tags containing one cysteine residue, which represents a convenient functionalisation site for a number of applications, including technetium-99m labelling. Here we describe a simple one-step method for 99m Tc labelling of cysteine-tagged recombinant antibodies with more than 50% radionuclide incorporation. The labelled antibodies displayed full retention of immuoreactivity and good stability. (orig.)

  6. Efficient one-step direct labelling of recombinant antibodies with technetium-99m

    Energy Technology Data Exchange (ETDEWEB)

    Liberatore, M. [Dipartimento di Medicina Sperimentale, Sezione di Medicina Nucleare, Policlinico Umberto I, Universita di Roma `La Sapienza` (Italy); Neri, D. [Cambridge Centre for Protein Engineering - MRC Centre (United Kingdom); Neri, G. [Dipartimento di Biologia Molecolare, Universita di Siena (Italy); Pini, A. [Dipartimento di Biologia Molecolare, Universita di Siena (Italy); Lurilli, A.P. [Dipartimento di Medicina Sperimentale, Sezione di Medicina Nucleare, Policlinico Umberto I, Universita di Roma `La Sapienza` (Italy); Ponzo, F. [Dipartimento di Medicina Sperimentale, Sezione di Medicina Nucleare, Policlinico Umberto I, Universita di Roma `La Sapienza` (Italy); Spampinato, G. [Laboratorio di Biochimica degli Ormoni Sessuali, Il Instituto di Clinica Ostetrica e Ginecologica, Universita di Roma `La Sapienza` (Italy); Padula, F. [Laboratorio di Biochimica degli Ormoni Sessuali, Il Instituto di Clinica Ostetrica e Ginecologica, Universita di Roma `La Sapienza` (Italy); Pala, A. [Laboratorio di Biochimica degli Ormoni Sessuali, Il Instituto di Clinica Ostetrica e Ginecologica, Universita di Roma `La Sapienza` (Italy); Colella, A.C. [Dipartimento di Medicina Sperimentale, Sezione di Medicina Nucleare, Policlinico Umberto I, Universita di Roma `La Sapienza` (Italy)

    1995-11-01

    High-affinity bacterially expressed antibody fragments can nowadays be cloned from established hybridomas or, more conveniently, isolated directly from antibody libraries displayed on filamentous phage. Such antibodies can be tagged with C-terminal peptide tags containing one cysteine residue, which represents a convenient functionalisation site for a number of applications, including technetium-99m labelling. Here we describe a simple one-step method for {sup 99m}Tc labelling of cysteine-tagged recombinant antibodies with more than 50% radionuclide incorporation. The labelled antibodies displayed full retention of immuoreactivity and good stability. (orig.)

  7. The labelling of antibody anti-PBP2a with 99mTc

    International Nuclear Information System (INIS)

    Mororo, Janio da Silva

    2012-01-01

    Staphylococcus aureus is a major cause of life-threatening infections such as bacteraemia and endocarditis. Unfortunately, many strains of this bacterial species have become resistant to certain antibiotics, including methicillin and amoxicillin. These strains are known as methicillin-resistant S. aureus (MRSA). The penicillin binding protein 2a (PBP2a) is the enzyme responsible for conferring resistance p-lactams antibiotics for MRSA, being one promising molecule for therapy with mAb. However, besides the therapy, the methods of diagnosis are also inefficient because the diagnosis currently takes several days to produce a reliable result. Taking into account, the objective of this research was radiolabeling one anti-PBP2a mAb developed by Bio-Manguinhos/FioCruz-RJ, utilizing 99m Tc, for in situ diagnostic of the infectious caused by MRSA. First, anti-PBP2a mAb was reduced utilizing 2-mecaptoethanol (2-ME) for generate sulphydryl groups (-SH) and after to be labeled with 99m Tc. In this work, were utilized two techniques of direct method: Method 1, using tartrate and gentisic acid reagents, acting like transchelant and stabilizer agents, respectively; and Method 2, using one commercial kit of MDP. Besides the radiolabeling, the mAb reduced and mAb labeled with 99m Tc were submitted to immunoreactivity analysis, with SDS-PAGE non-reducing, Immunoblotting, ELISA and neutralization assay in vitro methods. The quantity produced of sulphydryl groups by mAb was satisfactory, approximately 5 per mAb, utilizing 6.500:1 of 2-ME:mAb molar ratio. The better labeling method was Method 2, with labeling yield of 73.5%, and showed a good stability after 2 hours (73.2%). The better formulation was: 0.5 mg of mAb anti- PBP2a, 10 μU of MDP kit, after resuspended with 5 mL of saline, and 75.48 MBq (2.04 mCi) of 99m Tc, reacting by 15 minutes. The labeled mAb maintained the immunoreactivity, utilizing immunologic and in vitro experiments. (author)

  8. Reduced 99mTc labelled NCA-95/CEA-antibody uptake in liver due to gentle antibody reconstitution

    International Nuclear Information System (INIS)

    Reske, S.N.; Buell, U.

    1990-01-01

    The influence of reconstituting a murine monoclonal IgG 1 antibody kit with pertechnetate Tc99m on antibody distribution in the liver, spleen and sternal bone marrow of patients was examined. The 99m Tc-labelled antibody used is directed against non-specific cross-reacting antigen (NCA-95) and carcinoembryonic antigen (CEA) and has been successfully applied for imaging tissue inflammation and bone marrow scanning. Radioactivity uptake was determined in the liver, spleen, bone marrow and a precordial background region in a consecutive series of 25 patients, examined with an antibody preparation, routinely radiolabelled according to the manufacturer's recommendations and in 14 patients, in whom the antibody was reconstituted with special care, avoiding bubble formation and dropping of buffer into the antibody-containing vial. Gentle compared with routine antibody reconstitution caused a highly significant reduction of the antibody uptake in the liver, as determined by count densities, normalized to injected dose and acquisition time (13.2±5.5 vs 20.1±6.0 cpm per pixel, anti x±SD, P=0.008). The liver to background ratio was reduced from 3.4±1.4 to 1.9±0.5 (P<0.001). Spleen, sternal bone marrow and precordial background count rates were not significantly affected. These results clearly demonstrate that gentle antibody reconstitution can decrease non-specific antibody uptake in the liver by 34%±6.4% (anti x±SEM). Thus, scan quality is improved, and the potential deleterious camouflage of underlying structures is avoided. (orig.)

  9. Complexes of technetium-99m with tetrapeptides, a new class of 99mTc-labelled agents

    International Nuclear Information System (INIS)

    Vanbilloen, Hubert P.; Bormans, Guy M.; Roo, Michel J. de; Verbruggen, Alfons M.

    1995-01-01

    Tetrapeptides are a class of N4-tetraligands that can efficiently bind 99m Tc. In fact, tetrapeptides can be considered as derivatives of mercaptoacetyltriglycine (MAG3) in which the mercaptoacetyl moiety is replaced by a more stable and easier to handle aminoacyl group. Direct labelling of tetrapeptides with 99m Tc in alkaline medium (pH ≥ 11) in the presence of stannous ions gave a high yield (>95%) of one or two (probably isomeric) radiochemical species. Exchange labelling at different pH values in the presence of stannous tartrate resulted in lower yields of the same 99m Tc-labelled products as those formed during direct labelling. In addition, other radiochemical species were formed of which one was characterized as an oxotechnetium-complex with the cyclisized tetrapeptide. Tetrapeptides with a chiral centre in the first amino acid yield upon labelling with 99m Tc two radiochemical species, probably the two diastereomers with an oxotechnetium core respectively syn and anti with respect to the substituent on the amino acid. Only one diastereomer was observed when the chiral carbon atom is located in the second or third amino acid. Electrophoresis indicated that these new 99m Tc-labelled complexes are neutral in acidic medium and negatively charged in neutral and alkaline conditions. This correlates with a complex in which an oxotechnetium(V) group is bound to the ligand through three deprotonated nitrogen atoms of the amide functions and the free electron pair of the amine nitrogen atom. Biodistribution in mice showed for all studied 99m Tc-labelled tetrapeptides a rapid clearance from the blood mainly by the renal system. The presence of a methyl substituent in the tetrapeptide increased the urinary excretion. 99m Tc-labelledl -glycylalanylglycylglycine showed in mice a urinary excretion comparable to that of 99m Tc-MAG3. Further rise of lipophilicity by introduction of a dimethyl, isopropyl or isobutyryl group leads to increased hepatobiliary handling. It

  10. Development of Tc-99m labeled myocardial imaging agent

    International Nuclear Information System (INIS)

    Jeong, J. M.; Jang, Y. S.; Kim, Y. J.; Lee, Y. S.; Kim, H. W.; Ray, G.; Lee, M. S.

    2006-02-01

    Lipophilic cations have been widely used for myocardial SPECT. We synthesized novel +1 charged lipophilic Tc-99m-labeled N,N'-disubstituted N2S2 derivatives and investigated their biodistribution. The N,N'-dimethyl-, N,N'-diethyl-, N,N'-bis(methoxyethyl)-, and N,N'-bis(ethoxyethyl)N2S2 derivatives were synthesized by alkylating disulfide form of N2S2 with corresponding alkyl halides and subsequently reduced with LAH in THF. To label with Tc-99m, 50% gluconic acid (0.1 ml), SnCl2·2H2O (10 μg), Tc-99m-pertechnetate (370 MBq/2.5 ml) and 0.5 M Na2CO3 (0.3 ml) were added to the compounds. These mixtures were reacted in boiling water bath for 30∼60 min. Radiochemical purities were checked by Whatman No.1 chromatography (normal saline, Rf 0.3∼0.4). Biodistribution of each compound was investigated after injecting 74 kBq (0.1 ml) of each Tc-99m-labeled compound to ICR-mice through the tail vein. Chemical structures of synthesized compounds were confirmed by GC-MSD and 1H-NMR spectroscopy. All of the Tc-99m-labeled compound showed labeling efficiencies of higher than 93%. In biodistribution study, the myocardial uptake of Tc-99m-N,N'-dimethylN2S2, Tc-99m-N,N'-diethylN2S2, Tc-99m-N,N'-bis(methoxyethyl)N2S2 and Tc-99m-N,N'-bis(ethoxyethyl)N2S2 were 5.38 ±0.96, 2.98 ±0.16, 4.27 ±0.47, 7.24 ±1.01% ID/g at 10 min and 5.34 ±1.57, 2.05 ±0.40, 1.02 ±0.16, 1.69 ±0.04% ID/g at 2 hr, respectively. We successfully synthesized Tc-99m-labeled N,N-disubstituted N2S2 derivatives that are novel lipophilic +1 charged compounds. We thought our results prove the feasibility of these compounds to use for myocardial SPECT agent

  11. 99mTc labelled peptides for imaging of peripheral receptors

    International Nuclear Information System (INIS)

    Mustanser, J.; Anjum, A.

    2001-01-01

    Several peptides are being used as radiopharmaceuticals for receptor imaging scintigraphy. The peptide receptors are found in the tumours of various sites in the human body. Somatostatin is one of those, which is expressed by a variety of tumours say in brain cortex, medullary carcinoma of thyroid, adrenal glands, pancreas and gut. Therefore neuropeptides based on somatostatin analogues are labelled with different radionuclide, 123 I and 111 In. Efforts are underway to label RC-160 (an analogue of somatostatin) with 99m Tc because of its favourable radiation dosimetry, short half-life, low price, high count rate and better diagnostic efficacy. In this project various methods of labelling RC-160 with different radionuclides 125 I and 99m Tc have been studied in detail. Radioiodination of RC-160 was tried with 125 I using the iodogen method as directed and then with Chloramine T method. Labelling of RC-160 peptide with 99m Tc was done using two different aspects. Direct labelling with 99m Tc and indirect labelling with 99m Tc using double chelating agents. Radiochemical quality control was carried out applying instant thin layer chromatography using ITLC-SG strips in 85% of methanol. Later the HPLC analysis was used for its evaluation. To label RC-160 with 99m Tc the approach of direct labelling was attempted first. 46% labelling could be achieved with 95% of radiochemical purity. The biodistribution of 99m Tc-RC-160 complex in rats has also been studied to determine uptake in various sites of somatostatin receptors. Eventually, attempt was made to synthesize biomolecule by conjugating Boc protected RC-160 with benzoyl MAG-3. As a result 80% of Boc-RC-160 went under conjugation with benzoyl MAG-3. (author)

  12. Pharmaceutical design and pharmacological characterization of Tc99m [99mTc] labelled somatostatin and gastrin analogues

    International Nuclear Information System (INIS)

    Guggenberg, E. von

    2004-10-01

    The development of regulatory peptide analogues radiolabelled with 99m Tc is of great interest for nuclear medicine applications, as 99m Tc shows very favourable imaging characteristics, such as low radiation burden to the patient, optimal image quality in SPECT, one-day-acquisition-protocol, availability on demand and cost effectiveness. In this work the principles of pharmaceutical design and preclinical pharmacological characterization of regulatory peptide analogues labelled with 99m Tc with possible application in tumour diagnosis are described. [ 99m Tc-EDDA-HYNIC0,Tyr3]octreotide ( 99m Tc-EDDA-HYNIC-TOC) is a promising new radiopharmaceutical with the potential to replace [ 111 In-DTPA0]octreotide in receptor scintigraphy of somatostatin receptor-positive tumours. Radiolabelling at high labelling yields and high specific activities could be obtained applying a coligand exchange labelling approach from tricine for EDDA under optimized conditions of pH, EDDA and stannous ion concentration. The resulting complex was characterized via HPLC, receptor binding and LC-MS. For the development of a freeze-dried kit formulation with long shelf-life, high stability of the final preparation and retained biological activity, the addition of bulking agent, the pH of the freeze-drying solution and the content of stannous chloride were of major importance. Different methods of radiochemical purity testing were evaluated to guarantee high quality of the preparation in a clinical setting, forming the basis for a further clinical evaluation of this promising new radiopharmaceutical. Radiolabelling of [D-Glu1]minigastrin (MG) with 99m Tc was studied applying two different labelling approaches. HYNIC-MG could be labelled using tricine and EDDA as coligands; and (Nalpha-His)Ac-MG was used as tridentate ligand for the 99m Tc carbonyl core. Stability experiments by HPLC analysis in PBS, serum, histidine- and cysteine-solutions as well as rat liver and kidney homogenates, receptor

  13. ACS labelled with sup(99m)Tc and cartilage scintigraphy

    International Nuclear Information System (INIS)

    Dupuy, J.C.; Harmand, M.F.; Blanquet, P.

    1976-01-01

    ACS, chondroitine-sulphate acid, is the principal mucopolysaccharide of cartilagineous substance. We therefore thought it of interest to label this molecule with sup(99m)Tc so as to obtain a scintigraphic image of cartilagineous formations. sup(99m)Tc-pyrophosphate and the sup(99m)Tc-polyphosphates permit simultaneous imaging of hyperactive zones in bone and cartilage. The ACS-labelling technique is based on the reduction of sup(99m)Tc-pertechnetate by the tin-II-ion. Sephadex-gel chromatography at different pH-levels was used to study labelling gain, under optimum conditions it can attain 85%. The labelled product was administered intravenously and studied in rat and rabbit. An identical biological half-life of 15 minutes was found for both species. Scintigraphes from rabbits permitted clear visualization of the epiphyses of tubular bones, intervertebral cartilage, and auricular cartilage. These encouraging results point to interesting clinical applications

  14. Gel chromatography of sup(99m)Tc-labelled compounds

    International Nuclear Information System (INIS)

    Vilcek, S.; Machan, V.; Kalincak, M.

    1976-01-01

    The present state of gel chromatography of sup(99m)Tc-labelled compounds is reviewed. Examples are given of gel chromatography for preparing labelled compounds and for quality control analysis and the development of new types of sup(99m)Tc-labelled compounds. The factors which influence the gel chromatography of these compounds are discussed, i.e., the nature of the elution agent, the duration of the contact of the gel and the preparation the gel type, the nature of the labelled compound. The GCS method (gel chromatography scanning) is briefly described. The advantages of gel chromatography as compared with other chromatographic techniques for sup(99m)Tc-labelled compounds are summarized. (author)

  15. Studies on the porphine labeled with 99mTc-pertechnetate

    International Nuclear Information System (INIS)

    Ai-Yih Wang; Jiunn-Liang Lin; Wen-Chieh Lin

    2010-01-01

    The aim of this research is to use acetylacetonate as a 99m Tc chelating agent label with porphyrin and evaluate its radiochemical and biological characteristics. Stannous chloride was used as a reductant to determine the chemical and biological characterization of 99m Tc-complexes from labeling porphine (4',4'',4'''-(2lH,23H-Porphine-5,10,15,20-terayl)tetrakis-(benzoic acid), TPPB) with 99m Tc-pertechnetate. Instant thin layer chromatography (ITLC), size exclusion chromatography (SEC), paper electrophoresis, and UV/Vis spectrophotometry were used to evaluate chemical characterization. Finally, biodistribution and liver function tests were applied to evaluate biological characteristics. The results of this study show that the labeling efficiency of 99m Tc(acac)-TPPB was nearly 100% when using acetylacetone (acac) as a conjugator. Three major 99m Tc(acac)-TPPB complexes were separated by SEC, and all of them were hydrophilic. The UV-Vis spectra of 99m Tc(acac)-TPPB complexes closely resembled those of the TPPB, but the wave lengths of their peaks changed 430, 521, 556, 591 and 647 nm after complexation. The biodistribution study selected the liver as the target organ. The 99m Tc(acac)-TPPB complex may cause short-term liver injury. However, this injury can be repaired, and the reagent is quickly metabolized. Hence, the toxicity of the 99m Tc(acac)-TPPB complex is within an acceptable range, and making it a promising liver imaging agent. (author)

  16. Chemical aspects of labeling sucralfate with 99mTcO4

    International Nuclear Information System (INIS)

    Billinghurst, M.W.; Abrams, D.N.; Lawson, M.S.

    1989-01-01

    Two formulations of [ 99m Tc]sucralfate have been used to image gastric and duodenal ulcers and inflammatory bowel disease. One formulation is a complexation of [ 99m Tc]HSA with sucralfate. The second is prepared by directly labeling sucralfate with [ 99m Tc]pertechnetate in the presence of stannous ion. An in vitro study of the factors affecting the production and stability of these labeled sucralfate preparations was conducted. Both formulations were stable at the acidic pH likely encountered in the stomach. However, at pH greater than 6 the albumin-sucralfate complex began to dissociate while directly labeled sucralfate was stable to a pH of 9. Conversely it was shown that directly labeled sucralfate was more susceptible to loss of 99m Tc to other chelating species. Sucralfate complexed with [ 99m Tc]HSA was radiochemically stable up to a specific activity of 26 GBq (700 mCi) per gram while directly labeled sucralfate showed decreased 24-hr stability at specific activities greater than 837 mCi (31 GBq) per gram

  17. Scintigraphic myocardial imaging with sup(99m)Tc-labelled pyrophosphate of experimentally produced cardiomyopathy in dogs

    Energy Technology Data Exchange (ETDEWEB)

    Duska, F.; Novak, J.; Vizda, J.; Kubicek, J.; Kafka, P.; Mazurova, Y.; Bradna, P.

    1981-12-01

    Scintigraphic examination of the myocardium using sup(99m)Tc-labelled pyrophosphate was carried out in 10 dogs with experimentally produced cardiomyopathy. This was brought by introvenous administration of high doses of adrenalin and theophylline. The scan was positive in 8 out of 10 dogs. Hot foci were very extensive. The degree of accumulation was however low (2+). Histological examination of the myocardium using the light microscope showed only scarcely distinguishable damage to the tissue without the presence of necrosis. ECG examinations were normal in all cases. By means of sup(99m)Tc-labelled pyrophosphate even very small myocardial disorders can thus be detected. This fact may be of clinical importance for an early diagnosis of heart lesions.

  18. Study of {sup 99m}Tc-DMSA biodistribution in experimental animals

    Energy Technology Data Exchange (ETDEWEB)

    Castro, Thais O.M. de; Silva, Natanael G. da; Colturato, Maria T.; Felgueiras, Carlos F.; Mengatti, Jair; Fukumori, Neuza T.O.; Matsuda, Margareth M.N.; Araújo, Elaine B. de, E-mail: thais.castrom@gmail.com [Instituto de Pesquisas Energeticas e Nucleares (IPEN/CNEN-SP), Sao Paulo, SP (Brazil). Centro de Radiofarmacia

    2017-11-01

    {sup 99m}Tc-DMSA, succimer ({sup 99m}Tc), is a radiopharmaceutical commonly used in nuclear medicine for renal function evaluation by imaging. In order to achieve adequate labeling of the product with good radiochemical yield and standardized biological distribution, the interval of 185 - 3700 MBq should be kept in a maximum volume of 3 mL for product labeling. Moreover, one should avoid exposing the reconstituted solution to oxygen and using the product after four hours post labeling. The aim of the study was to quantify and evaluate the influence of different DMSA complexes on biological distribution of the radiopharmaceutical in experimental animals, taking in account variations in the labeling parameters. Radiochemical purity was determined by paper and thin layer chromatography using both acetone/Whatman 3MM, 0.9% NaCl/TLC-SG and n-propanol/ H{sub 2}O/acetic acid (4:3:1 V/V/V)/TLC-SG systems respectively for quantification of {sup 99m}TcO{sub 4} - and {sup 99m}TcO{sub 2} plus some {sup 99m}Tc-DMSA complexes. The labeling activity did not significantly affect the extent of the main complex generation. The presence of oxygen and the concentration of {sup 99}Tc did not markedly change the percentage of the radiochemical impurities in the preparation. Radiochemical purity tests of the DMSA-{sup 99m}Tc based on IPEN-CNEN DMSA-TEC reagent and on another producer's reagent showed similar results. Although the routine method used by IPEN-CNEN to determine the radiochemical yield of {sup 99m}Tc-DMSA was not able to discriminate among {sup 99m}Tc-DMSA complexes, the renal uptake and the kidney to liver plus spleen uptake ratio in rats met the official compendia criteria for the radiopharmaceutical. (author)

  19. Study of "9"9"mTc-DMSA biodistribution in experimental animals

    International Nuclear Information System (INIS)

    Castro, Thais O.M. de; Silva, Natanael G. da; Colturato, Maria T.; Felgueiras, Carlos F.; Mengatti, Jair; Fukumori, Neuza T.O.; Matsuda, Margareth M.N.; Araújo, Elaine B. de

    2017-01-01

    "9"9"mTc-DMSA, succimer ("9"9"mTc), is a radiopharmaceutical commonly used in nuclear medicine for renal function evaluation by imaging. In order to achieve adequate labeling of the product with good radiochemical yield and standardized biological distribution, the interval of 185 - 3700 MBq should be kept in a maximum volume of 3 mL for product labeling. Moreover, one should avoid exposing the reconstituted solution to oxygen and using the product after four hours post labeling. The aim of the study was to quantify and evaluate the influence of different DMSA complexes on biological distribution of the radiopharmaceutical in experimental animals, taking in account variations in the labeling parameters. Radiochemical purity was determined by paper and thin layer chromatography using both acetone/Whatman 3MM, 0.9% NaCl/TLC-SG and n-propanol/ H_2O/acetic acid (4:3:1 V/V/V)/TLC-SG systems respectively for quantification of "9"9"mTcO_4 - and "9"9"mTcO_2 plus some "9"9"mTc-DMSA complexes. The labeling activity did not significantly affect the extent of the main complex generation. The presence of oxygen and the concentration of "9"9Tc did not markedly change the percentage of the radiochemical impurities in the preparation. Radiochemical purity tests of the DMSA-"9"9"mTc based on IPEN-CNEN DMSA-TEC reagent and on another producer's reagent showed similar results. Although the routine method used by IPEN-CNEN to determine the radiochemical yield of "9"9"mTc-DMSA was not able to discriminate among "9"9"mTc-DMSA complexes, the renal uptake and the kidney to liver plus spleen uptake ratio in rats met the official compendia criteria for the radiopharmaceutical. (author)

  20. Synthesis and evaluation of 99mTc/99Tc-MAG3-biotin conjugates for antibody pretargeting strategies

    International Nuclear Information System (INIS)

    Gog, Frank B. van; Visser, Gerard W.M.; Gowrising, Radjish W.A.; Snow, Gordon B.; Dongen, Guus A.M.S. van

    1998-01-01

    Four 99m Tc-MAG3-biotin conjugates were synthesized to determine their potential use in antibody pretargeting strategies for radioimmunoscintigraphy (RIS). To use these 99m Tc-MAG3-biotin conjugates as model compounds for 186 Re-MAG3-biotin conjugates for radioimmunotherapy (RIT), nanomolar amounts of 99 Tc were added as carrier to 99m Tc. The biotin derivatives used for the preparation of the conjugates - biocytin, biotin hydrazide, biotinyl-piperazine, and biotinyl-diaminosuccinic acid - differed at the site that is regarded to be susceptible to hydrolysis by biotinidase present in human plasma. All four conjugates were produced with high radiochemical purity, were stable in PBS, and demonstrated full binding capacity to streptavidin. The 99m Tc/ 99 Tc-MAG3-labeled biotinyl-piperazine and biotinyl-diaminosuccinic acid conjugates were stable in mouse as well as human plasma, whereas the corresponding biocytin and biotin hydrazide conjugates were rapidly degraded. The biodistribution in nude mice at 30 min after injection was similar for all conjugates, and a rapid blood clearance and high intestinal excretion were both observed. It is concluded that the metabolic routing of a conjugate containing biotin and MAG3 is dominated by these two moieties. For this reason, MAG3-biotin conjugates do not seem suited for pretargeted RIT, for which quantitative and fast renal excretion is a prerequisite to minimize radiation toxicity. However, in a pretargeted RIS approach the 99m Tc-MAG3-biotin conjugates might have potential

  1. In vitro studies of leukocyte labeling with /sup 99m/Tc

    International Nuclear Information System (INIS)

    Uchida, T.; Vincent, P.C.

    1976-01-01

    A method for labeling leukocytes in vitro with /sup 99m/Tc is described. Separated leukocytes are incubated with /sup 99m/Tc, followed by reduction with stannous chloride and washing with acid citrate dextrose solution. Maximum labeling occurs after at least 5 min incubation with pertechnetate, followed by at least 10 min incubation with stannous chloride. Labeling is similar at room temperature and at 37 0 C. The labeled leukocytes are viable, and reutilization of label does not occur in vitro. In acid conditions (pH 5.2), the elution of /sup 99m/Tc from leukocytes is comparable with that of 32 P-diisopropylfluorophosphate, but /sup 99m/Tc elution is greater at pH 7.2 to 7.4. Neutrophils label more heavily with /sup 99m/Tc than do monocytes, lymphocytes, erythrocytes, or platelets

  2. 99mTc labeling of the scorpion (Tityus serrulatus) antivenom

    International Nuclear Information System (INIS)

    Cardoso, D.S.; Nunan, E.A.; Toledo, V.P.C.P.; Moraes-Santos, T.; Cardoso, V.N.

    2008-01-01

    F(ab') 2 is the fragment involved in the immunotherapy for scorpion stings and it would be convenient to label it with 99m Tc for organ distribution and pharmacokinetics studies. The aim of the present study was to label scorpion antivenom F(ab') 2 with 99m Tc keeping its biological activity, integrity and stability. High labeling yield was obtained using stannous chloride and sodium borohydride. Stability, immunoreactivity and integrity of 99m Tc-F(ab') 2 was preserved. It was not observed any difference between potencies of unlabeled and labeled antivenom. 99m Tc-F(ab') 2 can be a useful tool for use in biodistribution and pharmacokinetics studies on the evaluation of the efficacy of the antivenom against scorpion envenomation. (author)

  3. Labelling and optimization of PHOTOFRIN registered with 99mTc

    International Nuclear Information System (INIS)

    Fakhar-e-Alam, M.; Roohi, S.; Amir, N.; Zahoor, R.; Atif, M.; Firdous, S.

    2010-01-01

    PHOTOFRIN registered was labelled with 99m Tc using SnCl 2 .2H 2 O as reducing agent. Instant thin layer chromatography (ITLC-SG) in 0.05 M NaOH was used for evaluation of radiochemical purity. Labelling efficiency was dependent on various factors that include the ligand/reductant ratio, pH and time of incubation. Therefore, optimum conditions of labelling were also determined. The stability of 99m Tc-PHOTOFRIN registered in serum was checked by using fresh human serum. Tissue distribution of 99m Tc-PHOTOFRIN registered was evaluated in Sprague Dawley rats. PHOTOFRIN registered was labelled with an efficiency of > 95% under optimum conditions, which were PHOTOFRIN registered : 200 μg, pH: 3-4, SnCl 2 .2H 2 O: 15 μg and 30 min incubation at room temperature. The 99m Tc-labelled PHOTOFRIN registered remained stable in human serum for 24 h. Biodistribution study in rats revealed maximum concentration of the labelled compound in liver, lungs and spleen at 0.5 h, and significant activity was also seen in the bladder and urine, indicating the mode of urinary excretion of PHOTOFRIN registered . (orig.)

  4. A study of labelling of monoclonal antibody C50 with 99Tcm and using for radioimmunoimaging

    International Nuclear Information System (INIS)

    Huang Biao; Yang Min; Wang Yang; Lu Zhongwei; Guan Liang; Guo Wanhua; Zhu Chengmo

    2002-01-01

    Objective: To provide an accurate and scientific method of radionuclide imaging with 99 Tc m -C50. Methods: The labelled C50 was derived by imino-thiolane and ligand exchange from 99 Tc m O(GH) 2 - . HPLC ws used to analyse the modified antibody and labelled antibody, labelling efficiency was measured by paper chromatography. Radioimmunoimaging was performed on human colon tumor bearing nude mice. Results: The labelling efficiency of the labelled antibody was 97%, with 4% colloidal 99 Tc m in it; the in vitro competition test showed that 99 Tc m being bound up with the antibody at high affinity. The stability of the imino-thiolane modified antibody could be kept at 4 degree C for 3 months. The biodistribution study showed that the tumor radioactivity uptake at 24 h postinjection was the highest, the ratio of tumor to muscle was 4.03. Conclusion: The labelling method applied to the preparation of 99 Tc m labelled antibody C50 was successful, and appears to be equally applicable for labelling other antibodies

  5. Clinical estimation of sup(99m)Tc-labeled compounds produced by electrolysis

    International Nuclear Information System (INIS)

    Watanabe, Katsuji; Kawahira, Kenjiro; Kamoi, Itsuma; Morita, Kazunori

    1974-01-01

    Scintigrams were made using sup(99m)Tc-Sn-colloid, sup(99m)Tc-pyrophosphate, sup(99m)Tc-EDTA and sup(99m)Tc-albumin prepared by electrolysis, and a clinical evaluation was attempted. No side effects were recognized in 228 cases, therefore the object of this study could be attained. Future study was thought to be necessary because the pictures were somewhat indistinct. However, each sup(99m)Tc-labeled compound could be prepared very easily and was extremely convenient for daily use. sup(99m)Tc- is a nuclide which has many advantages for use with scintigrams. More useful sup(99m)Tc-labeled compounds will be explored in the future and is expected that electrolysis has many possibilities for use in the preparation of sup(99m)Tc-labeled compounds. (Tsunoda, M.)

  6. Effect of milking efficiency on Tc-99 content of Tc-99m derived from Tc-99m generators

    International Nuclear Information System (INIS)

    Bonnyman, J.

    1983-01-01

    Tc-99m obtained by separation from its parent Mo-99 always contains Tc-99 produced by decay of Tc-99m and Mo-99. Factors effecting the Tc-99/Tc-99m ratios are discussed. An HPLC method has been developed to measure the 99 TcO 4- content of sodium pertechnetate from generators with a detection limit of 0.9 ng Tc-99 for a 500 μl/ aliquot of TcO 4- -99m. First eluates of 10 chromatograph-ic generators gave Tc-99/Tc-99m ratios ranging from 3.5-46 ng Tc/mCi Tc-99m measured at the time of milking. The measurements indicate that Tc-99/Tc-99m ratios high enough to cause adverse labelling effects could be found in 'instant pertechnetate' and in the first eluate from Tc-99m generators for the activities normally used in radiopharmaceutical production

  7. 99mTc labeled VIP analog: evaluation for imaging colorectal cancer

    International Nuclear Information System (INIS)

    Rao, P.S.; Thakur, M.L.; Pallela, V.; Patti, R.; Reddy, K.; Li, H.; Sharma, S.; Pham, H.L.; Diggles, L.; Minami, C.; Marcus, C.S.

    2001-01-01

    Early and reliable diagnosis of colorectal cancer continues to be demanding and challenging. Colorectal cancer cells express Vasoactive Intestinal Peptide (VIP) receptors in high density. We have prepared a VIP analog (TP3654), labeled it with 99m Tc, and evaluated it in experimental animals as an agent for imaging colorectal cancer. The tissue distribution of 99m Tc-TP3654 has been compared with that of 111 In-DTPA-Octreotide and 99m Tc-anti-CEA scan in nude mice bearing human colorectal cancer LS174T. Finally, pharmacokinetic and tissue distribution studies of 99m Tc-TP3654 have been performed in four normal human volunteers. Data suggest that 99m Tc-TP3654 can be prepared efficiently without loss of its receptor specificity and biological activity. Although the 24 hr tumor uptake of 99m Tc-TP3654 in the animal model used was modest (0.21 ± 0.07% I.D./g), the tissue distribution profile was more favorable than that of 111 In-DTPA-Octreotide or 99m Tc-anti-CEA scan. Human studies indicated that 99m Tc-TP3654 had no adverse effect in any subject. Within 24 hours, approximately 70% of the injected dose cleared through the kidneys, and approximately 20% through the hepatobiliary system. In these non-fasting volunteers hepatobiliary clearance was slow and in cancer patients tumor uptake was rapid. Data suggest that 99m Tc-TP3654 is a promising agent for imaging colorectal cancer

  8. sup(99m)Tc-labeled monofluorophosphate as a skeletal imaging agent

    International Nuclear Information System (INIS)

    Ichikawa, Tsuneji; Ito, Yasuhiko; Muranaka, Akira; Yokobayashi, Tsuneo; Uchida, Masahiro

    1976-01-01

    The performance of sup(99m)Tc-monofluorophosphate was compared with those of sup(99m)Tc-pyrophosphate and sup(99m)Tc-diphosphonate in rabbits. Studies included chromatographic quality control, measurements of blood clearance, tissue distribution, urinary excretion, skeletal imaging, and measurements of the serum calcium. The labeling for sup(99m)Tc-monofluorophosphate was 98% on paper chromatography and 85% on thin layer chromatography. A large fraction of the activity of the three labeled agents was cleared very rapidly from the bloodstream: however, slow components of the curves were the highest for sup(99m)Tc-monofluorophosphate and lowest for sup(99m)Tc-diphosphonate. Three hours after injection 20% of the dose of sup(99m)Tc-monofluorophosphate was taken up by bone. The corresponding values of sup(99m)Tc-pyrophosphate and sup(99m)Tc-diphosphonate were 29.1% and 40.0% respectively. Ratio of concentration in bone to that in other major organs was highest with sup(99m)Tc-diphosphonate. Ratios were similar for both sup(99m)Tc-monofluorophosphate and sup(99m)Tc-pyrophosphate and much lower than those of sup(99m)Tc-diphosphonate. No significant differences were demonstrated in urinary excretion of the three labeled agents. Visual comparison of the scans obtained with three compounds confirmed the results of radioassay. All were excellent skeletal imaging agents, although sup(99m)Tc-diphosphonate appeared to be superior to the other two mainly because of a higher target to non-target ratio. With 50 mg of monofluorophosphate and 1 mg of stannous fluoride, no hypocalcemia was observed. (J.P.N.)

  9. Thrombus imaging with [sup 99m]Tc-HMPAO-labeled platelets and [sup 111]In-labeled monoclonal antifibrin antibodies

    Energy Technology Data Exchange (ETDEWEB)

    Vorne, M.S.; Honkanen, T.T.; Lantto, T.J.; Laitinen, R.O.; Karppinen, K.J.; Jauhola, S.V. (Depts. of Nuclear Medicine and Diagnostic Radiology, Paeijaet-Haeme Central Hospital, Lahti (Finland))

    1993-01-01

    Eighteen patients with suspicion of deep venous thrombosis (DVT) in the lower extremities were imaged both with autologous [sup 99m]Tc-HMPAO-labeled platelets (Tc-PLT) and [sup 111]In-labeled monoclonal antifibrin antibodies (In-MoAbs) on the same day. Precence or absence of thrombosis was verified by venography. Tc-PLT was given i.v. followed after 30 min by In-MoAbs. Anterior and posterior projections of the lower extremities were obtained with a large field-of-view gamma camera at 5 to 25 min, 2 h, 4 to 6 h, and 20 h after administration of the marker. Both Tc-PLT and In-MoAbs detected DVT well but less frequently than venography. Thrombi were visualized at 2 to 4 h after injection. The quality of images was better with Tc-PLT than with In-MoAbs. In the patients treated during the study, heparin significantly (p< 0.01) inhibited the uptake of Tc-PLT but not of In-MoAbs. We conclude that both Tc-PLT and In-MoAbs are suitable agents for the detection of DVT especially in patients without anticoagulation. (orig.).

  10. 99mTc labeled anti EGFR Nanobody pentamer for tumor radioimmunoimaging

    International Nuclear Information System (INIS)

    Ding Zhiling; Lan Xiaoli; Li Chongjiao; Pei Zhijun; Zhang Yongxue; Wang Lifei; Gao Bin

    2014-01-01

    Novel Nanobody has small molecular weight and lower affinity. Appropriate polymer would be more suitable for radioimmunoimaging. In this study, we labeled anti EGFR Nanobody pentamer with 99m Tc to prepare tumor targeting imaging agent and to investigate its binding characteristics of tumor cells and tissues in vitro and in vivo, and to explore the feasibility of 99m Tc-EGFR Nanobody pentamer for tumor radioimmunoimaging compared with anti EGFR Nanobody monomer. EGFR Nanobody labeled with 99m Tc through tricarbonyl intermediate. The labeled compounds were purified by an ultra centrifugal filter; The labeling efficiency was determined by thin layer chromatography (TLC), and the radiochemical purity more than 95%. In vitro, 99m Tc-EGFR Nanobody monomer and pentamer have the specific binding capability with EGFR overexpression A431 tumor cell. the binding rate of 99m Tc-EGFR Nanobody monomer higher than that of pentamer (11.32% ± 2.73% vs 5.80% ± 0.92%, P < O.05). In A431 xenografted tumor was clearly displayed after intravenous injection of 99m Tc-EGFR Nanobody pentamer at l.5 h, T/NT maximum was 2.9 (1.5 h), whereas, the tumor tissues was not obviously found using 99m Tc-EGFR Nanobody monomer. The negative EGFR expression OCM-I xenografted tumor was not showed in both monomer and pentamer tracer. The experiment indicated that 99m Tc-EGFR Nanobody pentamer are appropriate for tumor radioimmunoimaging and has the potential value for the further study. (authors)

  11. Labelling, biodistribution and compartmental analysis of N-acetylcysteine labelled with Tc-99m. Comparative investigation with with {sup 99m} Tc-MIBI in an in vivo tumoral model; Estudo de marcacao, biodistribuicao e analise compartimental da N-acetil cisteina marcada com Tc-99m. Investigacao comparativa com MIBI-{sup 99m}Tc em modelo tumoral in vivo

    Energy Technology Data Exchange (ETDEWEB)

    Faintuch, Bluma Linkowski

    1997-07-01

    Labelling and biodistribution studies were done with two different ligands, respectively Methoxy isobutyl isonitrile (MIBI) and N-acetylcysteine (NAC), employing Tc-99m as a tracer. The main objective was to assess the pharmacokinetic properties of the second substance, aiming at its possible application in cancer diagnosis. To this purpose an in vivo investigation was done using healthy and tumor-bearing rats with experimental cancer. Images of tumor-bearing rats registered in a scintillation camera indicated that with {sup 99m} Tc-MIBI none of the two selected times was adequate for visualization of the cancer mass. In contrast, {sup 99m} Tc-NAC permitted clear identification of the humor, four hours after injection. The results have demonstrated that {sup 99m} Tc-NAC is a radiopharmaceutical with affinity for cancer tissue and promising for further investigation concerning imaging diagnosis of tumors. (author)

  12. Biodistribution of 99mTc labelled anti TAG 72 chimeric McAb ccM4 in nude mice and preliminary clinical study

    International Nuclear Information System (INIS)

    Ma Qingjie; Zhao Jie; Zhang Yingnan; Gao Fengtong; Liu Shuqing

    1995-01-01

    Chimeric McAb ccM 4 was labelled with 99m Tc by direct method. The antibody was reduced by molar excess 2-mercaptoethanol (2-ME; Ab, 1000:1). The reduced ccM 4 chimeric McAb was mixed with 99m Tc reduced by SnCl 2 and 99m Tc labelling efficiency was 98%. The immunoreactivity did not change after labelling. The biodistribution of 99m Tc-ccM 4 was performed in nude mice and patients with stomach carcinoma. There was significantly more radioactivity in tumor than in the rest of the body in nude mice. Radioimmunoimaging of ccM 4 in 10 patients of gastric cancer was also presented

  13. Scintigraphy with /sup 111/In-labeled antimyosin F(ab)/sub 2/ monoclonal antibody and /sup 99m/Tc-pyrophosphate in rhabdomyolysis

    Energy Technology Data Exchange (ETDEWEB)

    Krause, T.; Schuemichen, C.; Hohenloser, S.; Kasper, W.; Meinertz, T.

    1988-02-01

    A report is presented of the scintigraphic diagnosis of a generalized rhabdomyolysis with myocardial involvement using /sup 111/In labelled antimyosin F(ab)/sub 2/ monoclonal antibodies as compared to /sup 99m/Tc pyrophosphate.

  14. Initial study with Tc99m antigranulocyte antibody (MAK-47) in detection sources of infection

    International Nuclear Information System (INIS)

    Cwikla, J.B.; Buscombe, J.R.; Hilson, A.J.; Janoki, G.A.

    1997-01-01

    Antigranulocytes antibodies (AGAB) are antibodies directed against glycoprotein on the surface of granulocytes and as such provides in vivo cell labelling. They are easily labelled with Tc99m and comes a one step labelling technique. 20 patients have been studied 1 h and 4-6 hours after administration of 200 MBq of Tc99m AGAB (MAK-47). Less then 0.5 mg of antibody was given to each patients. Sites of uptake and outside of the reticular-endothelial system were reported as showing positive accumulation. Clinical results were confirmed by microbiological, pathological examinations, clinical follow-up and autopsy. There were 8 patients who had sites of infection confirmed by additional examination. All patients were visualized by Tc99m AGAB (MAK-47). There were 4 cases of osteomyelitis and septic arthritis and 4 cases of focal intra-abdominal infection. Two patients had uptake in non-infected/inflammatory arthritis, both in the knee. The remaining patients had true negative studies. The diagnostic accuracy of this study was as follows: sensitivity 100%, specificity 83%, positive predictive value (PPV) was 80% and negative predictive value (NPV) was 100%. Antigranulocyte antibody (MAK-47) seems to by promising tool in detecting focal infection in bone and soft tissue, except physiological accumulation in some parts of the body. It should be considered that antibodies can have non-specific uptake in non-infected, inflammation sites. It is easy to use and no had allergic reaction and HAMA antibody (human antimouse antibody). (author)

  15. Experimental atheromatous plaque imaging with 99mTc labelled low density lipoproteins in rabbit

    International Nuclear Information System (INIS)

    Wang Quanshi; Chen Yu; Wu Chunshan; Zhang Yijin; Liu Dexuan

    1996-01-01

    Atheromatous plaque imaging with 99m Tc labeled low density lipoproteins ( 99m Tc-LDL) were evaluated in rabbits for its clinical prospect. The 99m Tc-LDL atheromatous plaque imaging were performed in 9 rabbit models of atherosclerosis and 4 controls. The imagings were compared with autoradiographic and pathological results. The rabbit models of atherosclerosis by high cholesterol and high fat diet were successful in 100%. The atheromatous plaques well visualized in 8 of 9 rabbit models 24 hours after injection. The site and density of radioactive accumulation was closely correlated in autoradiography also. There was no radioactive spot in 4 controls. 99m Tc-LDL imaging may have a significant value for the diagnosis of atherosclerosis

  16. Preparation of 99 sup(m)Tc labeled fibrinogen

    International Nuclear Information System (INIS)

    Almeida, M.A.T.M. de; Silva, C.P.G. da.

    1984-01-01

    A simple method for the preparation of 99 sup(m) TC labelled Fibrinogen using stannous chloride as reducing agent of 99 sup(m) TcO- 4 ion is presented. A sample of 20 mg of Fibrinogen is dissolved in 2 ml of buffer carbonate (pH=8) and 0.3 ml stannous chloride 0.2% is added. A sterile solution of sodium pertechnetate 99 sup(m) Tc eluted from a Mo-Tc generator is immediately added. The mixture rests for 30 minutes and after this period, the obtained yield is about 70%. The lyophilized kits also presented a yield of 70%, being therefore suitable for medical applications. (Author) [pt

  17. Technetium-99m labeling of antibodies to cardiac myosin Fab and to human fibrinogen

    International Nuclear Information System (INIS)

    Khaw, B.A.; Strauss, H.W.; Carvalho, A.; Locke, E.; Gold, H.K.; Haber, E.

    1982-01-01

    A method of labeling biologically active labile macromolecules, such as human fibrinogen (HF) and anticardiac-myosin Fab (AM-Fab), with Tc-99m at neutral pH was developed. This method uses dithionite reduction of pertechnetate and subsequent labeling to test the method with acid-labile macromolecules. Complexes of diethylene triamine pentaacetic acid with macromolecules such as human fibrinogen (D-HF) and anticardiac-myosin Fab (D-AM-Fab) were labeled and utilized in in vitro and in vivo studies. In biodistribution studies, the Tc-99m D-HF had a two-component blood clearance (half-times 1 hr and 15 hr) and was 80-88% coagulable. The Tc-99m AM-Fab retained its immunoreactivity as tested by affinity chromatography; also during in vivo localization in experimental myocardial infarction. This labeling technique provides an easy and efficient approach to the Tc-99m labeling of other biologically active and acid-labile macromolecules

  18. Milking technique of sup(99m)Tc generators and labeling efficiencies

    International Nuclear Information System (INIS)

    Salehi, N.; Guignard, P.A.

    1985-01-01

    Increased levels of 99 Tc in generator produced sup(99m)Tc have an adverse effect on the labelling efficiency of red blood cells and human serum albumin. A two-step milking technique in which the first 1-2 ml of eluate is discarded has been found to produce higher and more constant labelling efficiency of lymphocytes and platelets than a one-step procedure. Binding efficiency of platelet-rich plasma and lymphocytes with sup(99m)Tc is greater in the two-step technique. High activity concentration in the eluate for critical labelling is between 1.5-3 ml. (U.K.)

  19. Radioimmunoscintigraphy of experimental internal carotid arterial thrombi in dogs with 99mTc-labelled monoclonal anti-activated platelet antibody SZ-51

    International Nuclear Information System (INIS)

    Bao Shiyao; Li Wen; He Guangren; Shao Guofu; Zhang Zhilin; Wu Jinchang

    1995-05-01

    The capacity of McAbSZ-51, which is specific for an α-granule membrane protein (GMP-140) expressed on the surface of activated platelets, to bind to the grafted human thrombus in rabbits was studied. The feasibility of imaging thrombus with 99m Tc-labelled McAbSZ-51 in the internal carotid artery of dog was also explored. The results showed that McAbSZ-51 could bind to the grafted human thrombus in rabbits. The thrombus in internal carotid artery was clearly discerned at 2 to 6 h after injection of 99m Tc-SZ-51, with the optimal imaging time at 2 to 4 h after injection. The radioactivity ratio of thrombus to blood was 6.03 +- 1.09 at 6 to 8 h after injection. It is thus concluded that by using the 99m Tc-labelled McAbSZ-51, the early and specific detection of thrombi formed in vivo was fairly possible and feasible. (3 figs., 1 tab.)

  20. Diagnosis of colorectal carcinomas and recurrence with 99m Tc labeled monoclonal anti-CEA-antibody (BW 431/26)

    International Nuclear Information System (INIS)

    Lind, P.; Langsteger, W.; Koeltringer, P.; Eber, O.; Beham, A.

    1989-01-01

    With the introduction of 99m Tc labeled monoclonal antibodies against CEA, a clinically relevant extension can be expected in the diagnosis of colorectal tumors by immunoscintigraphy (IS). This study comprises a total of 31 patients (primary tumors, occult neoplasms with elevated CEA serum level, suspicious recurrences). In primary tumors (n = 14), all coloscopically diagnosed carcinomas were confirmed and correctly localised by IS (n = 8). In 4 cases IS was true negative, in one case false positive; in one patient a stomach adenocarcinoma could be demonstrated. In the diagnosis of recurrences (n = 17) IS revealed an uptake in TCT (transmission computed tomography) and coloscopically suspicious areas in 10 cases. In 6 cases IS was negative (5 true negative findings in scar or granulation tissue, 1 false negative finding in paraaortal lymphnodes). In one patient the raised CEA level was due to multiple liver metastases, a local recurrence could not be detected. Elevated serum CEA-levels were found only in 10 of 19 patients with true positive IS. In postoperative cancer care IS with 99m Tc-labeled anti-CEA antibody (MAK BW 431/26) plays a preeminent role in the exclusion or diagnosis of kolorectal recurrences in case of ambiguous TCT or endoscopic findings. (Author)

  1. 99mTc labelled peptides for imaging of peripheral receptors. Final report of a co-ordinated research project. 1995-1999

    International Nuclear Information System (INIS)

    2001-04-01

    99m Tc radiopharmaceuticals have remained the workhorse of diagnostic nuclear medicine over the last three decades ever since the introduction of the gamma camera as the main imaging instrument. Due to the near ideal nuclear properties such as gamma energy, half-life, lack of beta radiation and easy availability as a convenient generator system at an affordable cost of 99m Tc, it can be reasonably anticipated that 99m Tc will continue to retain this position in the foreseeable future. To a large extent this has been possible because of the successful development, over the years, of 99m Tc radiopharmaceuticals as substitutes for other clinically well established agents. Examples of these success stories are 99m Tc substitutes for 131 I hippuran and rose bengal 201 Tl and 123 I brain perfusion agents, which have come to be known collectively as 'second generation 99m Tc radiopharmaceuticals'. It should be acknowledged that each one of these developments was a result of innovative and sustained research and development efforts by scientists from different parts of the world. Concurrently these research efforts have made significant contributions to better understanding of the radiochemistry and co-ordination chemistry of 99m Tc. The radiopharmaceutical scientists are now in a much better position to design, prepare and evaluate 99m Tc complexes for specific applications. Building on this capability, the next step is development of 99m Tc substitutes for receptor specific radiopharmaceuticals, which have established clinical potential. Efforts in this direction are already ongoing and the work during the last decade on 99m Tc labelling of monoclonal antibodies can be considered the beginning of these 'third generation 99m Tc radiopharmaceuticals'. The International Atomic Energy Agency (IAEA) had organized two co-ordinated research projects (CRPs) in the past covering 99m Tc second generation agents and 99m Tc monoclonal antibodies, and the results were published in

  2. Current diagnostic efficacy of Tc-99m-labeled antitumor antibodies

    International Nuclear Information System (INIS)

    Morrison, R.T.; Lyster, D.M.; Szasz, I.; Alcorn, L.N.; Rhodes, B.A.; Breslow, K.; Burchiel, S.W.

    1983-01-01

    The authors have recently evaluated technetium 99 labeled antibodies specific to human chorionic gonadotropin (hCG) for the in vivo detection of a variety of human tumors. Both mouse monoclonal and sheep polyclonal antibodies were evaluated in this study. Another antibody specific to hCG studied, is an antigen-agglutinating monoclonal F(ab') 2 fragment. Some preliminary results are reported

  3. Inflammation Scan Using {sup 99m}Tc-HMPAO Labelled Leukocytes

    Energy Technology Data Exchange (ETDEWEB)

    Yang, Woo Jin; Chung, Soo Kyo; Shinn, Kyung Sub; Bahk, Yong Whee; Kim, Hoon Kyo [Catholic University College of Medicine, Seoul (Korea, Republic of)

    1989-07-15

    Inflammation scan using radiolabelled leukocytes has high sensitivity and specificity. Several methods for labelling leukocytes have been evaluated using P-32 diisopropyl fluorophosphate (DFP -32), H-3 thymidine, Cr-51 chromate, Ga-67 citrate and {sup 99m}Tc-sulfur colloid. In-111-oxine has proved so far to be the most reliable agent for labelling leukocytes. In-111-oxine is, however, expensive, not easily available when needed, and its radiation dose to leukocytes is relatively high. Moreover, resolution of the resultant image is relatively poor. {sup 99m}Tc is still the agent of choice because of, as compared with the indium, its favorable physical characteristics, lower cost and availability. Now the technique for labelling the leukocytes with technetium is successfully obtained using the lipophilic HMPAO with higher efficiency for granulocytes than for other cells. With this technique it is possible to label leukocytes in plans to improve the viability of the leukocytes. Inflammation scan using {sup 99m}Tc-HMPAO has been evaluated in several laboratories, and difference in methods for separation and labelling accounts for difference in efficiency, viability and biodistribution of the labelled leukocytes. We performed inflammation scan using leukocytes labelled with {sup 99m}Tc-HMPAO in three dogs 24 hours after inoculation of live E. Coli and S. Aureus in their right abdominal wall. We separated mixed leukocytes by simple sedimentation using 6% hetastarch (HES) and labelled the leukocytes with {sup 99m}Tc-HMPAO in 20% cell free plasma diluted with phosphate buffer solution. Uptake was high in the liver and spleen but is was minimal in the lungs on whole body scan. Kidneys and intestine showed minimal activity although it was high in the urinary bladder. Uptake of labelled leukocytes in the inflammation site was definite on 2 hour-postinjection scan and abscess was clearly delineated on 24 hour-delayed scan with high target-to-nontarget ratio. 4). Inflammation

  4. Rapid noninvasive detection of experimental atherosclerotic lesions with novel 99mTc-labeled diadenosine tetraphosphates

    Science.gov (United States)

    Elmaleh, David R.; Narula, Jagat; Babich, John W.; Petrov, Artiom; Fischman, Alan J.; Khaw, Ban-An; Rapaport, Eliezer; Zamecnik, Paul C.

    1998-01-01

    The development of a noninvasive imaging procedure for identifying atherosclerotic lesions is extremely important for the clinical management of patients with coronary artery and peripheral vascular disease. Although numerous radiopharmaceuticals have been proposed for this purpose, none has demonstrated the diagnostic accuracy required to replace invasive angiography. In this report, we used the radiolabeled purine analog, 99mTc diadenosine tetraphosphate (Ap4A; AppppA, P1,P4-di(adenosine-5′)-tetraphosphate) and its analogue 99mTc AppCHClppA for imaging experimental atherosclerotic lesions in New Zealand White rabbits. Serial gamma camera images were obtained after intravenous injection of the radiolabeled dinucleotides. After acquiring the final images, the animals were sacrificed, ex vivo images of the aortas were recorded, and biodistribution was measured. 99mTc-Ap4A and 99mTc AppCHClppA accumulated rapidly in atherosclerotic abdominal aorta, and lesions were clearly visible within 30 min after injection in all animals that were studied. Both radiopharmaceuticals were retained in the lesions for 3 hr, and the peak lesion to normal vessel ratio was 7.4 to 1. Neither of the purine analogs showed significant accumulation in the abdominal aorta of normal (control) rabbits. The excised aortas showed lesion patterns that were highly correlated with the in vivo and ex vivo imaging results. The present study demonstrates that purine receptors are up-regulated in experimental atherosclerotic lesions and 99mTc-labeled purine analogs have potential for rapid noninvasive detection of plaque formation. PMID:9435254

  5. Technetium-99m labelling of monoclonal antibodies for in vivo radioimmunodiagnostic use

    International Nuclear Information System (INIS)

    Beyers, M.

    1988-01-01

    The strong chelating agent diethylenetriaminepentaacetate (DTPA), either as the bicyclic or as the mixed anhydride, is most commonly used to link Tc-99m to proteinaceous compounds. A method for the batch production of DTPA-labelled antibody kits as well as a novel method of DTPA chelation of unpurified ascites fluid is given. Loss of immunoreactivity and in vivo stability occurs with this method. That DTPA conjugation is not the ideal method of labelling, is borne out by the fact that Hnatowich - a pioneer of DTPA-protein chelating - changed to an avidin-biotin labelling system. Modifications of the carbohydrate moiety have also been attempted. High molecular mass polymers with chelate-linkage to the antibodies can bind up to 150 di- or trivalent ions per mole without a loss in antigen-binding activity. Other than DTPA, several chelating agents such as bisthiosemicarbazones, metallothionein and diamide dimercaptide ligands may be used. The simple treatment of a proteinaceous substance with a disulpide-reducing agent, followed by exposure of the reduced protein to a suitable radionuclide, leads to a promising stable radiolabelled product. A Tc-99m-labelled antibody is, subject to FDA approval, scheduled for released by a Kodak-financed company in the near future

  6. Liver hemangioma: diagnosis with double 99mTc labelling

    International Nuclear Information System (INIS)

    Piga, M.; Satta, L.; Loi, G.; Careddu, A.; Corrias, N.; Montaldo, C.; Schiffini, P.; Dore, F.; Madeddu, G.

    1990-01-01

    The authors report on their experience with liver hemangioma (LH) diagnosis by means of a semplified method- that is, the simultaneous, in vivo, double labelling of liver reticuloendothelial system (RES) and of red blood cells (RBC) by 99m Tc. Twenty-eight patients with US diagnosis of suspected LH and 15 controls were examined after sequential iv injection of SnCl 2 , of 99m Tcμcolloid albumin and, after liver scintigraphy, of 99m Tc-pertechnetate to conclude in vivo RBC labelling. All patients underwent CT and, if necessary, CT-guided biopsy. Focal colloid defects were shown in 6/28 cases (expansive process). 15/15 controls showed unchanged non-filling defects after double labelling. Finally, the authors point out that, in the diagnosis of LH, sequential double labelling of liver RES and RBC appears to be a quicker scintigraphic techique than conventional ones. Moreover, this technique has the same high specificity and sensitivity as more time-consuming ones

  7. Click chemistry for [99mTc(CO)3] labeling of Lys3-bombesin

    International Nuclear Information System (INIS)

    Ferro-Flores, G.; Rivero, I.A.; Santos-Cuevas, C.L.; Sarmiento, J.I.; Arteaga de Murphy, C.; Ocampo-Garcia, B.E.; Garcia-Becerra, R.; Ordaz-Rosado, D.

    2010-01-01

    99m Tc-HYNIC labeled Lys 3 -bombesin has shown specific binding to gastrin-releasing peptide receptors (GRP-r) over-expressed in cancer cells. Click chemistry offers an innovative functionalization strategy for biomolecules such as bombesin. The aim of this research was to apply a click chemistry approach for [ 99m Tc(CO) 3 ] labeling of Lys 3 -bombesin and to compare the in vitro MCF7 breast cancer cell uptake and biodistribution profile in mice with that of 99m Tc-EDDA/HYNIC-Lys 3 -bombesin. The results suggest a higher lipophilicity for 99m Tc(CO) 3 -triazole-Lys 3 -bombesin which explains its higher in vivo hepatobiliary elimination. Pancreas-to-blood ratio for 99m Tc(CO) 3 -triazole-Lys 3 -bombesin was 4.46 at 3 h and both bombesin radiopharmaceuticals showed specific recognition for GRP receptors in MCF7 cancer cells. Click chemistry is a reliable approach for [ 99m Tc(CO) 3 ] labeling of Lys 3 -bombesin.

  8. Chemical aspects of labeling sucralfate with /sup 99m/TcO/sub 4/

    Energy Technology Data Exchange (ETDEWEB)

    Billinghurst, M.W.; Abrams, D.N.; Lawson, M.S.

    1989-04-01

    Two formulations of (/sup 99m/Tc)sucralfate have been used to image gastric and duodenal ulcers and inflammatory bowel disease. One formulation is a complexation of (/sup 99m/Tc)HSA with sucralfate. The second is prepared by directly labeling sucralfate with (/sup 99m/Tc)pertechnetate in the presence of stannous ion. An in vitro study of the factors affecting the production and stability of these labeled sucralfate preparations was conducted. Both formulations were stable at the acidic pH likely encountered in the stomach. However, at pH greater than 6 the albumin-sucralfate complex began to dissociate while directly labeled sucralfate was stable to a pH of 9. Conversely it was shown that directly labeled sucralfate was more susceptible to loss of /sup 99m/Tc to other chelating species. Sucralfate complexed with (/sup 99m/Tc)HSA was radiochemically stable up to a specific activity of 26 GBq (700 mCi) per gram while directly labeled sucralfate showed decreased 24-hr stability at specific activities greater than 837 mCi (31 GBq) per gram.

  9. 99mTc-N4-[Tyr3]Octreotate Versus 99mTc-EDDA/HYNIC-[Tyr3]Octreotide: an intrapatient comparison of two novel Technetium-99m labeled tracers for somatostatin receptor scintigraphy.

    Science.gov (United States)

    Gabriel, Michael; Decristoforo, Clemens; Maina, Theodosia; Nock, Berthold; vonGuggenberg, Elisabeth; Cordopatis, Paul; Moncayo, Roy

    2004-02-01

    Tetraamine-[Tyr3]octreotate (Demotate) is a somatostatin (SST) analogue that can be easily labeled with 99mTc at high specific activities and showed promising preclinical properties for SST receptor scintigraphy. This study reports on the first intra-patient comparison of 99mTc-Demotate and another 99mTc-labeled SST analogue, 99mTc-EDDA/HYNIC-TOC (HYNIC-TOC). Five patients with carcinoid tumors (n = 2) and endocrine pancreatic tumors (n = 3) were investigated with both radiopharmaceuticals. 99mTc-Demotate rapidly visualized somatostatin receptor positive tumors as early as 15 minutes post-injection (p.i.) with maximum tumor uptake and tumor/organ ratios already 1 hour p.i. Organs of predominant physiological uptake were the spleen and the kidneys with no intestinal excretion detectable up to 24 hours. 99mTc-Demotate exhibited faster pharmacokinetic properties compared to HYNIC-TOC. Tumor/organ ratios at equivalent time points were higher or comparable for 99mTc-Demotate in three patients with a matching scan result. Equivocal findings were observed in two patients, i.e. comparable uptake behavior in larger lesions with differences in smaller ones. 99mTc-Demotate is a promising agent for somatostatin receptor scintigraphy providing images of excellent quality as early as 1 hour after injection.

  10. Ciprofloxacin-99mTc: labeling and biodistribution in infection diagnostic

    International Nuclear Information System (INIS)

    Martins, Patricia de Andrade

    2004-01-01

    Labeling and biodistribution studies with the antibiotic ciprofloxacin were done using as radio marker Tc-99m. The aims were to optimize the labeling procedures as well as to analyze its efficacy in the diagnosis of infection sites, healthy and experimentally infected animals were employed to this purpose. On basis of optimized parameters a freeze-dried could be formulated containing 2 mg ciprofloxacin, 30 μg SnCl 2 H O and 5 mg ascorbic acid. This preparation could be easily activated by the addiction of Na 99m Tc) 4 a maximum value of 3700 MBq after a reaction time of 10 minutes only. Yield of the labeling technique higher than 95%, radiochemical stability reached 6 hours after preparation, and shelf life till 2 months was demonstrated. Biodistribution investigations revealed high renal excretion, low concentration in liver and soft tissues, along with affinity for the bacterial focus 1.7-2.4 times higher than for normal tissues. This protocol demonstrated the potential of ciprofloxacin- 99m Tcs a diagnostic agent for infections process. (author)

  11. Preparation and Evaluation of 99mTc-labeled anti-CD11b Antibody Targeting Inflammatory Microenvironment for Colon Cancer Imaging.

    Science.gov (United States)

    Cheng, Dengfeng; Zou, Weihong; Li, Xiao; Xiu, Yan; Tan, Hui; Shi, Hongcheng; Yang, Xiangdong

    2015-06-01

    CD11b, an active constituent of innate immune response highly expressed in myeloid-derived suppressor cells (MDSCs), can be used as a marker of inflammatory microenvironment, particularly in tumor tissues. In this research, we aimed to fabricate a (99m)Tc-labeled anti-CD11b antibody as a probe for CD11b(+) myeloid cells in colon cancer imaging with single-photon emission computed tomography (SPECT). In situ murine colon tumor model was established in histidine decarboxylase knockout (Hdc(-/-)) mice by chemicals induction. (99m)Tc-labeled anti-CD11b was obtained with labeling yields of over 30% and radiochemical purity of over 95%. Micro-SPECT/CT scans were performed at 6 h post injection to investigate biodistributions and targeting of the probe. In situ colonic neoplasma as small as 3 mm diameters was clearly identified by imaging; after dissection of the animal, anti-CD11b immunofluorescence staining was performed to identify infiltration of CD11b+ MDSCs in microenvironment of colonic neoplasms. In addition, the images displayed intense signal from bone marrow and spleen, which indicated the origin and migration of CD11b(+) MDSCs in vivo, and these results were further proved by flow cytometry analysis. Therefore, (99m)Tc-labeled anti-CD11b SPECT displayed the potential to facilitate the diagnosis of colon tumor in very early stage via detection of inflammatory microenvironment. © 2014 John Wiley & Sons A/S.

  12. Successful labeling of 99mTc-MDP using 99mTc separated from 99Mo produced by 100Mo(n,2n)99Mo

    International Nuclear Information System (INIS)

    Nagai, Yasuki; Hatsukawa, Yuichi; Kin, Tadahiro; Hashimoto, Kazuyuki; Motoishi, Shoji; Konno, Chikara; Ochiai, Kentaro; Takakura, Kosuke; Sato, Yuichi; Sato, Norihito; Ohta, Akio; Yamabayashi, Hisamichi; Tanase, Masakazu; Fujisaki, Saburo; Kawauchi, Yukimasa; Teranaka, Tomoyuki; Takeuchi, Nobuhiro; Igarashi, Takashi

    2011-01-01

    We have for the first time succeeded in separating 99m Tc from a MoO 3 sample irradiated with accelerator neutrons free from any radioactive impurities and in formulating 99m Tc-methylene diphosphonate ( 99 mTc-MDP). 99 Mo, the mother nuclide of 99m Tc, was produced by the 100 Mo(n,2n) 99 Mo reaction using about 14 MeV neutrons provided by the 3 H(d,n) 4 He reaction at the Fusion Neutronics Source of Japan Atomic Energy Agency. The 99m Tc was separated from 99 Mo by sublimation and its radionuclide purity was confirmed to be higher than 99.99% by γ-spectroscopy. The labeling efficiency of 99m Tc-MDP was shown to be higher than 99% by thin-layer chromatography. These values exceed the United States Pharmacopeia requirements for a fission product, 99 Mo. Consequently, a 99m Tc radiopharmaceutical preparation formed by using the mentioned 99 Mo can be a promising substitute for the fission product 99 Mo, which is currently produced using a highly enriched uranium target in aging research reactors. A longstanding problem to ensure a reliable and constant supply of 99 Mo in Japan can be partially mitigated. (author)

  13. Study of the viability of technetium-99m labeling of whole antimyosin antibody and its fragment: development of radiopharmaceutical for cardiac survey

    International Nuclear Information System (INIS)

    Carvalho, Guilherme Luiz de Castro

    2007-01-01

    In the acute myocardium infarction, the myocytes cell membrane loses its integrity, allowing the influx of extracellular macromolecules such as circulating antibody into the damaged cell. The use of the specific antibodies against cardiac myosin labeled with 99m Tc allows to determine the localization and extension of myocardial infarction. The purpose of this work was to study the viability of labeling of the antimyosin monoclonal antibody and its fragment F(ab')2 with 99m Tc. Because of the high cost of antimyosin antibody, others antibodies were used to optimize the methodology and the best condition was used for antimyosin antibody. The intact antibody was cleaved by pepsin to produce F(ab') 2 fragment. The F(ab') 2 and the intact antibody were reduced by treatment with Dithiothreitol (DTT) and 2-Mercaptoethanol (2-ME) and labeled with 99m Tc by direct method. Different concentrations of reductant, mixing conditions and incubation times were studied. In the standard condition, incubation at molar ratio 1:1000 (antibody:reducing agent) at room temperature for 30 minutes with continuous rotation (850 rpm), 13.28 - SH groups were formed per molecule. It was studied the influence of p H, of the concentration of stannous chloride (Sn 2+ ) and incubation time in the labeling condition. The better radiochemical yield (90.06 +- 1.53%) was obtained using 2.5 μg of Sn 2+ in p H 4.5 for 60 minutes. The labeling of the fragment F(ab') 2 did not present satisfactory results because of the low yield of the digestion. After purification by PD-10, the biodistribution study was performed and showed that the intact antimyosin antibody labeled with 99m Tc presented fast kinetic compatible with the biodistribution of an intact antibody labeled with 99m Tc. Scintigraphy image of the animal with myocardial infarction was obtained and compared with the image of a normal animal. The studies allow to conclude that the use of fragment F(ab') 2 are not viable, but the use of the labeled

  14. A rapid chemical method of labelling human plasma proteins with sup(99m)Tc-pertechnetate at pH 7.4

    International Nuclear Information System (INIS)

    Wong, D.W.; Mishkin, F.; Lee, T.

    1978-01-01

    A successful method for labelling human plasma proteins with sup(99m)Tc-pertechnetate by chemical means is described. The labelling methodology involves the production of Sup(99m)Tc-(Sn)citrate complex species with high protein binding capacity at pH 7.4 condition following initial chemical reduction of sodium sup(99m)Tc-pertechnetate by stannous chloride. A combined labelling efficiency range of 95-99% for sup(99m)Tc-labelled fibrinogen, immune gamma globulin and serum albumin is achieved. The actual amount of labelled protein content in the product is found to be 85-95% when assayed by ITLC and 74-85% by TCAA protein precipitation. In vitro experimental data indicate that sup(99m)Tc-fibrinogen contains an average of 85% clottable protein with an average clottability of 95%. This strongly suggests that the radioactive proteins retain much of their biological and physiological activities after the labelling process. (author)

  15. A new method for 99mTc-labelling of proteins, leucocytes and platelets for nuclear medicine application

    International Nuclear Information System (INIS)

    Sundrehagen, E.

    1984-01-01

    A reduced state of 99mTc was obtained by concentrated hydrocloric acid treatment of the 99mTc(VII)/0.15 M NaCl eluate from 99Mo/99mTc generators. Non-acidic reduced state of 99mTc in dry NaCl deposit was obtained by vacuum evaporation of concentrated HCl and water. A monitored vacuum evaporator built for this purpose is presented, as well as methods of formation of various 99mTc-protein and 99mTc-polypeptide complexes. After careful protein precipation or anionic adsorption of pertechnetate and 99mTc-gentisic acid complexes, high radiochemical purities of labelled proteins were demonstrated by gel chromatography studies, radioimmunological methods, radioaffinity testing studies and ampholyte displacement radiochromatography. Preparative methods for 99mTc-plasmin (at pH=2), 99mTc-secretin (at pH=3) and 99mTc-IgG (at pH=4) are presented. The role and the limitations of 99mTc-plasmin for diagnosis of deep vein thrombosis were investigated in experimentally induced jugular vein thrombosis in rabbits. The in vivo distribution of intravenously injected 99mTc-secretin was found to be in correspondance with that of unlabelled secretin. Labelling of platelets and leucoytes from human blood with 99mTc was carried out at pH=7.2. Data for a remarkable high stability of the labelled cells are presented

  16. Lymphoma imaging with a new technetium-99m labelled antibody, LL2

    International Nuclear Information System (INIS)

    Murthy, S.; Sharkey, R.M.; Goldenberg, D.M.; Lee, R.E.; Pinsky, C.M.; Hansen, H.J.; Burger, K.; Swayne, L.C.

    1992-01-01

    The lesion detection capability of a new technetium-99m labelled B-cell lymphoma monoclonal antibody (MoAb) imaging agent, LL2, was evaluated in 8 patients with non-Hodgkin's lymphoma and 1 patient with chronic lymphocytic leukaemia. The MoAb kit consists of a 1-vial, 1-mg Fab' form of LL2 ready for instant labelling with technetium. The patients were injected with ∝925 MBq (25 mCi) of 99m Tc-LL2 Fab' (1 mg), and planar and single photon emission tomography (SPET) studies were performed at 3-4 h post injection and at 24 h. There was no evidence of thyroid or stomach activity up to 24 h. Uniform splenic uptake was seen in all patients. Two non-lymphoma patients were also administered with the same agent and demonstrated a similar splenic distribution; therefore, splenic targeting was not scored as tumour-specific. A total of 29 from 48 tumour sites were detected by scintigraphy, including tumours of various grades and histological types. Excluding 1 patient who had a large tumour burden of over 500 g, 29 of 33 lesions were detected. One patient was free of disease at the time of the study and had a negative scan. Another patient showed excellent targeting of gallium-negative sites in the liver and bone. The bone involvement was not known prior to the antibody study and was subsequently confirmed by a bone scan. Additional sites of MoAb localization could not be followed in this group, since most patients went on to radioimmunotherapy immediately following the 99m Tc-LL2 study. However, these initial results suggest that this new 99m Tc-labelled antibody imaging kit should be further investigated for its potential role in the staging and follow-up of lymphoma patients. (orig.)

  17. Studies of labelling conditions for gentamicin with99mTc Biological uptake

    International Nuclear Information System (INIS)

    Carvalho, O.G. de; Almeida, M.A.T.M. de; Muramoto, E.

    1989-10-01

    Gentamicin sulphate is an aminoglycoside antibiotic type specifically used for treatment of infections produced by Gram-negative bacterias but on the hand it presents ototoxic reactions as a serious side effect. The optimal labelling conditions of gentamicin sulphate with 99m Tc, using sodium pertechnetate solutions eluted from a 99 Mo - 99m Tc generator, were stablished by testing differents masses of antibiotic and reducing agent (SnCl 2 .2H 2 O), and also different reaction times and final labelling pH. The labelling yields were determined through ascendent type crimatographic analysis using metylacetone and 0,9% NaCl solution as solvents. From the studies of the biological uptake of 99m Tc gentamicin sulphate per gram of eight different organs and tissues from Wistar rats, it was shown that for a dose of 0,3 mg of 99m Tc-gentamicin intravenously administered. The kidneys, presented the greatest affinity for the drug, being thus the main excretory organs of the product. (author) [pt

  18. Blood cell labeling with technetium-99m. II. Measurement of circulating blood volume by sup(99m)Tc-labeled red blood cells

    Energy Technology Data Exchange (ETDEWEB)

    Uchida, T; Yoshida, H; Matsuda, S; Kimura, H; Miura, N [Fukushima Medical Coll. (Japan)

    1978-02-01

    Using a labeling method with sup(99m)Tc-pertechnetate to red blood cells (RBC), circulating blood volume was measured in comparison with that from /sup 51/Cr-labeled RBC method. The technique is easier than already published methods, because CIS kit for sup(99m)Tc-RBC labeling (TCK-11) became to be available recently. Two mls of ACD-anticoagulated blood were withdrawn and 0.5 ml of reducing reagent prepared just before use was added to blood, waiting 5 minutes and discarding the serum after centrifugation, then adding 100 ..mu..Ci of sup(99m)Tc. After washing the labeled cells by isotonic saline, cells were re-suspended in 10 ml of saline and injected to the subject. Blood specimen was obtained 10, 30, 60 and 120 minutes after infusion and blood volume was calculated by the usual way. Circulating blood volume by sup(99m)Tc was well correlated with that by /sup 51/Cr (=0.98, p 0.01), however, the value calculated from sup(99m)Tc were 4.8 percent higher than those by /sup 51/Cr, which suggested the elution of sup(99m)Tc from labeled RBC. sup(99m)Tc method has the advantages that higher radioactivity can be obtained in small amount of blood, which is useful in the determination of blood volume in children or in small animals in the laboratory. The measurement of blood volume of the mouse was done by using sup(99m)Tc method. The results were 1.70 +- 0.06 ml (6.35 +- 0.18%/gm), which coincided with the values reported previously. Because of it's short half life and low radiation dosage to the patients, sup(99m)Tc method will be recommended in the field of pediatrics or in patients with polycythemia or congestive heart failure, who are requested the repeated measurement of blood volume.

  19. Gel chromatographic behavior of Tc-99m-labeled compounds in aqueous solution

    International Nuclear Information System (INIS)

    Suzuki, T.; Wagner, H.N. Jr.; Burns, H.D.; Dannals, F.F.

    1984-01-01

    The purpose of this study was to elucidate the interaction of Tc-99m-labeled compounds (Tc-99m 0/sub 4/-bar, Tc-99m glucoheptonate, Tc-99m DTPA, Tc-99m disofenin) with the chromatographic gels, to determine their relative molecular sizes and molecular structures in aqueous solution, which are based on their biomenbrane transport mechanism and quality control analysis. Each Tc-99m-labeled compound was eluted and analyzed by three different gel chromatrography systems varying buffers: Sephadex G-25, Sephadex LH-20 and Bio-Gel P-4. The best separation between the elution peaks of all compounds except Tc-99m glucoheptonate was achieved on Sephadex G-25 in methanol-0.025OM Tris-HCL buffer (pH 7.6) (1:1) which could avoid the aromatic interaction with the gels. Tc-99m glucoheptonate was well eluted only on a Bio-Gel P-4 column but its elution peak was not separated from other compounds' peaks. The elution of Tc-99m disofenin was delayed on Sephadex G-25 gel and Bio-Gel P-4 columns in 0.9% NaCl and Tris-HCl buffer(ph 7.6) and on Sephadex LH-20 column in methanol-Tris-HCl buffer, because of the aromatic ring interaction with the gels. The relative molecular size index ( Kav ) calculated from the elution volume of the gel chromatography. Kav of Tc-99m 0/sub 4/-bar(MW=163), Tc-99m DTPA (MW=492?) and TC-99m disofenin (MW=707) on Sephadex G-25 in methanol-0.025OM Tris-HCl buffer(pH 7.6) (1:1), which was the most suitable combination of the gel and the buffer, were 0.976, 0.477 and 0.200, respectively. They inversely correlated with their estimated molecular weight. The interaction of Tc-99m-labeled compounds with the chromatographic gels should be considered in quality control procedure for Tc-99m radiopharamaceuticals

  20. Biodistibution of 2,6 diisopropyliminodiacetic acid 99mTc (Disida-99mTc) in normal rats and with experimental hepatic lesion

    International Nuclear Information System (INIS)

    Colturato, M.T.; Muramoto, E.; Hamada, E.S.; Barbosa, M.R.F. de; Herrerias, R.; Silva, C.P.G. da.

    1988-07-01

    The biodistribution and elimination of 99m Tc-DISIDA were examined by performing scintigrams on rats at different times. Normal animals (rats) and those with experimental hepatobiliary alterations were used. Results showed a delayed clearance of 99m Tc-DISIDA into the small intestine of the experimental animals. The elimination of the labelled compound by the kidney was 14% dose/g 120 minutes after the injection of which 70% was found in its original form. The data indicate that in spite the compound is intact in bile it undergoes a degradative process, not yet known. (author) [pt

  1. 99mTc-EDTA and 99mTc-DTPA complexes as hydrological tracers

    International Nuclear Information System (INIS)

    Dominguez, J.; Borroto, J.; Nazco, J.; Perez, E.; Gamboa, R.; Cruz, J.

    2002-01-01

    The [ 99m Tc-DTPA] 2- and [ 99m Tc-EDTA] 1- were evaluated as radiotracers for short time hydrological studies. Their complex stability after labelling with 9.25 GBq of 99m Tc, the behaviour against pH variations, from 5 to 9, in simulated solutions and in natural river waters and the sorption of these compounds on the river sediments, were tested in laboratory experiments. Finally field double tracing experiments were carried out for each of labelling complexes and Rhodamine WT. From recovery calculations not losses of the 99m Tc activity were observed. The shape of the RTD curves of the [ 99m Tc-DTPA] 2- and [ 99m Tc-EDTA] 1 were quite similar to the Rhodamine Wt ones. May be concluded that both complexes behaved conservatively on the studied environmental conditions. (author)

  2. Influence of iron deficiency in the radiopharmaceutical behavior of red blood cells labeled with 99mTc(99mTC-RBC)

    International Nuclear Information System (INIS)

    Calmanovici, G.; Salgueiro, M.J.; Pernas, L.; Collia, N.; Leonardi, N.; Zubillaga, M.

    2005-01-01

    Full text: Red blood cells (RBCs) labeled with 99m Tc are commonly used in the evaluation of cardiac function, gastrointestinal tract bleeding, red blood cell volume or splenic sequestration. Generally stannous ion is used as reducing agent. A proposed mechanism is that once the stannous ion (Sn) and the pertechnetate ( 99m Tc) reach the interior of the RBC, the radionuclide is mainly house in the β-chain of hemoglobin. The aim of this study was to determine if hemoglobin content reduction, an indicator of iron deficiency anemia, could affect the efficiency of RBC labeling and the biological distribution of this radiopharmaceutical. We studied 30 rats fed for 3 weeks after weaning with diets with iron contents of 6.5 ppm (group A), 18 ppm (group B) and 100 ppm (control). For all groups, the labeling yields were always higher than 97%; the percentage of radioactivity was mostly founded in blood with almost negligible radioactivity the rest of the studied organs. We can conclude that the decrease in hemoglobin content, an indicator of iron deficiency anemia, does not interfere neither in the labeling nor in the biodistribution of red blood cells labeled with 99m Tc. (author)

  3. Labelling and optimization of PHOTOFRIN {sup registered} with {sup 99m}Tc

    Energy Technology Data Exchange (ETDEWEB)

    Fakhar-e-Alam, M. [Pakistan Institute of Engineering and Applied Sciences, Islamabad (Pakistan); Roohi, S.; Amir, N.; Zahoor, R. [Pakistan Institute of Nuclear Science and Technology, Islamabad (Pakistan). Isotope Production Div.; Atif, M.; Firdous, S. [National Institute of Laser and Optronics, Islamabad (Pakistan). Biophotonics Lab.

    2010-07-01

    PHOTOFRIN {sup registered} was labelled with {sup 99m}Tc using SnCl{sub 2}.2H{sub 2}O as reducing agent. Instant thin layer chromatography (ITLC-SG) in 0.05 M NaOH was used for evaluation of radiochemical purity. Labelling efficiency was dependent on various factors that include the ligand/reductant ratio, pH and time of incubation. Therefore, optimum conditions of labelling were also determined. The stability of {sup 99m}Tc-PHOTOFRIN {sup registered} in serum was checked by using fresh human serum. Tissue distribution of {sup 99m}Tc-PHOTOFRIN {sup registered} was evaluated in Sprague Dawley rats. PHOTOFRIN {sup registered} was labelled with an efficiency of > 95% under optimum conditions, which were PHOTOFRIN {sup registered}: 200 {mu}g, pH: 3-4, SnCl{sub 2}.2H{sub 2}O: 15 {mu}g and 30 min incubation at room temperature. The {sup 99m}Tc-labelled PHOTOFRIN {sup registered} remained stable in human serum for 24 h. Biodistribution study in rats revealed maximum concentration of the labelled compound in liver, lungs and spleen at 0.5 h, and significant activity was also seen in the bladder and urine, indicating the mode of urinary excretion of PHOTOFRIN {sup registered}. (orig.)

  4. Immunoscintigraphy with 99Tc-labelled monoclonal anti granulocyte antibodies in patients with inflammatory bowel disease

    International Nuclear Information System (INIS)

    Klisarova, A.; Tranulov, G.

    1996-01-01

    Antigranulocyte immunoscintigraphy with 99 Tc-labelled monoclonal antigranolocyte antibodies (MAb BW 250/83, Granulozyt) was carried out in ten patients with symptoms of inflammatory bowel disease to exclude or confirm the presence of an inflammatory process. A slow iv infusion of 740 MBq of the antibodies was performed 40 minutes after labelling. A whole-body scan was done at hours 4 and 24 post injection. In four patients planar scintigraphy of abdominal region only was also performed for better visualization of the pathological findings. Immunoscintigraphy provided evidence of an inflammatory bowel process in 8 cases (true positive), and excluded the diagnosis in one case (true negative). There was one false negative result.The study shows that immunoscintigraphy with 99 Tc-labelled antibodies (Granulozyt) is an easily performed procedure, with high specificity for diagnosing inflammatory bowel disease and can be carried out as a routine practice in nuclear medicine. 7 refs., 1 tab., 4 figs. (author)

  5. Determination of radiochemical purity and pharmacokinetic parameters of sup(99m)Tc-sulphur colloid and sup(99m)Tc-tin colloid

    International Nuclear Information System (INIS)

    Jovanovic, V.; Konstantinovska, D.; Milivojevic, K.; Bzenic, J.

    1981-01-01

    Labelling yield and radiochemical purity, higher than 95%, of sup(99m)Tc-colloid preparations were determined by using the paper chromatography method. Less than 3% of labelled citric acid, added to the preparation as a buffer solution, has been found in sup(99m)Tc-sulphur colloid. High radiochemical purity and optimum size of colloid particles has also been proved by biodistribution studies on experimental animals. The analysis performed has shown that more than 50% of sup(99m)Tc-colloid preparations excreted by urine is sup(99m)TcO - , the remaining past 50% being protein bound sup(99m)Tc. Biological half-time of excretion of the fast phase is the same for both preparations, i.e. 10 min, while for the slow component it is 120 min in sup(99m)Tc-S-colloid and 160 min in sup(99m)Tc-Sn colloid. (orig.) [de

  6. Evaluation of 99mTc-Labeled Bevacizumab-N-HYNIC Conjugate in Human Ovarian Tumor Xenografts.

    Science.gov (United States)

    Shah, Syed Qaiser; Mahmood, Samia

    2018-03-20

    The aim of the present investigation was to examine the suitability of 99m Tc-N-HYNIC-BZMB as a specific vascular endothelial growth factor (VEGF)-targeting agent. Bevacizumab is a recombinant humanized monoclonal antibody that inhibits VEGF. N-hydroxysuccinimide-2-hydrazinonicotinic acid (N-HYNIC) was conjugated to BZMB, followed by labeling with 99m Tc using N-[Tris(hydroxymethyl)methyl] glycine (tricine), ethylenediamine-N,N'-diacetic acid (EDDA), and nicotinic acid as coligands. 99m Tc-labeled BZMB was characterized in terms of 99m TcO 4 , radiocolloids, and labeled N-HYNIC-BZMB using thin-layer chromatography and HPLC. Poor metastatic SKOV-3 and high metastatic SKOV-3.ip1 human ovarian cancer cell lines were used for in vitro binding uptake of 99m Tc-N-HYNIC-BZMB. Biodistribution and scintigraphy accuracy were examined in human ovarian tumor xenografts in rats and rabbits. 99m Tc-N-HYNIC-BZMB prepared by using a mixture of tricine and EDDA demonstrated relatively high radiochemical purity (more than 98%). In L-cysteine and serum, it exhibited a stable behavior up to 16 hours. In vitro binding uptake indicated that it targets high metastatic SKOV-3.ip1 tumors. Biodistribution in human ovarian tumor xenografts in rats confirmed a significant uptake in SKOV-3.ip1 tumors (5.69% ± 1.86%, 4 hours). Scintigraphic accuracy in human ovarian tumor xenografts in rabbits validated its suitability as a high metastatic SKOV-3.ip1 radiotracer. High radiochemical purity, stability in saline and serum, biodistribution, and scintigraphy of 99m Tc-N-HYNIC-BZMB in human ovarian tumor xenografts in rats and rabbits confirmed its suitability as a potential radiotracer for imaging high metastatic SKOV-3.ip1 sites.

  7. Radioimmunoscintigraphy of colorectal carcinoma using technetium-99m-labeled, totally human monoclonal antibody 88BV59H21-2.

    Science.gov (United States)

    Gulec, S A; Serafini, A N; Moffat, F L; Vargas-Cuba, R D; Sfakianakis, G N; Franceschi, D; Crichton, V Z; Subramanian, R; Klein, J L; De Jager, R L

    1995-12-01

    Radioimmunoscintigraphy (RIS) using human monoclonal antibodies offers the important clinical advantage of repeated imaging over murine monoclonal antibodies by eliminating the cross-species antibody response. This article reports a Phase I-II clinical trial with Tc-99m-labeled, totally human monoclonal antibody 88BV59H21-2 in patients with colorectal carcinoma. The study population consisted of 34 patients with colorectal cancer (20 men and 14 women; age range, 44-81 years). Patients were administered 5-10 mg antibody labeled with 21-41 mCi Tc-99m by the i.v. route and imaged at 3-10 and 16-24 h after infusion using planar and single-photon emission computed tomographic (CT) techniques. Pathological confirmation was obtained in 25 patients who underwent surgery. Human antihuman antibody (HAHA) titers were checked prior to and 1 and 3 months after the infusion. RIS with Tc-99m-labeled 88BV59H21-2 revealed a better detection rate in the abdomen-pelvis region compared with axial CT. The combined use of both modalities increased the sensitivity in both the liver and abdomen-pelvis regions. Ten patients developed mild adverse reactions (chills and fever). No HAHA response was detected in this series. Tc-99m-labeled human monoclonal antibody 88BV59H21-2 RIS shows promise as a useful diagnostic modality in patients with colorectal cancer. RIS alone or in combination with CT is more sensitive than CT in detecting tumor within the abdomen and pelvis. Repeated RIS studies may be possible, due to the lack of a HAHA response.

  8. Preliminary studies of 99mTc labeled fatty acid analogs for myocardial imaging

    International Nuclear Information System (INIS)

    Guo Yuzhi; Kung, H.F.; Mack, R.H.

    1988-01-01

    Radio iodine labelled fatty acid analogs are potential myocardial imaging agents for SPECT. In this paper are reported three new 99m Tc labbeled fatty acid analogs: 9 '9 m Tc-BAT-TDA, 99m Tc-BAT-PDA and 99m Tc-BAT-H x DA. Ligand exchange reaction with 99m Tc stannous glucoheptonate in 50% aqueous ethanol is used for labelling. The yield of reactions is 87%, 70%, 49% respectively. 99m Tc-fatty acid is purified by extraction into chloroform and the purity as determined by reverse phase HPLC is 98%. In order to determine the structure of Tc-BAT-fatty acid, 99 Tc-BAT-PDA is synthesized with 99 Tc ammonium pertechnetate in 50% citric acid buffer (pH=6)/ethanol using stannous chloride as the reducing agent. 99 Tc-BAT-PDA displays the expected Tc=O UV absorption at 420nm and strong peak at 900cm -1 in the FTIR spectrum. Biodistribution studies of three 99m Tc-fatty acid analogs are conducted in rats using 125 I-ω- (p-iodophenyl) -penta-decanoic acid (IPPDA) as internal standard. The initial heart uptake of them is significantly lower than that of 125 I-IPPDA

  9. Analysis of 99mTc-labeled radiopharmaceuticals by high-performance liquid chromatography

    International Nuclear Information System (INIS)

    Muto, Toshio

    1990-01-01

    High-performance liquid chromatography (HPLC) equiped with on line radiometric and optical detectors (i.e. radio-HPLC) have been applied to the radiochemical analysis of commonly-used 99m Tc-radio pharma ceuticals with a view point to check the radiochemical purities of the compounds. Chromatographic conditions were determined by examination of the types of column, mobile phase and pH. An aqueous size-exclusion (Shim-pack Diol-300) and reversed-phase column (Zorbax-ODS) were found to be suitable for 99m Tc-HSA and the other 99m Tc-agents, respectively. The analysis of low molecular weight 99m Tc-agents (e.g. 99m Tc-DTPA, 99m Tc-DMSA, 99m Tc-pyrophosphate, 99m Tc-phytic acid, 99m Tc-MDS, 99m Tc-HMDP) were done by reversed-phaseion pairing chromatography using a optimized mobile phase consisted on a mixture of 50 mM phosphate buffer (pH 7.0) and 2 mM TBA (tetra nbutyl) ammonium hydroxide) in 30 % methanol. The mobile phases for analysis of medium molecular weight 99m Tc-HSA were consisted of a mixture of 50 mM phosphate buffer (ph 7.0) in 30 % methanol, and a mixtures of 1 % SDS (sodium dodecyl sulfonate) in Tris buffer (pH. 7.0), respectively. It was apparent from the radio-chromatograms obtained from these chromatographic conditions, that impurity of 99m TcO 4 was observed in 99m Tc-pyrophosphate, 99m Tc-phytic acid, 99m Tc-MDP, 99m Tc-HMDP, and impurities of 99m Tc-labeled species and 99m TcO 4 , were observed in 99m Tc-HIDA, 99m Tc-HIDA, 99m Tc-HSA. The radiochemical impurities of the 99m Tc-radiopharmaceuticals were ranged between 90 and 100 %. From these results, radio-HPLC has been shown to be suitable method for analysis of 99m Tc-radiopharmaceuticals, with rapidity and excellent precision. (author)

  10. Labelling of bilirubin with /sup 99m/Tc and pharmacokinetic behavior

    International Nuclear Information System (INIS)

    Kaempfer, I.; Schneider, G.; Blottner, A.; Deckart, H.; Staedtisches Klinikum Berlin-Buch

    1982-01-01

    The yield of the bilirubin labelling with /sup 99m/Tc amounted to 97%. The labelled complex has been stable for 24 hours with the pH range 2-7.5. As evidenced in animal experiments the labelled bilirubin is probably subjected to natural degradation processes. Side effects could not be noticed. A disadvantage seems to be the slow transfer of /sup 99m/Tc-bilirubin from the hepatic cell to the biliary capillary

  11. Technetium-99m pertechnetate - a tracer for radiolabelling antibody for inflammation detection

    International Nuclear Information System (INIS)

    Shaharuddin Mohd; Wan Hamirul Bahrin Wan Kamal; Shahrin A Hamid; Ang Woan Tze; Rosnani Hashim

    1999-01-01

    The polyclonal antibody, Human Immunoglobulin G (HlgG) was reduced by using 2-mercaptoethanol with molar ratio of 1000:1 (i.e. mercaptoethanol:antibody). The reduction of the antibody, was carried out for 30 minutes at room temperature. The reduced antibody was purified by using Sephadex G-25 fine column. The antibody kit for the detection of inflammation was prepared aseptically in Class 1 Laminar Flow cabinet. The kit passed the sterility test. Upon reconstitution of the antibody kit with sodium pertechnetate-99m ( 99m Tc) solution, the labelling efficiency obtained was more than 95%. This preparation was stable up to 24-hour stored at room temperature. Gamma camera scans showed the accumulation of technetium-99m labelled antibody ( 99m Tc-HIgG) at the turpentine-induced inflammation of female Sprague-Dawley rats. This indicated the possibility of using 99m Tc-HIgG for inflammation detection. (author)

  12. Comparative biological evaluation between 99mTc tricarbonyl and 99mTc-Sn(II) levosalbutamol as a β2-adrenoceptor agonist

    International Nuclear Information System (INIS)

    Sanad, Mahmoud H.; Borai, Emad H.

    2015-01-01

    This study describes the comparison between 99m Tc-tricarbonyl and 99m Tc-Sn (II) levosalbutamol as a β 2 -adrenoceptors radiopharmaceutical and evaluation of their different biological characteristics using experimental animals. Levosalbutamol was labeled firstly with 99m Tc in the presence of SnCl 2 . 2H 2 O as a reducing agent under the optimum conditions: pH 8, 50 μg SnCl 2 . 2H 2 O, room temperature, 40 μg levosalbutamol and 30 min reaction time to give a maximum radiochemical yield of 98 ± 0.1%. The obtained 99m Tc-levosalbutamol was stable for a time up to 8 h. Secondly, 99m Tc-tricarbonyl ([ 99m Tc(CO) 3 (H 2 O) 3 ] + ) levosalbutamol was prepare under 30 min heating at 100 C. Labeling yield and stability were analyzed by high performance liquid chromatography (labeling yield >99% and stability for 8 h). Biodistribution investigation showed that, the maximum uptake ratio of the 99m Tc-levosalbutamol ( 99m Tc-Lev) between lung and heart was 2.34 ± 0.62 % of the injected activity/g tissue organ, at 30 min post-injection. But in case of 99m Tc-tricarbonyl levosalbutamol ( 99m Tc-tricarbonyl Lev) the maximum uptake ratio was 3.6 ± 0.11 of the injected activity/g tissue organ, at 30 min post-injection. This indicates that 99m Tc-tricarbonyl levosalbutamol was more selective for lung β 2 -adrenoceptors than 99m Tc-levosalbutamol. These results introduce 99m Tc-tricarbonyl levosalbutamol as a novel potential radiopharmaceutical for lung imaging.

  13. Stabilization of Tc-99m D,L-HMPAO preparations as a leucocyte labelling agent

    International Nuclear Information System (INIS)

    Kao, C.H.; Huang, W.T.; Tsai, C.S.

    1998-01-01

    An attempt was made to use stabilized Tc-99m D,L-HMPAO (S-HMPAO) to label leucocytes. The radiochemical purity of Tc-99m D,L-HMPAO, labelling efficiency of leucocytes, cell viability of labelled leucocytes, and stability of S-HMPAO labelled leucocytes were calculated. In comparison with commercial Tc-99m D,L-HMPAO (C-HMPAO) without stabilization, immediately, at 0.5, 1, 2, 4, and 6 h after HMPAO preparation, the radiochemical purity of S-HMPAO and the labelling efficiencies of S-HMPAO labelled leucocytes were higher. S-HMPAO is more stable than C-HMPAO and can provide higher leucocyte labelling efficiency. S-HMPAO, therefore, has the potential to replace C-HMPAO as a leucocyte-labelling agent

  14. Preparation of Human Serum Albumin Macroaggregated (MAA) labelled with 99mTc via Ligand Exchange

    International Nuclear Information System (INIS)

    El-Mohty, A.A.; El-Ghany, E.A.; Amin, A.A.; El-Koaly, M.T.; Raieh, M.

    2000-01-01

    An alternative method for the preparation of human serum albumin macroaggregated (MAA) labelled with 99m Tc for lung scanning is described. The method is based on the use of stannous methylene diphosphonate (Sn-MDP) as a reducing agent. The may be also increase the number of binding sites in the MAA. The different parameters affecting the labelling yield and in-vitro stability of 99m Tc-MAA have been studied in order to determine the optimum conditions for labelling macroaggregated with 99m Tc. A high labelling yield (98.9%) was achieved and more than 98% of 99m Tc-MAA coated with Sn-MDP. The determined lung uptake in mice was found to be ≥ 90% which better than the reported data. A particular procedure compared to the existing reported procedures, which is recommended for the preparation of Sn-MDP coated MAA labelled with 99m Tc for lung perfusion imaging

  15. The labelling of antibody anti-PBP2a with {sup 99m}Tc; Estudo de marcacao do anticorpo monoclonal anti-PBP2a com {sup 99m}Tc

    Energy Technology Data Exchange (ETDEWEB)

    Mororo, Janio da Silva

    2012-07-01

    Staphylococcus aureus is a major cause of life-threatening infections such as bacteraemia and endocarditis. Unfortunately, many strains of this bacterial species have become resistant to certain antibiotics, including methicillin and amoxicillin. These strains are known as methicillin-resistant S. aureus (MRSA). The penicillin binding protein 2a (PBP2a) is the enzyme responsible for conferring resistance p-lactams antibiotics for MRSA, being one promising molecule for therapy with mAb. However, besides the therapy, the methods of diagnosis are also inefficient because the diagnosis currently takes several days to produce a reliable result. Taking into account, the objective of this research was radiolabeling one anti-PBP2a mAb developed by Bio-Manguinhos/FioCruz-RJ, utilizing {sup 99m}Tc, for in situ diagnostic of the infectious caused by MRSA. First, anti-PBP2a mAb was reduced utilizing 2-mecaptoethanol (2-ME) for generate sulphydryl groups (-SH) and after to be labeled with {sup 99m}Tc. In this work, were utilized two techniques of direct method: Method 1, using tartrate and gentisic acid reagents, acting like transchelant and stabilizer agents, respectively; and Method 2, using one commercial kit of MDP. Besides the radiolabeling, the mAb reduced and mAb labeled with {sup 99m}Tc were submitted to immunoreactivity analysis, with SDS-PAGE non-reducing, Immunoblotting, ELISA and neutralization assay in vitro methods. The quantity produced of sulphydryl groups by mAb was satisfactory, approximately 5 per mAb, utilizing 6.500:1 of 2-ME:mAb molar ratio. The better labeling method was Method 2, with labeling yield of 73.5%, and showed a good stability after 2 hours (73.2%). The better formulation was: 0.5 mg of mAb anti- PBP2a, 10 {mu}U of MDP kit, after resuspended with 5 mL of saline, and 75.48 MBq (2.04 mCi) of {sup 99m}Tc, reacting by 15 minutes. The labeled mAb maintained the immunoreactivity, utilizing immunologic and in vitro experiments. (author)

  16. Evaluation of leucocytes labelling technique with 99m Tc - HMPAO

    International Nuclear Information System (INIS)

    Moraes, D.W.; Marinho, N.S.; Rezende, M.E.X.; Buchpiguel, C.A.; Rockmann, T.M.B.

    1992-01-01

    An evaluation of the leukocytes labelling technique with HMPAO- 99m Tc, using low volume of blood and keeping the labelling efficiency and cellular viability in compatible levels with those preconized by the literature is presented. (C.G.C.)

  17. Bioavailability of {sup 99m}Tc-paclitaxel-glucuronide ({sup 99m}Tc-PAC-G)

    Energy Technology Data Exchange (ETDEWEB)

    Biber Muftuler, F.Z.; Demir, I.; Uenack, P.; Ichedef, C.; Yurt Kilcar, A. [Ege Univ., Izmir (Turkey). Dept. of Nuclear Applications

    2011-07-01

    An antitumor agent paclitaxel (PAC) has been proved to be efficient in the treatment of breast and ovarian cancer. Glucuronic acid-derived paclitaxel compound (paclitaxel-glucuronide (PAC-G)) was enzymatically synthesized using microsome preparate separated from rat livers. The biodistribution mechanism of PAC-G in healthy female Albino Wistar rats has been investigated. The expected structure is confirmed according to LC/MS results, and the possible attachment is to C2-hydroxyl group. PAC-G was labeled with {sup 99m}Tc and the radiochemical yield of radiolabeled compound ({sup 99m}Tc-PAC-G) was 98.0 {+-} 02.74% (n=9). The range of the breast/blood and breast/muscle ratios is approximately between 3 and 35 in 240 min. All these experimental studies indicate that {sup 99m}Tc-PAC-G may potentially be used in breast tissue as an imaging agent. (orig.)

  18. 99mTc labelled peptide for imaging of peripheral receptors

    International Nuclear Information System (INIS)

    Mishra, A.K.; Mishra, P.; Chuttani, K.; Sharma, R.K.; Lazar Mathew, T.

    2001-01-01

    Conjugates of somatostatin analogues, RC-160 with different bifunctional chelators to label with 99m Tc, were synthesized. Conjugates with hydrazinonicotinamide (HYNIC) and compounds (benzoyl MAG-3 and CITC-DTPA) were prepared on a small scale with high purity and evaluated as different types of chelators on RC-160. Stability studies performed under physiological conditions showed high stability. Peptide conjugates could be labelled at high specific activities (307inCi/umol) with 99m Tc and different transchelator were used for the HYNIC conjugates. The resulting radiolabelled with ( 99m Tc and 1251) complexes were highly stable and showed binding affinity to somatostatin receptors in the nanomolar range. The radioconjugates were administered to rabbits and mice in order to study their in vivo stability, biokinetics and biodistribution. (author)

  19. Labelling of m-trimethyl silylphenyl-ethylidene-1, i-bisphosphonate with /sup 99m/Tc and its evaluation as an imaging agent

    International Nuclear Information System (INIS)

    Sajid, K.M.; Mahmood, R.

    2012-01-01

    Technetium-99m labeled phosphates and phosphonates have since long been in use for bone imaging to diagnose bone infection, bone metastasis and bone fracture. /sup 131/ I -labeled bisphosphonates have also been prepared for targeted radiotherapy of bone metastasis. Although animal experiments show good accumulation of bisphosphonates in bone. The agent has never been tried in humans because of high gamma and beta energy. The agent must first be tested in humans using a relatively safe radioisotope. Technitium-99m (/sup 99m/Tc) a radioisotope with relatively low gamma energy 99m and short half-life can serve as a good label. Whether /sup 99m/Tc-labeled bisphosphonates can be used as good imaging agents is another aspect that needs further investigation. A study was therefore, conducted to label m-trimethyl silylphenyl)-ethylidene-1, 1-bisphosphonate with /sup 99m/Tc and standardize the labeling procedure. The labeling procedure - involved reduction of technetium (TcO/sub 4/) with stannous chloride followed by chelation of technetium with bisphosphonates. Radiochemical purity was checked by paper chromatography. Pyrogenicity was checked by administration of the labeled compound into rabbits. The stability of the compound was determined by noting the radiochemical binding at several intervals of half an hour after preparation. Biodistribution of the agent was studied by injecting the labeled compound into rabbits. The results showed that the compound could be labeled with /sup 99m/Tc without any difficulty. The ease of binding was excellent. There was more than 95% binding of technetium with the compound and the labelled compound was reasonably stable for 5 hours after labeling. The rectal temperature remained stable during this period, which showed that the animal accepted the compound and there were no pyrogenic reactions. Biodistribution studies on rabbit showed that accumulation of agent was poor in bones and the labeled compound remains in blood even after 4

  20. 99mTc-monoclonal antibody radiolabeled via hydrazino nicotinamide derivative for imaging disialoganglioside GD2-positive tumors

    International Nuclear Information System (INIS)

    Fonti, Rosa; Cheung, N.-K.V.; Bridger, Gary J.; Guo, H.-F.; Abrams, Michael J.; Larson, Steven M.

    1999-01-01

    3F8 is a murine IgG 3 monoclonal antibody (MAb) selective for the ganglioside G D2 . Previous studies using 131 I-3F8 have shown great potential in the imaging of neuroectodermal tumors and the therapy of human neuroblastoma. 131 I is commonly used in radioimmunodiagnosis, but its relatively long half-life (8 days) and its high energy γ-emission (364 KeV) are suboptimal for imaging purposes when compared with 99m Tc (6 h and 140 KeV, respectively). To label 3F8 with 99m Tc, the antibody was first coupled with a heterobifunctional linker, succinimidyl-6-hydrazinonicotinate hydrochloride (SHNH), obtaining a hydrazinonicotinamide-antibody conjugate. Using 99m Tc-Tricine as the precursor complex, 3F8-SHNH was coupled efficiently to 99m Tc, resulting in >90% radiometal incorporation, with a specific activity >10 mCi/mg and retaining full immunoreactivity. Immunoscintigraphy at 6, 22, and 46 h after intravenous injection of 1 mCi of 99m Tc-3F8 showed selective neuroblastoma localization in xenografted nude mice, comparable to that obtained with the injection of 100 μCi of 131 I-3F8. Biodistribution studies of 131 I-3F8 and 99m Tc-3F8 in mice demonstrated comparable %ID/g uptake in tumor (with a T/B ratio: ∼2.5 at 24 h and ∼3.5 at 48 h) and normal organs, including blood, except for spleen and liver which had about a three times higher uptake of the 99m Tc conjugate. In conclusion, 99m Tc can be coupled conveniently at high specific activity to 3F8 without compromising immunoreactivity. SHNH appears to be a useful linker for 99m Tc in tumor diagnostic imaging and may have potential utility in coupling other radioisotopes (e.g., 94m Tc) for positron imaging and therapy

  1. The new 99mTc myocardial perfusion imaging agents: 99mTc-sestamibi and 99mTc-teboroxime

    International Nuclear Information System (INIS)

    Berman, D.S.; Kiat, H.; Maddahi, J.

    1991-01-01

    The two new 99m (99mTc) labeled myocardial perfusion agents, 99mTc-Sestamibi and 99mTc-Teboroxime, are now available for routine clinical application. Both agents allow assessment of ejection fraction by the first-pass technique at rest or during exercise, thus providing additional information not available with thallium-201. 99mTc-Sestamibi has long myocardial residence time, as well as adequate myocardial extraction, providing images of higher count density and superior quality compared with thallium-201. 99mTc-Teboroxime has excellent myocardial uptake characteristics but is cleared very rapidly from the myocardium. Both tracers have shown results similar to those obtained with thallium-201 for detection of coronary artery disease and the assessment of defect reversibility. 99mTc-Sestamibi studies using the rest/stress imaging sequence can be accomplished in approximately 5 hours; studies using dual-isotope imaging (rest thallium-201 and stress 99mTc-Sestamibi injection) can be completed in 1 to 2 hours. Gated stress images can be performed with 99mTc-Sestamibi, providing simultaneous information of myocardial perfusion at stress and resting wall motion or thickening and allowing rapid differentiation of ischemic from infarcted tissue. Because of its slow myocardial clearance and absence of redistribution, 99mTc-Sestamibi allows uncoupling of the time of injection from the time of imaging and thus can be valuable in the evaluation of acute myocardial infarction and outcome of thrombolytic therapy. With 99mTc-Teboroxime, rapid serial studies are feasible. Pharmacologic stress and rest studies with 99mTc-Teboroxime single photon emission computed tomography potentially can be completed in under 30 minutes. 73 references

  2. The rabbit biodistribution of a therapeutic dose of zoledronic acid labeled with Tc-99m

    International Nuclear Information System (INIS)

    Asikoglu, Makbule; Gamze Durak, Funda

    2009-01-01

    The aim of the present study was to label a therapeutic dose of zoledronic acid (ZOL) with Tc-99m, evaluate its in vitro stability and compare its biodistribution to 99m Tc-methylene biphosphonate ( 99m Tc-MDP) in normal rabbits. Preparation of 0.50 mg of 99m Tc-ZOL was carried out by the reduction of 99m Tc-pertechnetate in the presence of stannous chloride. The radiolabeling efficiency was found to be greater than 99%. The labeled complex was stable at least up to 6 h at room temperature determined by paper chromatography. 99m Tc-ZOL and 99m Tc-MDP were administered intravenously to the rabbits for scintigraphic studies. Between 99m Tc-ZOL and 99m Tc-MDP, there were no significant differences in the ratios of femur/BG and lumbar vertebrae/BG, whereas epiphysis/BG and the kidney/BG ratios of 99m Tc-MDP were higher than 99m Tc-ZOL at the static studies.

  3. Isolation and labelling of human leucocytes with sup(99m)Tc

    International Nuclear Information System (INIS)

    Kalbaek, H.

    1986-01-01

    The role of the leucocyte isolation procedure on cell labeling with sup(99m)Tc has been evaluated. Separation of leucocytes was performed by two procedures: (1) sedimentation on methyl cellulose, followed by discontinuous gradient centrifugation; (2) methyl cellulose sedimentation and hypotonic haemolysis of residual red blood cells. After washing the cells in saline and incubation with a stannous pyrophosphate agent, the leucocytes were labelled with 5-10 mCi sup(99m)Tc. Procedure 1 gave a higher purity but lower recovery of polymorphonuclear leucocytes, and a minor contamination of red blood cells. sup(99m)Tc labelling of cells was slightly more efficient with this method, probably due to the presence of red blood cells. Procedure 1 is recommended for in vitro studies on cell kinetics and procedure 2 is recommended for clinical use. (orig.)

  4. Labelling of biological structures with technetium 99 m

    International Nuclear Information System (INIS)

    Bernardo Filho, M.

    1988-01-01

    The labelling of red blood cells (RBC) with technetium 99m ( 99m Tc) depends on several factors, as the stannous ion (Sn ++ ) concentration, the time and temperature of incubation, the anticoagulant utilized, the presence of plasma proteins (PP) and others. Although the blinding of 99m Tc with hemoglobin and PP are similar, they appear to have specific characteristics as demonstrated by precipitation with alcohol, acetone, trichloroacetic acid, hydrochloric acid and mercury chloride. The bacterial cultures labeled with Technetium- 99m , at optimal Sn ++ ion concentration, presents a large stability and their viability is not altered by this treatment. The electrophoretic mobility, the hydrophobicity, the cationized ferritin distribution and the adherence to human buccal epithelial cells are not modified either. The possibility of labelling with 99m Tc of planaria and cercariae of Schistossoma mansoni evaluative cycle increases the utilization of this radionuclide to an experimental level. The results described with the labelling of these biological structures with 99m Tc demonstrated that stable labeled and viable operations are obtained. (author)

  5. A Tc-99m-labeled long chain fatty acid derivative for myocardial imaging.

    Science.gov (United States)

    Magata, Yasuhiro; Kawaguchi, Takayoshi; Ukon, Misa; Yamamura, Norio; Uehara, Tomoya; Ogawa, Kazuma; Arano, Yasushi; Temma, Takashi; Mukai, Takahiro; Tadamura, Eiji; Saji, Hideo

    2004-01-01

    C-11- and I-123-labeled long chain fatty acid derivatives have been reported as useful radiopharmaceuticals for the estimation of myocardial fatty acid metabolism. We have reported that Tc-99m-labeled N-[[[(2-mercaptoethyl)amino]carbonyl]methyl]-N-(2-mercaptoethyl)-6-aminohexanoic acid ([(99m)Tc]MAMA-HA), a medium chain fatty acid derivative, is metabolized by beta-oxidation in the liver and that the MAMA ligand is useful for attaching to the omega-position of fatty acid derivatives as a chelating group for Tc-99m. On the basis of these findings, we focused on developing a Tc-99m-labeled long chain fatty acid derivative that reflected fatty acid metabolism in the myocardium. In this study, we synthesized a dodecanoic acid derivative, MAMA-DA, and a hexadecanoic acid derivative, MAMA-HDA, and performed radiolabeling and biodistribution studies. [(99m)Tc]MAMA-DA and [(99m)Tc]MAMA-HDA were prepared using a ligand-exchange reaction. Biodistribution studies were carried out in normal mice and rats. Then, a high initial uptake of Tc-99m was observed, followed by a rapid clearance from the heart. The maximum heart/blood ratio was 3.6 at 2 min postinjection of [(99m)Tc]MAMA-HDA. These kinetics were similar to those with postinjection of p-[(125)I]iodophenylpentadecanoic acid. Metabolite analysis showed [(99m)Tc]MAMA-HDA was metabolized by beta-oxidation in the body. In conclusion, [(99m)Tc]MAMA-HDA is a promising compound as a long chain fatty acid analogue for estimating beta-oxidation of fatty acid in the heart.

  6. Synthesis, 99m Tc-labeling, and preliminary biological evaluation of DTPA-melphalan conjugates.

    Science.gov (United States)

    Wang, Jianjun; Yang, Wenjiang; Xue, Jinquan; Zhang, Yanhua; Liu, Yu

    2017-12-01

    Melphalan (MFL) is a typical nitrogen mustard for the treatment of many types of cancer. For the purpose to develop novel 99m Tc-labeled tumor imaging agents with SPECT, MFL was directly labeled by 99m Tc using diethylene triamine pentacetate acid (DTPA) as bifunctional chelating agent. The novel ligands were successfully synthesized by conjugation of DTPA to MFL to get monosubstituted DTPA-MFL and bis-substituted DTPA-2MFL. Radiolabeling was performed in high yield to get 99m Tc-DTPA-MFL and 99m Tc-DTPA-2MFL, respectively, which were hydrophilic and stable at room temperature. The high initial tumor uptake with retention, good tumor/muscle ratios, and satisfactory scintigraphic images suggested the potential of 99m Tc-DTPA-MFL and 99m Tc-DTPA-2MFL for tumor imaging. However, the slow normal tissue clearance would be a great obstacle. Further modification on the linker and/or 99m Tc-chelate to improve the tumor targeting efficacy and in vivo kinetic profiles is currently in progress. Copyright © 2017 John Wiley & Sons, Ltd.

  7. Production of kits for the labelling with 113sup(m)In and sup(99m)Tc, at the CNEA

    International Nuclear Information System (INIS)

    Palcos, M.C.; Kurcbart, Horacio; Nowotny, G.; Ramos, Elsa; Riesgo, J.G.; Mitta, A.E.A.

    1978-05-01

    The actual state of the production of radiopharmaceuticals in the form of reagents kits at the C.N.E.A. is described. This could allow the users to label compounds with sup(113m)In and sup(99m)Tc in an easy and reproducible way. At present, the following sets are provided routinarily a) To label with sup(99m)Tc: Albumin macroaggregates: calcium gluconate; antimonium sulfide colloid, sodium phytate; sodium calcium DTPA; seroalbumin; sodium pyrophosphate; sodium citrate. b) To label with sup(113m)In: albumin macroaggregates; PVP-bicarbonate; DTPA; human seroalbumin. Regarding products in a developping stage, we have: to labed with sup(99m)Tc: dimercapto-succinic acid, set for the labelling of human erythrocytes, set for sup(113m)In and sup(99m)Tc concentration and bleomicin; to label with sup(113m)In: EDTMP sup(99m)In. (author) [es

  8. The synthesis, magnetic purification and evaluation of 99mTc-labeled microbubbles

    International Nuclear Information System (INIS)

    Lazarova, Neva; Causey, Patrick W.; Lemon, Jennifer A.; Czorny, Shannon K.; Forbes, John R.; Zlitni, Aimen; Genady, Afaf; Foster, F. Stuart; Valliant, John F.

    2011-01-01

    Introduction: Ultrasound (US) contrast agents based on microbubbles (MBs) are being investigated as platforms for drug and gene delivery. A methodology for determining the distribution and fate of modified MBs quantitatively in vivo can be achieved by tagging MBs directly with 99m Tc. This creates the opportunity to employ dual-modality imaging using both US and small animal SPECT along with quantitative ex vivo tissue counting to evaluate novel MB constructs. Methods: A 99m Tc-labeled biotin derivative ( 99m TcL1) was prepared and incubated with streptavidin-coated MBs. The 99m Tc-labeled bubbles were isolated using a streptavidin-coated magnetic-bead purification strategy that did not disrupt the MBs. A small animal scintigraphic/CT imaging study as well as a quantitative biodistribution study was completed using 99m TcL1 and 99m Tc-labeled bubbles in healthy C57Bl-6 mice. Results: The imaging and biodistribution data showed rapid accumulation and retention of 99m Tc-MBs in the liver (68.2±6.6 %ID/g at 4 min; 93.3±3.2 %ID/g at 60 min) and spleen (214.2±19.7 %ID/g at 4 min; 213.4±19.7 %ID/g at 60 min). In contrast, 99m TcL1 accumulated in multiple organs including the small intestine (22.5±3.6 %ID/g at 4 min; 83.4±5.9 %ID/g at 60 min) and bladder (184.0±88.1 %ID/g at 4 min; 24.2±17.7 %ID/g at 60 min). Conclusion: A convenient means to radiolabel and purify MBs was developed and the distribution of the labeled products determined. The result is a platform which can be used to assess the pharmacokinetics and fate of novel MB constructs both regionally using US and throughout the entire subject in a quantitative manner by employing small animal SPECT and tissue counting.

  9. A {sup 99m}Tc-labeled dual-domain cytokine ligand for imaging of inflammation

    Energy Technology Data Exchange (ETDEWEB)

    Liu Zhonglin, E-mail: zliu@radiology.arizona.edu [Department of Radiology, University of Arizona, Tucson, P.O. Box 245067 Tucson, AZ 85724-5067 (United States); Wyffels, Leonie; Barber, Christy [Department of Radiology, University of Arizona, Tucson, P.O. Box 245067 Tucson, AZ 85724-5067 (United States); Hui, Mizhou M. [AmProtein, Inc. San Gabriel, CA (United States); Woolfenden, James M. [Department of Radiology, University of Arizona, Tucson, P.O. Box 245067 Tucson, AZ 85724-5067 (United States)

    2011-08-15

    Introduction: Interleukin (IL)-1 and IL-18 are potent proinflammatory cytokines in inflammation-related diseases. Their actions are regulated by IL-1 receptor antagonist (IL-1ra) and IL-18 binding protein (IL-18bp). This study was designed to {sup 99m}Tc-radiolabel an IL-1ra and IL-18bp dual-domain cytokine ligand, IL-18bp-Fc-IL-1ra, for specific inflammation targeting. Methods: The {sup 99m}Tc-IL-18bp-Fc-IL-1ra was obtained by direct labeling via 2-iminothiolane reduction. Competitive binding of {sup 99m}Tc-labeled and unlabeled IL-18bp-Fc-IL-1ra to rat polymorphonuclear leukocytes was assessed in vitro. A mouse ear edema model was used to evaluate specific targeting properties of {sup 99m}Tc-IL-18bp-Fc-IL1ra in vivo. The correlation between {sup 99m}Tc-IL-18bp-Fc-IL-1ra uptake and {sup 111}In-labeled polymorphonuclear neutrophil infiltration was studied using ischemic-reperfused rat hearts. Results: Direct {sup 99m}Tc-labeling yielded a stable dual-domain cytokine radioligand with radiochemical purity greater than 95% after gel filtration. Competitive binding studies showed specific targeting of {sup 99m}Tc-IL-18bp-Fc-IL-1ra to inflammatory cells. The {sup 99m}Tc-IL-18bp-Fc-IL-1ra uptake was 1.80{+-}0.17 % injected dose per gram (%ID/g) in the inflamed ear without blocking, whereas uptake in the presence of IL-18bp-Fc-IL-1ra was 1.09{+-}0.08 %ID/g (P<.05). The amounts of IL-1{beta} and IL-18 were significantly increased in the inflamed ears compared to the vehicle controls. A significant correlation of {sup 99m}Tc-IL-18bp-Fc-IL-1ra with {sup 111}In-labeled neutrophil distribution was observed in the ischemic-reperfused hearts (P<.001). Conclusion: Targeting proinflammatory cytokines with {sup 99m}Tc-IL-18bp-Fc-IL-1ra may provide a suitable approach for specific detection of inflammatory sites.

  10. Development of methods of labeling pentavalent DMSA with 99mTc and 188Re

    International Nuclear Information System (INIS)

    Brambilla, Tania de Paula

    2009-01-01

    Technetium-99 m is the most useful radionuclide in diagnostic imaging procedures in Nuclear Medicine, more than 80 percent of radiopharmaceuticals are 99m Tc-labeled compounds. 99m Tc-DMSA(V) has been used for imaging of soft tissue, head and neck tumors. It shows a particularly high specificity for medullary thyroid carcinoma and bone metastases in a variety of cancers. Biodistribution studies of 188 Re-DMSA(V) have shown that its general pharmacokinetic properties are similar to that of 99m Tc-DMSA(V), so this agent could be used for targeted radiotherapy of these tumors. The aim of this work is the development of methods of labeling DMSA(V) with 99m Tc and 188 Re. 99m Tc-DMSA(V) can be prepared by two methods. One of them is the indirect one, through the use of a commercial kit of DMSA (III), by adjusting the pH from 2.5 to ∼ 8.5 with NaHCO 3 . This method was evaluated and optimized presenting high labeling yields. The other method is the direct one, through the preparation of a lyophilised kit ready for labeling with 99m Tc, being the method of interest of this work, due to the easy of its clinical use. The most adequate formulation of the kit was: 1.71 mg of DMSA, 0.53 mg of SnCl 2 .2H 2 O and 0.83 mg of ascorbic acid (pH 9). Labeling yields higher than 95% were achieved labeling this kit with 1 to 2 m L of 99m Tc with activities up to 4736 MBq (128 mCi). The kit was stable up to 6 months and biodistribution studies confirmed the quality of the DMSA (V) labeled with 99m Tc using this kit. The reduction potential of Re is lower than the one for Tc, so the labeling conditions of 188 Re-DMSA(V) are different from the ones used for 99m Tc- DMSA(V). 188 Re-DMSA(V) is prepared in acid solution, that makes it possible to use the DMSA (III) commercial kit developed for labeling with 99m Tc, prepared in pH 2.5, for labeling with 188 Re. Labeling yields higher than 95% were achieved with this methodology, with a rection time of 30 minutes at 100 deg C using no more

  11. A freeze dried kit formulation for the preparation of {sup 99m} Tc labelled human polyclonal IgG for the detection of infection and inflammation; Desarrollo del nucleo equipo {sup 99m} Tc-IgG humana para la deteccion `In vivo` de procesos inflamatorios

    Energy Technology Data Exchange (ETDEWEB)

    Pedraza L, M

    1996-11-01

    A freeze dried kit formulation for the preparation of {sup 99m}Tc-labelled human polyclonal IgG for the detection of infection and inflammation employing direct methods for protein labeling was developed. The method comprises reduction of intrinsic disulphide bridges within the antibody molecule by the use of the reductant 2-mercaptoethanol. Following a subsequent purification, the resulting reduced antibody is labeled via Sn{sup 2+} reduction of pertechnetate in the presence of a weak competing ligand ethane-1-hydroxy-1,1-diphosphonate (EHDP). High labeling efficiencies (>90%) were obtained with high in vitro stability and without effect upon antibody immunoreactivity. Methods of analysis were also established permitting identification of radiochemical impurities which may be present in radiopharmaceutical solution. {sup 99m} Tc-polyclonal IgG prepared by the kit method was evaluated for scintigraphic localization of inflammatory lesions and abscesses in rabbits. Data demonstrated that the {sup 99m} Tc-polyclonal IgG after kit-reconstitution shows excellent stability and is an effective imaging agent of infection and/or inflammation. (Author).

  12. 99mTc-Alafosfalin: an antibiotic peptide infection imaging agent

    International Nuclear Information System (INIS)

    Tsopelas, C.; Penglis, S.; Ruszkiewicz, A.; Bartholomeusz, F.D.L.

    2003-01-01

    The radiolabeled antibiotic peptide 99m Tc-alafosfalin was assessed as an infection imaging agent in a rat model by comparison with 99m Tc-DTPA and 99m Tc-leukocytes. 99m Tc-alafosfalin was prepared via an instant cold kit and 99m Tc-leukocytes were prepared using 99m Tc-stannous fluoride colloid in an ex vivo labeling procedure of whole blood. In separate experiments, the three radiotracers were administered to rats infected with staphylococcus aureus. Quantitative biodistribution studies were performed as well as scintigraphic images and histopathology. 99m Tc-alafosfalin is a stable product, obtained in high radiochemical purity (>95%). This agent was mainly renally excreted, with low liver, spleen and bone uptake, and resulted in a mean ratio of infected/non-infected thighs of 4.3/1.0 at 4 hr post radiotracer injection. 99m Tc-DTPA gave a corresponding ratio of 1.9/1.0 and 99m Tc-leukocytes gave 20.0/1.0 at the same time point. An in vitro assay found the level of 99m Tc-alafosfalin binding to staphylococcus aureas higher than 99m Tc-DTPA (10% versus 1% respectively). 99m Tc-alafosfalin accumulates at sites of infection in a rat model better than the perfusion molecule 99m Tc-DTPA, yet less than 99m Tc-leukocytes. The distribution characteristics of this 99m Tc-antibiotic peptide would be an advantage in imaging abdominal and soft tissue infection

  13. A review of 99mTc labeled myocardial imaging agents for tumor-positive imaging

    International Nuclear Information System (INIS)

    Xing Shian; Zhang Yongxue; An Rui

    2002-01-01

    The tumor-positive imaging with high sensitivity and specificity was useful in primary tumor and recurrences and metastases. The 99m Tc labeled myocardial imaging agents are easily available and stable and the radiochemical purity is high. 99m Tc is the preferred choice in routine works because its physical properties. The preparation, quality control, mechanism of accumulation and the clinical use of 99m Tc-sestamibi, 99m Tc-tetrofosmin, 99m Tc-furifosmin, and 99m Tc-N-NOET were reviewed

  14. Imaging diagnosis of protein-losing enteropathy by 99mTc-labeled serum albumin

    International Nuclear Information System (INIS)

    Kashiwagi, Toru; Fukui, Hiroyuki; Jyokou, Takeshi

    1990-01-01

    Abdominal scintigraphy with intravenous injection of 99m Tc-labeled serum albumin was performed in 6 patients with protein-losing enteropathy (PLE) and 3 patients with nongastrointestinal tract disorders. In 3 out of 6 patients with PLE, abnormal radioactivity was observed in the ileum region 3 hours after injection, and thereafter clear colon image was obtained. In the remaining 3 patients, the colon was visualized 24 hours after injection. On the other hand, in all patients with nongastrointestinal tract disorders, no abnormal radioactivity was observed in the abdomen until 24 hours after injection. These results indicate that gastrointestinal protein loss could be demonstrated by scintigraphy with intravenously administered 99m Tc-labeled serum albumin. In one healthy subject, 99m Tc-labeled serum albumin was administered orally and abdominal scintigraphy was performed. Gastrointestinal tract image was only observed and no other image was demonstrated until 24 hours after oral administration. This result suggests that 99m Tc excreted into the gastrointestinal tract is not reabsorbed. Therefore, abdominal scintigraphy with 99m Tc-labeled serum albumin appears to be a simple and useful method for diagnosis of PLE. (author)

  15. /sup 99m/Tc dextran: a new blood-pool-labeling agent for radionuclide angiocardiography

    International Nuclear Information System (INIS)

    Henze, E.; Robinson, G.D.; Kuhl, D.E.; Schelbert, H.R.

    1982-01-01

    We have explored the possibility of imaging the cardiac blood pool with dextran (Dx) labeled with /sup 99m/Tc (Tc) after Sn2+ reduction. Stannous dextran (SnDx) kits were prepared in advance and labeling was performed by adding /sup 99m/Tc. The labeling efficiency was greater than 95%. /sup 99m/Tc dextran (TcDx) was highly stable both in vivo and in vitro. In seven dogs we compared the quality of blood-pool images obtained with TcDx of different molecular weights (4 X 10(4) . Dx-40; 5 X 10(5) . Dx-500; 2 X 10(6) . Dx-2000) and with /sup 99m/Tc red blood cells (TcRBC) labeled in vitro, and determined the organ distribution of this new agent by whole-body scanning and blood sampling. TcDx provided high-quality cardiac blood-pool images up to 60 min after injection. The heart-to-lung ratios averaged 3.7 for TcDx-40, 3.9 for TcDx-500, and 5.4 for TcRBC at 60 min. Whereas TcDx-40 showed a relatively rapid initial urinary excretion and TcDx-2000 was degraded rapidly, TcDx-500 demonstrated the best kinetics for blood-pool imaging. Thus, TcDx is a new radiopharmaceutical with high labeling efficiency and stability. It overcomes a number of the limitations of currently used blood-labeling agents and may become useful for blood-pool imaging in man

  16. Sodium metabisulfite: a new reducer agent for direct labelling of immunoglobulins with 99mTc

    International Nuclear Information System (INIS)

    Zayas, F.; Hernandez, T.; Rodriguez, M.E.; Perera, A.; Hernandez, L.; Valdes, M.

    1998-01-01

    A method for direct labeling of antibodies with 99mTc is described. Sodium Metabisulfite (SMB) was evaluated as a new reducing agent of disulfide bridges of the IgG molecule. Under selected experimental conditions, radiochemical purities of the label higher than 90.0% were achieved in most of the experiments. On the basis of the obtained yields an empiric equation which describes the system was computed as: Y=93.6+2.1X5 - 1.36X6+0.9X7. The absence of X4 indicated that the purification on Sephadex of the reduced IgG was not relevant to the labeling process. The most important variables were tin ion concentration (X5), the volume of Tin-Tartrate solution (X6) and the incubating time between reduced IgG and Tin-Tartrate solution (X7). A low aggregation and fragmentation of the IgG molecule was obtained when a SMB/IgG molar relation of 750/1 was used. The stability of the 99mTc-IgG was assessed by DTPA, HSA and L-Cysteine challenge studies. An acceptable level of dissociation was observed in presence of DTPA and L-Cysteine, when the Tartrate anion was used. However the transchelation level for HSA was about 80.0 per cent. These preliminary results showed that SMB could be a useful reducing agent for direct labeling of IgG. Further studies are needed to correctly evaluate it. (author)

  17. Fundamental evaluation of in vivo labeling of red blood cells with Tc-99m using stannous chloride

    Energy Technology Data Exchange (ETDEWEB)

    Hiraki, T; Katayama, M; Ando, I; Ando, A [Kanazawa Univ. (Japan). School of Paramedicine; Hisada, K

    1982-04-01

    Stannous chloride was evaluated as a stannous ion source for the in vivo labeling of red blood cells(RBC) with Tc-99m. In this study, the labeling of RBC with Tc-99m was performed by two successive intravenous administrations of stannous chloride and Tc-99m-pertechnetate, and the optimal dose of stannous chloride and the optimal time interval between the two injections were evaluated. The labeling efficiency for this procedure was also evaluated as a function of time after the pertechnetate injection. The results of our investigation revealed that the maximal in vivo RBC labeling (86%) can be obtained at 15 min after the pertechnetate injection with an i.v. dose of 12.7 ..mu..g/kg of stannous chloride followed 15 min later by an i.v. injection of Tc-99m-pertechnetate. In conclusion, stannous chloride was found to be an excellent stannous ion source for the in vivo labeling of RBC with Tc-99m.

  18. Tc-99m direct radiolabeling of monoclonal antibody ior egf/r3: quality control and image studies in mice

    International Nuclear Information System (INIS)

    Dias, Carla Roberta; Marczewski, Barbara; Moraes, Vanessa; Barboza, Marycel Figols de; Osso Junior, Joao Alberto

    2005-01-01

    Monoclonal antibodies (Mabs) have been useful for immunoscintigraphic applications in clinical diagnosis since they were introduced in the practice of nuclear medicine. The ior egf/r3 (Centis, Cuba) is a murine monoclonal antibody against epidermal growth factor receptor (EGF-R) and has been widely used in the radioimmunodiagnosis of tumors of epithelial origin. Labeled with 99m Tc, its main application in Nuclear Medicine is the follow up, detection and evaluation of tumor recurrences. The objective of this work is to describe the preparation of a lyophilized formulation (kit) for radiolabeling the Mab ior egf/r3 with 99m Tc for immunoscintigraphic applications. Radiolabeling efficiency, effects on immunoreactivity, image studies and stability of the formulation are reported. The study demonstrated that the kit formulation can be labeled with 99m Tc at high yields and can be used to visualize in vivo human tumors of epithelial origin by immunoscintigraphy studies.(author)

  19. A freeze dried kit formulation for the preparation of 99m Tc labelled human polyclonal IgG for the detection of infection and inflammation

    International Nuclear Information System (INIS)

    Pedraza L, M.

    1996-01-01

    A freeze dried kit formulation for the preparation of 99m Tc-labelled human polyclonal IgG for the detection of infection and inflammation employing direct methods for protein labeling was developed. The method comprises reduction of intrinsic disulphide bridges within the antibody molecule by the use of the reductant 2-mercaptoethanol. Following a subsequent purification, the resulting reduced antibody is labeled via Sn 2+ reduction of pertechnetate in the presence of a weak competing ligand ethane-1-hydroxy-1,1-diphosphonate (EHDP). High labeling efficiencies (>90%) were obtained with high in vitro stability and without effect upon antibody immunoreactivity. Methods of analysis were also established permitting identification of radiochemical impurities which may be present in radiopharmaceutical solution. 99m Tc-polyclonal IgG prepared by the kit method was evaluated for scintigraphic localization of inflammatory lesions and abscesses in rabbits. Data demonstrated that the 99m Tc-polyclonal IgG after kit-reconstitution shows excellent stability and is an effective imaging agent of infection and/or inflammation. (Author)

  20. Bleeding rates necessary for detecting acute gastrointestinal bleeding with technetium-99m-labeled red blood cells in an experimental model

    International Nuclear Information System (INIS)

    Thorne, D.A.; Datz, F.L.; Remley, K.; Christian, P.E.

    1987-01-01

    Proponents of [/sup 99m/Tc]sulfur colloid for GI bleeding studies argue that, although labeled red blood cells are useful for intermittent bleeding, they are not capable of detecting low bleeding rates. Studies of dogs with experimental GI bleeding have indicated bleeding rates of 0.05 ml/min can be detected with [/sup 99m/Tc]sulfur colloid. Since similar data in the dog model were unavailable for /sup 99m/Tc-labeled red blood cells, we undertook this study. To simulate lower GI bleeding, catheters were inserted into the bowel lumen. Each dog's blood was labeled with /sup 99m/Tc using an in vitro technique. Venous blood was then withdrawn and re-infused into the lumen of the bowel using a Harvard pump. Fourteen dogs were studied, ten receiving a bleeding rate from 4.6-0.02 ml/min in the descending colon and four with proximal jejunal bleeds of 0.20-0.02 ml/min. Bleeding rates of 4.6-0.2 ml/min were detected within 10 min in the colon and bleeding rates as low as 0.04 ml/min were seen by 55 min. Slower bleeding rates were not detected. Similar findings were noted for proximal jejunal bleeds. Based on the time of appearance, a minimum volume of approximately 2-3 ml labeled blood was necessary to detect bleeding. We conclude that /sup 99m/Tc-labeled RBCs are sensitive for low bleeding rates in the dog model. The rates are comparable to those described for [/sup 99m/Tc]sulfur colloid in this experimental setting. The time of appearance of activity is related to the bleeding rate

  1. Labelling of insulin with 99mTc and its evaluation in rabbits

    International Nuclear Information System (INIS)

    Bhelose, A.; Raju, A.; Ramamoorthy, N.; George, R.; Soni, P.S.

    1998-01-01

    Full text: In order to assess the feasibility of administering insulin into the respiratory tract as aerosol and determining its efficacy for drug treatment, as an alternative to intramuscular injection, we have studied the labelling of insulin with 99m Tc. 99m Tc insulin was evaluated in rabbits by i.v. injection. Reduction of insulin was carried out with 2 mercaptoethanol (2-ME) at different molar ratios of 3250:1 to 100:1 of insulin 2-ME. The reduced insulin was purified over Sephadex G-75 (7 x 1 cm) column. The fractions were identified and estimated for insulin content by spectrophotometry (280 nm). The labelling of this reduced, purified insulin was carried out using the standard Sn-GHA kit of BRIT. The R.C. purity was determined using ITLC/ normal saline which was found to be 68% at molar ratio 3250:1 of insulin:2-ME and increased to >85% at 100:1 insulin:2-ME. Bioactivity of insulin, after labelling was confirmed by injecting i.v. 99m Tc-insulin in rabbits. The blood sugar level dropped from 96 mg % to 88 % within 30 min which indicated that no significant alteration to the biomolecule structure took place during labelling. This approach thus seems to be promising and further studies with 99m Tc-insulin aerosols are warranted to establish the efficacy

  2. Altered [99mTc]Tc-MDP biodistribution from neutron activation sourced 99Mo.

    Science.gov (United States)

    Demeter, Sandor; Szweda, Roman; Patterson, Judy; Grigoryan, Marine

    2018-01-01

    Given potential worldwide shortages of fission sourced 99 Mo/ 99m Tc medical isotopes there is increasing interest in alternate production strategies. A neutron activated 99 Mo source was utilized in a single center phase III open label study comparing 99m Tc, as 99m Tc Methylene Diphosphonate ([ 99m Tc]Tc-MDP), obtained from solvent generator separation of neutron activation produced 99 Mo, versus nuclear reactor produced 99 Mo (e.g., fission sourced) in oncology patients for which an [ 99m Tc]Tc-MDP bone scan would normally have been indicated. Despite the investigational [ 99m Tc]Tc-MDP passing all standard, and above standard of care, quality assurance tests, which would normally be sufficient to allow human administration, there was altered biodistribution which could lead to erroneous clinical interpretation. The cause of the altered biodistribution remains unknown and requires further research.

  3. Technetium-99m-labelled monoclonal antibody fragment (99mTc-DD-3B6/22Fab') for ovarian cancer

    International Nuclear Information System (INIS)

    Fernandes, V.; Donaghy, T.; Prabakaran, K.; Smith, S.; Clingan, P.; Bartolo, N.; Bundesen, P.; Hillyard, C.

    1998-01-01

    Full text: This study is the first to assess 99m Tc-DD-3B6/22Fab'' as an agent for detecting OC recurrence. Five informed consenting volunteers with stages 3 or 4 OC (mean age 54.2 y) and with negative skin prick test to Fab'' were recruited. All had suspicion of OC recurrence, with elevated serum tumour marker CA125, and in some, OC confirmation on CT scans. Aggressive treatment was continued so that tumour regression was possible prior to 99m Tc-DD-3B6/22Fab''scan. CA125, FBC, biochemical and clot markers were measured pre-and post-study. All received IV 600-800 MBq of 99 mTc-DD-3B6/22Fab''. Temperature, pulse and BP were monitored for one hour. Data were acquired with a single head LFOV gamma camera and HIRES collimator at 1,4,6 and 24 hours. Studies were read for OC lesions which were scored as probably normal (PN) or abnormal (PAb), definitely abnormal (DAb). The gold standard was CA125 immediately post-scan and, when possible, confirmation with CT. Of 5 patients, 1 was disease negative with 99 mTc-DD-3B6/22Fab'', CA125 suggesting remission, and 4 were positive on all modalities (Sensitivity, specificity, 100% respectively). 99 mTc-DD-3B6/22Fab'' identified 15 lesions (100% DAb). CT detected 7 lesions (71% Dab) pre- 99 mTc-DD-3B6/22Fab''. Repeat CT detected 8 (100% DAb). Correlation with CA125 levels was best with 99 mTc-DD3B6/22Fab''. No side effects or adverse change in serum markers were noted. 99 mTc-DD-3B6/22Fab'' is sensitive and specific for detecting OC recurrence

  4. Development of 99mTc labelled somatostatin analogues with high affinity for somatostatin receptors

    International Nuclear Information System (INIS)

    Maina, T.; Nock, B.; Nicolopoulou, A.; Tsipra, C.; Poppe, M.; Chiotellis, E.

    2001-01-01

    A recent development in oncology involves the use of metabolically stabilized peptide hormone analogues labelled with metallic radionuclides for the diagnosis or therapy of malignant disease. This approach was successfully applied for the first time in the visualization of somatostatin positive tumours and their metastases with 111 In DTPA-octreotide. In an effort to obtain a 99m Tc somatostatin receptor affine radioligand we describe herein the synthesis, radiochemistry and preliminary biological evaluation of two novel 99m Tc labelled somatostatin analogues, N 4 -TOC and N 4 -RC-160. In these compounds a tetraamine bifunctional unit was covalently attached to the N-terminal (D)Phe 1 of the peptide chain using Boc-protection strategies. The peptide conjugates were purified by high performance liquid chromatography (HPLC) and characterized by UV/Vis and ES-MS spectroscopies. As revealed by HPLC, 99m Tc labelling was quantitative under mild conditions, leading to a single 99m Tc species in high specific activities. Affinity of 99m Tc N 4 -TOC for the somatostatin receptor, as determined by in vitro binding assays in rat brain cortex membranes, was found unaffected by the presence of the bulky metal chelate. The binding properties of 99m Tc N 4 -RC-160 could not be determined by this assay due to an extremely high non-specific binding of this radioligand, and will be shortly investigated by other methods. Tissue distribution in healthy mice revealed that 99m Tc N 4 -TOC is clearing mainly through the kidneys and the urinary tract whereas 99m Tc N 4 -RC-160 shows a high accumulation in the liver as a result of its lipophilicity. Analysis of urine samples by HPLC showed that 99m Tc N 4 -TOC is excreted integer from the body of mice, while 99m Tc N 4 -RC-160 is totally transformed to an unidentified hydrophilic metabolite in vivo. The location of this metabolism is currently investigated. In vivo blocking experiments using animals pre-treated with 50 μg octreotide

  5. Technetium labeling of monoclonal antibodies with functionalized BATOs. 1. TcCl(DMG)3PITC.

    Science.gov (United States)

    Linder, K E; Wen, M D; Nowotnik, D P; Malley, M F; Gougoutas, J Z; Nunn, A D; Eckelman, W C

    1991-01-01

    BATO (boronic acid adduct of technetium dioximes) complexes, TcCl(dioxime)3BR, were prepared in which the boron substituent (R) was the protein-reactive m-phenyl isothiocyanate (PITC). The 99TcCl(dioxime)3PITC complexes [dioxime = dimethylglyoxime (DMG) or cyclohexanedione dioxime (CDO)] were prepared from 99Tc(dioxime)3(mu-OH)SnCl3 and characterized. The X-ray crystal structure of 99TcCl(DMG)3PITC was determined. The 99mTc complexes were prepared from 99mTcO4- in a process using a freeze-dried kit, either in a one-step procedure or via 99mTcCl(dioxime)3. Initial labeling studies with 99mTcCl(dioxime)3PITC were performed on glycine and polylysine and, subsequently, on mouse IgG and the B72.3 monoclonal antibody. Covalent attachment of 99mTcCl(DMG)3PITC to B72.3 was demonstrated by SDS-PAGE electrophoresis. B72.3 labeled with 99mTcCl(DMG)3PITC displayed high binding to a TAG 72 affinity column and had a distribution in normal mice similar to that reported for iodine-labeled B72.3.

  6. Biodistribution of 99mTc-labeled anti-human epidermal growth factor receptor (EGF-R) humanized monoclonal antibody h-R3 in a xenograft model of human lung adenocarcinoma

    International Nuclear Information System (INIS)

    Morales-Morales, Alejo; Duconge, Jorge; Caballero-Torres, Idania; Nunez-Gandolff, Gilda; Fernandez, Eduardo; Iznaga-Escobar, Normando

    1999-01-01

    The anti-human epidermal growth factor receptor (EGF-R) humanized monoclonal antibody (MAb) h-R3 is an (IgG 1 ), which binds to an extracellular domain of EGF-R. It was used to evaluate the biodistribution on nude mice xenografted with H-125 human lung adenocarcinoma cell line. Results were compared with its murine version of the MAb ior-egf/r3. Twenty-one athymic female 4NMRI nu/nu mice were injected intraperitoneally with 10 μg/100 μCi of 99m Tc-labeled MAbs. Immunoreactivity of 99m Tc-labeled MAbs were measured by enzyme-linked immunosorbent assay (ELISA) on H-125 cell line and the immunoreactive fractions was determined by the Lindmo method. Among all organs, significant accumulation was found in serum (27.05 ± 2.08 %ID/g) and tumor (3.903 ± 0.89 %ID/g) at 4 h after injection. These values decreased to 5.03 ± 0.50 %ID/g and 2.19 ± 0.56 %ID/g for serum and tumor, respectively. The immunoreactive fraction was found to be 0.70, with a correlation coefficient r=0.9984. With the good biodistribution and tumor uptake of the 99m Tc-labeled humanized antibody h-R3, a phase I diagnostic clinical trial of tumor with epithelial origin should be pursued

  7. Kinetic study on ligand exchange reaction between ethylenedicysteine and 99mTc- glucoheptonate (99mTc-GH)

    International Nuclear Information System (INIS)

    Wu, C.Y.; Ji, S.R.; Lu, C.X.; Ding, S.Y.; Chen, Z.P.; Lin, X.T.

    2002-01-01

    Aim: 99m Tc-L,L-ethylenedicysteine( 99m Tc-EC)is a new type of renal imaging agent. It can be labeled very easily and efficiently at room temperature through direct labeling at pH 12. The need for direct labeling at pH 12 does not compromise the simplicity and ease of preparation of 99m Tc-EC and its practical usefulness in daily routine. On the basis of the labeling experiments, we developed a ligand exchange labeling method, in which the labeling EC with 99m Tc can be performed at pH 8. In order to provide a theoretic basis, a detailed kinetic study of ligand exchange reaction between 99m Tc- glucoheptonate( 99m Tc-GH) and EC was carried out. Materials and Methods: 99m Tc-EC is prepared as follows: 99m Tc-GH + EC → 99m Tc-EC + GH, labeling can be easily performed by adding 99m TcO 4 - (2∼6ml generator elute) to glucoheptonate solution containing SnCl 2 .2H 2 O solution to form 99m Tc-GH, then freshly prepared 99m Tc-GH is transferred to the aqueous solution of different concentrations of EC at different pH value, after being shaken, 99m Tc-EC was formed. Radiolabeling yield(RLY) and radiochemical purity(RCP) of 99m Tc-GH and 99m Tc-EC were measured by Xinhua No.1 paper with developing system of Me 2 CO/H 2 O/con.NH 3 .H 2 O=9/3/1(V/V). 99m Tc-GH(RCP must be over 98%, 80ul, 3.6∼7.4MBq) was added to 1ml of 0.5mol/L phosphate buffer(pH 12) containing different amount of EC(150, 75, 50 and 15ug), the sample was taken out at different time intervals and RCP was determined. The solution of EC(30ul, 5g/L) was added to 1ml of 0.5mol/L phosphate buffer at different pH value(pH11, 10, 9, 8, 7), after completely vortexed, 99m Tc-GH(RCP must be over 98%, 80ul, 3.6∼7.4MBq) was then added, the sample was taken out and RCP was determined as above. The rate constant(k) of ligand exchange reaction at different concentrations of EC and different reaction pH values were calculated out by integrating. Plot ln[1/(1-RLY)] vs t(time) showed a liner relationship, and the rate

  8. Click chemistry for [{sup 99m}Tc(CO){sub 3}] labeling of Lys{sup 3}-bombesin

    Energy Technology Data Exchange (ETDEWEB)

    Ferro-Flores, G., E-mail: ferro_flores@yahoo.com.m [Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Carretera Mexico-Toluca S/N, La Marquesa, Ocoyoacac, Estado de Mexico, C.P. 52750 (Mexico); Rivero, I.A. [Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Carretera Mexico-Toluca S/N, La Marquesa, Ocoyoacac, Estado de Mexico, C.P. 52750 (Mexico); Instituto Tecnologico de Tijuana, Baja California (Mexico); Santos-Cuevas, C.L. [Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Carretera Mexico-Toluca S/N, La Marquesa, Ocoyoacac, Estado de Mexico, C.P. 52750 (Mexico); Universidad Autonoma del Estado de Mexico (Mexico); Sarmiento, J.I. [Instituto Tecnologico de Tijuana, Baja California (Mexico); Arteaga de Murphy, C. [Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran (Mexico); Ocampo-Garcia, B.E. [Departamento de Materiales Radiactivos, Instituto Nacional de Investigaciones Nucleares, Carretera Mexico-Toluca S/N, La Marquesa, Ocoyoacac, Estado de Mexico, C.P. 52750 (Mexico); Garcia-Becerra, R.; Ordaz-Rosado, D. [Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran (Mexico)

    2010-12-15

    {sup 99m}Tc-HYNIC labeled Lys{sup 3}-bombesin has shown specific binding to gastrin-releasing peptide receptors (GRP-r) over-expressed in cancer cells. Click chemistry offers an innovative functionalization strategy for biomolecules such as bombesin. The aim of this research was to apply a click chemistry approach for [{sup 99m}Tc(CO){sub 3}] labeling of Lys{sup 3}-bombesin and to compare the in vitro MCF7 breast cancer cell uptake and biodistribution profile in mice with that of {sup 99m}Tc-EDDA/HYNIC-Lys{sup 3}-bombesin. The results suggest a higher lipophilicity for {sup 99m}Tc(CO){sub 3}-triazole-Lys{sup 3}-bombesin which explains its higher in vivo hepatobiliary elimination. Pancreas-to-blood ratio for {sup 99m}Tc(CO){sub 3}-triazole-Lys{sup 3}-bombesin was 4.46 at 3 h and both bombesin radiopharmaceuticals showed specific recognition for GRP receptors in MCF7 cancer cells. Click chemistry is a reliable approach for [{sup 99m}Tc(CO){sub 3}] labeling of Lys{sup 3}-bombesin.

  9. Radiolabeling, quality control and kit formulation of a new 99mTc-labeled antibiotic. 99mTc-doxycycline hyclate

    International Nuclear Information System (INIS)

    Derya Ilem-Oezdemir; Makbule Asikoglu; Hayal Oezkilic

    2013-01-01

    Since radiolabeled antibiotics specifically bind to the bacterial components they are promising radiopharmaceuticals for the precise diagnosis and detection of infectious lesions. Doxycycline hyclate (DOX) was chosen to investigate as a new radiolabeled antibacterial agent since its bacteriostatic activity against a wide variety of microorganisms. The aim of the present study is to develop simple and easy formulation of DOX with 99m Tc ready to use kit. 99m Tc-DOX was developed and standardized under varying conditions of reducing and antioxidant agent concentration, pH, radioactivity dose and reducing agent type. Labeling studies were performed by changing the selected parameters one by one and optimum labeling conditions were determined. After observing the conditions for maximum labeling efficiency and stability, lyophilized freeze dry kits were prepared accordingly. Radiochemical purity was determined with RTLC and RHPLC which was found more than >95 %. Two different freeze dry kits were formulated with optimum labeling conditions. The improved kits were found stable up to 6 months. (author)

  10. Radioimmunoimaging of experimental thrombi in dogs using technetium-99m-labeled monoclonal antibody fragments reactive with human platelets

    International Nuclear Information System (INIS)

    Som, P.; Oster, Z.H.; Zamora, P.O.; Yamamoto, K.; Sacker, D.F.; Brill, A.B.; Newell, K.D.; Rhodes, B.A.

    1986-01-01

    Monoclonal antibody 50H.19, which reacts with human platelets, was converted to fragments, pretinned, and made into kits for subsequent radiolabeling with /sup 99m/Tc. The antibody, which cross-reacts with dog platelets, was used to evaluate in vitro binding to blood clots and in vivo in experimental thrombi in dogs. After radiolabeling, 97.4 +/- 6.4% of the /sup 99m/Tc was antibody-associated. The preparations retained immunoreactivity, as determined by: binding studies using whole blood and determining the ratio of cell-to-plasma radioactivity (ratios of 57.6-61.2) and binding of the antibody to clots (clot/serum ratios were 57.2-74.6%). Approximately 50% of the radioactivity was cleared from the blood in 3-6 min and 18-24% was excreted in urine within 3 hr. Experimental thrombi in dogs could be visualized consistently within 2-3 hr postinjection in peripheral veins and arteries, pulmonary arteries, and the right ventricle. In addition, damage to blood vessel intima without visible thrombi could also be detected. This method has the following advantages: short and simple pre-imaging preparation, and rapid visualization of thrombi with no need for blood-pool subtraction or delayed imaging

  11. Tc-{sup 99m} direct radiolabeling of monoclonal antibody ior egf/r3: quality control and image studies in mice

    Energy Technology Data Exchange (ETDEWEB)

    Dias, Carla Roberta; Marczewski, Barbara; Moraes, Vanessa; Barboza, Marycel Figols de; Osso Junior, Joao Alberto [Instituto de Pesquisas Energeticas e Nucleares (IPEN-CNEN/SP), SP (Brazil). Centro de Radiofarmacia]. E-mail: crdias@ipen.br

    2005-10-15

    Monoclonal antibodies (Mabs) have been useful for immunoscintigraphic applications in clinical diagnosis since they were introduced in the practice of nuclear medicine. The ior egf/r3 (Centis, Cuba) is a murine monoclonal antibody against epidermal growth factor receptor (EGF-R) and has been widely used in the radioimmunodiagnosis of tumors of epithelial origin. Labeled with 99m Tc, its main application in Nuclear Medicine is the follow up, detection and evaluation of tumor recurrences. The objective of this work is to describe the preparation of a lyophilized formulation (kit) for radiolabeling the Mab ior egf/r3 with 99m Tc for immunoscintigraphic applications. Radiolabeling efficiency, effects on immunoreactivity, image studies and stability of the formulation are reported. The study demonstrated that the kit formulation can be labeled with 99m Tc at high yields and can be used to visualize in vivo human tumors of epithelial origin by immunoscintigraphy studies.(author)

  12. Freeze-dried formulation for direct 99mTc-labeling ior-egf/r3 MAb: additives, biodistribution, and stability

    International Nuclear Information System (INIS)

    Morales, Alejo A. Morales; Nunez-Gandolff, Gilda; Perez, Niuvis Perez; Veliz, Belkis Chico; Caballero-Torres, Idania; Duconge, Jorge; Fernandez, Eduardo; Crespo, Francisco Zayas; Veloso, Ana; Iznaga-Escobar, Normando

    1999-01-01

    Monoclonal antibodies (MAbs) have been useful for immunoscintigraphic applications in clinical diagnosis since they were introduced in nuclear medicine practice. The MAb ior egf/r3 developed at the Center of Molecular Immunology (Havana, Cuba) is a murine antibody that recognizes the human epidermal growth factor receptor (EGF-R) and has been used widely in the radioimmunodiagnosis of tumors of epithelial origin. Based on the direct Schwarz method, the present report describes the preparation of a freeze-dried formulation for radiolabeling the MAb ior egf/r3 with 99m Tc for immunoscintigraphic applications. Radiolabeling efficiency, effects on immunoreactivity, biodistribution, pharmacokinetic, and stability of the formulation are reported. The study demonstrated that the freeze-dried formulation can be labeled with 99m Tc at high yield. The resulting 99m Tc-labeled ior egf/r3 MAb can be used to visualize in vivo human tumors of epithelial origin by immunoscintigraphy studies. The kit does not need any other addition or purification at the time of tagging other than the requisite amount of pertechnetate (40-50 mCi). Because the contents of the kit are lyophilized, no special storage or transportation is required

  13. Experimental and clinical studies on hepatobiliary scintigraphy and function test with sup(99m)Tc-E-HIDA

    International Nuclear Information System (INIS)

    Narabayashi, Isamu; Otsuka, Nobuaki; Terashima, Hideaki; Yokobayashi, Tsuneo; Kaji, Tatsumi

    1980-01-01

    In experimental and clinical studies, the usefulness of sup(99m)Tc-E-HIDA has been evaluated for dynamic imaging and function test. Biological distribution of sup(99m)Tc-E-HIDA in rabbits at 1 hour after the intravenous administration indicated that activity was 62% of the injected dose in the gallbladder and intestine, 2% in the liver, and 9% in the kidneys and urine. Hepatic uptake and excretion of sup(99m)Tc-E-HIDA were discussed in comparison with those of sup(99m)Tc-p-butyl-IDA, sup(99m)Tc-HIDA, sup(99m)Tc-PI and 123 I-RB. Radiochemical purity was ascertained by thin layer chromatography in saline. Labelling was nearly 100%, namely no unreacted pertechnetate was detected. In clinical study, the imaging of liver, bile ducts, gallbladder and intestine was satisfactory with sup(99m)Tc-E-HIDA. There was no or faint renal visualization in cases with hepatic uptake on the hepatogram. Quantitative analysis of blood retention, blood clearance and hepatogram with sup(99m)Tc-E-HIDA reflected excretory liver function in various hepatobiliary disorders. We concluded that sup(99m)Tc-E-HIDA has a lower urinary excretion and seems more effective than the other sup(99m)Tc-labels, such as sup(99m)Tc-HIDA and sup(99m)Tc-PI, at higher bilirubin levels. However, when the level of the bilirubin in blood rises above 7.4 mg/dl, no hepatic uptake of sup(99m)Tc-E-HIDA was obtained with greater renal excretion. (author)

  14. Clinical application study of bone marrow immunoscintigraphy using 99mTc-labelled anti-granulocyte monoclonal antibody BW250/183

    International Nuclear Information System (INIS)

    Liu Zengli; Wu Jinchang; Shi Yizhen; Tang Jun

    2001-01-01

    Objective: To study: (1) The labelling method of 99m Tc-BW250/183 and its organ distribution pattern after injection. (2) The clinical value of bone marrow immunoscintigraphy of evaluation of patients with aplastic anemia. (3) The clinical value of bone marrow immunoscintigraphy of determination of bone metastasis. Methods: (1) Whole body imaging was performed to one volunteer after injection of 555 MBq 99m Tc-BW250/183, meanwhile, 2 ml blood samples was taken from a cubital vein. The percentage of radioactivity of different organs and the kinetic data of in-vivo 99m Tc-BW250/183 was then calculated. In all the blood samples the peripheral leukocytes were counted by a standard procedure. (2) Bone marrow immunoscintigraphy were performed to 8 patients with aplastic anemia 4 h after injection of 99m Tc-BW250/183, 6 of them also underwent bone marrow imaging with 99m Tc-SC. (3) Bone marrow immunoscintigraphy and conventional bone scan were performed to 14 patients with suspected bone metastases to detect bone metastases. The results was compared with X-ray, X-CT or MRI. Results: 99m Tc-BW250/183 is a safe and ideal bone marrow imaging agent. Bone marrow immunoscintigraphy plays an important role in evaluating patients with aplastic anemia and determining bone metastases

  15. Testing of 99mTc labelled sucralfate in induced gastric and duodenal ulcers

    International Nuclear Information System (INIS)

    Pallagi, Katalin; Janoki, Gyoezoe

    1988-01-01

    The conditions of in vitro labelling of sucralfate available in medical practice were established according to literature data including some modifications. Labelling efficiency proved to be 98.1%. The radiopharmaceutical is stable over 6 hours in vitro. 99m Tc-sucralfate accumulates in experimentally induced gastric and duodenal ulcers thus tracing the site of the ulcerous lesion. (author) 14 refs.; 3 tabs

  16. Biodistribution of {sup 99m}Tc-labeled anti-human epidermal growth factor receptor (EGF-R) humanized monoclonal antibody h-R3 in a xenograft model of human lung adenocarcinoma

    Energy Technology Data Exchange (ETDEWEB)

    Morales-Morales, Alejo; Duconge, Jorge; Caballero-Torres, Idania; Nunez-Gandolff, Gilda; Fernandez, Eduardo; Iznaga-Escobar, Normando E-mail: normando@ict.cim.sld.cu

    1999-04-01

    The anti-human epidermal growth factor receptor (EGF-R) humanized monoclonal antibody (MAb) h-R3 is an (IgG{sub 1}), which binds to an extracellular domain of EGF-R. It was used to evaluate the biodistribution on nude mice xenografted with H-125 human lung adenocarcinoma cell line. Results were compared with its murine version of the MAb ior-egf/r3. Twenty-one athymic female 4NMRI nu/nu mice were injected intraperitoneally with 10 {mu}g/100 {mu}Ci of {sup 99m}Tc-labeled MAbs. Immunoreactivity of {sup 99m}Tc-labeled MAbs were measured by enzyme-linked immunosorbent assay (ELISA) on H-125 cell line and the immunoreactive fractions was determined by the Lindmo method. Among all organs, significant accumulation was found in serum (27.05 {+-} 2.08 %ID/g) and tumor (3.903 {+-} 0.89 %ID/g) at 4 h after injection. These values decreased to 5.03 {+-} 0.50 %ID/g and 2.19 {+-} 0.56 %ID/g for serum and tumor, respectively. The immunoreactive fraction was found to be 0.70, with a correlation coefficient r=0.9984. With the good biodistribution and tumor uptake of the {sup 99m}Tc-labeled humanized antibody h-R3, a phase I diagnostic clinical trial of tumor with epithelial origin should be pursued.

  17. Detection of sites of infection in mice using 99mTc-labeled PN2S-PEG conjugated to UBI and 99mTc-UBI: a comparative biodistribution study

    International Nuclear Information System (INIS)

    Melendez-Alafort, Laura; Nadali, Anna; Pasut, Gianfranco; Zangoni, Elena; De Caro, Raffaele; Cariolato, Luca; Giron, Maria Cecilia; Castagliuolo, Ignazio; Veronese, Francesco M.; Mazzi, Ulderico

    2009-01-01

    The antimicrobial peptide ubiquicidin (UBI) directly labeled with technetium-99m ( 99m Tc) has recently been shown to be specifically taken up at sites of infection; however, its chemical structure is not well defined. To address this problem, the aim of the present study was to label UBI using poly(ethyleneglycol)-N-(N-(3-diphenylphosphinopropionyl)glycyl) -S-tritylcysteine ligand (PEG-PN 2 S) in order to compare its ability to detect infection sites with that of 99m Tc-UBI. Methods: The PN 2 S-PEG-UBI conjugate was prepared and labeled with 99m Tc, and its radiochemical purity was subsequently assessed. The stability of the conjugate to cysteine challenge and dilution with both saline solution and phosphate buffer was determined and serum stability and protein binding were also assessed. In vivo studies were carried out in healthy mice to study the biodistribution of 99m Tc-PN 2 S-PEG-UBI and its precursor 99m Tc-PN 2 S-PEG and in infected mice to compare the uptakes of 99m Tc-UBI and 99m Tc-PN 2 S-PEG-UBI at the site of infection using scintigraphic imaging and ex vivo tissue counting. Results: 99m Tc-PN 2 S-PEG-UBI was obtained with high radiochemical purity (98±1%) and high stability. The amphiphilic nature of the conjugate leads to a tendency to form micellar aggregates that explain the high protein binding values obtained. Biodistribution studies in mice showed low renal clearance followed by a predominant reticuloendothelial system clearance that limits its application in the abdominal area. Statistical analysis revealed no significant difference between 99m Tc-UBI and 99m Tc-PN 2 S-PEG-UBI uptake in infected mouse thigh, and the site of infection was clearly visualized using scintigraphic imaging. Conclusions: 99m Tc-PN 2 S-PEG-UBI proved to be as effective as 99m Tc-UBI in detecting sites of infection; however, the well-defined chemical structure of 99m Tc-PN 2 S-PEG-UBI makes it a better candidate for clinical imaging of infection

  18. Preparation and labelling hydroxyapatite with 223Ra and 99mTc

    International Nuclear Information System (INIS)

    Malkova, E.; Micolova, P.; Vlk, M.; Kozempel, J.; Rabyk, M.

    2015-01-01

    The aim of this study was the preparation, studies and investigation of novel nanoparticles suitable for targeted delivery of 223 Ra and 99 mTc. Preliminary experiments were focused on the synthesis of hydroxyapatite nanoparticles (HANPs) and their affinity to 223 Ra and 99m Tc. Technetium-99m ( 99 mTc, T 1 /2 = 6.0 h) is the most commonly used medical radionuclide for diagnostic procedures. Radium-223 is the first -emitting radionuclide approved for targeted radionuclide therapy. The physical half-life of 223 Ra of 11.4 days is providing sufficient time for the synthesis, distribution and administration of the radiopharmaceutical to patients. HANPs labelling yields with 223 Ra were 95 - 100 % and with 99m Tc were 93 - 94 % depending on the reaction conditions. HANPs were studied on FT-IR (Fourier transform infrared spectroscopy), XRPD (X-Ray Powder Diffraction), DLS (Dynamic Light Scattering), and the sizes of nanoparticles were studied at temperatures 80, 120 and 200 grad C. (authors)

  19. Development of an instant 99mTc labelled HIG kit for localization of infection/inflammation

    International Nuclear Information System (INIS)

    Chen Fang; Zhang Yumin; Zhou Qian

    1995-01-01

    99m Tc labelled polyclonal human immunoglobulin G(HIG) is a novel agent for detecting infection and inflammation. We report the preparation, quality control, pharmacology and preliminary clinical evaluation of this imaging agent. After modification of HIG and purification, the HIG kit was formulated and lyofilized. Labelling yield and radiochemical purity were determined by TLC-SG, PC and Sephadex G-50 column chromatography. Animal models for pharmacologic experiments were mice, rats and rabbits. The labelling yield was 99% immediately after mixing HIG with 99m Tc and more than 90% of radioactivity was retained after keeping the labelled product at room temperature 24 hours post labelling. There were good accumulation and high T/B ratio in animal models (rats and rabbits bearing turpentine and Staphylococcus aureus induced inflammatory or infections foci). The results showed that this new agent is nearly ideal for localization of infections/inflammatory lesions

  20. The preparation of Tc-99m labeled liposomes by a cationic SP/DOPE formulation for tumor imaging

    International Nuclear Information System (INIS)

    Yu, M.D.; Hsieh, D.S.; Huang, W.S.

    2002-01-01

    Aim: Liposomes can provide a gene delivery system to be used in the cancer gene therapy. Radiolabeled liposomes can be used in tumor imaging and tumor therapy. A new cationic liposome formulation of sphingosin e (SP) and dioleoylphosphatidylethanolamine (DOPE) was developed and showed very efficient transfection in a wide variety of mammalian cancer cells, including SKOV-3 (human ovarian carcinoma cells), NPC076 (human nasopharyngeal carcinoma cells), and A431 (human epidermoid carcinoma cells) (Kao et al., Oncol Reports. 5:625-629, 1998). The present study is designed and evaluated the labeling and stability of Tc-99m liposomes by SP/DOPE formulation. Material and Methods: A mixture of 8 mg of SP (Sigma Chemical) and 8 mg of DOPE (Sigma Chemical) dissolved in 4 ml absolute ethanol and used as a lipid stock solution (4 mg/ml). In the direct labeling method, taking 0.25 ml (1 mg) stock solution dried under nitrogen gas and then added 1 ml 20 mM HEPES buffer for hydration 8 hours. The remaining stock solution was dried, hydrated 8 hours, and sonicated 10 min to form liposomes for after-loading labeling method (preformed liposomes). The labeling studies included Tc-99m direct labeling (1), Tc-99m HMPAO direct labeling (2), Tc-99m stannous chloride after-loading labeling (3), Tc-99m HMPAO after-loading labeling (4), and Tc-99m pCMVβ DNA inclusion labeling (5). The labeling efficiency (LE) was determined by thin layer chromatography. The labeled liposomes were incubated with fetal bovine serum (FBS) 30 min to evaluate their stability. Results: It is shown that LE (48%) of Tc-99m direct labeling was the highest in the five methods; however, the LE was reduced to 9% (corrected to original LE) after incubating with serum. Tc-99m may be loosely conjugated to the outer surface of the liposomes. The LE (32%) of Tc-99m HMPAO direct labeling was the second; however, LE was most stable when incubating with serum. The LE of the after-loading labeling was not better than that of

  1. The labeling of white blood cells with 99mTc and 111In complexes

    International Nuclear Information System (INIS)

    Hadizad, T.; Najafi, R.

    1993-01-01

    Leukocytes have been labelled with a variety of gamma emitters and labelled (mixed) leukocytes are used clinically to detect and localize sites of abscess in the abdominal area and inflammatory processes surrounding grafts, ulcerative colitis and study of leukocyte kinetics. In this project we used 99m Tc-Sn-Pyp, 99m Tc-Hexamethyl propenylamine oxine, 111 In-Tropolone and 111 In-Oxine Sulfate for the labelling of leukocytes. All the in vitro and in vivo tests have been done to get an optimum condition for injection

  2. Osteomyelitis diagnosis by 99mTc radiolabeled aptamers

    International Nuclear Information System (INIS)

    Santos, S.R.; Ferreira, I.M.; Andrade, A.S.R.; Barros, A.L.B.; Cardoso, V.N.; Diniz, O.F.

    2015-01-01

    Osteomyelitis, which is characterized by progressive inflammatory destruction and new opposition of bone, is still a difficult infection to treat. The clinical diagnosis in late stages is achieved easily, but an early diagnosis is more challenging. Staphylococcus aureus is a common agent found in osteomyelitis and bone prostheses infection. Diagnosis by scintigraphy has advantages because it is a non-invasive procedure and is able to perform an early diagnosis even before anatomic changes. Thus, nuclear medicine could contribute to an accurate diagnosis since specific radiopharmaceuticals were developed. In this study, aptamers selected to Staphylococcus aureus were labeled with 99m Tc and used for bacteria identification in an osteomyelitis experimental model. The aptamers selected to S. aureus were directly labelled with 99m Tc and were evaluated by biodistribution studies. Wistar rats with intraosseous infection in the right paw were used. A random aptamer labelled with 99m Tc was as control. Six animals were used in each group. The aptamers labeled with 99m Tc were able to identify the infection foci caused by S. aureus displaying a target/non-target ratio of 2,23 ± 0,20, after 3 h. The control group presented a target/non-target ratio 1,08 ± 0.23. The results indicated that the radiolabeled aptamers were able to identify specifically the infection foci and they should be further explored for infection diagnosis by scintigraphy. (author)

  3. Synthesis and animal experiment of 99mTc-labeled hepatobiliary imaging agents

    International Nuclear Information System (INIS)

    Zhou Xirui; Chen Shaoliang; Chen Guohui; Xu Qinfeng

    1993-01-01

    Six new compounds based on the principle of isosterism and hybridization had been synthesized. Methobrofenin was prepared by reduction of nitro mesitylene, followed by bromination and acylation with nitrilotriacetic acid. The 99m Tc-complexes of these compounds were prepared by stannous chloride reduction of sodium pertechnetate in aqueous solution. These labeled compounds, being similar to 99m Tc-mebrofenin, all were quick in the uptake by the liver cells, rapidly cleared off from the blood in mice, and had higher cumulative hepatobiliary excretion rates than Tc-99m-EHIDA

  4. Technetium-99m labeled monoclonal antibodies in the detection of metastatic melanoma

    International Nuclear Information System (INIS)

    Serafini, A.N.; Kotler, J.; Feun, L.; Dewanjee, M.; Robinson, D.; Salk, D.; Sfakianakis, G.; Abrams, P.; Savaraj, N.; Goodwin, D.

    1989-01-01

    Twenty-six stage II/III malignant melanoma patients with 321 measurable metastatic lesions were imaged using Fab fragments of an IgG murine monoclonal antibody labeled specifically with 10-30 mCi Tc-99m with a bi-functional chelating method (NeoRx, Seattle, WA). There were no side effects or adverse reactions. Immunoscintigraphy demonstrated 66.6% of lesions larger than 1 cm and 92.5% of lesions larger than 3 cm. Most frequently detected metastases were in lymph nodes, subcutaneous areas, and bone. Of lesions less than 1 cm, 23.6% were detected if superficial cutaneous lesions were excluded. The smallest detectable lesion was 4 mm. Twenty-one additional clinically unsuspected sites were visualized in 12 of the 26 patients studied. Of these, 56% were confirmed as metastasis by other tests. There were apparent nonspecific localizations owing to other causes, including fracture, varicosities, skin abscess and pneumonitis. Increased experience in image analysis facilitates correct interpretation of these localizations. This study demonstrates that imaging with Tc-99m labeled antibody fragments detects melanoma lesions in organs routinely surveyed and in other areas not routinely assessed by other imaging techniques. The procedure is readily performed and safe. The principal advantage of the test is its ability to survey the entire body and all organs with a single test. Its principal limitation, in common with other diagnostic imaging procedures, is its poor sensitivity for detecting lesions less than 1 cm

  5. Labelling malaria-infected human erythrocytes with Tc-99m

    International Nuclear Information System (INIS)

    Garmelius-Larsson, B.; Pettersson, F.; Vogt, A.; Jonsson, C.

    2002-01-01

    Aim: Malaria is an old and a very common disease, especially in undeveloped countries. The malaria parasites infect the erythrocytes and the aim of this work was to label infected cells for future studies of their distribution and life span. Material and Method: With a commercial kit containing stannous fluoride and sodium medronate, which is used to label erythrocytes in vivo, in vitro and in vivo/vitro methods, we labelled the cells by using a modified method and a small volume, 5 - 50 microlitre, of packed cells. The cells were labelled with Tc-99m in the range of 60 - 1500 MBq. The kit was reconstituted with saline and the pH was adjusted to 7.0. The cells were incubated with 1 ml of the kitsolution in 37 0 C for 5 min. The remaining Sn-ions were reduced by adding NaOCl and then the solution was centrifuged.The supernantant was discarded and the Tc-99m was added to the precipitate and incubated 37 0 C for 20 min and then washed 3 times. This labelling procedure was performed on both infected and on non-infected cells. Results: Ten samples of cells have been labelled. The best labelling result was obtained using 7 - 20 MBq per 10 microlitre of packed cells. The labelling efficiency was, on average, 35%. Conclusion: It is possible to label both infected and non-infected cells in very small volumes. The cells were visually inspected in a microscope and were viable after labelling. Furthermore, the cell distribution was traced in vivo in an animal model by a gamma camera

  6. New series of Tc-99m-labeled hepatobiliary tracers: N'-acyl- and N'-sulfonyl ethylenediamine-N,N-diacetic acids

    International Nuclear Information System (INIS)

    Karube, Y.; Kono, A.; Maeda, T.; Ohya, M.; Matsushima, Y.

    1981-01-01

    Various Tc-99m-labeled N'-substituted derivatives of ethylenediamine-N,N-diacetic acid (EDDA) are evaluated as hepatobiliary imaging agents. N-substituted aromatic acyl and aromatic sulfonyl derivatives of EDDA, labeled with Tc-99m, were administered to rabbits and golden hamsters, and the distribution indicated clearance by the hepatobiliary system. N'-aromatic sulfonyl EDDAs were labeled with Tc-99m by the SnCl 2 method with more than 99% yield. Clearance of Tc-99m-p-toluenesulfonyl EDDA from the blood and the liver was as rapid as that of TC-99m N-(2,6-diethylphenylcarbamoylmethyl)iminodiacetic acid (Tc-99m benzenesulfonyl EDDA lowered urinary excretion. It is concluded that the sulfonyl EDDAs provide a fruitful source for Tc-99m-labeled hepatobiliary radiopharmaceuticals

  7. New series of Tc-99m-labeled hepatobiliary tracers: N'-acyl- and N'-sulfonyl ethylenediamine-N,N-diacetic acids

    International Nuclear Information System (INIS)

    Karube, Y.; Kono, A.; Maeda, T.; Ohya, M.; Matsushima, Y.

    1981-01-01

    Various Tc-99m-labeled N'-substituted derivatives of ethylenediamine-N,N-diacetic acid (EDDA) are evaluated as hepatobiliary imaging agents. N'-substituted aromatic acyl and aromatic sulfonyl derivatives of EDDA, labeled with Tc-99m, were administered to rabbits and golden hamsters, and the distribution indicated clearance by the hepatobiliary system. N'-aromatic sulfonyl EDDAs were labeled with Tc-99m by the SnCl 2 method with more than 99% yield. Clearance of Tc-99m-p-toluenesulfonyl EDDA from the blood and the liver was as rapid as that of Tc-99m N-(2,6-diethylphenylcarbamoylmethyl)iminodiacetic acid (Tc-99m diethyl IDA). Substitution of a bulky group at the aromatic ring in Tc-99m benzene-sulfonyl EDDA lowered urinary excretion. It is concluded that the sulfonyl EDDAs provide a fruitful source for Tc-99m-labeled hepatobiliary radiopharmaceuticals

  8. Freeze-dried formulation for direct {sup 99m}Tc-labeling ior-egf/r3 MAb: additives, biodistribution, and stability

    Energy Technology Data Exchange (ETDEWEB)

    Morales, Alejo A. Morales; Nunez-Gandolff, Gilda; Perez, Niuvis Perez; Veliz, Belkis Chico; Caballero-Torres, Idania; Duconge, Jorge; Fernandez, Eduardo; Crespo, Francisco Zayas; Veloso, Ana; Iznaga-Escobar, Normando E-mail: normando@ict.sld.cu

    1999-08-01

    Monoclonal antibodies (MAbs) have been useful for immunoscintigraphic applications in clinical diagnosis since they were introduced in nuclear medicine practice. The MAb ior egf/r3 developed at the Center of Molecular Immunology (Havana, Cuba) is a murine antibody that recognizes the human epidermal growth factor receptor (EGF-R) and has been used widely in the radioimmunodiagnosis of tumors of epithelial origin. Based on the direct Schwarz method, the present report describes the preparation of a freeze-dried formulation for radiolabeling the MAb ior egf/r3 with {sup 99m}Tc for immunoscintigraphic applications. Radiolabeling efficiency, effects on immunoreactivity, biodistribution, pharmacokinetic, and stability of the formulation are reported. The study demonstrated that the freeze-dried formulation can be labeled with {sup 99m}Tc at high yield. The resulting {sup 99m}Tc-labeled ior egf/r3 MAb can be used to visualize in vivo human tumors of epithelial origin by immunoscintigraphy studies. The kit does not need any other addition or purification at the time of tagging other than the requisite amount of pertechnetate (40-50 mCi). Because the contents of the kit are lyophilized, no special storage or transportation is required.

  9. Inferior vena cava filter thrombus: A possible cause of an unanticipated finding of {sup 99m} Tc-labeled red blood cell scintigraphy

    Energy Technology Data Exchange (ETDEWEB)

    Song, Hee Sung; Choi, Joon Hyouk; Kim, Young Suk [Jeju National University School of Medicine, Jeju (Korea, Republic of)

    2016-06-15

    {sup 99m}Tc-labeled red blood cell scintigraphy, a sensitive and specific diagnostic test, is useful for patients suspected of suffering from active gastrointestinal bleeding. This study follows a case of a patient who was suspected of gastrointestinal bleeding after an inferior vena cava filter was inserted due to a deep vein thrombosis of the femoral vein. To evaluate an exact focus of bleeding, {sup 99m}Tc-labeled red blood cell scintigraphy was executed. Herein, an unanticipated finding of {sup 99m}Tc-labeled red blood cell scintigraphy probably due to a thrombus on the inferior vena cava filter is reported.

  10. Somatostatin analogues labelled with 99mTc

    International Nuclear Information System (INIS)

    Obenaus, Esteban R.; Crudo, Jose L.; Edreira, Martin M.; Castiglia, Silvia G.

    1999-01-01

    Biological and radiochemical studies have been carried out on two labelled somatostatin analogues, the peptide RC-150 and the Tyr 3 -Octreotide. Both analogues have been labelled with 99m Tc using the direct and the indirect method and MAG-3 and HYNIC as chelating agents. By the direct method RC-150 was labelled using sodium ascorbate and dithionite as reducing agents. The radiochemical purity was 70%. By the indirect method, in the case of RC-160 with MAG-3 a radiochemical purity higher than 70% was attained while a purity of 100% was reached in the case of Tyr 3 -Octreotide with HYNIC. The biological distribution of HYNIC-Tyr 3 -Octreotide has been studied in rats. (author)

  11. 99mTc-labeling of HYNIC-conjugated cyclic RGDfK dimer and tetramer using EDDA as coligand.

    Science.gov (United States)

    Wang, Jianjun; Kim, Young-Seung; Liu, Shuang

    2008-03-01

    In this study, EDDA (ethylenediamine- N, N'-diacetic acid) was used as the coligand for 99mTc-labeling of cyclic RGDfK conjugates: HYNIC-dimer (HYNIC = 6-hydrazinonicotinamide; dimer = E[c(RGDfK)]2) and HYNIC-tetramer (tetramer = E{E[c(RGDfK)]2}2). First, HYNIC-dimer was allowed to react with 99mTcO4 (-) in the presence of excess tricine and stannous chloride to form the intermediate complex [99mTc(HYNIC-dimer)(tricine)2], which was then allowed to react with EDDA to afford [99mTc(HYNIC-dimer)(EDDA)] with high yield (>90%) and high specific activity ( approximately 8.0 Ci/micromol). Under the same radiolabeling conditions, the yield for [99mTc(HYNIC-tetramer)(EDDA)] was always EDDA bonding to the 99mTc-HYNIC core in [99mTc(HYNIC-dimer)(EDDA)]. The athymic nude mice bearing subcutaneous U87MG human glioma xenografts were used to evaluate the impact of EDDA coligand on the biodistribution characteristics and excretion kinetics of the 99mTc-labeled HYNIC-dimer and HYNIC-tetramer. Surprisingly, [99mTc(HYNIC-dimer)(EDDA)] and [99mTc(HYNIC-tetramer)(EDDA)] had almost identical tumor uptake over the 2 h period. The use of EDDA as coligand to replace tricine/TPPTS (TPPTS = trisodium triphenylphosphine-3,3',3''-trisulfonate) did not significantly change the uptake of the 99mTc-labeled HYNIC-dimer in noncancerous organs, such as the liver, kidneys, and lungs; but it did result in a significantly lower kidney uptake for the 99mTc-labeled HYNIC-tetramer due to faster renal excretion. It was also found that the radiotracer tumor uptake decreases in a linear fashion as the tumor size increases. The smaller the tumors are, the higher the tumor uptake is regardless of the identity of radiotracer.

  12. Peptic ulcer imaging with /sup 99m/Tc sucralfate and possible advantages of /sup 99m/Tc sucrose octasulfate

    International Nuclear Information System (INIS)

    CentiColella, A.; Scopinaro, F.

    1986-01-01

    Sucralfate is a basic aluminum salt of sucrose octasulfate that protects the damaged mucosa and also the normal mucosa from peptic aggression. In fact sucralfate adheres to the mucosa as pH decreases below 4, and buffers the acid, slowly releasing sucrose octasulfate that forms insoluble complexes with the proteins exuded by the ulcers, or is washed out of the stomach. Sucralfate itself is also able to precipitate with proteins in the ulcers. Sucralfate may be labelled by several methods: /sup 99m/Tc HSA, /sup 99m/Tc DTPA, /sup 75/Se, /sup 111/In. The aims of this study were to evaluate the clinical results obtained using /sup 99m/Tc DTPA sucralfate, which the authors believe is the only labelled sucralfate suitable for clinical studies and to discuss the possible diagnostic uses of /sup 99m/Tc sucrose octasulfate. In fact, it has been possible to label the sucrose octasulfate either with /sup 99m/Tc DTPA or with /sup 99m/Tc without the use of intermediate ligands

  13. Nifedipine effect on the labelling of blood cells and plasma proteins with Tc-99m

    International Nuclear Information System (INIS)

    Gutfilen, B.; Boasquevisque, E.M.; Bernardo Filho, M.

    1988-01-01

    The labeling of red blood cells (RBC) with Tc-99m depends on the presence of stannous ion (Sn) that helps this radionuclide's fixation on the hemoglobin molecule. Nifedipine is an agent capable to block a specific way where calcius (Ca) ion acrosses the cellular membrane and to bind itself on plasma proteins. The effect of nifedipine in the labeling of RBC and plasma proteins with Tc-99m was studied because of similarities between Ca and Sn ions. Blood with anticoagulant was treated with nifedipine concentration of 10 -6 M for 15 min at 37 0 C. The labeling of RBC with Tc-99m was done incubating with Sn ion solution (3 uM) for different times. The % of radioactivity in RBC was determined. Samples of plasma were precipited with trichloroacetic acid and the % of radiocctivity in insoluble fraction was calculated. The same procedure was done using different nifedipine concentrations and the blood was incubated for 60 min with Sn ion. The determination of the % of Tc-99m labeled in RBC and plasma proteins showed that this drug does not have the capability to alter this incorporation because the results are similar to control. It is suggested that the Sn ions passage across RBC is not altered by nifedipine although this drug could bind to plasma protein, it does not modify the Tc-99m fixation on it. (author) [pt

  14. Synthesis and biological evaluation of a novel 99mTc-labelled MPP

    International Nuclear Information System (INIS)

    Lin Yan; Zhang Junbo; Tang Zhigang; Wang Xuebin; Zhang Xianzhong

    2008-01-01

    The 5-HT 1A receptor is tightly implicated in numerous mental illnesses, such as depression, anxiety, eating disorders and so on. Thus, it has become a key target for various efforts in developing in vivo imaging agents. Many efforts have been focused on the development of 99m Tc labeled 5-HT 1A receptor-bound radiotracer. In this study, a dithiocarbamate ligand containing the MPP ((2-methoxyphenyl)piperazine) moiety was labeled with [ 99m TcN] 2+ core and evaluated as potential imaging agent for 5-HT 1A receptor. (authors)

  15. Optimizing labeling conditions for cysteine-based peptides with 99mTc

    International Nuclear Information System (INIS)

    Sabahnoo, Hamideh; Hosseinimehr, Seyed Jalal

    2016-01-01

    Radiolabelled peptides have attracted a great deal of attention due to their wide applicability in the development of target-specific radiopharmaceuticals. They can easily be used in diagnostic imaging as carriers for the delivery of radionuclides to tumors as well as for therapy. Previous investigations revealed that technetium(V) could form stable complexes with peptide-based ligands of N 3 S type such as Cys-Gly-Gly-Gly. Herein, a targeting HER-2 receptor peptide was labeled with technetium- 99m ( 99m Tc) with two different types of tetrapeptide-based ligands, Cys-Gly-Gly-Gly and Cys-Ser-Ser-Ser. The effect of experimental parameters in the labeling procedure such as type of buffer solutions, pH of media, and type of exchange ligands were optimized toward obtaining maximum labeling yield. The optimum labeling conditions were different for two peptides. Shelf life of both labeled peptides was determined by analytical reversed-phase high-performance liquid chromatography (RP-HPLC) and thin layer chromatography (TLC) that showed radiochemical yield up to 95% even after 4 h. (author)

  16. Labelling study of galacturonic acid with Tc-99m and investigation of the biokinetic behaviour in experimental animals

    International Nuclear Information System (INIS)

    1988-01-01

    The main criterion in the selection of a proper ligand to be labelled with Technetium is to match the requirement of a radiopharmaceutical of good biological specificity, where the target organ-to-background ratio is considerably high. Perliminary study on experimental animals has shown, that galacturonic acid is among those ligands of high renal specificity after complexing with Tc-99. In this communication we describe for the first time the labelling of galacturonic acid with Tc-99, using stannous chloride as a reducing agent for pertechnetate. The radioanalytical results assessed by gelchromatography column scanning (GCS) method, reveal that, the labelling efficiency of (Tc)99-galacturonate complex is promoted by raising the pH of the reaction mixture to a value higher than 7 using tris (hydroxymethyl) aminomethane buffer. The optimal amounts of the reactants to obtain a high labelled and stable complex with high kidney uptake, were found to be not less than 50 mg galacturonic acid and not more than 200 Mg SnCl2.H2O in the preparation

  17. Huge Varicose Inferior Mesenteric Vein: an Unanticipated 99mTc-labeled Red Blood Cell Scintigraphy Finding

    International Nuclear Information System (INIS)

    Hoseinzadeh, Samaneh; Shafiei, Babak; Salehian, Mohamadtaghi; Neshandar Asli, Isa; Ghodoosi, Iraj

    2010-01-01

    Ectopic varices (EcV) are enlarged portosystemic venous collaterals, which usually develop secondary to portal hypertension (PHT). Mesocaval collateral vessels are unusual pathways to decompress the portal system. Here we report the case of a huge varicose inferior mesenteric vein (IMV) that drained into peri rectal collateral veins, demonstrated by 99m Tc-labeled red blood cell (RBC) scintigraphy performed for lower gastrointestinal (GI) bleeding in a 14-year-old girl. This case illustrates the crucial role of 99m Tc-labeled RBC scintigraphy for the diagnosis of rare ectopic lower GI varices.

  18. Evaluation of 99mTc labelled human immunoglobulin (99mTc-HIG) in infection/inflammatory foci imaging. Final report for the period 15 December 1996 - 15 August 1997

    International Nuclear Information System (INIS)

    Shimpi, H.H.

    1997-10-01

    The aim of the study was to investigate whether the labelling efficiency biodistribution and inflammatory focus detection are dependent on the source of the human immunoglobulin G (HIG) and the chelating agent used in the labelling of the HIG with 99mTc. Three forms of immunoglobulins; Gamma venin P, Intraglobulin F and Sandoglobulin were used in this study. Reduction of HIG was done by 2-mercaptoethanol at molar ratio 1000:1, with 30 minutes reaction time at room temperature. The reduced HIG was then purified, membrane filtered aliquoted and lyophilised. Lyophilised HIG was dissolved in sterile normal saline and chelated with one of the following ligands Sn-MDP, SN PYP, Sn DTPA, SN-GH and Sn-citrate and then added 99m Tc04 for labelling. The radiochemical purity of the labelled compound was 90%. The biodistribution studies were done wistar rats where in the experimental groups were sacrifised at 3,5 and 24 hours following 99mTc HIG injection intravenously. Imaging studies were carried out in rabbits. Sterile inflammatory lesions were produced in the thigh muscle of these animals by injection of turpentine oil and the contralateral thigh muscle served as-controls. The results showed that there was no significant difference in biodistribution and inflammatory focus uptake of 9gmTc HIG with respect to the sources of HIG. There was favourable biodistribution characteristics when the ligands used were Sn MDP and Sn-Citrate

  19. /sup 99m/Tc-aminohexylidendiphosphonate and /sup 99/mTc-Pyrophosphate in the scintigraphic diagnosis of experimental cardiomyopathy in dogs

    Energy Technology Data Exchange (ETDEWEB)

    Duska, F; Kafka, P; Mazurova, Y; Hadas, L; Vizda, J; Palicka, V; Grossman, V

    1987-10-01

    Experimental cardiomyopathy was provoked in 24 dogs with high intravenous doses of adrenaline and theophylline. These lesions were studied by means of the new agent /sup 99m/Tc-AHDP and /sup 99m/Tc-PYP in comparison. Cardiomyopathy could be imaged as early as 4 h after the onset of involvement but not later than 7 days. A maximum accumulation occurred in lesions 24 h old, /sup 99m/Tc uptake in the myocardium was graded scintigraphically, /sup 99m/Tc-AHDP was accumulated in the altered myocardium to a greater extent than /sup 99m/Tc-PYP. Scintigraphic findings were in good agreement with plasma levels of creatine-kinase. A comparison with histology demonstrated that the maximum accumulation of radiopharmaceuticals occurred at the time when the development of myocardium involvement reached the stage of myocytolysis.

  20. Study of the properties of sup(99m)Tc-DTPA-ferroascorbinate and sup(99m)Tc-dextrose as radiopharmaceuticals for renal scintiscanning

    International Nuclear Information System (INIS)

    Salambashev, L.; Konstantinov, P.; Ketskarova, S.; Kovacheva, S.; Babeva, S.

    1979-01-01

    Description is made of an own method for labelling of the complex DTPA-ferroascorbinate and dextrose with sup(99m)Tc for the purpose of renal scintiscanning. Experimental investigations on rabbits were carried out, and afterwards conventional scintiscanning and follow-up of the intake into the renal parenchyma by means of gamma camera were performed on 15 patients. The observations revealed that sup(99m)Tc-DTPA-ferroascorbinate was more rapidly excreted (40 min to 2 h following the intravenous administration). For this reason it is more convenient for gamma camera examination, while sup(99m)Tc-dextrose is fixing more lastingly in the parenchyma and respons to all requirements with respect to radiopharmaceuticals for conventional renal scintiscanning. (author)

  1. Osteomyelitis diagnosis by {sup 99m}Tc radiolabeled aptamers

    Energy Technology Data Exchange (ETDEWEB)

    Santos, S.R.; Ferreira, I.M.; Andrade, A.S.R., E-mail: sararoberta7@hotmail.com, E-mail: imendesf@yahoo.com.br, E-mail: antero@cdtn.br [Centro de Desenvolvimento da Tecnologia Nuclear (CDTN/CNEN-MG), Belo Horizonte, MG (Brazil); Barros, A.L.B.; Cardoso, V.N.; Diniz, O.F., E-mail: brancodebarros@yahoo.com.br, E-mail: valbertcardoso@yahoo.com.br, E-mail: simoneodilia@yahoo.com.br [Universidade Federal de Minas Gerais (UFMG), Belo Horizonte, MG (Brazil). Faculdade de Farmacia. Departamento de Analises Clinicas e Toxicologicas

    2015-07-01

    Osteomyelitis, which is characterized by progressive inflammatory destruction and new opposition of bone, is still a difficult infection to treat. The clinical diagnosis in late stages is achieved easily, but an early diagnosis is more challenging. Staphylococcus aureus is a common agent found in osteomyelitis and bone prostheses infection. Diagnosis by scintigraphy has advantages because it is a non-invasive procedure and is able to perform an early diagnosis even before anatomic changes. Thus, nuclear medicine could contribute to an accurate diagnosis since specific radiopharmaceuticals were developed. In this study, aptamers selected to Staphylococcus aureus were labeled with {sup 99m}Tc and used for bacteria identification in an osteomyelitis experimental model. The aptamers selected to S. aureus were directly labelled with {sup 99m}Tc and were evaluated by biodistribution studies. Wistar rats with intraosseous infection in the right paw were used. A random aptamer labelled with {sup 99m}Tc was as control. Six animals were used in each group. The aptamers labeled with {sup 99m}Tc were able to identify the infection foci caused by S. aureus displaying a target/non-target ratio of 2,23 ± 0,20, after 3 h. The control group presented a target/non-target ratio 1,08 ± 0.23. The results indicated that the radiolabeled aptamers were able to identify specifically the infection foci and they should be further explored for infection diagnosis by scintigraphy. (author)

  2. In vitro assessment of cytotoxicity and labeling efficiency of 99mTc-HMPAO with stromal vascular fraction of adipose tissue

    International Nuclear Information System (INIS)

    Verma, V.K.; Beevi, S.S.; Tabassum, A.; Kumaresan, K.; Kamaraju, R.S.; Arbab, A.S.; Chelluri, L.K.

    2014-01-01

    Introduction: Noninvasive radionuclide imaging of cells using technetium99m-hexamethylpropyleneamine oxime ( 99m Tc-HMPAO) is a potential diagnostic tool for several applications. Herein we aimed to evaluate the labeling efficiency and cellular toxicity of 99m Tc-HMPAO with Stromal Vascular Fraction (SVF) of adipose tissue to develop a process tool for theranostic purposes, in particular imaging cardiac stem cell therapy. Methods: Ten million cells of SVF were labeled with 99m Tc-HMPAO complex and excess radiolabel was cleared off through washing in PBS. The labeling efficiency of 99m Tc-HMPAO was detected in labeled cells and their subsequent supernatant wash using isotope dose calibrator and gamma camera. The cytotoxicity was assessed for the comparative reactive oxygen species (ROS) by H 2 DCFDDA, apoptotic events by annexin-V and TUNEL assay and mitochondrial potential by JC-1. Results: An encouraging labeling efficiency of 33% was observed with 99m Tc-HMPAO complex. The radionuclide labeling of SVF demonstrated significant safety profile as evaluated by apoptotic assays. Conclusion: 99m Tc-HMPAO labeling efficiency of 33% of total SV fraction would produce sufficient radioactive signals that would enable for in vivo tracking of cells by SPECT-CT. The radionuclide did not demonstrate any significant impact on the structural or functional organization of the labeled cells. Our study indicates that SVF can be safely labeled with 99m Tc-HMPAO without adverse cytotoxic events and for its potential role in imaging cardiac stem cell therapy

  3. Biodistribution studies of 99mTc-labeled myoblasts in a murine model of muscular dystrophy

    International Nuclear Information System (INIS)

    Colombo, F.R.; Torrente, Y.; Casati, R.; Benti, R.; Corti, S.; Salani, S.; D'Angelo, M.G.; DeLiso, A.; Scarlato, G.; Bresolin, N.; Gerundini, P.

    2001-01-01

    The purpose of this study was twofold: first, to evaluate the myoblast labeling of various 99m Tc complexes and to select the complex that best accomplishes this labeling, and second to evaluate the biodistribution of myoblasts labeled with this complex using mice with MDX muscular dystrophy (the murine homologue of Duchenne's muscular dystrophy). The following ligands were used to prepare the corresponding 99m Tc complexes: hexakis-methoxy-isobutyl-isonitrile (MIBI), bis(2-ethoxyethyl)diphosphinoethane (Tf), (RR,SS)-4,8-diaza-3,6,6,9-tetramethyl-undecane-2,10-dione-bisoxime (HM-PAO), bis(N-ethyl)dithiocarbamate (NEt), and bis(N-ethoxy, N-ethyl)dithiocarbamate (NOEt). One million murine myoblasts were incubated for 30-60 minutes with 5 mCi of each of the 99mTc complexes prepared from the above ligands. Viability was assessed by microscopic counting after trypan blue staining, and the radioactivity absorbed in the cells was measured after centrifugation. The compound with the highest uptake in cellular pellets was [ 99m Tc]N-NOEt. The biodistribution of myoblasts labeled with this complex was evaluated after intraaortic injection in dystrophic mice. Such an approach has the potential of effecting widespread gene transfer through the bloodstream to muscles lacking dystrophin

  4. Pharmacokinetics, biodistribution and dosimetry of 99mTc-labeled anti-human epidermal growth factor receptor humanized monoclonal antibody R3 in rats

    International Nuclear Information System (INIS)

    Escobar, Normando Iznaga; Morales, Alejo Morales; Duconge, Jorge; Torres, Idania Caballero; Fernandez, Eduardo; Gomez, Jose A.

    1998-01-01

    The pharmacokinetics, biodistribution and dosimetry of 99m Tc-labeled anti-human epidermal growth factor receptor (anti-hEGF-r) humanized monoclonal antibody (MAb) R3 was investigated following intravenous injection in normal Wistar rats. Serum disappearance curves were best fit by a two-compartment model having a mean distribution half-life (t (1(2α)) ) of 0.250 h and a mean elimination (t (1(2β)) ) of 13.89 h. Among the various organs, a little accumulation of the radiolabeled antibody was found only in kidneys. Biodistribution and dosimetry studies in humans were performed by extrapolation of the animal data to humans. Absorbed dose to normal organs and the remainder of the whole body were estimated using the medical internal radiation dose formula, and dose contributions from radioactivity in transit through the gastrointestinal tract were estimated using a compartment model. Extrapolated values of radiation absorbed dose to normal organs in rads per millicurie administered were whole body, 0.0085; lower large intestine wall, 0.0898; small intestine, 0.0530; upper large intestine wall, 0.0731; and kidneys, 0.0455. The effective dose equivalent predicted was 0.0162 rem/mCi and the effective dose was found to be 0.015 rem/mCi. On the basis of the pharmacokinetics, biodistribution and internal radiation dosimetry information obtained in this study, a diagnostic phase I clinical trial with 99m Tc-labeled humanized MAb R3 conjugate in patients should be supported

  5. Labeling of scorpion venom with 99mTc and its biodistribution

    International Nuclear Information System (INIS)

    Amin, A.M.

    2013-01-01

    Labeling of scorpion venom (SV) was successfully achieved with 99m Tc using direct chelating method. Venom was labeled with 99m Tc using stannous chloride as reducing agent. Preliminary studies were done to establish the optimum conditions for obtaining the highest yield of the labeled venom. The labeling technique is effective, as a maximum labeling yield (97 %) was obtained after 30-min reaction time by using 80 μg SV in phosphate buffer of pH 7 and 25 μg Sncl 2 ·2H 2 O at room temperature. Venom was injected into normal mice to determine the excretion pathway. Biodistribution studies in normal mice with SV shows rapid clearance of the venom from blood and tissue except for kidneys. The improvement of the immunotherapeutic treatment of envenomation requires a better knowledge of the biological actions of the SV since tissue distribution studies are very important for clinical purpose. (author)

  6. Clearance of 99mTc-DTPA and experimentally increased alveolar surfactant content

    International Nuclear Information System (INIS)

    Bos, J.A.H.; Wollmer, P.; Bakker, W.; Hannappel, E.; Lachmann, B.

    1992-01-01

    The authors measured clearance of 99m Tc-labeled diethylenetriamine pentaacetic acid ( 99m Tc-DTPA) in rabbits with experimentally increased alveolar surfactant content. In one group of animals, surfactant production was increased by treatment with ambroxol, and another group of animals was treated with tracheal instillation of natural surfactant. A group of untreated control animals and animals treated with instillation of saline were also studied. Clearance was measured during standard conditions of mechanical ventilation and during ventilation with large tidal volumes. In ambroxol- and surfactant-treated groups, clearance rate was reduced compared with untreated control animals. In contrast, clearance rate increased after saline instillation. The differences were observed at both modes of ventilation. The findings indicate that the pulmonary surfactant system is a rate-limiting factor for the clearance of 99m Tc-DTPA and that the volume dependence of clearance is not explained by stretching of the alveolar wall only. 28 refs., 2 figs., 1 tab

  7. Radiopharmaceuticals to 99mTc

    International Nuclear Information System (INIS)

    Leon Cabana, Alba

    1994-01-01

    Studies about 99m Tc had demonstrated that have favorable properties for support diagnostic proceedings in nuclear medicine. This physical and chemical properties used for obtain another radiopharmaceuticals have been employed through re actives kits labelled with Tc 99m . A brief description was given about 99m utilities in diagnostic techniques such as endothelium reticular system,renal and hepatic studies,bone scintillators,cardiac diagnostic and cerebral perfusion

  8. Assessment of the direct cyclotron production of (99m)Tc: An approach to crisis management of (99m)Tc shortage.

    Science.gov (United States)

    Rovais, Mohammad Reza Aboudzadeh; Aardaneh, Khosro; Aslani, Gholamreza; Rahiminejad, Ali; Yousefi, Kamran; Boulouri, Fatemeh

    2016-06-01

    Nowadays, the cyclotron production of technetium-99m ((99m)Tc) has been increased, due to the worldwide (99m)Tc generator shortage. In the present work, an improved strategy for the production of (99m)Tc, using the proton irradiation of the enriched (100)Mo was developed. The performance of this method in terms of the production yield, chemical purity, radiochemical purity, as well as radionuclide purity was evaluated. The average production yield was measured to be 356MBqμA(-1)h(-1). A good agreement was found between the calculated production yield and the experimental one. The radiochemical separation and total recovery yields of (99m)Tc were 92% and 69%, respectively. The radiochemical and the radionuclide purities of the (99m)Tc were 99% and >99.99% at the end of purification, respectively. The results of quality control tests (QC) support the concept that cyclotron-produced (99m)Tc is suitable for preparation of USP-compliant. Copyright © 2016 Elsevier Ltd. All rights reserved.

  9. Comparison of carrier-added [99mTc] EDTMP and carrier-free preparations of [99mTc] EDTMP and [99mTc] DPD

    International Nuclear Information System (INIS)

    Krcal, A.; Kletter, K.; Dudczak, R.; Pirich, C.; Mitterhauser, M.

    2002-01-01

    Full text: High uptake of bone-seeking radiopharmaceuticals in malignant bone lesions is a prerequisite for adequate bone scanning. Visual image analysis is impaired due to high soft-tissue activity with currently available [ 99m Tc]-EDTMP-kits. This study aimed to compare carrier-added [ 99m Tc]-EDTMP with carrier-free [ 99m Tc]-EDTMP and [ 99m Tc]-DPD preparations in clinical routine. 15 μg and 150 μg perrhenic acid respectively were added to [ 99m Tc]-pertechnetate (>6 GBq in 3 ml phys. saline). The solution was then transferred into a vial, containing 1 mg of EDTMP, 3.6 mg stannous(II)chloride and 10 mg ascorbic acid under inert conditions. Under vigorous stirring the reaction mixture was heated to 45 o C for 10 min. After cooling down to room temperature the labelling mixture was sterile filtrated (millipore 0.22 μm). Quality control was performed using radio-ITLC (Whatman SG; acetone or ethanol: R f perrhenate/pertechnetate 0.87, colloid/product 0.05; phys. saline: R f colloid 0.00, perrhenate/pertechnetate and product 0.9) allowing rapid and efficient assessment of the product. Carrier free [ 99m Tc]-EDTMP and [ 99m Tc]-DPD were prepared according to instructions of the manufacturer. Clinical studies were performed in 29 patients according to a routine bone scanning protocol by injecting 700-800 MBq of the respective tracer and whole body imaging 3 h thereafter. Radiochemical purity and radiochemical yield relied on various parameters such as concentration of carrier and reducing agent and reaction conditions (pH, reaction time, temperature). Means of the labelling yield were 22 % for the preparation using 150 μg of carrier (5 preparations), 80 % for the preparation using 15 μpg of carrier (10 preparations) and 91 % for the carrier free products (5 preparations). Radiochemical purity was >96 % in all experiments. Colloid was formed in very low amounts, and was completely removed by sterile filtration. In clinical studies quantitative analysis

  10. Preparation, quality control and biological evaluation of 99mTc-labelled cationic steroid antibiotic (CSA-13)

    International Nuclear Information System (INIS)

    Roohi, S.; Amir, N.; Mushtaq, A.; Salahuddin, S.M.; Jehangir, M.; Savage, P.B.

    2009-01-01

    Ceragenins (CSAs) are a new class of antimicrobial agents that display broad spectrum antibacterial activity and may find use in the treatment of various infections. A member of this class CSA-13 was labelled with 99m Tc using SnCl 2 .H 2 O as a reducing agent. The labelling efficiency depended on the ligand/reductant ratio, pH and volume of the reaction mixture. The radiochemical purity and stability of 99m Tc-CSA was determined by thin layer chromatography. Biodistribution studies of 99m Tc-CSA were performed in Sprague Dawley rats. Liver and spleen uptake was quite high. A significantly higher accumulation of 99m Tc-CSA was seen at sites of S. aureus infected rats. The results were compared with 99m Tc-Ciprofloxacin. (orig.)

  11. Biodistribution of a 14C- and sup(99m)Tc-labeled N-substituted nitrosourea (CCNU) in an animal tumor model

    International Nuclear Information System (INIS)

    Castronovo, F.P.; Potsaid, M.S. Jr.; Kopiwoda, S.; Peterson, M.

    1980-01-01

    One formulation of 14 C labelled and another of sup(99m)Tc labelled 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU) were administered i.v. to tumour (glioma) bearing rats. The radiopharmacokinetics of 14 C-CCNU were followed up to 24 hours post injection. On a per organ basis the blood, liver, small bowel, kidney cortex and muscle contained most of the activity. Optimum tumour to organ ratios occurred at 4-12 hours. The sup(99m)Tc-CCNU biodistribution was determined at 4 hours and compared to sup(99m)Tc-NaTcO 4 . Tumour capsule to brain (29.5) and to muscle (10.59) ratios suggest sup(99m)Tc-CCNU to be a potential tumour seeking agent. (author)

  12. Radiolabelling of antibodies with technetium-99m and their clinical evaluation

    International Nuclear Information System (INIS)

    Varvarigou, A.D.

    1998-01-01

    Our study referred mainly to the comparative evaluation of two different methods, one direct and the other indirect, for the labelling of MoAbs with 99 Tc m . With the direct method, disulphide bridges were cleaved by the sue of 2-mercaptoethanol (2-ME), as reductant, while with the indirect method, the antibody was coupled to 2-iminothiolane (2-IM). The latter reacts with the amine groups of the protein's lysine molecules, thus creating free thiol groups, capable of binding reduced 99 Tc m . In both cases a preformed intermediate chelate was used for the 99 Tc m exchange. The 99 Tc m labelled species were analyzed by Instant Thin Layer Chromatography (ITLC), High Performance Liquid Chromatography (HPLC), and Polyacrylamide Gel Electrophoresis (PAGE). We investigated the influence of the labelling systems on MoAbs' integrity, as well as the ability of the labelled species to tag on human cancer cells. The biodistribution of the labelled derivatives was comparatively evaluated in normal male Swiss mice and the stability of labelling was measured by cysteine challenge. The in vitro stability was comparatively studied at different temperatures and by incubation with human serum for 24 h

  13. Reduction of 99mTc-sestamibi and 99mTc-tetrofosmin uptake in MRP-expressing breast cancer cells under hypoxic conditions is independent of MRP function

    International Nuclear Information System (INIS)

    Kinuya, Seigo; Li, Xiao-Feng; Yokoyama, Kunihiko; Michigishi, Takatoshi; Tonami, Norihisa; Mori, Hirofumi; Shiba, Kazuhiro; Watanabe, Naoto; Shuke, Noriyuki; Bunko, Hisashi

    2003-01-01

    Hypoxia reduces the uptake of technetium-99m sestamibi (MIBI) in human cancer cell lines. In the current investigation, we attempted to identify the relationship between hypoxia-induced alteration of 99m Tc-MIBI accumulation and expression of multi-drug resistance-associated protein (MRP) in the MCF7/WT breast cancer cell line and its subclonal cell line, MCF7/VP, which expresses high levels of MRP1. A second cationic compound, 99m Tc-tetrofosmin (TF), was also examined. Cellular uptake of 99m Tc-MIBI and 99m Tc-TF was significantly higher in parental MCF7/WT cells than in MCF7/VP cells. Hypoxic conditions generated with a mixture of 95% N 2 and 5% CO 2 reduced cellular uptake of the two tracers in both parental MCF7/WT cells and MRP1-expressing MCF7/VP cells. Cell binding assay with iodine-125-labelled anti-MRP1 antibody demonstrated its specific binding to MCF7/VP cells. Hypoxia did not affect the amount of antibody bound to MCF7/VP cells. These results indicate that hypoxia-induced reduction of tracer uptake in tumour cells is a phenomenon independent of MRP function. (orig.)

  14. labeling of some organic compounds of expected biological activity with Tc-99m eluted from a chromatographic column packed with zirconium molybdate containing mo-99

    International Nuclear Information System (INIS)

    Abd Elaal, M.A.A.

    2011-01-01

    The growth of nuclear medicine has been due mainly to the availability of 99m Tc-radiopharmaceuticals; this single isotope is used in over 80% of all diagnostic procedures. Each year, roughly 25 million procedures are carried out with 99m Tc-radio-pharmaceuticals, the universal use of this radioisotope (Technetium-99m, t 1/2 = 6.02 h) is due to its advantageous properties such as suitable half-life (it is short enough to save the patient from high radiation dose, and long enough to carry out labeling and scintigraphic measurements), γ-ray energy (140 keV; 89.4%) reasonable for SPECT, and very low abundance β - emission. Technetium-99m is readily available in a sterile, pyrogen free, and no-carrier added state from 99 Mo/ 99m Tc generators.The selection of iminodiacetic acid (IDA) derivatives to target 99m Tc as radioactive element to the hepatobiliary system is based on the reported finding that iminodiacetic acid capable of complexing reduced Tc-99m and easily incorporated into biologically active molecules. 99m Tc labeled iminodiacetic acid (IDA) derivatives offer a high degree of specificity for localization in the gallbladder with rapid extraction by the polygonal cells of the liver and very low urinary excretion. Various diseases related to liver function, such as jaundice and biliary obstruction, are diagnosed by the use of 99m Tc-labeled IDA derivatives. Chronic and acute cholecystitis can be differentiated with 99m Tc-IDA derivatives.In the presented work, 99m Tc in an acceptable radionuclidic, radiochemical and chemical purity using an easy and cheap method was produced. The produced 99m Tc was suitable to be used in the labeling techniques and in studying of the biological behavior of some synthesized iminodiacetic acid derivatives (1-naphthyl carbamoylmethyl iminodiacetic acid (NIDA), Diphenyl methyl carbamoylmethyl iminodiacetic acid (DMIDA) and Biphenyl-2-yl carbamoylmethyl iminodiacetic acid (BPIDA)). NIDA, DMIDA and BPIDA were synthesized and well

  15. Labeling bombesin-like peptide with 99mTc via hydrazinonicotinamide. Description of optimized radiolabeling conditions

    International Nuclear Information System (INIS)

    Yurt Lambrecht, F.; Durkan, K.; Bayrak, E.

    2010-01-01

    Bombesin (BNN)-like peptides have very high binding affinity for the gastrin-releasing peptide (GRP) receptor. The goal of the current study was to optimize the labeling conditions of a new 99m Tc-radiolabeled BNN-like peptide based on the bifunctional chelating ligand HYNIC using different co-ligands (EDDA and tricine). The radiolabeling conditions (pH, amount of co-ligand, amount of stannous chloride, temperature and reaction time) for newly-formed 99m Tc-tricine-HYNIC-Q-Litorin and 99m Tc-EDDA-HYNIC-Q-Litorin were optimized and evaluated by RHPLC and RTLC. Radiochemical yields for 99m Tc-tricine-HYNIC-Q-Litorin and 99m Tc-EDDA-HYNIC-Q-Litorin were 98.0 ± 1.7 and 97.5 ± 2.5%, respectively. When EDDA was used as co-ligand, the labeling of 99m Tc-EDDA-HYNIC-Q-Litorin was optimal in the following reaction mixture: HYNIC-peptide: EDDA: 10 μg/5 mg, pH 3, SnCl 2 concentration: 12 μg/0.1 mL, reaction temperature: 100 deg C, reaction time: 15 min. Besides, the optimum conditions were HYNIC-peptide:tricine: 10 μg/50 mg, pH 5, SnCl 2 concentration: 12 μg/0.1 mL, reaction temperature: 100 deg C, reaction time: 15 min for preparing 99m Tc-tricine-HYNIC-Q-Litorin. The manufactured 99m Tc-HYNIC-Q-Litorin conjugates may offer new possibilities for imaging cancer cells expressing bombesin receptors. (author)

  16. Technetium-99 labelling of DD-3B6/22 antifibrin monoclonal antibody fragmented Fab' for thrombus imaging

    International Nuclear Information System (INIS)

    Lee, F-T.; Boniface, G.R.; Lambrecht, R.M.; Rylatt, D.B.; Bundesen, P.G.

    1993-01-01

    The antifibrin DD-3B6/22 monoclonal antibody Fab' fragment, a murine immunoglobulin, IgG3, has been labelled with technetium-99m ( 99mTc ) via a transchelation reaction, to specific activity in excess of 30 mCi/mg protein. The radiolabelling of Fab' was dependent on time, temperature, pH, antibody concentrations and nature intermediary transchelation complex used. The resultant radioconjugate was stable in vitro and in vivo. Blood clearance of 99m Tc-Fab' in rat followed two compartment kinetics with the half time of the fast phase being 0.5 h. The main route of excretion was via the kidneys with little uptake indicated by other tissues. The results suggest that the inherent specificity of the antibody, small molecular size, rapid plasma clearance, high specific radioactivity, together with the physical properties of the 99m Tc label, combine to make this labelled monoclonal antibody (MoAb), potentially suitable as a radiopharmaceutical for the scintigraphic detection of thrombi in humans. 17 refs., 3 tabs., 5 figs

  17. Investigation of {sup 99m}Tc-labelling of recombinant human interleukin-2 via hydrazinonicotinamide

    Energy Technology Data Exchange (ETDEWEB)

    Karczmarczyk, Urszula, E-mail: ukarczmarczyk@o2.p [Department of Radiopharmaceuticals, National Medicines Institute, 00-725 Warsaw (Poland); Garnuszek, Piotr; Maurin, Michal [Department of Radiopharmaceuticals, National Medicines Institute, 00-725 Warsaw (Poland); Di Gialleonardo, Valentina [Nuclear Medicine, Ospedale S. Andrea, Via di Grottarossa 1035, 00189 Rome (Italy); Department of Nuclear Medicine and Molecular Imaging, University of Groningen, 9700 RB Groningen (Netherlands); Galli, Filippo [Nuclear Medicine, Ospedale S. Andrea, Via di Grottarossa 1035, 00189 Rome (Italy); Signore, Alberto [Nuclear Medicine, Ospedale S. Andrea, Via di Grottarossa 1035, 00189 Rome (Italy); Department of Nuclear Medicine and Molecular Imaging, University of Groningen, 9700 RB Groningen (Netherlands); Mikolajczak, Renata [Institute of Atomic Energy, Radioisotope Centre POLATOM, 05-400 Swierk (Poland)

    2010-10-15

    Introduction: Interleukin-2 (IL-2) when radiolabelled with {sup 99m}Tc has been proved useful in imaging the side of lymphocytic infiltration in patients with autoimmune disorders and plays a significant role as a T-cell imaging agent. However, the labelling procedures used so far appeared to be rather complex and laborious. The aim of present study was to develop an efficient procedure of {sup 99m}Tc-labelling of recombinant human interleukin-2 (rhIL-2) via hydrazinonicotinamide (HYNIC) to develop a dry kit formulation. Methods: Various molar ratios of rhIL-2/HYNIC (from 1:2 to 1:12) were used at the conjugation step. The conjugates were purified on a PD-10 column to remove the excess of unbound HYNIC, as well as of any aggregates. The final peptide concentration was quantified by the BCA method, and the number of HYNIC molecules incorporated into a rhIL-2 molecule was determined based on the reaction with 2-sulfobenzaldehyde. The {sup 99m}Tc-labelling was optimized using various amounts of HYNIC-rhIL-2, {sup 99m}Tc, SnCl{sub 2}, tricine and nicotinic acid (NA). Quality control included GF-HPLC, ITLC, SDS-PAGE and biological assay. Biodistribution studies were performed in Swiss mice and Wistar rats. Results: Generally, the highest radiolabelling yields were achieved when the HYNIC-rhIL-2 conjugates of ca. 2-4 HYNIC molecule substitution ratios were used. The optimal pH of the reaction medium was found to be in the range of 6.5 to 7.0. GF-HPLC analysis indicated that monomer and aggregates of {sup 99m}Tc-HYNIC-rhIL-2 are formed during radiolabelling. At optimized conditions of wet radiolabelling, the {sup 99m}Tc-HYNIC-rhIL-2 monomer was obtained with radiochemical purity >99%, specific activity of ca. 4 GBq/mg rhIL-2 and overall yield of ca. 65%. The two-vial freeze-dried kit was prepared: the first vial contained 30 {mu}g HYNIC-rhIL-2, co-ligands, buffer and antioxidant; the second vial contained tricine and SnCl{sub 2}. The monomer of {sup 99m}Tc-HYNIC-rhIL-2

  18. Detection of gastrointestinal blood loss with 99mTc-labeled, heat-treated red blood cells

    International Nuclear Information System (INIS)

    Som, P.; Oster, Z.H.; Atkins, H.L.; Goldman, A.G.; Sacker, D.F.; Harold, W.H.; Fairchild, R.G.; Richards, P.; Brill, A.B.

    1981-01-01

    Studies in dogs showed that heat-treated 99mTc-labeled red blood cells (HT/RBC) afford a highly sensitive means of detecting gastrointetinal bleeding as low as 0.12 ml/min., which could not be seen with unheated 99mTc-RBC, 99mTc-sulfur colloid, or 99mTc-DTPA. In addition, as the right upper quadrant and epigastrium remained free of activity, only one fifth to one tenth of the dose of 99mTc was needed. The safety of HT/RBC in humans has been documented, and the experiments in dogs suggest that it may have advantages over other agents in detecting gastrointestinal bleeding

  19. Kit for instant 99mTc labeling of the antimicrobial peptide ubiquicidin 29-41

    International Nuclear Information System (INIS)

    Ferro-Flores, G.; Arteaga de Murphy, C.; Pedraza-Lopez, M.; Palomares-Rodriguez, P.; Melendez-Alafort, L.

    2005-01-01

    The ubiquicidin 29-41 fragment (UBI) is a cationic antimicrobial peptide. An instant kit formulation was developed for the preparation of 99m Tc-UBI 29-41 in high radiochemical yield and its use as an infection imaging agent in humans was evaluated. The components were selected to produce a direct 99m Tc labeling, presumably to the amine groups of Lys and Arg7. 99m Tc-UBI 29-41 obtained from the lyophilized kit showed radiochemical purity of >97% with an average target/non-target ratio of 2.3±0.6 in positive infection sites at 2 hours. Kits were stable at 4 deg C for over 6 months. (author)

  20. Development of methods of labeling pentavalent DMSA with {sup 99m}Tc and {sup 188}Re; Desenvolvimento de metodos para marcacao de DMSA pentavalente com {sup 99m}Tc e {sup 188}Re

    Energy Technology Data Exchange (ETDEWEB)

    Brambilla, Tania de Paula, email: jtoniolo@ipen.br

    2009-07-01

    Technetium-99 m is the most useful radionuclide in diagnostic imaging procedures in Nuclear Medicine, more than 80 percent of radiopharmaceuticals are {sup 99m}Tc-labeled compounds. {sup 99m}Tc-DMSA(V) has been used for imaging of soft tissue, head and neck tumors. It shows a particularly high specificity for medullary thyroid carcinoma and bone metastases in a variety of cancers. Biodistribution studies of {sup 188}Re-DMSA(V) have shown that its general pharmacokinetic properties are similar to that of {sup 99m}Tc-DMSA(V), so this agent could be used for targeted radiotherapy of these tumors. The aim of this work is the development of methods of labeling DMSA(V) with {sup 99m}Tc and {sup 188}Re. {sup 99m}Tc-DMSA(V) can be prepared by two methods. One of them is the indirect one, through the use of a commercial kit of DMSA (III), by adjusting the pH from 2.5 to {approx} 8.5 with NaHCO{sub 3}. This method was evaluated and optimized presenting high labeling yields. The other method is the direct one, through the preparation of a lyophilised kit ready for labeling with {sup 99m}Tc, being the method of interest of this work, due to the easy of its clinical use. The most adequate formulation of the kit was: 1.71 mg of DMSA, 0.53 mg of SnCl{sub 2}.2H{sub 2}O and 0.83 mg of ascorbic acid (pH 9). Labeling yields higher than 95% were achieved labeling this kit with 1 to 2 m L of {sup 99m}Tc with activities up to 4736 MBq (128 mCi). The kit was stable up to 6 months and biodistribution studies confirmed the quality of the DMSA (V) labeled with {sup 99m}Tc using this kit. The reduction potential of Re is lower than the one for Tc, so the labeling conditions of {sup 188}Re-DMSA(V) are different from the ones used for {sup 99m}Tc- DMSA(V). {sup 188}Re-DMSA(V) is prepared in acid solution, that makes it possible to use the DMSA (III) commercial kit developed for labeling with {sup 99m}Tc, prepared in pH 2.5, for labeling with {sup 188}Re. Labeling yields higher than 95% were

  1. Tc-99m labeled Sparfloxacin: A specific infection imaging agent

    International Nuclear Information System (INIS)

    Singh, A.K.; Verma, J.; Bhatnagar, A.; Ali, A.

    2003-01-01

    Radiolabeled antibiotics are being used for the specific diagnosis of infection by exploiting their specific binding properties to the bacterial component, thereby making it possible to differentiate infection from sterile lesions. A new radiopharmaceutical, Tc-99m Sparfloxacin has been developed for infection imaging. Sparfloxacin is a quinolone based broad-spectrum antibiotic, which is more potent than Ciprofloxacin. Radiolabeling of Sparfloxacin with Tc-99m was standardized using direct labeling protocol. Labeling efficiency, in-vitro and in-vivo stability, blood kinetics and organ distribution studies (in balb/c mice and New Zealand White Rabbits at different time interval up to 24hrs) were carried out. Biological activity of Sparfloxacin after its labeling with Tc-99m was evaluated with S.aureus using Peptone water (DIFCO) as media. Turpentine oil (100 μl) in left thigh and S.aureus (100μl of 3x10 7 cells) in right thigh were injected intramuscularly to create sterile and infective inflammation respectively in six New Zealand white rabbits. The localization kinetics of the radiolabeled complex were studied in the animal model by injecting 70-75MBq of Tc-99m Sparfloxacin intravenously in the ear of rabbit and the images were taken with a Gamma-camera (ECIL) at different post-injection time intervals. Standardized protocol produced >95% labeled complex. About 8% of tracer leached out at 24 hrs when incubated in serum at 37 0 C, confirming high stability of the complex. Blood clearance in rabbit revealed biphasic pattern and 50% of the complex clears from the blood within 5 min. Biodistribution studies in balb/c mice showed hepatobiliary route of excretion. Presence of insignificant amount of tracer at 24 hrs in the stomach confirmed high in vivo stability of the complex. Imaging in rabbits showed significant concentration of tracer in lesions with infection. Typical imaging patterns revealed initial accumulation of radiotracer in both sterile inflammatory

  2. Detection of sites of infection in mice using {sup 99m}Tc-labeled PN{sub 2}S-PEG conjugated to UBI and {sup 99m}Tc-UBI: a comparative biodistribution study

    Energy Technology Data Exchange (ETDEWEB)

    Melendez-Alafort, Laura [Department of Pharmaceutical Sciences, University of Padua, 35131 Padova (Italy)], E-mail: lmalafort@yahoo.com; Nadali, Anna; Pasut, Gianfranco; Zangoni, Elena [Department of Pharmaceutical Sciences, University of Padua, 35131 Padova (Italy); De Caro, Raffaele [Department of Anatomy and Physiology, University of Padua, 35131 Padova (Italy); Cariolato, Luca [Department of Pharmaceutical Sciences, University of Padua, 35131 Padova (Italy); Giron, Maria Cecilia [Department of Pharmacology and Anesthesiology, University of Padua, 35131 Padova (Italy); Castagliuolo, Ignazio [Department of Histology, Microbiology and Medical Biotechnologies, University of Padua, 35131 Padova (Italy); Veronese, Francesco M.; Mazzi, Ulderico [Department of Pharmaceutical Sciences, University of Padua, 35131 Padova (Italy)

    2009-01-15

    The antimicrobial peptide ubiquicidin (UBI) directly labeled with technetium-99m ({sup 99m}Tc) has recently been shown to be specifically taken up at sites of infection; however, its chemical structure is not well defined. To address this problem, the aim of the present study was to label UBI using poly(ethyleneglycol)-N-(N-(3-diphenylphosphinopropionyl)glycyl) -S-tritylcysteine ligand (PEG-PN{sub 2}S) in order to compare its ability to detect infection sites with that of {sup 99m}Tc-UBI. Methods: The PN{sub 2}S-PEG-UBI conjugate was prepared and labeled with {sup 99m}Tc, and its radiochemical purity was subsequently assessed. The stability of the conjugate to cysteine challenge and dilution with both saline solution and phosphate buffer was determined and serum stability and protein binding were also assessed. In vivo studies were carried out in healthy mice to study the biodistribution of {sup 99m}Tc-PN{sub 2}S-PEG-UBI and its precursor {sup 99m}Tc-PN{sub 2}S-PEG and in infected mice to compare the uptakes of {sup 99m}Tc-UBI and {sup 99m}Tc-PN{sub 2}S-PEG-UBI at the site of infection using scintigraphic imaging and ex vivo tissue counting. Results: {sup 99m}Tc-PN{sub 2}S-PEG-UBI was obtained with high radiochemical purity (98{+-}1%) and high stability. The amphiphilic nature of the conjugate leads to a tendency to form micellar aggregates that explain the high protein binding values obtained. Biodistribution studies in mice showed low renal clearance followed by a predominant reticuloendothelial system clearance that limits its application in the abdominal area. Statistical analysis revealed no significant difference between {sup 99m}Tc-UBI and {sup 99m}Tc-PN{sub 2}S-PEG-UBI uptake in infected mouse thigh, and the site of infection was clearly visualized using scintigraphic imaging. Conclusions: {sup 99m}Tc-PN{sub 2}S-PEG-UBI proved to be as effective as {sup 99m}Tc-UBI in detecting sites of infection; however, the well-defined chemical structure of {sup 99m}Tc

  3. Evaluation of 99mTc-labeled antibiotics for infection detection

    International Nuclear Information System (INIS)

    Lambrecht, F.Y.

    2011-01-01

    One of the fields of research in nuclear medicine is the development of new radiopharmaceuticals for imaging infection and inflammation in humans. For this development, several antimicrobial peptides, antibiotics, antibiotic peptide and chemotactic peptides, etc., have been radiolabeled with different radionuclides ( 67 Ga, 99m Tc, 111 In, 18 F, 131 I, etc.) and their imaging potentials studied. Actually, it is very important to distinguish between infection and inflammation. In this respect, radiolabeled antibiotics have advantages because many of the properties of the ideal infection-specific agent through antibiotics localizes in infection site. In this review, only 99m Tc-labeled antibiotics are evaluated and discussed. (author)

  4. Radiochemical synthesis and tissue distribution of Tc-99m-labeled 7α-substituted estradiol complexes

    International Nuclear Information System (INIS)

    Skaddan, Marc B.; Wuest, Frank R.; Jonson, Stephanie; Syhre, Rosemarie; Welch, Michael J.; Spies, Hartmut; Katzenellenbogen, John A.

    2000-01-01

    The diagnosis and staging of breast cancer could be improved by the development of radiopharmaceutical imaging agents that provide a noninvasive determination of the estrogen receptor (ER) status of tumor cells. Agents labeled with 99m Tc would be especially valuable in this regard. In attempting to achieve this goal, we synthesized four 99m Tc-labeled 7α-substituted estradiol complexes. One complex utilizes the 3+1 mixed ligand design to introduce the Tc metal, whereas the other three took advantage of the cyclopentadienyltricarbonylmetal (CpTM) design. The Tc moieties were attached to the 7α position of estradiol with a hexyl tether, a monoether tether, or a polyether tether. The corresponding rhenium compounds have binding affinities for the ER of 20-45% compared with estradiol. Radiochemical yields of the 99m Tc-labeled compounds ranged from approximately 15% for the CpT-Tc complexes to 95% for the 3+1 inorganic complex. Tissue distribution studies in immature female rats showed low nonreceptor-mediated uptake in the target organs and high uptake in nontarget organs such as the liver and fat. These complexes represent the first time that estradiol has been labeled at the 7α position with 99m Tc and provide a further refinement of our understanding of ligand structure-binding affinity correlations for the ER

  5. Ventilation scintigraphy of the lung with sup(99m)Tc-DTPA or with sup(99m)Tc-sulfur colloid

    Energy Technology Data Exchange (ETDEWEB)

    Koehler, D; Matthys, H; Coates, G; Dolovich, M; Newhouse, M

    1983-04-01

    Ventilation scintigraphy of the lung, obtained with sufficiently small sup(99m)Tc-labelled aerosol particles, provides an image of ventilation distribution that is acceptable in clinical routine. Whether sup(99m)Tc-DTPA or sup(99m)Tc-sulfur colloid is more suitable as a carrier was studied in 6 smokers and 8 non-smokers with chronic obstructive pulmonary disease. sup(99m)Tc-sulfur colloid was not absorbed by the bronchial mucosa and therefore appears to be an almost ideal agent. In contrast, sup(99m)Tc-DTPA was absorbed by the bronchial mucosa in all smoking patients more rapidly and inhomogenously than in non-smokers. The quantitative and qualitative comparison of the two dorsal ventilation scans taken both immediately after inhalation and 20 min later, showed in all 6 smoking patients after 20 min significant differences which influenced the diagnostic result. sup(99m)Tc-DTPA is therefore not recommended for use in ventilation lung scintigraphy, especially in smoking patients.

  6. In vivo tumor angiogenesis imaging with site-specific labeled 99mTc-HYNIC-VEGF

    International Nuclear Information System (INIS)

    Blankenberg, Francis G.; Backer, Marina V.; Patel, Vimalkumar; Backer, Joseph M.; Levashova, Zoia

    2006-01-01

    We recently developed a cysteine-containing peptide tag (C-tag) that allows for site-specific modification of C-tag-containing fusion proteins with a bifunctional chelator, HYNIC (hydrazine nicotinamide)-maleimide. We then constructed and expressed C-tagged vascular endothelial growth factor (VEGF) and labeled it with HYNIC. We wished to test 99m Tc-HYNIC-C-tagged VEGF ( 99m Tc-HYNIC-VEGF) for the imaging of tumor vasculature before and after antiangiogenic (low continuous dosing, metronomic) and tumoricidal (high-dose) cyclophosphamide treatment. HYNIC-maleimide was reacted with the two thiol groups of C-tagged VEGF without any effect on biologic activity in vitro. 99m Tc-HYNIC-VEGF was prepared using tin/tricine as an exchange reagent, and injected via the tail vein (200-300 μCi, 1-2 μg protein) followed by microSPECT imaging 1 h later. Sequencing analysis of HYNIC-containing peptides obtained after digestion confirmed the site-specific labeling of the two accessible thiol groups of C-tagged VEGF. Tumor vascularity was easily visualized with 99m Tc/VEGF in Balb/c mice with 4T1 murine mammary carcinoma 10 days after implantation into the left axillary fat pad in controls (12.3±5.0 tumor/bkg, n=27) along with its decrease following treatment with high (150 mg/kg q.o.d. x 4; 1.14±0.48 tumor/bkg, n=9) or low (25 mg/kg q.d. x 7; 1.03±0.18 tumor/bkg, n=9) dose cyclophosphamide. Binding specificity was confirmed by observing a 75% decrease in tumor uptake of 99m Tc/biotin-inactivated VEGF, as compared with 99m Tc-HYNIC-VEGF. 99m Tc can be loaded onto C-tagged VEGF in a site-specific fashion without reducing its bioactivity. 99m Tc-HYNIC-VEGF can be rapidly prepared for the imaging of tumor vasculature and its response to different types of chemotherapy. (orig.)

  7. Imaging human atherosclerosis with /sup 99m/Tc-labeled low density lipoproteins

    International Nuclear Information System (INIS)

    Lees, A.M.; Lees, R.S.; Schoen, F.J.; Isaacsohn, J.L.; Fischman, A.J.; McKusick, K.A.; Strauss, H.W.

    1988-01-01

    The feasibility of localizing human atherosclerotic plaques by gamma scintillation camera external imaging with technetium-99m-labeled low density lipoproteins (99mTc-LDL) was tested in 17 patients who had atherosclerosis. Imaging demonstrated focal accumulation of radiolabel consistent with 99mTc-LDL sequestration by plaques in the carotid, iliac, or femoral vessels of four patients 8 to 21 hours after intravenous injection of the radiopharmaceutical. Focal accumulation of 99mTc-LDL also appeared in the location of coronary lesions in four patients, but this accumulation could not be distinguished with certainty from residual blood pool radioactivity. When carotid endarterectomy specimens from six patients who received 99mTc-LDL 1 day before endarterectomy were examined, the specimens had focal accumulations of radiolabel, with two to four times greater radioactivity in some regions of each specimen than in others; this occurred whether or not the lesions were detected on the gamma camera images. Lesion composition may have determined whether accumulation was quantitatively sufficient to produce an external image. Histologically, the imaged carotid specimen had abundant foam cells and macrophages and poorly organized intramural blood consistent with a plaque hemorrhage; in contrast, nonimaged endarterectomy specimens were mature, fibrocalcific plaques. We conclude that: 1) 99mTc-LDL did accumulate in human atherosclerotic plaques; 2) in some patients, the accumulation of 99mTc-LDL was sufficient for detection by gamma camera imaging; 3) the amount of LDL that accumulated appeared to depend on lesion composition; and 4) the design of new radiopharmaceuticals with reduced residual blood pool activity relative to plaque accumulation should lead to improved external imaging of atherosclerosis

  8. The study of x-ray photo-electron spectroscopy of 99mTc-RBC

    International Nuclear Information System (INIS)

    Song Chunyi

    1994-01-01

    99m Tc-RBC are widely used as visualization agents for a blood pool. In this research 99m Tc-RBC was prepared by in vivo labeling. The chemical state and changes of 99m Tc atoms in 99m Tc-RBC was determined by x-ray photo-electron spectroscopy (XPS). The stability of 99m Tc-RBC is best shown by the determination of XPS at one hour or at two hours after labeling. There are two ways of coordination of bonding of RBC and 99m Tc: One is the coordination of 99m Tc with the oxygen atom which carries a negative charge of the carboxyl radical on the polypeptide bond, the other is the coordination of 99m Tc with a sulfur atom which caries the negative charge of cysteine. From the E b value of 99m Tc-RBC 99m Tc 3d5/2, it can be inferred that 99m Tc of 99m Tc-RBC is less than a trivalent. At the same time, the results of the determination by XPS with the compounds containing 99 TcO 4 - , 99 Tc(V), 99 Tc(IV) and 99 Tc(III) show that the chemical shift is lowered as the reduction state is lowered. Experimental results coincide with theoretical inferences

  9. Development of superior bone scintigraphic agent from a series of {sup 99m}Tc-labeled zoledronic acid derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Lin Jianguo [Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063 (China); Qiu Ling, E-mail: qiulingwx@gmail.com [Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063 (China); Cheng Wen [Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063 (China); Luo Shineng, E-mail: shineng914@yahoo.com.cn [Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063 (China); Xue Li; Zhang Shu [Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063 (China)

    2012-05-15

    Two novel zoledronic acid (ZL) derivatives, 1-hydroxy-4-(1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (IBDP) and 1-hydroxy-5-(1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (IPeDP), were prepared and labeled with the radionuclide technetium-99m in a high labeling yield. In vitro stabilities of these radiolabeled complexes were measured by the radio-HPLC analysis as a function of time, which showed excellent stability with the radiochemical purity of over 95% at 6 h post preparation. Their in vivo biological performances were evaluated and compared with those of {sup 99m}Tc-ZL and {sup 99m}Tc-MDP (methylenediphosphonic acid). The biodistribution in mice and scintigraphic images of the rabbit showed that the tracer agent {sup 99m}Tc-IPeDP had highly selective uptake in the skeletal system and rapid clearance from the blood and soft tissues and an excellent scintigraphic image can be obtained in a shorter time post injection with clear visualization of the skeleton and low soft tissue activity. These preclinical studies suggest that {sup 99m}Tc-IPeDP would be a novel superior bone scintigraphic agent. - Highlights: Black-Right-Pointing-Pointer Two novel diphosphonic acids were labeled with the {sup 99m}Tc in high labeling yield. Black-Right-Pointing-Pointer {sup 99m}Tc-IPeDP had high uptake in skeletal system and rapid clearance from blood. Black-Right-Pointing-Pointer {sup 99m}Tc-IPeDP reveals attractive biological features as superior bone scanning agent.

  10. Somatostatine analogs marked with 99m-TC

    International Nuclear Information System (INIS)

    Obenaus, E; Crudo, J; Edreira, M; Castiglia, S.G. de

    2003-01-01

    The aim of the present work was to study the biological and radiochemical behaviour of two somatostatin analogues, the RC-160 and Tyr 3 Octreotide(TOC) peptides when labeling with 99m Tc by an indirect method using S-Benzoyl- mercaptoacetyl triglycine (MAG3) and hydrazino nicotinamide (HYNIC) as chelating agents. The synthesis of RC160 with S-Benzoyl MAG3 and TOC with HYNIC, for labeling with 99m Tc are also described. The conjugates were prepared on a small scale and labeled with the radionuclide using tricine as coligands for HYNIC conjugates. Chromatographic studies were performed using an HPLC system and radiochemical purities higher than 75% and 95% were obtained respectively. Biodistributions studies in normal Wistar rats were performed and results were correlated with chromatographic and protein binding properties. Lower lipophilicity of the labeled conjugates resulted in a higher renal excretion. HYNIC-TOC complex showed promising results when labeling with 99m Tc using tricine as coligand although higher stability should be found for ternary coligands compared to tricine (Au)

  11. Study on synthesis, kit formulation and chemical kinetics of dissociation of 99mTc labeled PnAO biotin complex

    International Nuclear Information System (INIS)

    Afshan, A.; Jafri, S.R.A.; Maecke, H.

    2004-01-01

    Full text: A bifunctional ligand of PnAO-biotin has recently been synthesized, with a better percentage yield of 63% in the presence of newly developed coupling agent 0-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexaflorophos phate (HATU). Then lyophilized kit with 150μg of PnAObiotin has been developed and labeled with high specific activity of technetium-99m (2500-3000MBq) to get maximum radiochemical purity of 99mTc-PnAO-biotin complex i.e. > 97%. The association of avidin and streptavidin is among the strongest known non-covalent protein ligand interaction Ka 1015 M-1 and 1013 M-1 respectively. We measured the dissociation rate constant of PnAO-biotin from avidin and streptavidin challenged with excess of cold biotin. For the separation of bound and free-labeled biotin we employed ultrafilteration technique. The results of these experiments demonstrated that the non-covalent binding between 99mTc-PnAO-biotin with avidin and 99mTc-PnAO-biotin with streptavidin is more than 99%. Both biotin-binding proteins exhibited a faster initial phase and the rate of dissociation of 99mTc-PnAO-biotin with avidin is found to be 8.2x10-8 at 250C and 2.6x10-7 at 370C while the rate of dissociation 99mTc-PnAO-biotin from streptavidin is found to be 6x10-7 at 250C and 1.06x10-6 at 370C. The in-vitro study of the kinetics of dissociation exhibits the strong interaction of 99mTc-PnAO-biotin complex with both proteins, which suggests that this bifunctional PnAO-biotin ligand can be used for tumor localization with monoclonal antibodies to achieve high tumor to non-tumor ratio. (author)

  12. 99mTc-rituximab radiolabelled by photo-activation: a new non-Hodgkin's lymphoma imaging agent

    International Nuclear Information System (INIS)

    Gmeiner Stopar, T.; Fettich, J.; Hojker, S.; Mlinaric-Rascan, I.; Mather, S.J.

    2006-01-01

    Rituximab was the first chimeric monoclonal antibody to be approved for treatment of indolent B-cell non-Hodgkin's lymphoma (NHL). It is directed against the CD20 antigen, which is expressed by 95% of B-cell NHLs. The aim of this study was to explore the possibility of radiolabelling rituximab with 99m Tc for use as an imaging agent in NHL for early detection, staging, remission assessment, monitoring for metastatic spread and tumour recurrence, and assessment of CD20 expression prior to (radio)immunotherapy. Rituximab was purified from Mabthera solution (Roche), photo-activated at 302 nm by UV irradiation and radiolabelled with 99m Tc. The effectiveness of the labelling method was evaluated by determination of the number of free thiol groups per photoreduced antibody, radiochemical purity and in vitro stability of 99m Tc-rituximab. On average, 4.4 free thiol groups per photoreduced antibody were determined. Radiolabelling yields greater than 95% were routinely observed after storage of the photo-activated antibody at -80 C for 195 days. The direct binding assay showed preserved ability of 99m Tc-rituximab to bind to CD20, with an average immunoreactive fraction of 93.3%. The internalisation rate was proven to be low, with only 5.3% of bound 99m Tc-rituximab being internalised over 4 h at 37 C. Our results demonstrate that 99m Tc-rituximab of high radiochemical purity and with preserved binding affinity for the antigen can be prepared by photoreduction and that the method shows good reproducibility. 99m Tc-rituximab will be further explored as an imaging agent applicable in NHL for the purposes mentioned above. (orig.)

  13. Development and preclinical characterisation of 99mTc-labelled Affibody molecules with reduced renal uptake

    International Nuclear Information System (INIS)

    Ekblad, Torun; Karlstroem, Amelie Eriksson; Tran, Thuy; Orlova, Anna; Feldwisch, Joachim; Widstroem, Charles; Abrahmsen, Lars; Wennborg, Anders; Tolmachev, Vladimir

    2008-01-01

    Affibody molecules are low molecular weight proteins (7 kDa), which can be selected to bind to tumour-associated target proteins with subnanomolar affinity. Because of rapid tumour localisation and clearance from nonspecific compartments, Affibody molecules are promising tracers for molecular imaging. Earlier, 99m Tc-labelled Affibody molecules demonstrated specific targeting of tumour xenografts. However, the biodistribution was suboptimal either because of hepatobiliary excretion or high renal uptake of the radioactivity. The goal of this study was to optimise the biodistribution of Affibody molecules by chelator engineering. Anti-HER2 Z HER2:342 Affibody molecules, carrying the mercaptoacetyl-glutamyl-seryl-glutamyl (maESE), mercaptoacetyl-glutamyl-glutamyl-seryl (maEES) and mercaptoacetyl-seryl-glutamyl-glutamyl (maSEE) chelators, were prepared by peptide synthesis and labelled with 99m Tc. The tumour-targeting capacity of these conjugates was compared with each other and with the best previously available conjugate, 99m Tc-maEEE-Z HER2:342, in nude mice bearing SKOV-3 xenografts. The tumour-targeting capacity of the most promising conjugate, 99m Tc-maESE-Z HER2:342, was compared with radioiodinated Z HER2:342 . All novel conjugates demonstrated successful tumour targeting and a low degree of hepatobiliary excretion. The renal uptakes of serine-containing conjugates, 33±5, 68±21 and 71±10%IA/g, for 99m Tc-maESE-Z HER2:342 , 99m Tc-maEES-Z HER2:342 and 99m Tc-maSEE-Z HER2:342 , respectively, were significantly reduced in comparison with 99m Tc-maEEE-Z HER2:342 (102 ± 13%IA/g). For 99m Tc-maESE-Z HER2:342 , a tumour uptake of 9.6±1.8%IA/g and a tumour-to-blood ratio of 58±6 were reached at 4 h p.i. A combination of serine and glutamic acid residues in the chelator sequence confers increased renal excretion and relatively low renal uptake of 99m Tc-labelled Affibody molecules. In combination with preserved targeting capacity, this improved imaging of targets

  14. Studies on quality control of technetium-99m labelling kits

    International Nuclear Information System (INIS)

    Kim, Jae Rok; Park, Kyung Bae; Awh, Ok Doo

    1987-12-01

    Various experiments for the quality control of Tc-99m labelled radiopharmaceuticals such as Tc-99m-phytate, Tc-99m-MDP, Tc-99m-Tin Colloid, Tc-99m-DISIDA, Tc-99m-DTPA,Tc-99m-DMSA, Tc-99m-Gulcoheptonate, TC-99m-Pyrophosphate, Tc-99m-HSA, and Tc-99m-HAM were carried out. Labelling yield and radiochemical purity of each of the instant labelling kit of KAERI made were determined by means of radiochromatography. Biodistribution in mice and whole body or specific organ imagings of rabbits were also carried out and discussed the relationship between the data of biodistributions and radiochemical purities. Labelling yeilds were above 98% for almost all of the labelling kits. The radio-pharmaceuticals were accumulated at each target organ with moderate specifities. In case of radiochemical purity of above 98%, the biodistribution and gamma imagings were also better. The kits of MDP and DISIDA were stable at least for four moths while the other kits at least eight months. (Author)

  15. Huge Varicose Inferior Mesenteric Vein: an Unanticipated {sup 99m}Tc-labeled Red Blood Cell Scintigraphy Finding

    Energy Technology Data Exchange (ETDEWEB)

    Hoseinzadeh, Samaneh; Shafiei, Babak; Salehian, Mohamadtaghi; Neshandar Asli, Isa; Ghodoosi, Iraj [Shaheed Beheshti Medical University, Tehran (Iran, Islamic Republic of)

    2010-09-15

    Ectopic varices (EcV) are enlarged portosystemic venous collaterals, which usually develop secondary to portal hypertension (PHT). Mesocaval collateral vessels are unusual pathways to decompress the portal system. Here we report the case of a huge varicose inferior mesenteric vein (IMV) that drained into peri rectal collateral veins, demonstrated by {sup 99m}Tc-labeled red blood cell (RBC) scintigraphy performed for lower gastrointestinal (GI) bleeding in a 14-year-old girl. This case illustrates the crucial role of {sup 99m}Tc-labeled RBC scintigraphy for the diagnosis of rare ectopic lower GI varices.

  16. 99m Tc-labeled heparin test in orthopaedic surgery

    International Nuclear Information System (INIS)

    Bouvier, J.F.; Lafon, J.C.; Colin, M.; Chatelut, J.; Beaubatie, F.

    1983-01-01

    99m Tc-labeled heparin test was performed for early detection of phlebitis or pulmonary embolism after orthopaedic prothesis. Heparinic treatment and surgery per se were demonstrated to have no effect on the results. If this test demonstrates a statistical difference for pathologic patients, it is of greater value to consider ratio between rates before and after intervention [fr

  17. /sup 99m/Tc-labelled hepatobiliary radiopharmaceuticals

    International Nuclear Information System (INIS)

    Galli, G.; Maini, C.L.

    1986-01-01

    During the last 15 years many compounds labelled with /sup 99m/Tc have been proposed for use in cholescintigraphy. A short chronological list includes: toluidine blue, penicillamine, tetracycline, dihydrothioctic acid, mercaptoisubutyric acid, pyridoxals, pyridoxylideneaminates, carboxyl-hydroxyquinoline, substituted acetanilide iminodiacetates (so called IDAs), ethylenediamine-N, N-diacetate derivatives (such as sulfonyl-EDDA and benzoyl-EDDA), and orthoiodohippurate analogues. Among all these compounds the IDAs have been those most extensively used for basic and clinical research. A large series of IDA derivatives has been developed, and the properties of 33 of them have recently been tested

  18. Optimizing labeling conditions for cysteine-based peptides with {sup 99m}Tc

    Energy Technology Data Exchange (ETDEWEB)

    Sabahnoo, Hamideh; Hosseinimehr, Seyed Jalal, E-mail: sjhosseinim@yahoo.com [Department of Radiopharmacy, Faculty of Pharmacy, Pharmaceutical Sciences Research Center, Mazandaran University of Medical Sciences, Sari (Iran, Islamic Republic of)

    2016-07-01

    Radiolabelled peptides have attracted a great deal of attention due to their wide applicability in the development of target-specific radiopharmaceuticals. They can easily be used in diagnostic imaging as carriers for the delivery of radionuclides to tumors as well as for therapy. Previous investigations revealed that technetium(V) could form stable complexes with peptide-based ligands of N{sub 3}S type such as Cys-Gly-Gly-Gly. Herein, a targeting HER-2 receptor peptide was labeled with technetium-{sup 99m} ({sup 99m}Tc) with two different types of tetrapeptide-based ligands, Cys-Gly-Gly-Gly and Cys-Ser-Ser-Ser. The effect of experimental parameters in the labeling procedure such as type of buffer solutions, pH of media, and type of exchange ligands were optimized toward obtaining maximum labeling yield. The optimum labeling conditions were different for two peptides. Shelf life of both labeled peptides was determined by analytical reversed-phase high-performance liquid chromatography (RP-HPLC) and thin layer chromatography (TLC) that showed radiochemical yield up to 95% even after 4 h. (author)

  19. Human monoclonal antibody 99mTc-88BV59: detection of colorectal cancer, recurrent or metastatic disease and immunogenicity assessment.

    Science.gov (United States)

    Krause, B J; Baum, R P; Staib-Sebler, E; Lorenz, M; Niesen, A; Hör, G

    1997-01-01

    This study presents immunoscintigraphic results in 24 patients suffering from primary colorectal cancer, recurrent or metastatic disease after the injection of 1197-1351 MBq technetium-99m labelled totally human monoclonal antibody 88BV59. Labelling efficacy of 99mTc-88BV59 ranged from 97% to 99%. Immunoscintigraphy was performed 18-20 h after injection. Scintigraphic findings were compared with those of computed tomography (CT). Patients underwent surgery in order to evaluate immunoscintigraphic findings histologically. Sera of the patients (before injection and 1 and 3 months post infusion) were analysed for the presence of human anti-human antibodies (HAHA). None of the patients showed a HAHA response as assessed by a solid-phase ELISA assay. The antibody scan detected about 25% more lesions than CT. In the detection of extrahepatic disease, the sensitivity of the antibody scan proved to be 68%, whereas the sensitivity of CT was 41%.

  20. Biodistribution studies of {sup 99m}Tc-labeled myoblasts in a murine model of muscular dystrophy

    Energy Technology Data Exchange (ETDEWEB)

    Colombo, F.R. E-mail: colombof@policlinico.mi.it; Torrente, Y.; Casati, R.; Benti, R.; Corti, S.; Salani, S.; D' Angelo, M.G.; DeLiso, A.; Scarlato, G.; Bresolin, N.; Gerundini, P

    2001-11-01

    The purpose of this study was twofold: first, to evaluate the myoblast labeling of various {sup 99m}Tc complexes and to select the complex that best accomplishes this labeling, and second to evaluate the biodistribution of myoblasts labeled with this complex using mice with MDX muscular dystrophy (the murine homologue of Duchenne's muscular dystrophy). The following ligands were used to prepare the corresponding {sup 99m}Tc complexes: hexakis-methoxy-isobutyl-isonitrile (MIBI), bis(2-ethoxyethyl)diphosphinoethane (Tf), (RR,SS)-4,8-diaza-3,6,6,9-tetramethyl-undecane-2,10-dione-bisoxime (HM-PAO), bis(N-ethyl)dithiocarbamate (NEt), and bis(N-ethoxy, N-ethyl)dithiocarbamate (NOEt). One million murine myoblasts were incubated for 30-60 minutes with 5 mCi of each of the 99mTc complexes prepared from the above ligands. Viability was assessed by microscopic counting after trypan blue staining, and the radioactivity absorbed in the cells was measured after centrifugation. The compound with the highest uptake in cellular pellets was [{sup 99m}Tc]N-NOEt. The biodistribution of myoblasts labeled with this complex was evaluated after intraaortic injection in dystrophic mice. Such an approach has the potential of effecting widespread gene transfer through the bloodstream to muscles lacking dystrophin.

  1. sup(99m)Tc-2-mercaptopropionylglycine

    International Nuclear Information System (INIS)

    Saji, Hideo; Odori, Teruo; Morita, Rikushi; Yokoyama, Akira; Tanaka, Hisashi.

    1979-01-01

    Labeling of 2-mercaptopropionylglycine (2-MPG) with sup(99m)Tc, was studied and its chemical characteristics were examined. Further, biliary excretion behavior of this complex was comparatively estimated in mice, rats and rabbits. sup(99m)Tc-2-MPG was rapidly excreted in large quantities into the bile in mice and rats: within 1 hr after injection, 51% of the injected dose was recovered from the bile in rats. On the other hand, the ligand exchange reaction between this complex and penicillamine indicates that a low hydrolyzed sup(99m)Tc species is coordinated with 2-MPG. These results suggest that a low hydrolyzed sup(99m)Tc state is an effective feature in biliary excretion behavior of sup(99m)Tc compounds. Another interesting in vivo behavior of sup(99m)Tc-2-MPG is the difference observed in mice and rabbits: in mice, very high sup(99m)Tc activity is concentrated in the gallbladder and the clearance from tissues other than the gallbladder is rapid, whereas in rabbits, although a rapid and high excretion into the gallbladder is observed, a considerable high sup(99m)Tc activity is retained in the liver and the kidney. One reason for this different in vivo behavior is the low stability of this complex at high dilution: a big animal has the large dilution volume which lead to higher decomposition estimated by the higher liver and kidney retention or the lower bile excretion. In conclusion, studies carried on sup(99m)Tc-2-MPG showed a good biliary excretion behavior but an in vivo unstableness in big animals. (author)

  2. Labelling and quality control of somatostatin analogues with 99mTc

    International Nuclear Information System (INIS)

    Verdera, S.; Balter, H.; Rodriguez, G.; Robles, A.; Oliver, P.; Laiz, J.; Souto, B.

    2001-01-01

    Techniques and methodologies for labelling peptides with 99m Tc and methods for their purification, chemical, radiochemical and biological controls were evaluated. With the purpose of gaining experience, labelling with 125 I was also studied. RC-160 was labelled with 125 I using iodogen as well as chloramine-T method. Higher yields were obtained with chloramine-T method (60%), rendering 125 I-peptide with 98% of radiochemical purity, with specific activity of 240 μCi/μg - 274 μCi/μg. The product was stable for five weeks (at -20 deg. C). For somatostatin receptors studies rat brain cortex membrane was prepared. Maximum binding capacity was 24.7% and Kaff for the binding of RC-160 to receptor was estimated as 2.0x10 10 M -1 . Other peptides as β-(2-Naphthyl)- D Ala-Cys-Tyr- D Trp-Lys-Val-Cys-Thr amide (N-9642, Σ) and mouse epidermal growth factor (mEGF) were also labelled by means of limiting chloramine-T method. In case of mEGF the availability of membrane receptors allowed us to experiment in mice as well as in vitro. The reaction yields were up to 60% and 70% respectively. Biodistribution of 125 I-mEGF in a mouse with adenoma demonstrated preferential uptake in tumour (21,7% injected dose). The radioimmunoassay system gave 39% maximum binding (MB) and 50% displacement (ED 50 ) for 10 ng/mL unlabelled mEGF. Direct method and BFC's for labelling peptides with 99m Tc were investigated and purification and quality controls studies were performed by TLC, HPLC (UV and gamma detection). RC-160 was labelled by a direct method using sodium dithionite as reducing agent with radiochemical purity >95%. The product was stable up to six hours (at RT). Considerable adsorption problems were observed. Biological behavior was in accordance with the compounds' lipophilicity. The synthesis of TOC conjugates with HYNIC as BFC was done with 45%±5% (n=3) yield. Labelling of HYNIC-TOC with tricine as co-ligand was conducted with up to 90% yield. Studies of RC-160 labelling using

  3. Simultaneous acquisition of (99m)Tc- and (123)I-labeled radiotracers using a preclinical SPECT scanner with CZT detectors.

    Science.gov (United States)

    Kobayashi, Masato; Matsunari, Ichiro; Nishi, Kodai; Mizutani, Asuka; Miyazaki, Yoshiharu; Ogai, Kazuhiro; Sugama, Jyunko; Shiba, Kazuhiro; Kawai, Keiichi; Kinuya, Seigo

    2016-05-01

    Simultaneous acquisition of (99m)Tc and (123)I was evaluated using a preclinical SPECT scanner with cadmium zinc telluride (CZT)-based detectors. 10-ml cylindrical syringes contained about 37 MBq (99m)Tc-tetrofosmin ((99m)Tc-TF) or 37 MBq (123)I-15-(p-iodophenyl)-3R,S-methyl pentadecanoic acid ((123)I-BMIPP) were used to assess the relationship between these SPECT radioactive counts and radioactivity. Two 10-ml syringes contained 100 or 300 MBq (99m)Tc-TF and 100 MBq (123)I-BMIPP to assess the influence of (99m)Tc upscatter and (123)I downscatter, respectively. A rat-sized cylindrical phantom also contained both 100 or 300 MBq (99m)Tc-TF and 100 MBq (123)I-BMIPP. The two 10-ml syringes and phantom were scanned using a pinhole collimator for rats. Myocardial infarction model rats were examined using 300 MBq (99m)Tc-TF and 100 MBq (123)I-BMIPP. Two 1-ml syringes contained 105 MBq (99m)Tc-labeled hexamethylpropyleneamine oxime ((99m)Tc-HMPAO) and 35 MBq (123)I-labeled N-ω-fluoropropyl-2β-carbomethoxy-3β-(4-iodophenyl) nortropane ((123)I-FP-CIT). The two 1-ml syringes were scanned using a pinhole collimator for mice. Normal mice were examined using 105 MBq (99m)Tc-HMPAO and 35 MBq (123)I-FP-CIT. The relationship between SPECT radioactive counts and radioactivity was excellent. Downscatter contamination of (123)I-BMIPP exhibited fewer radioactive counts for 300 MBq (99m)Tc-TF without scatter correction (SC) in 125-150 keV. There was no upscatter contamination of (99m)Tc-TF in 150-175 keV. In the rat-sized phantom, the radioactive count ratio decreased to 4.0 % for 300 MBq (99m)Tc-TF without SC in 125-150 keV. In the rats, myocardial images and radioactive counts of (99m)Tc-TF with the dual tracer were identical to those of the (99m)Tc-TF single injection. Downscatter contamination of (123)I-FP-CIT was 4.2 % without SC in 125-150 keV. In the first injection of (99m)Tc-HMPAO and second injection of (123)I-FP-CIT, brain images and radioactive counts

  4. IL-2 labeled with 99mTechnetium by an indirect method

    International Nuclear Information System (INIS)

    Bocco, R.; Obenaus, Esteban; Rabiller, Graciela; Castiglia, Silvia G. de

    2003-01-01

    IL-2 and the other cytokines labeled with 99m Tc are an interesting option to early diagnosis of autoimmune diseases and monitoring with nuclear medicine images. The aim of this study was to obtain by indirect method IL-2 labeled with 99m Technetium using Benzoyl MAG3 chelating agent, for in vivo diagnosis of lymphocytic infiltration. IL-2 is a small, relatively fragile protein, and it is essential to retain its receptor binding capacity after labeling. Two different methods of labeling have been proven: Pre-conjugation labeling method: we used NHS- Hynic as a chelator agent and labeled this conjugated protein with 99m Tc using tricine as coligand. Albumin was used as a model for the conjugation and labeling steps. The albumin was labeled by this method with a good labeling efficiency but the IL-2 protein could not be labeled with this approach. Post- conjugation labeling method: we used the bifunctional chelating agent, benzoyl MAG3, this ligand is first labeled with 99m Tc and then is conjugated to the protein. The N 3 S Logan complex was incubated for 30 minutes and then measured by RP- HPLC. An active ester of the labeled Logan was formed and was incubated with Il-2 at room temperature and basic pH to promote the conjugation between the active ester and the protein. The labeling efficiency was determined by RP-HPLC using a C 18 column. The albumin protein was also labeled by this method and the radiochemical purity was measured by RP- HPLC using a GPC column and the labeling efficiency was 80%. The next objectives are to explore different strategies for purifying the 99m Tc-IL-2 and to evaluate the capacity of IL-2 to bind to its receptor after labeling. (author)

  5. In vitro assessment of cytotoxicity and labeling efficiency of {sup 99m}Tc-HMPAO with stromal vascular fraction of adipose tissue

    Energy Technology Data Exchange (ETDEWEB)

    Verma, V. K.; Beevi, S. S. [Department of Transplant Biology, Immunology and Stem Cell Lab, Global Hospitals, Hyderabad (India); Tabassum, A.; Kumaresan, K. [KK Nuclear Scans, Raj Bhavan Road, Somajiguda, Hyderabad (India); Kamaraju, R. S. [Department of Transplant Biology, Immunology and Stem Cell Lab, Global Hospitals, Hyderabad (India); Arbab, A. S. [Cancer Centre, GA Regents University, Augusta, GA (United States); Chelluri, L.K., E-mail: lkiran@globalhospitalsindia.com [Department of Transplant Biology, Immunology and Stem Cell Lab, Global Hospitals, Hyderabad (India)

    2014-10-15

    Introduction: Noninvasive radionuclide imaging of cells using technetium99m-hexamethylpropyleneamine oxime ({sup 99m}Tc-HMPAO) is a potential diagnostic tool for several applications. Herein we aimed to evaluate the labeling efficiency and cellular toxicity of {sup 99m}Tc-HMPAO with Stromal Vascular Fraction (SVF) of adipose tissue to develop a process tool for theranostic purposes, in particular imaging cardiac stem cell therapy. Methods: Ten million cells of SVF were labeled with {sup 99m}Tc-HMPAO complex and excess radiolabel was cleared off through washing in PBS. The labeling efficiency of {sup 99m}Tc-HMPAO was detected in labeled cells and their subsequent supernatant wash using isotope dose calibrator and gamma camera. The cytotoxicity was assessed for the comparative reactive oxygen species (ROS) by H{sub 2}DCFDDA, apoptotic events by annexin-V and TUNEL assay and mitochondrial potential by JC-1. Results: An encouraging labeling efficiency of 33% was observed with {sup 99m}Tc-HMPAO complex. The radionuclide labeling of SVF demonstrated significant safety profile as evaluated by apoptotic assays. Conclusion: {sup 99m}Tc-HMPAO labeling efficiency of 33% of total SV fraction would produce sufficient radioactive signals that would enable for in vivo tracking of cells by SPECT-CT. The radionuclide did not demonstrate any significant impact on the structural or functional organization of the labeled cells. Our study indicates that SVF can be safely labeled with {sup 99m}Tc-HMPAO without adverse cytotoxic events and for its potential role in imaging cardiac stem cell therapy.

  6. Radiopharmacokinetic data for 99mTc-ABP - A new radiopharmaceutical for bone scanning: Comparison with 99mTc-MDP

    International Nuclear Information System (INIS)

    Murphy, Consuelo Arteaga de; Melendez-Alafort, Laura; Montoya-Molina, Carlos E.; Sepulveda-Mendez, Jesus

    1997-01-01

    Technetium-99m-labeled alendronate is a new radiopharmaceutical for bone scanning developed under strict quality control at the INNSZ. The purpose of this work was to compare the radiopharmacokinetic data and the dosimetry of 99m Tc-ABP and 99m Tc-MDP in 10 volunteers, after it was tested in laboratory animals. 99m Tc-ABP has shorter mean residence time (MRT) and t (1(2)) β; is less protein bound; has a higher renal clearance; smaller Vdss, and similar bone uptake at 1 and 2 h. 99m Tc-ABP gives less radiation exposure to the patient with a 740 MBq dose, and the quality of the bone scan is excellent. 99m Tc-ABP is a better radiopharmaceutical than 99m Tc-MDP for bone scanning

  7. In vitro assessment of Tc-99m labeled bovine thrombin and streptokinase-activated human plasmin: concise communication

    International Nuclear Information System (INIS)

    Wong, D.W.; Tanaka, T.; Mishkin, F.; Lee, T.

    1979-01-01

    Bovine thrombin and streptokinase-activated human plasmin have been labeled with Tc-99m using stannous reduction of pertechnetate under physiological conditions (pH 7.4). The binding efficiency of radiotechnetium to these enzymes is greater than 94%, with less than 5% of reduced but unbound Tc-99m (Sn) complex as assayed by ascending paper radiochromatography using ITLC silica gel plate. Free or unbound pertechnetate is less than 1%. In vitro enzymatic analyses of the Tc-99m-labeled enzymes demonstrate no evidence of protein denaturation or significant loss of enzymatic activity after labeling. Both labeled enzymes are biochemically active in vitro with their respective substrates

  8. Recent developments in 99mTc and 123I-radiopharmaceuticals for SPECT imaging

    International Nuclear Information System (INIS)

    Kulkarni, P.V.

    1991-01-01

    Availability of 123 I of high radionuclidic purity has encouraged the development of 123 I-based radiopharmaceuticals for the assessment of myocardial fatty acid metabolism, myocardial neuronal activity, and for receptor and antibody imaging. Advances in the chemistry of technetium have resulted in the development of novel agents for myocardial and cerebral perfusion and renal function studies. Monoclonal antibodies labeled with 99m Tc show promise for imaging neoplastic lesions, myocardial infarcts, and thrombus localization. Recent developments in 123 I and 99m Tc agents for myocardial and brain imaging studies are discussed. (author)

  9. Platelet labelled radioisotope studies with Tc-99m-HM-PAO - own experience

    International Nuclear Information System (INIS)

    Dobkowski, P.; Krolicki, L.; Serafin-Krol, M.; Kielin, Z.; Staszkiewicz, W.

    1992-01-01

    The protocol of platelet labelling and results of 28 examinations with Tc- 99m labelled thrombocytes have been presented. In 6 cases this method was the only one, which allowed to show thrombotic lesions in carotid arteries. (author). 2 figs, 1 tab

  10. Tc-99m-labeled red blood cells for the measurement of red cell mass in newborn infants: concise communication

    International Nuclear Information System (INIS)

    Linderkamp, O.; Betke, K.; Fendel, H.; Klemm, J.; Lorenzen, K.; Riegel, K.P.

    1980-01-01

    In vitro and in vivo investigations were performed to examine the binding of Tc-99m to neonatal red blood cells (RBC). Labeling efficiency was about 90%, and unbound Tc-99m less than 3% after one washing, in premature and full-term newborns and in children. Thus presence of high percentages of fetal hemoglobin (Hb F) did not influence the labeling of RBCs with Tc-99m. RBCs of 11 newborns were hemolysed and the distribution of Tc-99m on RBC components was analyzed. Although Hb F percentage averaged (60.0 +- 8.10)% (s.d.), only (11.9 +- 3.7)% of Tc-99m was bound by Hb F, whereas (45.0 +- 6.1)% was associated with Hb A. RBC membranes bound (13.7 +- 4.3)% and (29.3 +- 4.0)% were found unbound in hemolysates. These results indicate that Tc-99m preferentially binds to beta chains. In vivo equilibration of Tc-99m RBCs and of albumin labeled with Evans blue was investigated in five newborn infants. Tc-99m RBCs were stable in each case during the first hour after injection. Elution of Tc-99m from RBCs was (3.4 +- 1.5)% per h. Body-to-venous hematocrit ratio averaged 0.86 +- 0.03

  11. Studies on the preparation of sup(99m)Tc labelled medical tracer compounds: pt. 4

    International Nuclear Information System (INIS)

    Kim, J.R.; Park, K.B.; Shim, H.S.

    1981-01-01

    A crude extract from a Korean native plant, Banha (Pinellia ternata), has been known to agglutinate the erythrocytes of rabbit, mouse and especially erythrocytes of leukemic patients, Sarcoma-180 cell and Ehrlich ascite cell. The Banha lectin was labelled either with 125 with 125 I by means of chloramine-T method or with sup(99m)Tc by using aqueous sodium pertechnetate (- sup(99m)Tc) solution and stannous chloride as a reducing agent. Their labelling yield was 60% and 98%, respectively. These labelled compounds were administered to mice by intraperitoneal injections and their radioactivity distributions were measured after 3 hours. The uptake of 125 I labelled compound to tissue in mice appeared in the order of kidney, pancreas, spleen, liver, blood, and stomach, but in the case of sup(99m)Tc, it appeared in the order of kidney, pancreas, stomach, liver, spleen and blood

  12. Development of 99mTc labelled somatostatin analogues and evaluation of their radiochemical and biological behaviour

    International Nuclear Information System (INIS)

    Gano, L.; Patricio, L.

    2001-01-01

    Conjugates of two somatostatin analogues, octreotide and RC-160, with HYNIC were synthesized, characterized and purified by reverse phase HPLC. Radiolabelling of the conjugates with 99m Tc was achieved using tricine as co-ligand. High labelling efficiencies were obtained and 99m Tc peptides with high radiochemical purity were found when analysed both by ITLC and HPLC. In vitro stability of 99m Tc-peptides in human serum and towards cysteine challenge was determined by Cellogel electrophoresis and HPLC after ultrafiltration of serum solution through a 20 kDa cut off membrane. Biodistribution studies were performed in healthy mice at 5 and 30 minutes and 1, 2, 4 and 24 h post-injection. Urine and blood samples were collected at sacrifice time. Samples of urine and ultrafiltrate murine serum were analysed by electrophoresis and reverse phase HPLC in order to get some information about radiocompounds metabolism. Biological distribution of 99m Tc octreotide was also assayed in mice pre-treated with an excess of unlabelled peptide. From our results we conclude that this labelling method led to stable 99m Tc complexes both in vitro and in vivo when high specific activities (37-72 GBq/μmole) were used. Biodistribution studies of both 99m Tc-peptides indicated a radioactivity distribution profile with significant differences especially in the liver uptake that is higher for 99m Tc RC-160. However, a rapid blood clearance was obtained for both radiolabelled peptides, and the urine analysis indicated that 99m Tc peptide is mostly excreted as the initial complex. Pre-treatment with unlabelled peptide did not affect renal excretion of 99m TOC but pancreas and intestine radioactive uptake was significantly lower, indicating saturation of somatostatin receptors and selective uptake. (author)

  13. 99mTc complexes of 1,3-propanedithiol derivatives

    International Nuclear Information System (INIS)

    Alagui, A.; Apparu, M.; Vidal, M.; Mathieu, J.P.

    1987-01-01

    The labelling of 1,3-n alkylpropanedithiols and of 15-(1,3-dimercapto 2-propyl)pentadecanoic acid by 99m Tc was performed by an exchange reaction with the hexachlorotechnetate ion 99m TcCl 6 2- and by reduction of 99m TcO 4 - with Sn(II) in the presence of the ligand. The biological distribution of the exotechnetium complexes obtained by the latter method in mouse does not reveal a high tropism of these labelling compounds in relation to a particular tissue. (author) 14 refs.; 2 tabs

  14. Synthesis and comparison of 99mTc-enrofloxacin and 99mTc-ciprofloxacin.

    NARCIS (Netherlands)

    Siaens, R.H.; Rennen, H.J.J.M.; Boerman, O.C.; Dierckx, R.A.; Slegers, G.

    2004-01-01

    The use of (99m)Tc-ciprofloxacin as a tracer for infection and inflammation has been examined and discussed in the literature extensively. Its alleged ability to discriminate between sterile inflammation and bacterial versus nonbacterial infections has led to an intense debate. Other labeled

  15. Synthesis, Characterization, and Initial Biological Evaluation of [99m Tc]Tc-Tricarbonyl-labeled DPA-α-MSH Peptide Derivatives for Potential Melanoma Imaging.

    Science.gov (United States)

    Gao, Feng; Sihver, Wiebke; Bergmann, Ralf; Belter, Birgit; Bolzati, Cristina; Salvarese, Nicola; Steinbach, Jörg; Pietzsch, Jens; Pietzsch, Hans-Jürgen

    2018-06-06

    α-Melanocyte stimulating hormone (α-MSH) derivatives target the melanocortin-1 receptor (MC1R) specifically and selectively. In this study, the α-MSH-derived peptide NAP-NS1 (Nle-Asp-His-d-Phe-Arg-Trp-Gly-NH 2 ) with and without linkers was conjugated with 5-(bis(pyridin-2-ylmethyl)amino)pentanoic acid (DPA-COOH) and labeled with [ 99m Tc]Tc-tricarbonyl by two methods. With the one-pot method the labeling was faster than with the two-pot method, while obtaining similarly high yields. Negligible trans-chelation and high stability in physiological solutions was determined for the [ 99m Tc]Tc-tricarbonyl-peptide conjugates. Coupling an ethylene glycol (EG)-based linker increased the hydrophilicity. The peptide derivatives displayed high binding affinity in murine B16F10 melanoma cells as well as in human MeWo and TXM13 melanoma cell homogenates. Preliminary in vivo studies with one of the [ 99m Tc]Tc-tricarbonyl-peptide conjugates showed good stability in blood and both renal and hepatobiliary excretion. Biodistribution was performed on healthy rats to gain initial insight into the potential relevance of the 99m Tc-labeled peptides for in vivo imaging. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

  16. Human monoclonal antibody 99mTc-88BV59: detection of colorectal cancer, recurrent or metastatic disease and immunogenicity assessment

    International Nuclear Information System (INIS)

    Krause, B.J.; Baum, R.P.; Staib-Sebler, E.; Lorenz, M.; Niesen, A.; Hoer, G.

    1997-01-01

    This study presents immunoscintigraphic results in 24 patients suffering from primary colorectal cancer, recurrent or metastatic disease after the injection of 1197-1351 MBq technetium-99m labelled totally human monoclonal antibody 88BV59. Labelling efficacy of 99m Tc-88BV59 ranged from 97% to 99%. Immunoscintigraphy was performed 18-20 h after injection. Scintigraphic findings were compared with those of computed tomography (CT). Patients underwent surgery in order to evaluate immunoscintigraphic findings histologically. Sera of the patients (before injection and 1 and 3 months post infusion) were analysed for the presence of human anti-human antibodies (HAHA). None of the patients showed a HAHA response as assessed by a solid-phase ELISA assay. The antibody scan detected about 25% more lesions than CT. In the detection of extrahepatic disease, the sensitivity of the antibody scan proved to be 68%, whereas the sensitivity of CT was 41%. (orig.). With 3 figs., 1 tab

  17. On the organ distribution of several 99mTc-labelled tetracyclines

    International Nuclear Information System (INIS)

    Weinhold, S.E.M.

    1983-01-01

    Experiments in rats have pointed to a high stability of 99m Tc-labelled tetracyclines, which are found in vivo in the form of chemically stable chelate complexes. Their biokinetic behaviour in most organs (the lungs) and the blood is predominantly determined by convection processes. In other organs (notably the kidneys and, to a lesser extent, the liver and spleen) their passage can be described in terms of influx and efflux, with accumulation, metabolisation and excretion of the drug administered being the main steps involved. 3 H-Labelled tetracyclines are chemically unchanged tetracyclines showing pronounced lipophilia that tend to be taken up and eliminated via influx and efflux processes in the large majority of organs. The highest blood levels were measured for 99m TcO 4 , which is a hydrophilic substance. None of the substances tested appeared to be able to cross the blood-brain barrier. As far as their chemical structure and solubility in water is concerned, 99m Tc-labelled tetracyclines occupy a position intermediate between the two comparative substances and the blood concentrations measured here were only moderately high. As they are accumulated to a considerable degree in the kidneys, the possibility of these substances' use in connection with renal scintiscans does not seem remote. In view of the fact that only one tenth of the dose of pertechnetate would be required for this purpose, radiation exposure could be reduced to a reasonable minimum. (TRV) [de

  18. Labelling of red blood cells with 99m pertechnetate

    International Nuclear Information System (INIS)

    Vyth, A.; Raam, C.F.

    1979-07-01

    This paper describes a method for labelling red blood cells with 99mTc in vitro, using electrolytically generated stannous ions as the reducing agent for 99mTc-pertechnetate. A labelling of 95% was found. A method for the in vivo labelling of red blood cells is also reported. This involves an injection of a stanno-DTPA-complex followed 20 minutes later by a 99mTc-pertechnetate solution scintillation camera images show more background activity when the in vivo method of labelling is used

  19. HYNIC a bifunctional prosthetic group for the labelling of peptides with 99mTc and 18FDG

    International Nuclear Information System (INIS)

    Sepideh Khoshbakht; Omid Sabzevari; Mohsen Amini; Faramarz Mehrnejad; Kimia Tabib; Soraya Shahhosseini; Shahid Beheshti University of Medical Sciences, Tehran

    2016-01-01

    With regard to high reactivity and chemoselectivity of HYNIC towards carbonyl of acyclic form of 18 FDG and its stable complexes with 99m Tc, in this study, LIKKPF as the model peptide was conjugated with HYNIC and labelled with 99m Tc (RCP[90 %) and 18 FDG for the first time. The RCP of [70 % was achieved for labelling with 18 FDG, in the presence of glucose (50-250 lg/mL). Our results showed the high potential of HYNIC conjugated peptides for labelling with 99m Tc and 18 FDG as 18 F-fluorinated prosthetic group, to be clinically accepted for the radiolabelling of peptides. (author)

  20. labelling and quality control of some 99m Tc-radiopharmaceuticals of expected biological activity

    International Nuclear Information System (INIS)

    Abdallah, A.B.I.

    2009-01-01

    this thesis addresses the labelling and quality control of some 99m Tc-radiopharmaceuticals which could be used for infection imaging. this study focuses on the labelling of sarafloxation, gatifloxation and cefepine with technetium-99m and biological evaluation of these labeled complexes and biodistribution in both normal and inflamed mice. the thesis is organized into two chapters: chapter I :labelling of some antibiotics chapter II :biological evaluation.

  1. Clinical application of 99mTc-HMPAO labeled leucocytes imaging in detecting bone joint infection

    International Nuclear Information System (INIS)

    Li Biao; Barthe, N.; Basse-Cathalinat, B.

    1995-01-01

    99m Tc-MDP scintigraphy and 99m Tc-HMPAO-leucocytes imaging were performed in twenty five patients with clinically suspected bone joint infection. All of the 25 cases were confirmed by surgery, microbiological and histologic examinations. Among them 21 cases were definitively diagnosed as infections, while 3 cases were non-infection. The results of 99m Tc-MDP scintigraphy showed that all of 25 cases demonstrated anomalous accumulation of radioactivity in the clinically suspected infections sites, while in 99m Tc-HMPAO-leucocytes imaging, concentrated radioactivity in proved infectious sites was observed in 19 cases, non-anomalous radioactivity found in 4 cases of non-infectious sites, but there were 2 cases false negative with long term antibiotics treatment, none of the case was false positive. Thereby a sensitivity of the labelled leucocytes imaging of 90.5%, a specificity of 100%, and a accuracy of about 92% were found. Present research work concluded that 99m Tc-HMPAO labelled leucocytes imaging provided a non-invasive, effective, and reliable diagnostic method in detecting patients with clinically suspected bone joint infection and afforded strong evidence for effective therapy

  2. Splenic scintigraphy using Tc-99m-labeled heat-denatured red blood cells in pediatric patients: concise communication

    International Nuclear Information System (INIS)

    Ehrlich, C.P.; Papanicolaou, N.; Treves, S.; Hurwitz, R.A.; Richards, P.

    1982-01-01

    Ten children underwent splenic imaging with heat-denatured red blood cells labeled with technetium-99m (Tc-99m DRBC). The presenting problems included the heterotaxia syndrome, recurrent idiopathic thrombocytopenic purpura following splenectomy, mass in the left posterior hemithorax, and blunt abdominal trauma. In nine patients, the presence or absence of splenic tissue was established. A splenic hematoma was identified in the tenth patient. All patients were initially scanned with Tc-99m sulfur colloid (Tc-99m SC), and were selected for Tc-99m DRBC scintigraphy only after the results of the SC scans failed to establish the clinical problem beyond doubt. The availability of kits containing stannous ions, essential for efficient and stable labeling of red blood cells with Tc-99m and requiring only a small volume of blood, make splenic scintigraphy in children a relatively simple and definitive diagnostic procedure, when identification of splenic tissue is of clinical importance

  3. Splenic scintigraphy using Tc-99m-labeled heat-denatured red blood cells in pediatric patients: concise communication

    Energy Technology Data Exchange (ETDEWEB)

    Ehrlich, C.P.; Papanicolaou, N.; Treves, S.; Hurwitz, R.A.; Richards, P.

    1982-03-01

    Ten children underwent splenic imaging with heat-denatured red blood cells labeled with technetium-99m (Tc-99m DRBC). The presenting problems included the heterotaxia syndrome, recurrent idiopathic thrombocytopenic purpura following splenectomy, mass in the left posterior hemithorax, and blunt abdominal trauma. In nine patients, the presence or absence of splenic tissue was established. A splenic hematoma was identified in the tenth patient. All patients were initially scanned with Tc-99m sulfur colloid (Tc-99m SC), and were selected for Tc-99m DRBC scintigraphy only after the results of the SC scans failed to establish the clinical problem beyond doubt. The availability of kits containing stannous ions, essential for efficient and stable labeling of red blood cells with Tc-99m and requiring only a small volume of blood, make splenic scintigraphy in children a relatively simple and definitive diagnostic procedure, when identification of splenic tissue is of clinical importance.

  4. Diagnosis of infected bone and joint diseases with 99mTc-HM-PAO labeled leukocytes

    International Nuclear Information System (INIS)

    Kanegae, Kakuko; Itoh, Kazuo; Tsukamoto, Eriko; Nagao, Kazuhiko; Nakada, Kunihiro; Hurudate, Masayori

    1992-01-01

    The usefulness of 99m Tc-hexamethylpropylene amine oxime (HM-PAO) labeled leukocytes scans was studied in 15 patients with suspected infection of the bone and joints. All spot images of lesions were obtained 4 and 24 hours after injection of 70.3-236.8 MBq (a mean, 149.5 MBq). 99m Tc-HM-PAO leukocytes scans were positive in 5 patients, negative in 8, and equivocal in 2. It had a sensitivity of 83% (5/6), specificity of 100% (6/6), and accuracy of 93% (14/15) for diagnosing infections. Equivocal uptake, seen on the 4-hr image in 2 patients, became negative on the 24-hr image. In view of ready availability and simple labeling procedure, 99m Tc-HM-PAO labeled leukocytes scans can be used as one of the specific diagnostic procedures for infections. (N.K.)

  5. Labeling capability of the eluent of gel-type 99Mo-99mTc generator

    International Nuclear Information System (INIS)

    Wu Xiuduo; Zhang Jingu

    1995-01-01

    The results of more than 7909 imaging of various organs which have been carried out on domestic gel-type 99 Mo- 99m Tc generators in the last seven years are presented. In all the 220 times of determination for the radiochemical purity of a portion of imaging agents, there were 15 times in which the labeling efficiency was lower than 90% and only 3 times in which the radiolabeling failed. In comparison with labeling capability of nuclear fission generators, it is showed that there are no evident differences between the eluent's labeling efficiency of the two kinds of generators

  6. 99mTechnetium labelled Escherichia coli

    International Nuclear Information System (INIS)

    Diniz, S.O.F.; Cardoso, V.N.; Resende, B.M.; Nunan, E.A.; Simal, C.J.R.

    1999-01-01

    Samples of a culture of unlabeled Escherichia coli were incubated with different concentrations of stannous chloride for various time periods. 99m Tc (26.0 MBq) was added to each preparation and the results showed a labelling yield of 98% for E. coli. Since the bacterial viability of 99m Tc-E. coli and E. coli did not show any statistical differences, these results demonstrate that labelling of E. coli with 99m Tc does not modify the bacterial viability, and the radiolabelled bacteria may be a good model to study bacterial translocation

  7. A comparative study of 99mTc-HL91 and 99mTc-MIBI imaging in experimental tumor and inflammatory models

    International Nuclear Information System (INIS)

    Cao, W.; Zhang, X.Y.; An, R.

    2002-01-01

    Aim: 99m Tc-HL91 is a newly developed hypoxic imaging agent for ischemic myocardium and tumor imaging. 99m Tc-MIBI is one of imaging agent for mammary tumor imaging. The aim of this experiment is to evaluate the diagnostic value of 99m Tc-HL91 in detection of solid tumor in experimental tumor and inflammatory models, via comparative study with 99m Tc-MIBI. Material and Methods: HL91 kits was provided by China Nine Star Co. Three kinds of bearing solid neoplasm mice groups (bearing Ehrlich carcinoma mice, bearing H 22 carcinoma mice and bearing human ovarian COC 1 neoplasm nude mice) and two inflammatory model groups (chemical and bacterial inflammation) underwent static whole body planar images at 1 and 4 hours post injection of 99m Tc-HL91. Two kinds of bearing neoplasm mice groups (bearing Ehrlich carcinoma mice, bearing H 22 carcinoma mice) and two inflammatory model groups (chemical and bacterial inflammation) underwent static planar images post injection of 99m Tc-MIBI, at early phase (10∼20 minutes) and delayed phase (2 hrs). All of mice were sacrificed at 4 hrs. The tumors, or inflammatory lesions, blood and contralateral muscles were removed, weighed and the radioactivity was measured. Regions of interesting (ROIs) were drawn around tumor, inflammatory lesions and contralateral muscles in planar images, and the radioactivity ratios of target (tumor or inflammatory lesions)-to-blood (T/B), target-to-non target (contralateral muscles) i. e. T/NT was calculated. Results: Neoplasm can be clearly visible in planar images at 1hr and 4 hrs post injection of 99m Tc-HL91 in all tumor models. At same time inflammatory lesions cannot be seen clearly. Neoplasm can be seen in delayed phase in 99m Tc-MIBI groups, but not easy to distinguish them from inflammation. Conclusion: Compared with 99m Tc-MIBI imaging, 99m Tc-HL91 has much more diagnostic value in detection of solid neoplasm, and can distinguish neoplasm from inflammation

  8. Pharmacokinetics, biodistribution and dosimetry of {sup 99m}Tc-labeled anti-human epidermal growth factor receptor humanized monoclonal antibody R3 in rats

    Energy Technology Data Exchange (ETDEWEB)

    Escobar, Normando Iznaga; Morales, Alejo Morales; Duconge, Jorge; Torres, Idania Caballero; Fernandez, Eduardo; Gomez, Jose A

    1998-01-01

    The pharmacokinetics, biodistribution and dosimetry of {sup 99m}Tc-labeled anti-human epidermal growth factor receptor (anti-hEGF-r) humanized monoclonal antibody (MAb) R3 was investigated following intravenous injection in normal Wistar rats. Serum disappearance curves were best fit by a two-compartment model having a mean distribution half-life (t{sub (1(2{alpha}}{sub ))}) of 0.250 h and a mean elimination (t{sub (1(2{beta}}{sub ))}) of 13.89 h. Among the various organs, a little accumulation of the radiolabeled antibody was found only in kidneys. Biodistribution and dosimetry studies in humans were performed by extrapolation of the animal data to humans. Absorbed dose to normal organs and the remainder of the whole body were estimated using the medical internal radiation dose formula, and dose contributions from radioactivity in transit through the gastrointestinal tract were estimated using a compartment model. Extrapolated values of radiation absorbed dose to normal organs in rads per millicurie administered were whole body, 0.0085; lower large intestine wall, 0.0898; small intestine, 0.0530; upper large intestine wall, 0.0731; and kidneys, 0.0455. The effective dose equivalent predicted was 0.0162 rem/mCi and the effective dose was found to be 0.015 rem/mCi. On the basis of the pharmacokinetics, biodistribution and internal radiation dosimetry information obtained in this study, a diagnostic phase I clinical trial with {sup 99m}Tc-labeled humanized MAb R3 conjugate in patients should be supported.

  9. Detection of gastrointestinal blood loss with /sup 99m/Tc-labeled, heat-treated red blood cells

    International Nuclear Information System (INIS)

    Som, P.; Oster, Z.H.; Atkins, H.L.; Goldman, A.G.; Sacker, D.F.; Harold, W.H.; Fairchild, R.G.; Richards, P.; Brill, A.B.

    1981-01-01

    Studies in dogs showed that heat-treated /sup 99m/Tc-labeled red blood cells (HT/RBC) afford a highly sensitive means of detecting gastrointestinal bleeding as low as 0.12 ml/min, which could not be seen with unheated /sup 99m/Tc-RBC, /sup 99m/Tc-sulfur colloid, or /sup 99m/Tc-DTPA. In addition, as the right upper quadrant and epigastrium remained free of activity, only one fifth to one tenth of the dose of /sup 99m/Tc was needed. The safety of HT/RBC in humans has been documented, and the experiments in dogs suggest that it may have advantages over other agents in detecting gastrointestinal bleeding

  10. sup(99m)Tc-labeled N-phosphoryl-aminoethyl-phosphate (sup(99m)Tc-PAEP), as bone and myocardial infarct agent. Studies in experimental animals

    International Nuclear Information System (INIS)

    Chiotellis, E.; Varvarigou, A.; Vavouraki, H.

    1982-01-01

    99m-Tc-PAEP appears as a promising new bone-seeking radiopharmaceutical. The biological experiments indicate high bone affinity and satisfactory localization in experimentally produced myocardial infarctions in rats and dogs. The data obtained suggest a further evaluation of this derivative in comparison to other technetium-phosphorus complexes

  11. 99mTc labelled peptides for imaging of peripheral receptors

    International Nuclear Information System (INIS)

    Mikolajczak, R.; Markiewicz, A.; Deptula, C.Z.; Zulczyk, W.; Birnbaum, G.; Zakrezewska, E.; Wozniak, I.

    2001-01-01

    The first trials of 99m Tc labelling by direct method using dithionite as a reducing agent (prepared in the freeze-dried form) gave the yields of around 30%. RC-160 labelling with 125 I by chloramine-T method resulted in 40-80% labelling yield. Our efforts were focused on BFC approach. HYNIC-TOC and HYNIC-RC-160 conjugates obtained in our laboratory were successfully labelled with 99m Tc with the yields over 90%. HPLC and TLC methods were applied for quality control (QC) of the labelled preparation. Methods of in vitro (stability and protein binding) testing of the labelled preparations were adopted to our laboratory conditions. First attempts on dry kit formulation based on HYNIC-TOC conjugates with tricine, tricine/nicotinic acid and EDDA were described. Various amounts of tin (II) (as SnCl 2 ) were added to the kits. Incubation conditions (time, temperature) were investigated. The kits were tested for labelling yield and radiochemical purity. It was shown that the results are at the same level or better than obtained in liquid phase but the procedure of labelling is significantly easier. Kit produced with tricine as co-ligand was labelled with 97% labelling yield after 30 min of incubation at room temperature, which is considered acceptable for diagnostic radiopharmaceutical preparation. Tricine/nicotinic acid kit requires heating to get labelling of around 95%. Similarly EDDA kit gives around 70% labelling after 30 min incubation at 80 deg. C. Further experiments on optimal kit composition and stability are required. Results of DOTA-RC-160 labelling with 90 Y show that this isotope, manufactured by Radioisotope Centre POLATOM, can be successfully used for medical applications. (author)

  12. Binding of 99mTc-labelled polyclonal human immunoglobulin to bacteria as a mechanism for scintigraphic detection of infection

    International Nuclear Information System (INIS)

    Calame, W.; Furth, R. van

    1991-01-01

    The aim of the present study was to determine whether 99m Tc-labelled polyclonal human immunoglobulin ( 99m Tc-HIG) binds to bacteria in vitro as well as in vivo. In vitro, the binding of 99m Tc-HIG to various gram-positive and gram-negative bacteria was determined. In vivo, mice were infected with Staphylococcus aureus Cowan I (protein A rich) or S. aureus EMS (protein A deficient) in a tigh muscle and then 99m Tc-HIG or 99m Tc-labelled human serum albumin ( 99m Tc-HSA) was administered; scintigrams were made 1, 4 and 18 h later. In vitro binding of 99m Tc-HIG to bacteria was higher for gram-positive than for gram-negative forms. A positive correlation was found between the protein A content and the degree of binding to S. aureus. This was also found in vivo. The accumulation of 99m Tc-HIG at the site of infection was significantly (P 99m Tc-HSA, for both strains of S. aureus. It is concluded that vascular permeability cannot fully explain the accumulation of 99m Tc-HIG at the site of infection and that binding of 99m Tc-HIG to bacteria plays a role in this respect. (orig.)

  13. Towards kit formulation of 99mTc labelled somatostatin receptor binding peptides of high specific activity for tumour localization

    International Nuclear Information System (INIS)

    Behe, M.; Powell, P.; Maecke, H.R.

    2001-01-01

    The project aimed to develop 99m Tc octreotide analogue for use in nuclear oncology. Several attempts to label SRIF analogues with 99m Tc have used a direct labelling approach but, for this project, HYNIC was chosen as a technetium ligand. A comparison of two different SRIF analogues designed for high specific activity labelling with 99m Tc was done. HYNIC-Octreotide and HYNIC-TOC were prepared and a kit formulation that can be labelled conveniently is currently being studied in a clinical setting. (author)

  14. Development of (99m)Tc-Labeled Pyridyl Benzofuran Derivatives To Detect Pancreatic Amylin in Islet Amyloid Model Mice.

    Science.gov (United States)

    Yoshimura, Masashi; Ono, Masahiro; Watanabe, Hiroyuki; Kimura, Hiroyuki; Saji, Hideo

    2016-06-15

    While islet amyloid deposition comprising amylin is one of pathological hallmarks of type 2 diabetes mellitus (T2DM), no useful amylin-imaging probe has been reported. In this study, we evaluated two (99m)Tc-labeled pyridyl benzofuran derivatives as novel amylin-imaging probes using the newly established islet amyloid model mouse. Binding experiments in vitro demonstrated that [(99m)Tc]1 displayed a higher affinity for amylin aggregates than [(99m)Tc]2. Autoradiographic studies using human pancreas sections with T2DM revealed that [(99m)Tc]1 clearly labeled islet amyloid in T2DM pancreatic sections, while [(99m)Tc]2 did not. Although the initial uptake of [(99m)Tc]1 by the normal mouse pancreas was low (0.74%ID/g at 2 min post-injection), [(99m)Tc]1 showed higher retention in the model mouse pancreas than that of the normal mouse, and exhibited strong binding to amylin aggregates in the living pancreas of the model mice. These results suggest that [(99m)Tc]1 is a potential imaging probe targeting islet amyloids in the T2DM pancreas.

  15. Quality control of 99mTc-labeled dextran for lymphoscintigraphy

    International Nuclear Information System (INIS)

    Yang, K.A.; Chen Yujeng; Yang Lihwei; Jong Shiangbin; Wu Chungchieng; Chen Jingyeh

    1989-01-01

    99m Tc-labeled dextran has been suggested as a lymphoscintigraphic agent. However, quality-control results from previous studies have been controversial. In this study, the optimal concentration of stannous ion and pH value were determined to obtain maximal labeling. Paper and thin-layer chromatography showed total labeling efficiency as high as 98.4%. Anthrone test of the supernatant of the segments from thin-layer chromatographic strip was performed. Colorimetric determinations verified that dextran was found in the same locations as the peak radioactivity. (orig.)

  16. Evaluation of Tc-99M labeled ethylene diamine tetra acetic acid biotin monomer (EB1) as an inflammation imaging agent

    International Nuclear Information System (INIS)

    Imran, M.B.; Qaiser, I.; Jehangir, M.; Irfan, J.

    2004-01-01

    Objective:This study was aimed at the evaluation of EB1 as an inflammation-imaging agent in animal models after ascertaining its normal biodistribution. Methods: Kit was formulated by adding SnC12 as reducing agent in EB 1 compound. EDTA was used as chelating agent. Buffer was added to lower the pH of solution to 5. Freeze dried kits were prepared for later use in experiments. Kits were reconstituted with 0.5 ml of fresh eluate of 99m-TcO4 containing total activity of about 370 MBq. Radiochemical quality control was checked by conventional strip method using double solvent technique.Biodistribution was assessed in 15 Sprague Dawley rats. An injection of 10 MBq was given in tail vein in each animal. Animals were killed at pre-specified time intervals; organs were separated, weighed and counted. Counts recovered were corrected for decay. Inflammation models were prepared by injecting turpentine oil in the thigh muscles of 14 rabbits. In one rabbit inflammation was not induced and was used as control for EB 1. In 3 of inflammation models plain 99m-TcO4 was injected (control II). In another group of 3 animals 99m-TC-EDTA was injected (control II). In the last group of 8 animals 99m-TcO4-EB 1 was injected (experimental gp). Animals were serially imaged under Seimens' E-Cam gamma camera for the distribution of activity in different organs and at the site of inflammation. Results: Kit labeling efficiency was 90.5 + 2.5% with 2.5 + 0.8% free activity and 7 + 1.1% hydrolyzed form. Animal study on rats showed that pharmaceutical is mainly excreted by kidneys (51.57 + 9.2% at 15 minutes and 81.73 + 7.9% at 4 hours). Uptake in liver was 7.52 + 2.2% at 15 minutes that decreased to 2.3 + 0.5% at 4 hours. Activity in intestine increased from 5.48 + 2.9% to 7.05 + 1.6% at 15 minutes to 4 hours. Activity in background (=blood) decreased from 0.13% (at 15 minutes) to 0.04% at 4 hrs. In bones EB1 uptake decreased from 0.68% to 0.15% at 15 minutes to 4 hours. In inflammation models

  17. Technetium-99m-Labeled Diethylcarbamazine Citrate (99mTc-DEC as a New Diagnostic Agent for Lymphatic Filariasis Detection

    Directory of Open Access Journals (Sweden)

    N. K. Oekar

    2017-11-01

    Full Text Available Lymphatic filariasis or more commonly known as elephantiasis disease has infected more than 120 million people in 80 countries; and more than 40 million of them are unable to work, in addition to disruption of aesthetic values. The problem faced by almost all people in combating this infectious disease is delayed diagnosis. The sufferers do not realize that they have been infected with this disease. A specific and accurate method of early detection is therefore needed. 99mTc-labeled Diethylcarbamazine-citrate (99mTc-DEC has been successfully prepared. However, as part of the discovery and development of new drugs, the fulfillment of pharmaceutical and safety requirements have to be evaluated. Physico-chemical aspects such as stability, purity levels, and other pharmaceutical requirements, as well as pharmacokinetic studies and route of administration, are important parameters to be studied. The stability test showed that after seven months of storage, a preparation in a dry kit retains an efficiency of labeling and a purity level of more than 90 % and its physico-chemical and biological characteristics remained steady. Biodistribution test in Wistar rat showed that the greatest accumulation occurred in the lymphatic system, especially in the popliteal glands and in lumbar and mesenteric lymph nodes. Imaging with a gamma camera after intradermal and intravenous injections to the experimental animals resulted in a positive image that showed 99mTc-DEC accumulation in the target organ. The results of this innovation are expected to contribute significantly to improving public health, particulary in early detection of filarial infections. In addition, this result is expected to be a concrete contribution to the program of "The Global Goal of Elimination of Lymphatic Filariasis as a Public Health Problem by the Year 2020”.

  18. In vivo distribution of Tc-99m labeled recombinant tissue-type plasminogen activator in control and thrombus-bearing rats

    International Nuclear Information System (INIS)

    Tsukamoto, Eriko

    1992-01-01

    In vivo distribution of Tc-99m labeled recombinant tissue-type plasminogen activator (Tc-99m-rt-PA) was studied in control rats and thrombus-bearing rats. To compare fibrin binding in vivo with that in vitro, Tc-99m-rt-PA binding to fibrin gel in vitro was also imaged. Rapid blood clearance and accumulation into the liver and kidneys were observed in both control and thrombus-bearing rats. Accumulation in the stomach, which indicates instability of labeled rt-PA in vivo, was very low until two hours after injection. Tc-99m-rt-PA accumulation in the clots was higher than that in skeletal and heart muscles, although it was lower than in blood, liver, and kidneys. Administration of aprotinin, an antifibrinolytic agent, significantly prolonged clot accumulation of Tc-99m-rt-PA at 30 minutes after injection. These results suggest that fibrinolysis is responsible for the low rt-PA concentration in the clots. A scintigram of a thrombus-bearing rat demonstrated increased radioactivity at the clot forming site. On the other hand, Tc-99m-labeled human albumin, which was used as a control, was not accumulated in the clot. Tc-99m-rt-PA binding to fibrin gel in vitro was clearly imaged. By comparison, in vivo fibrin binding of Tc-99m-rt-PA was much lower than in vitro. The reasons for low thrombus uptake in vivo may be: (1) biochemical inactivation of extrinsically administered rt-PA by t-PA inhibitor; (2) fibrinolysis by rt-PA activated plasminogen. Overcoming these limitations will enable Tc-99m-rt-PA to reach the stage of clinical trials. (author)

  19. Problems in clinical practice of domestic supply of 99Mo/99mTc. Considerations on the domestic production of 99Mo/99mTc

    International Nuclear Information System (INIS)

    Yamabayashi, Hisamichi

    2012-01-01

    At present, a bulky import product, 99 Mo supplied in Japan is produced by a nuclear fission method which enables to produce a generator system with no need of commercially preparing 99m Tc-labeled radiopharmaceuticals due to its high specific activity. However its usage of enriched uranium target leads to avoiding the fission method from the option of domestic production. In order to secure the domestic supply of 99 Mo/ 99m Tc, the neutron activation method, aiming to meet about 20% of domestic demand, is under development along with the re-start program of JMTR. Development of various production methods using accelerators are also in progress. In those non-fission methods with reactors or accelerators, rapid and effective procedures for concentration and refinement of 99m Tc solution eluted from 99 Mo of low specific activity are the subjects to be considered for attaining the stable labeling performances. (author)

  20. Clinical experience with sup(99m)Tc-hexamethylpropylene-amineoxime for labelling leucocytes and imaging inflammation

    Energy Technology Data Exchange (ETDEWEB)

    Peters, A.M.; Danpure, H.J.; Osman, S.; Hawker, R.J.; Henderson, B.L.; Hodgson, H.J.; Kelly, J.D.; Neirinckx, R.D.; Lavender, J.P.

    1986-10-25

    Hexamethylpropylene-amineoxime (HMPAO) forms a lipid-soluble neutral complex with sup(99m)Tc which is rapidly incorporated into leucocytes in vitro. In six patients with suspected or known inflammatory disease, a 'mixed' leucocyte suspension isolated from 85 ml blood anticoagulated with acid-citrate-dextrose was labelled by sup(99m)Tc-HMPAO with a mean efficiency of 47% (SE2%), of which 78% (3) was taken up by granulocytes. Activity eluted more rapidly from other cell types in vitro than from granulocytes, which remained firmly labelled. Mean initial biodistribution of the label and granulocyte recovery in blood of 32% (8) at 30-40 min showed that the granulocytes were not significantly activated during labelling. All six patients were positive for inflammatory disease, as early as 30 min in five patients and at 3 h in the sixth; they all remained positive at 20-24 h. Four patients also received /sup 111/In-labelled 'pure' granulocytes. In terms of detail, the sup(99m)Tc images were comparable or superior to the /sup 111/In images.

  1. Development, preparation and control of sup(99m)Tc or sup(113m)In labelled stannous hydroxide radiopharmaceuticals. Part of a coordinated programme on radiopharmaceuticals

    International Nuclear Information System (INIS)

    Alvarez Cervera, J.

    1975-01-01

    The preparation of different sup(99m)Tc and sup(113m)In radiopharmaceuticals using stannous chloride was investigated. Chemical and radiochemical procedures for the quality control of these preparations were studied. Toxicity and biological controls of the preparation were carried out. Procedures for the preparation and control of the following radiopharmaceuticals have been standardized by the authors; albumin macroaggregates labelled with sup(99m)Tc, sup(113m)In and other isotopes for lung scanning; albumin microspheres labelled with sup(99m)Tc for lung scanning; sup(99m)Tc or sup(113m)In-labelled stannous hydroxide colloid for liver scanning; sup(99m)Tc-stannous phytate for liver scanning; sup(99m)Tc-Sn-dextrose, a new radiopharmaceutical which has been proposed by the authors and is now used in Mexico for renal and cerebral scanning and sup(99m)Tc-Sn pyrophosphate and diphosphonate for bone scanning

  2. The diagnostic value of monoclonal antibody scan (leucoscan) compared with 99mTc MDP bone scan and Ga 67 in diagnosing bone and joint infection

    International Nuclear Information System (INIS)

    Koukouraki, S.I.; Velidaki, A.; Prassopoulos, V.; Karkavitsas, N.; Vavouranakis, H.; Hatjipavlou, A.

    2002-01-01

    Full text: Nowadays different radiopharmaceuticals have been developed as 99mTc MDP, 67Ga citrate, 111In oxine- and 99mTc HMPAO labeled leucocytes for the accurate localization of bone/joint infection, but all of them have limitations that encouraged the search of new agents characterized from high and early uptake in infectious/inflammatory tissues, low toxicity and no accumulation in non inflamed tissues. The purpose of this study is to compare the diagnostic value of a 99mTc labeled antigranulocyte Fab' fragment (Leucoscan) with 99mTc MDP bone scan and 67 Ga. The monoclonal antibody, Leucoscan, is an IgG murine Fab' fragment directed against a NCA-90 epitope located on the surface of granulocytes. 45 patients with suspected bone and joint infection (18 total hip prosthesis, 4 knee prosthesis, 8 vertebral infection and 15 long bones) were included in this study. All patients underwent conventional Rx, bone scan, 67Ga scan and Leucoscan. Three phase 99mTc MDP bone scan and 67Ga scan were performed using standard procedures. For Leucoscan the antibody was labeled with 25 mCi of 99mTc and was infected intravenously over 30 seconds. Ten minutes planar images were taken 1 h and 2 hrs p.i using a GE Millennium γ camera provided with a LEGP collimator. Images were evaluated as score 1 (no abnormal uptake), score 2 (probably positive), score 3 (definitely infected) according the intensity of abnormally increased uptake. Results were compared with 99mTc MDP bone scan and 67Ga scans. The final diagnosis was given by the surgical verification with histopathology or culture. All 45 patients had pathologic proof of presence/absence of bone and joint infection. 36/45 were positive for bone or joint infection and 9/45 were negative.30/36 patients with surgically proven bone and joint infection had true positive Leucoscan, 26/36 had true positive MDP bone scan and 20/36 true positive 67Ga scan. Nine out of 9 patients with proven absence of inflammation had true negative

  3. Bacterial infection identification by an anti-peptidoglycan aptamer labeled with Technetium-99m

    Energy Technology Data Exchange (ETDEWEB)

    Andrade, Antero Silva Ribeiro; Ferreira, Iêda Mendes [Centro de Desenvolvimento da Tecnologia Nuclear (CDTN/CNEN-MG), Belo Horizonte, MG (Brazil); Barros, Andre Luis Branco de; Cardoso, Valbert Nascimento [Universidade Federal de Minas Gerais (UFMG), Belo Horizonte, MG (Brazil)

    2017-07-01

    Full text: Introduction: A variety of radiopharmaceuticals is used to detect infection, but long-term clinical use has shown that the majority of them cannot distinguish between inflammation and infection. Nuclear medicine clinics are still awaiting the optimal scintigraphic imaging agents capable of discriminating between infection and inflammation, and between fungal and bacterial infections. Aptamers are oligonucleotides that display high affinity and specificity for their molecular targets and are emerging as promising molecules for radiopharmaceuticals development. Material and Methods: An aptamer for the peptidoglycan (main constituent of bacterial cell walls) termed Antibac1 was selected in a previous work. In the present study, this aptamer were labeled with {sup 99m}Tc and evaluated for bacterial infections identification by scintigraphy. All protocols were approved by the local Ethics Committee for Animal Experimentation of the Federal University of Minas Gerais (CETEA / UFMG), Protocol number 108/2014. Labeling with {sup 99m}Tc was performed by the direct method and the complex stability was evaluated in saline, plasma and presence of cysteine. The biodistribution and scintigraphic imaging studies with the {sup 99m}Tc-Antibac1 were carried out in two distinct experimental infection models: Swiss mice infected in the right thigh with Staphylococcus aureus or Candida albicans. {sup 99m}Tc radiolabeled library, consisting of oligonucleotides with random sequences, was used as a control in both experimental models. The direct radiolabeling allowed radiolabel yields above 90%. Results: A high complex stability was obtained in saline solution and plasma, but 51% of transchelation was verified after 24 h in the presence of cysteine. Scintigraphic images of S. aureus infected mice that received the {sup 99m}Tc-Antibac1 showed target to non-target ratios of 4.7 ± 0.90 and 4.6 ± 0.10 at 1.5 and 3.0 h, respectively. These values were statistically higher than

  4. Bacterial infection identification by an anti-peptidoglycan aptamer labeled with Technetium-99m

    International Nuclear Information System (INIS)

    Andrade, Antero Silva Ribeiro; Ferreira, Iêda Mendes; Barros, Andre Luis Branco de; Cardoso, Valbert Nascimento

    2017-01-01

    Full text: Introduction: A variety of radiopharmaceuticals is used to detect infection, but long-term clinical use has shown that the majority of them cannot distinguish between inflammation and infection. Nuclear medicine clinics are still awaiting the optimal scintigraphic imaging agents capable of discriminating between infection and inflammation, and between fungal and bacterial infections. Aptamers are oligonucleotides that display high affinity and specificity for their molecular targets and are emerging as promising molecules for radiopharmaceuticals development. Material and Methods: An aptamer for the peptidoglycan (main constituent of bacterial cell walls) termed Antibac1 was selected in a previous work. In the present study, this aptamer were labeled with 99m Tc and evaluated for bacterial infections identification by scintigraphy. All protocols were approved by the local Ethics Committee for Animal Experimentation of the Federal University of Minas Gerais (CETEA / UFMG), Protocol number 108/2014. Labeling with 99m Tc was performed by the direct method and the complex stability was evaluated in saline, plasma and presence of cysteine. The biodistribution and scintigraphic imaging studies with the 99m Tc-Antibac1 were carried out in two distinct experimental infection models: Swiss mice infected in the right thigh with Staphylococcus aureus or Candida albicans. 99m Tc radiolabeled library, consisting of oligonucleotides with random sequences, was used as a control in both experimental models. The direct radiolabeling allowed radiolabel yields above 90%. Results: A high complex stability was obtained in saline solution and plasma, but 51% of transchelation was verified after 24 h in the presence of cysteine. Scintigraphic images of S. aureus infected mice that received the 99m Tc-Antibac1 showed target to non-target ratios of 4.7 ± 0.90 and 4.6 ± 0.10 at 1.5 and 3.0 h, respectively. These values were statistically higher than found for the 99m Tc

  5. Evaluation of 99mTc-nitroimidazole in animal of myocardial necrosis

    International Nuclear Information System (INIS)

    Shimpi, H.H.; Mahapatra, S.; Noronha, O.P.D.

    1998-01-01

    Full text: Extensive studies carried out using 99m Tc-nitroimidazole (BMS 181321) suggested that it is a useful agent to investigate the status of hypoxia in solid tumors and ischemic myocardium. In vitro studies also showed that 99m Tc nitroimidazole is preferentially trapped in and retained by hypoxic, but viable cardiac muscle. We have evaluated the compound in an animal (rat) model of myocardial necrosis. 99m Tc-nitromidazole was labelled with 99m Tc by using cyclan and Sn-glucaric acid. The radiochemical purity was >95%. It was found to be very stable. Experimental (rat) animal of myocardial necrosis or ischemic necrosis was obtained by injecting iso proternol HCl subcutaneously (S.C.) at a dose of 5.25 mg/kg body weight. After 48 h, gross and microscopic necrotic changes were seen in the heart which closely resembled the myocardial infarct of necrotic lesion akin to ischemic necrosis of the myocardium. Animal biodistribution study demonstrated that 99m Tc nitroimidazole cleared very fast from the blood stream of both normal system. Significantly higher uptake was seen in heart of experimental animals compared to normal animals at 60 min. The ratios of heart to blood, liver and kidneys in both normal and experimental animals showed significantly higher ratios in experimental animals. The heart to blood ratio of experimental animal remained same up to 60 min. compared to a sharp decline with time in normal animals. The above results show that 99m Tc-nitroimidazole could be used for detection of myocardial necrosis or myocardial infarct in clinical conditions

  6. Chemical form of tumor-tropic 99mTc-DL-homocysteine

    International Nuclear Information System (INIS)

    Takeda, A.; Okada, S.

    1989-01-01

    Analyses of the chemical forms of 99m Tc-complexes provide important information for the development of a new tumor-tropic 99m Tc-labeled radiopharmaceutical. We attempted to determine the chemical form of 99m Tc-DL-homocysteine ( 99m Tc-Hcy) which was previously reported to be tumor-tropic. By analyzing the functional residues of Hcy in the 99m Tc-Hcy molecule, it was estimated that the sulfhydryl and amino residues participated in the chelate formation. Gel filtration analysis of 99m Tc-Hcy indicated that its molecular size was bigger than that of 99m Tc-penicillamine monomer. The analysis also indicated that 99m Tc-Hcy complex seemed to be a relatively small oligomer. Although an uncertainty remains on the valency of Tc in 99m Tc-Hcy molecule and the accurate molecular size of this complex, its putative chemical form is described. (author)

  7. A novel electrochemical technique for the production of clinical grade 99mTc using (n, γ)99Mo

    International Nuclear Information System (INIS)

    Chakravarty, Rubel; Dash, Ashutosh; Venkatesh, Meera

    2010-01-01

    Introduction: In order to meet the growing demand for 99m Tc and to reduce the reliance on fission-produced 99 Mo, an electrochemical pathway for accessing 99m Tc through the (n, γ) 99 Mo was explored as a back-up measure and to supplement 99m Tc supply for radiopharmaceuticals application. Methods: 99m Tc from an equilibrium mixture of 99 Mo/ 99m Tc was selectively deposited on a platinum cathode in an electrochemical cell by applying optimal voltage and stripped back again into the 0.9% saline solution. The radiochemical and radionuclidic purity of the product were determined using standard techniques. 99m Tc thus obtained was used for labeling standard ligands such as dimercaptosuccinic acid (DMSA) and ethylene dicysteine (EC), to ascertain the usability. Results: Selective deposition of 99m Tc on the platinum electrode was achieved at a potential of 5 V over a period of 1 h in NaOH electrobath. The overall yield of 99m Tc was >90%, with >99.99% radionuclidic purity and >99% radiochemical purity. The performance of the generator remained consistent over a period of 10 days. The compatibility of the product in the preparation of 99m Tc-labeled formulations such as 99m Tc-DMSA and 99m Tc-EC was found to be satisfactory in terms of high labeling yields (>98%). Conclusion: A novel and attractive method has been developed to obtain highly concentrated 99m Tc, without using fission-produced 99 Mo.

  8. Media Fill Test for validation of autologous leukocytes separation and labelling by (99m)Tc-HmPAO.

    Science.gov (United States)

    Urbano, Nicoletta; Modoni, Sergio; Schillaci, Orazio

    2013-01-01

    Manufacturing of sterile products must be carried out in order to minimize risks of microbiological contamination. White blood cells (WBC) labelled with (99m)Tc-exametazime ((99m)Tc-hexamethylpropyleneamine oxime; (99m)Tc-HMPAO) are being successfully applied in the field of infection/inflammation scintigraphy for many years. In our radiopharmacy lab, separation and labelling of autologous leukocytes with (99m)Tc-HMPAO were performed in a laminar flow cabinet not classified and placed in a controlled area, whereas (99m)Tc-HMPAO radiolabelling procedure was carried out in a hot cell with manipulator gloves. This study was conducted to validate this process using a Media Fill simulation test. The study was performed using sterile Tryptic Soy Broth (TSB) in place of active product, reproducing as closely as possible the routine aseptic production process with all the critical steps, as described in the our internal standard operative procedures (SOP). The final vials containing the media of each processed step were then incubated for 14 days and examined for the evidence of microbial growth. No evidence of turbidity was observed in all the steps assayed by the Media Fill. In the separation and labelling of autologous leukocytes with (99m)Tc-HmPAO, Media-Fill test represents a reliable tool to validate the aseptic process. Copyright © 2013 Elsevier Inc. All rights reserved.

  9. Human monoclonal antibody {sup 99m}Tc-88BV59: detection of colorectal cancer, recurrent or metastatic disease and immunogenicity assessment

    Energy Technology Data Exchange (ETDEWEB)

    Krause, B.J. [Department of Nuclear Medicine, Johann Wolfgang Goethe University Medical Center, Frankfurt/Main (Germany); Baum, R.P. [Department of Nuclear Medicine, Johann Wolfgang Goethe University Medical Center, Frankfurt/Main (Germany); Staib-Sebler, E. [Department of General and Abdominal Surgery, Johann Wolfgang Goethe University Medical Center, Frankfurt/Main (Germany); Lorenz, M. [Department of General and Abdominal Surgery, Johann Wolfgang Goethe University Medical Center, Frankfurt/Main (Germany); Niesen, A. [Department of Nuclear Medicine, Johann Wolfgang Goethe University Medical Center, Frankfurt/Main (Germany); Hoer, G. [Department of Nuclear Medicine, Johann Wolfgang Goethe University Medical Center, Frankfurt/Main (Germany)

    1997-01-01

    This study presents immunoscintigraphic results in 24 patients suffering from primary colorectal cancer, recurrent or metastatic disease after the injection of 1197-1351 MBq technetium-99m labelled totally human monoclonal antibody 88BV59. Labelling efficacy of {sup 99m}Tc-88BV59 ranged from 97% to 99%. Immunoscintigraphy was performed 18-20 h after injection. Scintigraphic findings were compared with those of computed tomography (CT). Patients underwent surgery in order to evaluate immunoscintigraphic findings histologically. Sera of the patients (before injection and 1 and 3 months post infusion) were analysed for the presence of human anti-human antibodies (HAHA). None of the patients showed a HAHA response as assessed by a solid-phase ELISA assay. The antibody scan detected about 25% more lesions than CT. In the detection of extrahepatic disease, the sensitivity of the antibody scan proved to be 68%, whereas the sensitivity of CT was 41%. (orig.). With 3 figs., 1 tab.

  10. Comparative in vivo evaluation of two novel 99mTc labelled bombesin derivatives

    International Nuclear Information System (INIS)

    Gourni, Eleni; Bouziotis, Penelope; Zikos, Christos; Loudos, George; Xanthopoulos, Stavros; Fani, Melpomeni; Archimandritis, Spyridon C.; Varvarigou, Alexandra D.

    2006-01-01

    Bombesin (BN), a 14 amino acid peptide, is an analogue of human gastrin-releasing-peptide (GRP) that binds to GRP receptors (GRP-R) with high affinity and specificity. In addition to this physiological role, GRP, through its interaction with GRP-R, promotes tumour growth in a number of human cancer cell lines. The GRP receptors are over-expressed on a variety of human cancer cells. Aim of the present work is the study of two novels BN-like peptides, by investigating the radiochemical and radiopharmacological behaviour of their complexes with metals. The derivatives under study are: Gly-Gly-Cys-Aca-BN [2-14] where Aca: 6-amino-hexanoic acid. Pyroglutamic acid in the bombesin molecule has been replaced by the chemical group Gly-Gly-Cys-Aca, which bears an amino-acid combination capable of complexing a variety of radiometals. The other derivative under study is: Gly-Gly-Cys-Aca-BN [7-14]. This moiety of the peptide has been chosen because it has been proven to be a potent GRP agonist. The peptide derivatives were synthesized by SPPS, according to the Fmoc strategy and were identified by reverse phase high performance liquid chromatography (RP-HPLC). Radiolabelling with 99m Tc was performed via the precursor 99m Tc-gluconate. The stability of the radiolabelled species was examined with time. In vivo studies of the two 99m Tc-labelled derivatives were performed, comparatively, in normal mice, attention being focused on GRP receptor-bearing organs, and in experimentally induced prostate cancer models. Experimental tumours were imaged in a small field-of-view animal gamma camera

  11. Blood cell labeling with technetium-99m, (2)

    International Nuclear Information System (INIS)

    Uchida, Tatsumi; Yoshida, Hiroshi; Matsuda, Shin; Kimura, Hideo; Miura, Nobuo

    1978-01-01

    Using a labeling method with sup(99m)Tc-pertechnetate to red blood cells (RBC), circulating blood volume was measured in comparison with that from 51 Cr-labeled RBC method. The technique is easier than already published methods, because CIS kit for sup(99m)Tc-RBC labeling (TCK-11) became to be available recently. Two mls of ACD-anticoagulated blood were withdrawn and 0.5 ml of reducing reagent prepared just before use was added to blood, waiting 5 minutes and discarding the serum after centrifugation, then adding 100 μCi of sup(99m)Tc. After washing the labeled cells by isotonic saline, cells were re-suspended in 10 ml of saline and injected to the subject. Blood specimen was obtained 10, 30, 60 and 120 minutes after infusion and blood volume was calculated by the usual way. Circulating blood volume by sup(99m)Tc was well correlated with that by 51 Cr (=0.98, p 0.01), however, the value calculated from sup(99m)Tc were 4.8 percent higher than those by 51 Cr, which suggested the elution of sup(99m)Tc from labeled RBC. sup(99m)Tc method has the advantages that higher radioactivity can be obtained in small amount of blood, which is useful in the determination of blood volume in children or in small animals in the laboratory. The measurement of blood volume of the mouse was done by using sup(99m)Tc method. The results were 1.70 +- 0.06 ml (6.35 +- 0.18%/gm), which coincided with the values reported previously. Because of it's short half life and low radiation dosage to the patients, sup(99m)Tc method will be recommended in the field of pediatrics or in patients with polycythemia or congestive heart failure, who are requested the repeated measurement of blood volume. (auth.)

  12. Development and evaluation of electro chemical methods for the separation of Tc-99m labelled compounds of medical importance

    International Nuclear Information System (INIS)

    Mani, R.S.

    1978-03-01

    The preparation of sup(99m)Tc radiopharmaceuticals using the electrolytic reduction of sup(99m)Tc pertechnetate was investigated. The effect of current intensity, amount of current, pH and applied voltage on the reduction of the Tc-VII and its incorporation into the radiopharmaceuticals was evaluated. The results indicate that the electrolytic method gives high and reproducible labelling yields and compounds with good radiochemical purity. Procedures for the preparation and control of the following sup(99m)Tc radiopharmaceuticals were standardized by the authors: Tc-tin colloid, Tc-red blood cells, Tc-HSA, Tc-albumin microspheres, Tc-EHDP, Tc-gluconate and Tc-glucoheptonate. A portable electrolytic labelling instrument was designed for use in hospitals

  13. Synthesis of 99mTc-nimotuzumab with tricarbonyl ion: in vitro and in vivo studies.

    Science.gov (United States)

    Garcia, Maria Fernanda; Camacho, Ximena; Calzada, Victoria; Fernandez, Marcelo; Porcal, Williams; Alonso, Omar; Gambini, Juan Pablo; Cabral, Pablo

    2012-01-01

    The Epidermal growth factor receptor (EGFR) family plays an important role in carcinogenesis. CIMAher® (Nimotuzumab), is a humanized monoclonal antibody, which recognizes EGFR with high affinity. The aim of this work was to perform the direct labeling of Nimotuzumab with [99mTc(CO)3(H2O)3]+ as precursor and to evaluate its labeling conditions, in vitro and in vivo stability and biodistrution in normal C57 BL/6J mice. 99mTc(CO3)-Nimotuzumab labeling yields were up to 90%. More than 90% of the complex remained intact after 24 h of incubation with L-Histidine (1/300 molar ratio). Biodistribution studies in normal mice were also performed. Inmunoreactivity was confirmed by cell binding assays with A431cells. These results encourage the evaluation of the potential role of 99mTc(CO)3-Nimotuzumab as a novel tumor-avid radiotracer for targeting in vivo EGFR expression.

  14. Gastrointestinal scintigraphy using sup(99m)Tc- or 111In-labelled polymer beads

    International Nuclear Information System (INIS)

    Jordaan, J.H.; Dormehl, I.C.; Pilloy, W.J.

    1984-01-01

    In order to establish normal and pathological stomach emptying characteristics by external measurement of a radioactive meal using a gamma camera and computer system, it is necessary for the radioactively labelled substance to have the same behaviour in the stomach as the ingested food. Resins containing chelating groups which enable binding to either reduced sup(99m)TcO 4 - or 111 In +3 were tested for their suitability as tracers mixed into solid food. The preparation of such styrene-divinyl-benzene resins containing either triethylenetetramine substituents or the fully carboxymethylated derivatives is discussed, as well as the procedures of labelling with either sup(99m)Tc-pertechnetate or 111 In-chloride. An evaluation of the resins for gastrointestinal scintigraphy was performed on 3 chacma baboons and a male human volunteer with encouraging results. (orig.) [de

  15. Development of a kit lyophilized of Anti-CEA to be labeled with Tc-99m, radionuclide obtained by extraction with MEK, complemented with studies of stability

    International Nuclear Information System (INIS)

    Robles Nique, Anita E.

    2006-01-01

    The colorectal cancer places the sixth place in Peru, more than 350 persons are diagnosed annually with this illness, for that reason, the present work contributes with the development of a lyophilized kit of monoclonal antibody Anti-CEA to be labelled by the radionuclide Tc-99m, for the early diagnosis of tumours embryonic adenocarcinoma. For the lack of a generator of adsorption of 99 Mo / 99m Tc in the country, the Tc-99m is used instead of this, coming from a generator of extraction, that use the methylethylketone (MEK) like solvent. First, it was designed systematically 4 lyophilized formulations and through the determination of the radiochemical purity of 99m Tc-Anti-CEA, the effect of the molar relation has been evaluated of the MoAb: 2-ME (1:1000 and 1:2000), the increasing of the reductor agent (3,50 to 5,95 μg SnF2) and the reduced protein (1,0 to 1,2 mg Anti-CEA). Second. On the base of the evaluation of the results of these 4 lyophilized formulations, 4 experimental lots have been prepared. The developed methodology initiates with the reduction of the protein for the direct method with 2-ME, the purification in column of PD10, then the addition of the SnF 2 and MDP, finally the lyophilization. Lyophilized kit is labeled by Tc-99m by the direct method to obtain 99m Tc-Anti-CEA and the radiochemical purity is determined by chromatography in ITLC-SG and HPLC, activity support and volume of Tc-99m, biological distribution in healthy mice, immunoreactivity is determined by chromatography of affinity, challenge with L-cysteine determined by chromatography in ITLC-SG. It complements itself with studies of stability in real-time for the lyophilized kit and for 99m Tc-Anti-CEA. The results of the first part, its 1st; 2nd; 3rd and 4th lyophilized formulation had a radiochemical purity of 71, 92, 94 and 97 % respectively, to a pH of labelled between 7,0 to 7,5. The results of the second part, 4 experimental lots had in average of radiochemical purity more than 95

  16. Confirmation of hydrazone formation in HYNIC-peptide conjugate preparation, and its hydrolysis during labeling with 99mTc

    International Nuclear Information System (INIS)

    Gandomkar, M.; Najafi, R.; Shafiei, M.; Ebrahimi, S.E.S.

    2007-01-01

    Because of its monodenticity, 6-hydrazinopyridine-3-carboxylic acid (HYNIC) is of interest as a bifunctional chelator for labeling peptide with 99m Tc. Here, we confirm the formation of hydrazone in HYNIC-conjugated peptide. The preparative HPLC was used to purify the HYNIC conjugated somatostatin-based peptide and the result showed two peaks, even after two consecutive purifications. Analysis of these peaks by mass spectrometry indicated the presence of hydrazone, produced during preparation conjugate. Further, we have shown that presence of hydrazone really does not matter because under 99m Tc-labeling conditions, hydrazone is hydrolyzed back to HYNIC that then chelates 99m Tc. A HYNIC-peptide conjugate freeze-dried kit was also prepared in a mildly acidic or neutral condition with a final pH of 6-7. The kit was then labeled by 99m Tc and incubated in 100 dec. C for 10 min, and a labeling yield of >95% was obtained

  17. Tc-99m Labeled Red Blood Cell by Ultra Tag RBC Kit in Patients Suspected of Gastrointestinal Bleeding

    International Nuclear Information System (INIS)

    Pusuwan, Pawana; Leaungwutiwong, Suraphong; Tocharoenchai, Chiraporn; Chaiwatanarat, Tawatchai; Sirisatipoch, Sasitorn; Rajadara, Samart; Naktong, Thanyada; Thanyarak, Sucheera

    2001-06-01

    Twenty patients suspected of gastrointestinal bleeding who underwent Tc-99m labeled red blood cell (RBC) by ultraTag RBC kit at Division of Nuclear Medicine, Bumrungrad Hospital between January 2000 and December 2002 were studied. The histories of patients together with either endoscopic results or angiographic findings or pathological reports were used as gold standards. Two by Two decision matrix was used for data analysis and the sensitivity together with specificity were calculated. The results show that the sensitivity and specificity of Tc-99m labeled RBC by ultraTag RBC kit are 87.5% and 91.7%, respectively. We conclude that Tc-99m labeled RBC by ultraTag RBC kit gives high percentages of sensitivity and specificity. Moreover, the image quality is improved because of the absence of free Tc-99m pertechnetate uptake in the stomach in all patients

  18. Synthesis, quality control and biodistribution of 99mTc-Kanamycin

    International Nuclear Information System (INIS)

    Roohi, S.; Mushtaq, A.; Jehangir, M.; Malik, S.A.

    2006-01-01

    Kanamycin is an antibiotic used for treatment of infections when penicillin or other less toxic drugs cannot be used. Kanamycin was labeled with technetium-99m pertechnetate using SnCl 2 x 2H 2 O as reducing agent. The labeling efficiency depends on the ligand/reductant ratio, pH, and volume of reaction mixture. Radiochemical purity and stability of 99m Tc-Kanamycin was determined by thin layer chromatography. Biodistribution studies of 99m Tc-Kanamycin were performed in rats and rabbits. A significantly higher accumulation of 99m Tc-Kanamycin was seen at sites of S. aureus infected animals (rat/rabbit). (author)

  19. Labeling of creatinine with technetium-99m

    Energy Technology Data Exchange (ETDEWEB)

    Yurt Lambrecht, F. [Ege Univ., Bornova, Izmir (Turkey). Dept. of Nuclear Applications, Inst. of Nuclear Sciences; Durkan, K. [Dokuz Eylul Univ., Buca, Izmir (Turkey). Chemistry Technicianship Program, Izmir Vocational School; Soylu, A. [Dokuz Eylul Univ., Narlidere, Izmir (Turkey). Dept. of Pediatrics, Medical Faculty

    2004-07-01

    Creatinine is a clinically important index of renal glomerular filtration rate. Urine creatinine levels can be used as a screening test to evaluate kidney function or can be part of the creatinine clearance test. In case of kidney dysfunction or muscle disorders the creatinine concentration in serum/plasma may rise to a higher value than in healthy body. Technetium- 99m has been used in nuclear medicine and in biomedical research to label molecular and cellular structures employed as radiotracers. {sup 99m}Tc is utilized to label molecules and cells, used as radiopharmaceuticals, and also to label biological species. It presents many desirable characteristics. SnCl{sub 2} method is frequently used as a reducing agent in the {sup 99m}Tc- labeling process. Creatinine metabolism might be investigated by using labeled {sup 99m}Tc- creatinine in healthy or uremic rats. (orig.)

  20. Evaluation of fresh and old eluate of 99Mo/99mTc generators used for labeling of different pharmaceutical kits

    International Nuclear Information System (INIS)

    Urbano, N.; Chinol, M.; Modoni, S.; Guerra, M.

    2005-01-01

    Sixty 99 Mo/ 99m Tc wet column generators, loaded with two different 99 Mo activities, were analyzed in order to assess the quality of their eluates. Each elution was used for labeling of different radiopharmaceuticals, in order to evaluate whether 'risky' elutions, namely those performed just after generator delivery and at 72 hours or more from the last elution, could be conveniently employed when fresh available radioactivity is not enough for the planned labeling or when shipping problems arise, or delay in delivery of a new generator occurs. Radiochemical quality control of all radiopharmaceuticals labeled with these elutions was performed. The elutions differed mainly in 99 Tc ground state ( 99g Tc) and amounts of oxidizing impurities. Radiolabeling procedures, however, were not affected, suggesting that these 'risky' elutions might be appropriately used, in 'emergency' conditions, for labeling radiopharmaceuticals although their radiochemical purity control is recommended prior to patient administration. (author)

  1. Mismatched uptake of Tc-99m-ECD and Tc-99m-HMPAO in subacute cerebral infarction: Tc-99m-ECD for viability and Tc-99m-HMPAO for flow restoration

    Energy Technology Data Exchange (ETDEWEB)

    Lee, D. S.; Hyun, I. Y.; Kim, S. K. [College of Medicine, Seoul National Univ., Seoul (Korea, Republic of)] [and others

    1997-07-01

    Tc-99m-HMPAO reflects tissue perfusion but Tc-99m-ECD uptake is affected by tissue viability in addition to tissue perfusion which the varied state of cellular retention of Tc-99m-ECD reflects. Luxuriously perfused area on Tc-99m-HMPAO SPECT implies that this cortex was already reperfused either spontaneously or after thrombolysis and that accompanied paralysis of vascular reactivity in those zones warms progressive deterioration. We tried to find out if we can use sequential Tc-99m-ECD/Tc-99m-HMPAO SPECT to reveal cortical perfusion and severity and range of risky areas of cerbral cortex despite reperfusion in sub-acute infarction. In 13 patients (M ; F =7 : 6, mean age 57 (range: 26-84)) with cortical (n=12) and basal ganglia infarction (1), we performed sequential Tc-99m-ECD/Tc-99m-HMPAO SPECT at the same position. At first, 555 MBq of Tc-99m-ECD was injected and imaged and then 1110 MBq of Tc-99m-HMPAO was injected again and imaged with the patients in situ, and the first image (Tc-99m-ECD) and the subtracted image (2nd- 1st : Tc-99m-HMPAO) were compared slice by slice. Study was done from 3 days to 31 days (16{+-}9) after ictus. Tc-99m-ECD uptake was always less than or equal to Tc-99m-HMPAO uptake at the lesion in all cases. Luxury perfusion was prominent in four patients. Mismatched uptake was found in 10 patients. Severity of mismatch showed diverse spectrum and was ranged from total middle cerebral artery territory (1 case) to peripheral thin zones around infarction (2 cases). The other 7 showed intermediate amount of tissues with mismatch , i.e., Tc-99m-ECD defects where Tc-99m-HMPAO uptake is in part increased, normal or decreased. Upon discharge, patients having more uptake with Tc-99m-ECD predicted improvement. Patients having mismatched uptake went dichotomous way. In conclusion, Tc-99m-ECD/Tc-99m-HMPAO sequential SPECT is feasible and reveal both tissue perfusion (Tc-99m-HMPAO ) and discrepant Tc-99m-ECD uptake probably reflecting viability in acute

  2. Synthesis and evaluation of novel Tc-99m labeled NGR-containing hexapeptides as tumor imaging agents.

    Science.gov (United States)

    Kim, Dae-Weung; Kim, Woo Hyoung; Kim, Myoung Hyoun; Kim, Chang Guhn

    2015-02-01

    Asparagine-glycine-arginine (NGR)-containing peptides targeting aminopeptidase N (APN)/CD13 can be an excellent candidate for targeting ligands in molecular tumor imaging. In this study, we developed two NGR-containing hexapeptides, and evaluated the diagnostic performance of Tc-99m labeled hexapeptides as molecular imaging agents in an HT-1080 fibrosarcoma-bearing murine model. Peptides were synthesized using Fmoc solid-phase peptide synthesis. Radiochemical purity of Tc-99m was evaluated using instant thin-layer chromatography. The uptake of two NGR-containing hexapeptides within HT-1080 cells was evaluated in vitro. In HT-1080 fibrosarcoma tumor-bearing mice, gamma images were acquired. A biodistribution study was performed to calculate percentage of the injected dose per gram of tissue (%ID/g). Two hexapeptides, glutamic acid-cysteine-glycine (ECG)-NGR and NGR-ECG were successfully synthesized. After radiolabeling procedures with Tc-99m, the complexes Tc-99m hexapeptides were prepared in high yield. The uptake of Tc-99m ECG-NGR within the tumor cells had been assured by in vitro studies. The gamma camera imaging in the murine model showed that Tc-99m ECG-NGR was accumulated substantially in the subcutaneously engrafted tumor. However, Tc-99m NGR-ECG was accumulated minimally in the tumor. Two NGR-containing hexapeptides, ECG-NGR and NGR-ECG were developed as molecular imaging agents to target APN/CD13 in HT-1080 fibrosarcoma. Tc-99m ECG-NGR showed a significant uptake in the tumor, and it is a good candidate for tumor imaging. Copyright © 2015 John Wiley & Sons, Ltd.

  3. 99 mTc-sulphur-colloid and heat-denatured 99mTc-labelled red cell scans demonstrating a giant intrapelvic spleen in a girl after splenectomy

    International Nuclear Information System (INIS)

    Kao, P.F.; Tzen, K.Y.; Tsai, M.F.; Lin, J.N.

    2001-01-01

    A 17 x 12 x 5-cm giant intrapelvic mass in a 14-year-old girl is reported. This mass developed 6 years after a splenectomy for splenic torsion. The heat-denatured 99 m Tc-labelled red cell scan and 99 m Tc- sulphur-colloid scan confirmed the specific red cell sequestration function and reticuloendothelial activity in the giant intrapelvic spleen. The size and development of the giant intrapelvic spleen are unusual. The usefulness of functional images to diagnosis the nature of the intrapelvic mass is well demonstrated. (orig.)

  4. Labeling of unnatural amino acids with sup(99m)Tc and tissue distribution of the labeled products in mice

    International Nuclear Information System (INIS)

    Tamemasa, Osamu; Goto, Rensuke; Takeda, Atsushi

    1981-01-01

    The selective affinity of amino acids for pancreas, due to its high rate of protein synthesis, has prompted us to synthesize new radio-labeled amino acids for pancreatic imaging. Labeling of 19 unnatural amino acids with sup(99m)Tc was tried in the usual way, and 10 labeled products were obtained with low yields. The highest distribution of radioactivity from all these labeled amino acids, which had been injected intravenously into mice, was found in the kidney, whereas little activity was found in the pancreas. Their low distributions in stomach suggest little dissociation of the labeled amino acids into sup(99m)TcO 4 - in mice. It is presumed that these labeled amino acids behave unlike their original amino acids in the body. (author)

  5. Neutral and stereospecific Tc-99m complexes: [99mTc]N-benzyl-3,4-di-(N-2-mercaptoethyl)-amino-pyrrolidines (P-BAT)

    International Nuclear Information System (INIS)

    Zhuang Zhiping; Ploessl, Karl; Kung Meiping; Mu Mu; Kung, Hank F.

    1999-01-01

    Technetium-99m-labeled radiopharmaceuticals are currently the most commonly used agents in nuclear medicine. To prepare binding site-specific small molecules containing a Tc-99m complexing core, it is important to consider a ligand system, which selectively forms only one stereoisomer. A novel series of bisaminoethanethiol (BAT) derivatives as a model system were prepared. Stereoisomers of N-benzyl-3,4-di-(N-2-mercaptoethyl)-amino pyrrolidines (P-BAT): (3R,4R)-P-BAT (R,R-4) and (3,4)meso-P-BAT (8), the trans and meso isomer, respectively, as a chelating group were prepared successfully. The desired Tc-99m P-BAT complexes were obtained by using Sn(II)/glucoheptonate as the reducing agent for [ 99m Tc]pertechnetate. As predicted, after complexation with [ 99m Tc]Tc v O, the trans isomer, (3R,4R)-P-BAT (R,R-4), showed only one isomer; whereas the corresponding meso isomer, (3,4)meso-P-BAT (8), produced two distinctive complexes isolated readily by high performance liquid chromatography (HPLC). The [ 99m Tc](R,S)meso-P-BAT (8) isomers showed a different lipophilicity (partition coefficient [P.C.]=54.3 and 55.4 for peak A and peak B, respectively), as compared with that of the corresponding [ 99m Tc](3R,4R)-P-BAT (R,R-4), trans isomer ( P.C.=163). Results of the biodistribution study in rats of these isomers show different heart and brain uptake, suggesting that the intrinsic differences in biodistribution are due to structural and stereospecific factors. Examples in this report confirm that it is possible to design stereospecific Tc-99m complexes based on the bisaminoethanethiol (N 2 S 2 , BAT) ligand system. Consideration on stereoselectivity of site-specific agents labeled with Tc-99m is likely an essential requirement on developing binding-site specific radiopharmaceuticals

  6. In vitro assessment of Tc-99m labeled bovine thrombin and streptokinase-activated human plasmin: concise communication. [Iodine 125

    Energy Technology Data Exchange (ETDEWEB)

    Wong, D.W.; Tanaka, T.; Mishkin, F.; Lee, T.

    1979-09-01

    Bovine thrombin and streptokinase-activated human plasmin have been labeled with Tc-99m using stannous reduction of pertechnetate under physiological conditions (pH 7.4). The binding efficiency of radiotechnetium to these enzymes is greater than 94%, with less than 5% of reduced but unbound Tc-99m (Sn) complex as assayed by ascending paper radiochromatography using ITLC silica gel plate. Free or unbound pertechnetate is less than 1%. In vitro enzymatic analyses of the Tc-99m-labeled enzymes demonstrate no evidence of protein denaturation or significant loss of enzymatic activity after labeling. Both labeled enzymes are biochemically active in vitro with their respective substrates.

  7. Production of the antimicrobial peptide UBI 29-41 labelled with 99mTc by an indirect method

    International Nuclear Information System (INIS)

    Nevares, Noemi; Crudo, Jose L.; Zapata, Miguel; Castiglia, Silvia G. de

    2003-01-01

    The infection processes are a major problem in human health causing a high number of human deaths all around the world. Diagnostic imaging in nuclear medicine is an attractive option in the detection of infection processes due to its sensitivity. The antimicrobial peptides are very important in the development of new radiopharmaceuticals, since their antimicrobial activity towards a great variety of microorganisms have been proven. The aim of this work was to obtain the antimicrobial peptide UBI 29-41 labelled with technetium 99 m, by an indirect method via NHS-Hynic and tricine as a coligand, and evaluate its stability and its ability to discriminate between infection and inflammation sites. The radiochemical purity of the labeling procedure was 95.5±1,2 %. The cysteine challenge showed a great stability of the 99mTc UBI-Hynic, and the stability in human serum showed that the 81% of the radioactivity remained bounded to UBI-Hynic at 48 hs of incubation. The bio distribution's studies showed main elimination via kidney of 99mTc UBI-Hynic and the target/non target ratio was 1,81 for infected mice and 1,16 for inflamed mice. (author)

  8. Radiolabeling of rituximab with 188Re and 99mTc using the tricarbonyl technology

    International Nuclear Information System (INIS)

    Dias, Carla Roberta; Jeger, Simone; Osso, Joao Alberto; Mueller, Cristina; De Pasquale, Christine; Hohn, Alexander; Waibel, Robert; Schibli, Roger

    2011-01-01

    Introduction: The most successful clinical studies of immunotherapy in patients with non-Hodgkin's lymphoma (NHL) use the antibody rituximab (RTX) targeting CD20 + B-cell tumors. Rituximab radiolabeled with β - emitters could potentiate the therapeutic efficacy of the antibody by virtue of the particle radiation. Here, we report on a direct radiolabeling approach of rituximab with the 99m Tc- and 188 Re-tricarbonyl core (IsoLink technology). Methods: The native format of the antibody (RTX wt ) as well as a reduced form (RTX red ) was labeled with 99m Tc/ 188 Re(CO) 3 . The partial reduction of the disulfide bonds to produce free sulfhydryl groups (-SH) was achieved with 2-mercaptoethanol. Radiolabeling efficiency, in vitro human plasma stability as well as transchelation toward cysteine and histidine was investigated. The immunoreactivity and binding affinity were determined on Ramos and/or Raji cells expressing CD20. Biodistribution was performed in mice bearing subcutaneous Ramos lymphoma xenografts. Results: The radiolabeling efficiency and kinetics of RTX red were superior to that of RTX wt ( 99m Tc: 98% after 3 h for RTX red vs. 70% after 24 h for RTX wt ). 99m Tc(CO) 3 -RTX red was used without purification for in vitro and in vivo studies whereas 188 Re(CO) 3 -RTX red was purified to eliminate free 188 Re-precursor. Both radioimmunoconjugates were stable in human plasma for 24 h at 37 o C. In contrast, displacement experiments with excess cysteine/histidine showed significant transchelation in the case of 99m Tc(CO) 3 -RTX red but not with pre-purified 188 Re(CO) 3 -RTX red . Both conjugates revealed high binding affinity to the CD20 antigen (K d =5-6 nM). Tumor uptake of 188 Re(CO) 3 -RTX red was 2.5 %ID/g and 0.8 %ID/g for 99m Tc(CO) 3 -RTX red 48 h after injection. The values for other organs and tissues were similar for both compounds, for example the tumor-to-blood and tumor-to-liver ratios were 0.4 and 0.3 for 99m Tc(CO) 3 -RTX red and for 188 Re

  9. Labelling of Klebsiella pneumoniae with technetium-99m: a preliminary communication

    International Nuclear Information System (INIS)

    Bernardo Filho, M.; Pereira, J.A.A.; Boasquevisque, E.M.

    1986-01-01

    The labeling of Klebsiella pneumoniae with technetium-99m (Tc-99m) seems to depend on the stannous ion (Sn ++ ) concentration. Starting at 3μg/ml of this ion is the suspension fluid an uptake of Tc-99m close to 90% was observed. The labeling is apparently strong, since the eluation of Tc-99m, after incubation of the tagged culture, in a water-bath at 37 0 C for several hours, was very weak. The viability of the culture was unaltered after treatment with tin and Tc-99m. (Author) [pt

  10. Synthesis of Ethane-1-Hydroxy-1,1-diphosphonic acid (EHDP) and preparation of labeled kits by 99mTc for bone studies

    International Nuclear Information System (INIS)

    Yassin, T.; Assaad, T.; Ghanem, E.; Ajaia, R.; Karajoli, N.

    2013-08-01

    Ethane-1-Hydroxy-1,1-diphosphonic acid monohydrate (EHDP) is very important precursor in radiopharmaceutical applications for bone diagnosis after labeling with 99mTc, was synthesized in high yield and purity. The compound was characterized by spectroscopic method. EHDP kit for bone imaging after labeling with technetium 99m was prepared according to an optimum conditions, Each vial contains 15 mg of EHDP and 25 mg of stannous chloride SnCl2. The prepared kit showed high quality satisfying the requirements of international pharmacopeias from of physical, chemical and radiochemical properties. The labeling yield exceeded 95% with an average value 99.6%. Biodistribution study of 99mTc-EHDP showed better clearance after three hours of injection in comparison with 99mTc-MDP kit (author).

  11. Development of Tc99m-Saccharic Acid for Heart Imaging

    International Nuclear Information System (INIS)

    Shafii Khamis; Mohd Azfar Adenan; Bohari Yaacob; Amir Fitri Shafii

    2014-01-01

    Cardiovascular disease especially the coronary heart disease (CHD) is the leading cause of death worldwide. Coronary heart disease is a common term for the buildup of plaque in the heart coronary arteries that could block the blood supply to the myocardial and this could lead to heart attack. An estimated 17 million people died from cardiovascular disease in 2008 representing 30% of all global death. In United Kingdom, coronary heart disease killed as much as 82,000 people each year. Hence, early detection of the coronary heart disease is very important in reducing the mortality among the world population. One of the most sensitive detection methods is by radioimaging using Technetium-99m radiopharmaceuticals. Several different radio imaging agents such as Tc99m radiopharmaceutical were developed as radiagnostic agent in determining the CHD especially in identifying the blockage of the coronary artery of the heart muscle. Despite the success of Tc99m-sestamibi and Tc99m-tetrofosmin as effective agents for myocardial perfusion study, the search for other Tc99m heart imaging agents has never been interrupted. This report described the formulation of the Tc99m-saccharic acid radiopharmaceutical kit, radiolabelling of the kit, radiochemical purity evaluation of the Tc99m labeled saccharaic acid, and animal study involving radio imaging using gamma camera. The animal are then sacrificed and the biological distribution of the Tc99m-saccharic acid in-vivo was determined. Comparative study was also conducted using commercially available Tc99m-tetrafosmin, a CHD radiopharmaceutical kit. The Tc99m-saccharic acid developed gave a very high labeling efficiency of >92% with Tc99m and good uptake in the heart muscle. The saccharic acid kit developed was also found to be comparable in quality to the commercially available Tc99-tetrafosmin kit. (author)

  12. Development of a formulation lyophilized for the obtention of a antimicrobial peptide Ubiquicidine labelled with 99m Tc

    International Nuclear Information System (INIS)

    Palomares R, P.; Hernandez B, C.A.; Contreras N, G.; Garcia P, M.L.; Pantoja H, I.E.; Ferro F, G.

    2004-01-01

    The 99m Tc-UBI 29-41 are a labelled fragment of the antimicrobial human peptide Ubiquicidine proposed as a new radiopharmaceutical able to differentiate an infectious process of an inflammatory one through the gamma graphic image. It has been demonstrated that the 99m Tc-UBI 29-41 unite to bacteria in vitro and that accumulates in infection sites in human with minimum captivation in inflammation sites. In this work the development of a pharmaceutical lyophilized formulation is presented for the instantaneous marked one of the UBI 29-41 with 99m Tc. The selection of the components of the formulation settled down by means of the employment of an experimental design of 3 factors with mixed levels, evaluating the effect of the diluent type, concentration of tinny chloride and the reaction volume. The obtained formulations showed to be stable until for 6 months, being obtained complexes of the radiolabelled peptide with radiochemical purity > 95 % in sterile form and apirogen. The developed pharmaceutical form, will facilitate the routinary use of this new radiopharmaceutical in the diverse hospital departments of nuclear medicine. (Author)

  13. Development of lyophilized kit of Tin-Glucoheptonate for in vitro labeling of leucocytes with 99mTc

    International Nuclear Information System (INIS)

    Nascimento, Rosemeire Fagundes

    2007-01-01

    The study and localization of inflammatory and infection process in Nuclear Medicine represents a relevant tool in diagnostic procedures. In same cases, the diagnostic is easy and based on anamnesis and clinical observation; in other cases, the patients are asymptomatic or present non specific symptoms that difficult the diagnostic. The early diagnostic of inflammatory or infectious process allow the early introduction of therapy and prevents complications. Farther, the differentiation between inflammation and infection is of extreme importance as well as the localization of the focus. The use of labeled leucocytes, studied and applied in much pathologies, is the method of choice for the visualization of inflammation and infection. The scintigraphy using labeled leucocytes was introduced at 1976 by McAffe and Thakur and since of this is used in the diagnostic of different pathologies related to leucocyte infiltration like intestinal inflammatory disease, bone or prosthetic-vascular infections. The in vitro labeling of leucocytes with 111 In was performed using oxime or tropolone as ligand and with 99m Tc using hexamethylpropylene amine oxime (HMPAO) as ligand, resulting in a lipophilic complex. The 99m Tc-HMPAG complex was preferably employed in many indications and countries do to the ideal physical properties of 99m Tc that results in low dose to the patient. However, the labeling employing the HMPAO complex results in some disadvantages like the low stability of the complex, and some requirements related to the 99m Tc elution (like the time pos elution), beyond the high cost of the compound that is imported. The aim of this work was the development of a tin-glucoheptonate lyophilized kit for in vitro leucocytes labeling with 99m Tc using the pre-stannization method. The optimization of the labeling technique was developed using leucocytes isolated from total blood and employing different volumes of the tinglucoheptonate reagent and different incubation times at

  14. In vivo crossmatching with Tc-99m-RBC's and In-111-oxine-RBC's

    International Nuclear Information System (INIS)

    Marcus, C.S.; Myhre, B.A.; Angulo, M.C.; Salk, R.D.; Essex, C.E.

    1984-01-01

    In vitro crossmatching techniques are often inadequate for patients who have received multiple prior transfusions. These patients usually have multiple antibodies to minor blood groups, not all of which are necessarily important to vivo. It becomes increasingly difficult to obtain appropriate units for transfusion, and often units are used with hopes that a minor group antibody will not be significantly active in vivo. If a transfusion reaction occurs, the unit is stopped. The authors have developed and successfully tested a method whereby 1.5 to 3c of potential donor RBC's are labeled with 25-50 μCi of Tc-99m using the BNL kits. After injection, samples are drawn at 10, 20, 60, and 120 minutes and the RBC survival is measured. If it is desirable to test 2 units simultaneously, the authors use 400 μCi Tc-99m to label an RBC aliquot of one unit and 25 μCi In-111-oxine to label the other; both labeled aliquots are injected together. The method is simple and reliable. In addition to assessing compatibility, the authors may also estimate the % viability of transfused, compatible RBC's by starting with 400 μCi of Tc-99m and multiplying % survival at 24 hours by 1.2. For 24 hr. survival measurements of IN-111-oxine-RBC's, 25 μCi is adequate and no multiplication factor is necessary. The authors have performed 13 in vivo crossmatches, 4 of which were double, in 6 patients. One documented mild transfusion reaction occurred. There were no false positive or false negative results

  15. Labelling and biodistribution of /sup 99m/Tc-ceftriaxone: a new imaging agent

    International Nuclear Information System (INIS)

    Khurshid, Z.; Roohi, S.; Zahoor, R.; Tariq, S.

    2012-01-01

    Most commonly used infection imaging agents are specific for inflammation. Some newer agents like labeled antimicrobials and peptides have shown infection seeking properties. Research is underway for synthesis of newer imaging agents specific for infections. In this quest we have labeled and bio evaluated /sup 99m/Tc-ceftriaxone. Ceftriaxone is a commonly used third generation cephalosporin antibiotic having a broad anti-bacterial spectrum but has more specificity for gram-negative bacteria. /sup 99m/Tc-ceftriaxone was prepared at ph 7 by adding 30 mg of ligand to /sup 99m/Tc in the presence of 50 mu g of SnCl/sub 2/./sup 2/H/sub 2/O. Boiling for ten minutes gave maximum labeling yield (96+1.76%). The stability at room temperature both with and without human serum was more than 90% till 24 hours. In-vitro binding revealed maximum binding of 68% and 47% with E.coli and S.aureus respectively after 4 hours incubation. Biodistribution studies in normal rats showed maximum uptake in hepatobiliary system followed by kidney. In infection and inflammation models the maximum target to non- target ratios of 12.66 +- 2.59, 2.36 +- 0.30 and 1.44 +- 0.53 were achieved with E. coli, S. aureus and oil inflammation respectively 4 hours post injection. Scintigraphic findings also correlated with biodistribution results. (Orig./A.B.)

  16. Confirmation of hydrazone formation in HYNIC-peptide conjugate preparation, and its hydrolysis during labeling with {sup 99m}Tc

    Energy Technology Data Exchange (ETDEWEB)

    Gandomkar, M. [Radioisotope Division, Nuclear Research Center, Atomic Energy Organization of Iran (AEOI), Tehran (Iran, Islamic Republic of)]. E-mail: msgandomkar@yahoo.com; Najafi, R. [Radioisotope Division, Nuclear Research Center, Atomic Energy Organization of Iran (AEOI), Tehran (Iran, Islamic Republic of); Shafiei, M. [Radioisotope Division, Nuclear Research Center, Atomic Energy Organization of Iran (AEOI), Tehran (Iran, Islamic Republic of); Ebrahimi, S.E.S. [Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran (Iran, Islamic Republic of)

    2007-07-15

    Because of its monodenticity, 6-hydrazinopyridine-3-carboxylic acid (HYNIC) is of interest as a bifunctional chelator for labeling peptide with {sup 99m}Tc. Here, we confirm the formation of hydrazone in HYNIC-conjugated peptide. The preparative HPLC was used to purify the HYNIC conjugated somatostatin-based peptide and the result showed two peaks, even after two consecutive purifications. Analysis of these peaks by mass spectrometry indicated the presence of hydrazone, produced during preparation conjugate. Further, we have shown that presence of hydrazone really does not matter because under {sup 99m}Tc-labeling conditions, hydrazone is hydrolyzed back to HYNIC that then chelates {sup 99m}Tc. A HYNIC-peptide conjugate freeze-dried kit was also prepared in a mildly acidic or neutral condition with a final pH of 6-7. The kit was then labeled by {sup 99m}Tc and incubated in 100 dec. C for 10 min, and a labeling yield of >95% was obtained.

  17. Introduction of an 8-aminooctanoic acid linker enhances uptake of 99mTc-labeled lactam bridge-cyclized α-MSH peptide in melanoma.

    Science.gov (United States)

    Guo, Haixun; Miao, Yubin

    2014-12-01

    The purpose of this study was to examine the effects of amino acid, hydrocarbon, and polyethylene glycol (PEG) linkers on the melanoma targeting and imaging properties of (99m)Tc-labeled lactam bridge-cyclized HYNIC-linker-Nle-CycMSHhex (hydrazinonicotinamide-linker-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-CONH2) peptides. Four novel peptides (HYNIC-GGGNle-CycMSHhex, HYNIC-GSGNle-CycMSHhex, HYNIC-PEG2Nle-CycMSHhex, and HYNIC-AocNle-CycMSHhex) were designed and synthesized. The melanocortin-1 receptor binding affinities of the peptides were determined in B16/F1 melanoma cells. The biodistribution of (99m)Tc(ethylenediaminediacetic acid [EDDA])-HYNIC-GGGNle-CycMSHhex, (99m)Tc(EDDA)-HYNIC-GSGNle-CycMSHhex, (99m)Tc(EDDA)-HYNIC-PEG2Nle-CycMSHhex, and (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex were determined in B16/F1 melanoma-bearing C57 mice at 2 h after injection to select a lead peptide for further evaluation. The melanoma targeting and imaging properties of (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex were further examined because of its high melanoma uptake. The inhibitory concentrations of 50% (IC50) for HYNIC-GGGNle-CycMSHhex, HYNIC-GSGNle-CycMSHhex, HYNIC-PEG2Nle-CycMSHhex, and HYNIC-AocNle-CycMSHhex were 0.7 ± 0.1, 0.8 ± 0.09, 0.4 ± 0.08, and 0.3 ± 0.06 nM, respectively, in B16/F1 melanoma cells. Among these four (99m)Tc-labeled peptides, (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex displayed the highest melanoma uptake (22.3 ± 1.72 percentage injected dose/g) at 2 h after injection. (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex exhibited high tumor-to-normal-organ uptake ratios except for the kidneys. The tumor-to-kidney uptake ratios of (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex were 3.29, 3.63, and 6.78 at 2, 4, and 24 h, respectively, after injection. The melanoma lesions were clearly visualized by SPECT/CT using (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex as an imaging probe at 2 h after injection. High melanoma uptake and fast urinary clearance of (99m)Tc(EDDA)-HYNIC-AocNle-CycMSHhex highlighted its

  18. Introduction of an 8-Aminooctanoic Acid Linker Enhances the melanoma uptake of Tc-99m-labeled Lactam Bridge-Cyclized Alpha-MSH Peptide

    Science.gov (United States)

    Guo, Haixun; Miao, Yubin

    2015-01-01

    The purpose of this study was to examine the effects of amino acid, hydrocarbon and polyethylene glycol (PEG) linkers on melanoma targeting and imaging properties of 99mTc-labeled lactam bridge-cyclized HYNIC-linker-Nle-CycMSHhex {hydrazinonicotinamide-linker-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-CONH2} peptides. Methods four novel peptides {HYNIC-GGGNle-CycMSHhex, HYNIC-GSGNle-CycMSHhex, HYNIC-PEG2Nle-CycMSHhex and HYNIC-AocNle-CycMSHhex} were designed and synthesized. The melanocortin-1 (MC1) receptor binding affinities of the peptides were determined in B16/F1 melanoma cells. The biodistribution of 99mTc(EDDA)-HYNIC-GGGNle-CycMSHhex, 99mTc(EDDA)-HYNIC-GSGNle-CycMSHhex, 99mTc(EDDA)-HYNIC-PEG2Nle-CycMSHhex and 99mTc(EDDA)-HYNIC-AocNle-CycMSHhex were determined in B16/F1 melanoma-bearing C57 mice at 2 h post-injection to select a lead peptide for further evaluation. The melanoma targeting and imaging properties of 99mTc(EDDA)-HYNIC-AocNle-CycMSHhex were further examined because of its high melanoma uptake. Results The IC50 values of HYNIC-GGGNle-CycMSHhex, HYNIC-GSGNle-CycMSHhex, HYNIC-PEG2Nle-CycMSHhex, and HYNIC-AocNle-CycMSHhex were 0.7 ± 0.1, 0.8 ± 0.09, 0.4 ± 0.08, and 0.3 ± 0.06 nM in B16/F1 melanoma cells, respectively. Among these four 99mTc-labeled peptides, 99mTc(EDDA)-HYNIC-AocNle-CycMSHhex displayed the highest melanoma uptake (22.3 ± 1.72% ID/g) at 2 h post-injection. 99mTc(EDDA)-HYNIC-AocNle-CycMSHhex exhibited high tumor to normal organ uptake ratios except for the kidneys. The tumor/kidney uptake ratios of 99mTc(EDDA)-HYNIC-AocNle-CycMSHhex were 3.29, 3.63 and 6.78 at 2, 4 and 24 h post-injection. The melanoma lesions were clearly visualized by single photon emission computed tomography (SPECT)/CT using 99mTc(EDDA)-HYNIC-AocNle-CycMSHhex as an imaging probe at 2 h post-injection. Conclusion High melanoma uptake and fast urinary clearance of 99mTc(EDDA)-HYNIC-AocNle-CycMSHhex highlighted its potential for metastatic melanoma detection in the future

  19. Efficient preparation of {sup 99m}Tc(III) '4+1' mixed-ligand complexes for peptide labeling with high specific activity

    Energy Technology Data Exchange (ETDEWEB)

    Kunstler, Jens-Uwe [Biotectid GmbH, Deutscher Platz 5c, 04103 Leipzig (Germany); Seidel, Gesine [Institute of Radiopharmacy, Forschungszentrum Dresden-Rossendorf, P.O. Box 510 119, 01314 Dresden (Germany); Pietzsch, Hans-Jurgen, E-mail: h.j.pietzsch@fzd.d [Institute of Radiopharmacy, Forschungszentrum Dresden-Rossendorf, P.O. Box 510 119, 01314 Dresden (Germany)

    2010-09-15

    An improved labeling procedure for peptides attached to organometallic {sup 99m}Tc(III) '4+1' mixed-ligand complexes in which the radiometal is coordinated by a tripodal tetradentate chelator 2,2',2''-nitrilotriethanethiol (NS{sub 3}) and a monodentate isocyanide ligand is presented. The labeling procedure was evaluated by the synthesis of [{sup 99m}Tc(NS{sub 3})(L2-RGD)]. The containing radiopharmaceutically interesting RGD-peptide cyclo[Arg-Gly-Asp-D-Tyr-Lys] was modified with 4-isocyanobutanoic acid (L2) as linker conjugated to N{sup 6}-Lys to get the monodentate ligand L2-RGD. The structural identity of the {sup 99m}Tc-conjugate was confirmed by comparison to a Re reference compound. The Tc- and Re-conjugates had matching retention times under identical HPLC conditions. The {sup 99m}Tc-labeling was performed in a novel one-step procedure using the eluate of a {sup 99}Mo/{sup 99m}Tc generator, NS{sub 3}, the isocyanide modified peptide, SnCl{sub 2}, Na{sub 2}EDTA, mannitol and ascorbic acid in the reaction mixture. Using optimized reagents it is possible to label 50 nmol peptide with {sup 99m}Tc within 60 min at room temperature with a radiochemical yield higher than 95% and a specific activity of {approx}20 GBq/{mu}mol.

  20. 99mTc-tetrapeptides: radiolabelling and biodistribution in rats

    International Nuclear Information System (INIS)

    Laznickova, A.; Laznicek, M.; Trejtnar, F.; Mather, S.J.

    1998-01-01

    Preparation of 99m Tc-labelled tetrapeptides, namely acetyl-Gly-Gly-Cys-Gly (I), acetyl-Ser-Ser-Cys-Gly (II) and acetyl-Gly-Gly-Cys-Lys (III), analysis of their radiochemical purity and biodistribution were investigated in rats. The aim was to determine the relationship between structure and biological behaviour of 99m Tc-labelled peptides which are formed by amino-acid sequences capable of chelating technetium useful as universal chelators in ''hybrid'' peptides composed of receptor-specific part and the part chelating technetium. For labelling with 99m Tc, a conventional transchelation from 99m Tc-gluconate was used and radiolabelled peptides were purified by filtration on Whatman microfilters 12 kD. Radiochemical purity was higher than 98%. Biodistribution studies in rats showed that all agents are rapidly cleared from the body mostly via urine, but some part of administered radioactivity also in the faces was found. The later route of elimination way increased in the order III 99m Tc-MAG3. The results obtained will assist with design of optimal biocompatible tetrapeptides as chelators for formation of hybrid receptor-specific peptides. (author)

  1. Influence of bilirubin on the distribution of 99mTc-HIDA and 99mTc-IODIDA in rats and their interaction with HSA

    International Nuclear Information System (INIS)

    Jovanovic, M.S.; Zmbova, B.; Zivanov-Stakic, D.; Vladimirov, S.

    1993-01-01

    The interaction of bilirubin and 99m Tc-HIDA and 99m Tc-IODIDA has been studied in rats. The mechanism of this interaction has been examined at the level of binding with human serum albumin (HSA) by the in vitro method. Percentage of binding with HSA, and affinity constants for 99m Tc-IODIDA were determined with and without bilirubin. Bilirubin was labeled with 99m Tc and its interaction with HSA was also examined. (author) 8 refs.; 2 figs.; 4 tabs

  2. Tc 99m - scorpion venom: labelling, biodistribution and scintiimaging

    International Nuclear Information System (INIS)

    Murugesan, S.; Noronha, O.P.D.; Samuel, A.M.; Murthy, K. Radha Krishna

    1999-01-01

    Labelling of scorpion (Mesobuthus tamulus concanesis Pocock) venom was successfully achieved with Tc 99m using direct tin reduction procedure. Biodistribution studies were carried out in Wistar rats at different time intervals after i.v. administration of the labelled venom. Scintiimages were obtained after scorpion envenoming using a large field of view gamma camera to ascertain the pharmacological action of venom in the body. Within 5 min of administration, labelled venom was found in the blood (27.7%), muscle (30.11%), bone (13.3%), kidneys (11.5%), liver (10.4%) and other organs. The level of venom in the kidneys was higher than in the liver. The labelled venom was excreted through renal and hepatobiliary pathways. An immunoreactivity study was carried out in rabbits after i.v. injection of labelled scorpion venom followed by the injection of the species specific antivenom. A threefold increase in uptake by the kidneys ss was observed compared with that seen with scorpion venom alone. the neutralisation of the venom in the kidneys was higher than in the liver. (author)

  3. 99mTc renal tubular function agents: Current status

    International Nuclear Information System (INIS)

    Eshima, D.; Fritzberg, A.R.; Taylor, A. Jr.

    1990-01-01

    Orthoiodohippuric (OIH) acid labeled with 131I is a widely used renal radiopharmaceutical agent and has been the standard radiopharmaceutical agent for the measurement of effective renal plasma flow (EPRF). Limitations to the routine clinical use of 131I OIH are related to the suboptimal imaging properties of the 131I radionuclide and its relatively high radiation dose. 123I has been substituted for 131I; however, its high cost and short shelf-life have limited its widespread use. Recent work has centered on the development of a new 99mTc renal tubular function agent, which would use the optimal radionuclidic properties and availability of 99mTc and combine the clinical information provided by OIH. The search for a suitable 99mTc renal tubular function agent has focused on the diamide dithiolate (N2S2), the paraaminohippuric iminodiacetic acid (PAHIDA), and the triamide mercaptide (N3S) donor ligand systems. To date, the most promising 99mTc tubular function agent is the N3S complex: 99mTc mercaptoacetyltriglycine (99mTc MAG3). Studies in animal models in diuresis, dehydration, acid or base imbalance, ischemia, and renal artery stenosis demonstrate that 99mTc MAG3 behaves similarly to 131I OIH. A simple kit formulation is available that yields the 99mTc MAG3 complex in high radiochemical purity. Studies in normal subjects and patients indicate that 99mTc MAG3 is an excellent 99mTc renal tubular agent, but its plasma clearance is only 50% to 60% that of OIH. In an effort to develop an improved 99mTc renal tubular function agent, changes have been made in the core N3S donor ligand system, but to date no agent has been synthesized that is clinically superior to 99mTc MAG3. 61 references

  4. Nitriles form mixed-coligand complexes with 99mTc-HYNIC-Peptide

    International Nuclear Information System (INIS)

    Liu Guozheng; Wescott, Charles; Sato, Aaron; Wang Yi; Liu Ning; Zhang Yumin; Rusckowski, Mary; Hnatowich, Donald J.

    2002-01-01

    Using a 12-amino acid peptide conjugated with HYNIC as a model, we investigated nitriles as possible coligands for labeling with 99m Tc. After the preparation of the 99m Tc labeled HYNIC-peptide using tricine as coligand, the addition of acetonitile was found by reverse phase HPLC to block further coligand exchange with ethylenediamine diacetic acid (EDDA) at room temperature. The addition of this nitrile changed the pharmacokinetics of the 99m Tc labeled peptide in normal mice towards faster clearance and significant differences in accumulation in most tissues sampled. By replacing acetonitrile with cyanoacetate, a nitrile not present in the HPLC eluant, it was possible to show the existence of a new, more hydrophilic, species by reverse phase HPLC. We conclude that nitriles can act as coligands for HYNIC-conjugated peptides labeled with 99m Tc and tricine. Furthermore, the presence of acetonitrile during Sep-Pak or HPLC purification may inadvertently generate a mixed tricine/acetonitile coligand 99m Tc-HYNIC-peptide complex

  5. {sup 99m}Tc-rituximab radiolabelled by photo-activation: a new non-Hodgkin's lymphoma imaging agent

    Energy Technology Data Exchange (ETDEWEB)

    Gmeiner Stopar, T.; Fettich, J.; Hojker, S. [University Medical Centre Ljubljana, Department for Nuclear Medicine, Ljubljana (Slovenia); Mlinaric-Rascan, I. [University of Ljubljana, Faculty of Pharmacy, Ljubljana (Slovenia); Mather, S.J. [St Bartholomew' s Hospital, Cancer Research UK, Department Nuclear Medicine, London (United Kingdom)

    2006-01-01

    Rituximab was the first chimeric monoclonal antibody to be approved for treatment of indolent B-cell non-Hodgkin's lymphoma (NHL). It is directed against the CD20 antigen, which is expressed by 95% of B-cell NHLs. The aim of this study was to explore the possibility of radiolabelling rituximab with {sup 99m}Tc for use as an imaging agent in NHL for early detection, staging, remission assessment, monitoring for metastatic spread and tumour recurrence, and assessment of CD20 expression prior to (radio)immunotherapy. Rituximab was purified from Mabthera solution (Roche), photo-activated at 302 nm by UV irradiation and radiolabelled with {sup 99m}Tc. The effectiveness of the labelling method was evaluated by determination of the number of free thiol groups per photoreduced antibody, radiochemical purity and in vitro stability of {sup 99m}Tc-rituximab. On average, 4.4 free thiol groups per photoreduced antibody were determined. Radiolabelling yields greater than 95% were routinely observed after storage of the photo-activated antibody at -80 C for 195 days. The direct binding assay showed preserved ability of {sup 99m}Tc-rituximab to bind to CD20, with an average immunoreactive fraction of 93.3%. The internalisation rate was proven to be low, with only 5.3% of bound {sup 99m}Tc-rituximab being internalised over 4 h at 37 C. Our results demonstrate that {sup 99m}Tc-rituximab of high radiochemical purity and with preserved binding affinity for the antigen can be prepared by photoreduction and that the method shows good reproducibility. {sup 99m}Tc-rituximab will be further explored as an imaging agent applicable in NHL for the purposes mentioned above. (orig.)

  6. Scintigraphic findings on 99mTc-MDP, 99mTc-sestamibi and 99mTc-HMPAO images in Gaucher's disease

    International Nuclear Information System (INIS)

    Mariani, G.; Molea, N.; La Civita, L.; Porciello, G.; Lazzeri, E.; Ferri, C.

    1996-01-01

    We report here on the use of the lipophilic cationic complex technetium-99m sestamibi ( 99m Tc-MIBI), employed as an indicator of increased cellular density and metabolic activity, to evaluate Gaucher cell infiltrates in the bone marrow; 99m Tc-hexametazime ( 99m Tc-HMPAO) was also employed, as a pure indicator of lipidic infiltration in the bone marrow. A 67-year-old patient with known type 1 Gaucher's disease presented with a painful left hip and knee and difficulty in gait subsequent to traumatic fracture of the left femoral neck that had required implant of a fixation screw-plaque. Bone scan with 99m Tc-methylene diphosphonate revealed reduced uptake at the distal metaphyseal-epiphyseal femoral region. In addition, whole-body maps and spot-view acquisitions of the thighs and legs were recorded at both 30 min and 2.5 h after the injection of 99m Tc-MIBI: the scintigraphic pattern clearly showed increased uptake at several sites involved by Gaucher deposits in the bone marrow (both knees, with variable intensity in different areas), matching the bone changes detected by conventional x-ray. The target to non-target ratios slowly decreased with time, from an average value of 2.25 in the early scan to an average value of 2 in the delayed scan. The lipid-soluble agent 99m Tc-HMPAO exhibited a superimposable scintigraphic pattern of accumulation at the involved sites, though with lower target to non-target ratios (1.27-1.48). The results obtained in this patient suggest a potential role of 99m Tc-MIBI in the scintigraphic evaluation of Gaucher's lipid deposits in the bone marrow. If the results are confirmed in other patients, this radiopharmaceutical would offer clear advantages over 133 Xe because of its wider availability and greater practicality (i.v. administration of 99m Tc-MIBI versus inhalation of 133 Xe, and use of a single gamma camera instead of two as with 133 Xe). (orig.). With 3 figs

  7. Lys and Arg in UBI: A specific site for a stable Tc-99m complex?

    International Nuclear Information System (INIS)

    Melendez-Alafort, Laura; Ramirez, Flor de Maria; Ferro-Flores, Guillermina; Murphy, Consuelo Arteaga de; Pedraza-Lopez, Martha; Hnatowich, Donald J.

    2003-01-01

    The aim of this study was to help establish if ubiquicidin peptide 29-41 fragment (UBI) contains a specific site for 99m Tc labeling by a new direct method under alkaline conditions. Since this peptide does not have cysteine residues, it is possible that neighboring arginine and lysine in the peptide amino acid sequence (Thr-Gly-Arg-Ala-Lys-Arg-Arg-Met-Gln-Tyr-Asn-Arg-Arg) could be a specific coordination site to form a stable 99m Tc-UBI complex. Following direct labeling, the in vitro stability of 99m Tc-UBI was compared to UBI radiolabeled by one indirect method using HYNIC/tricine and HYNIC/tricine/EDDA. Radiochemical purity of 99m Tc-UBI averaged 97% compared to 88% for 99m Tc-HYNIC-UBI/tricine and 98% for 99m Tc-HYNIC-UBI/tricine/EDDA. Both 99m Tc-HYNIC-UBI (tricine or EDDA) and 99m Tc-UBI showed stability in human serum and solutions of cysteine. 99m Tc-UBI radiochemical purity 24 h after dilution in 0.9% NaCl was greater than 90% at pH 9 and greater than 95% at pH 6.5. Under one set of experimental conditions, in vitro binding to bacteria of 99m Tc-UBI was 35% and identical to that of 99m Tc-HYNIC-UBI/tricine and 99m Tc-HYNIC-UBI/tricine/EDDA at 32% and 31% respectively. The biodistribution of 99m Tc-UBI in mice showed a rapid renal clearance. To help identify the site(s) of 99m Tc binding following direct labeling, molecular mechanics and quantum-mechanical calculations were performed which showed that the amine groups of Arg 7 and Lys are the most probable site. The calculations show that these groups can form a square pyramid with two water molecules for the Tc cation (dxysp 3 ). It will be necessary to isolate and characterize the 99 Tc(V)(O)-UBI . (H 2 O) n complex to confirm these results

  8. Homologous labelling of leukocytes with Tc 99m- dimeric ethylcysteinate (DEC): 'in vitro' and 'in vivo' tests

    International Nuclear Information System (INIS)

    Soroa, Victoria E.; Ozker, K.

    1999-01-01

    Preliminary tests have been carried out to validate the use of DEC -Tc 99m labelled leukocytes as a more stable substitute for Tc 99m-HMPAO in the diagnosis of infectious and inflammatory diseases. Although in all the patients the infectious focuses have been detected and the results are promissory, further studies with different infections /inflammations are needed to validate the procedure as an alternative routine technique

  9. Synthesis and preliminary evaluation of novel 99mTc-labeled folate derivative via click reaction for SPECT imaging

    International Nuclear Information System (INIS)

    Guo, Zhide; Zhang, Pu; Song, Manli; Wu, Xiaowei; Liu, Chang; Zhao, Zuoquan; Lu, Jie; Zhang, Xianzhong

    2014-01-01

    The folate receptor is over expressed in a wide variety of human tumors. In this study, a novel 99m Tc-labeled folate derivative ( 99m Tc-HYNIC-T-FA) was synthesized as a potential FR-targeting imaging probe and its efficiency was evaluated. This 99m Tc-complex could be obtained through practical manner and showed improved in vivo characteristics compared with other radiofolates. Thus, this novel 99m Tc-HYNIC-T-FA compound could serve as a potential imaging agent for folate receptor positive tumors. - Highlights: • An efficient synthetic strategy (click chemistry) was used to improve the overall efficiency. • 99m Tc-HYNIC-T-FA showed a high tumor uptake but low no-target tissues uptakes. • Excellent tumor-to-kidney ratio was achieved by injecting PMX. • A kit formulation was developed to obtain the desired product without any purification

  10. Labeling cellular elements of blood with Technetium-99m

    Energy Technology Data Exchange (ETDEWEB)

    Dewanjee, M.K.

    1990-08-01

    The purpose of this proposal is to develop new technique of labeling platelets and white cells with Tc-99m radionuclide. The conditions of labeling canine platelets and white cells with the lipid-soluble Tc-99m HMPAO have been optimized. The function of labeled platelets were evaluated by the determination of platelet survival time and recovery and these values were compared with that of In-111 tropolone labeled platelets. We developed the bilateral femoral catheterization model for the evaluation of platelet-thrombosis on control and heparin-bonded catheters in dogs. We are evaluating platelet thrombosis in the hollow-fiber hemodialyzer with Tc-99m and In-111 labeled platelets. We have developed the flow-loop for in vitro studies and are using a pig model for quantitation of platelet-consumption during hemodialysis. We are currently evaluating the new technique of platelet and white cell-labeling with Tc-99m and testing them in animal models of thrombosis and infection (osteo-myelitis). We are also using the Tc-99m HMPAO labeled mixed white cells in the early diagnosis (3-hour post-injection) of acute and chronic infection in patients and comparing the results with that of IN-111 oxine labeled white cells.

  11. Pharmacological study of 99mTc-CO-MIBI, a new mycoardial perfusion imaging agent comparison to 99mTc-MIBI

    International Nuclear Information System (INIS)

    Zhao Jiandong; Wang Jincheng; Mi Hongzhi

    2004-01-01

    For many years, 99m Tc-MIBI has been widely used for the diagnosis of ischemic heart disease. Although it has been regarded as a successful myocardial imaging agent, it has a notable defect of high liver radioactivities due to high uptake and slowly excrete. Recently, researchers had developed a new intermediate [ 99m Tc(CO) 3 (OH 2 ) 3 ] + , considering 99m Tc-MIBI excellent biodistribution, they synthesized a new class of compound- 99m Tc-CO-MIBI with [ 99m Tc(CO) 3 ] + core and ligand MIBI. Previous studies have preliminary demonstrated the following favorable properties: rapid blood-pool clearance, high myocardial extraction and rapid clearance kinetics from liver that indicated 99m Tc-CO-MIBI a promising new myocardial perfusion imaging agent. Furthermore, researchers separated the compound by changing liquid pH value and prepared single alkaline component 99m Tc-CO-MIBI. The pharmacological experiments in rat have provided better results on its biodistribution in vivo and much faster clearance kinetics from liver compared to 99mTc-MIBI. To evaluate the potential application of 99m Tc-CO-MIBI, further investigations are necessary to determine the evidence for enhanced ability in clinical decision making as a novel new myocardial perfusion imaging agent. Objective: Here, perform pharmacological experiment of 99m Tc-CO-MIBI, a new technetium-99m-labeled myocardial imaging agent compared to 99m Tc-MIBI in canines. To identify whether it is feasible in clinical application as a novel myocardial imaging agent, or not. Results: Accordingly, prepared the single alkaline component of 99m Tc-CO-MIBI. The complex was stable up to at least 7 hours after synthesized in vitro at either room temperature or 37 degree C water bath. Labeling yield and radiochemical purity (RCP) of the complex were evaluated by TLC and HPLC, the labeling percent was 93%-97% and the RCP was over 90%. Then administer 555MBq to every dog each times. A total of 5 dogs were involved. The data of

  12. 99m Tc- la bed somatostatin analogs for imaging somatostatin-receptor-positive tumors

    International Nuclear Information System (INIS)

    Gandomkar, M.; Najafi, R.; Shafiei, A.; Sadat Ebrahimi, E.; Babaie, M.H.; Rabani, M.

    2002-01-01

    Over the least few years, 111 In-DTPA- Octreotide has found widespread clinical applicability, especially in oncology. However limitation, especially concerning availability, imaging properties, and costs, remain and have stimulated research on radiolabeling with many alternative radionuclides. The purpose of this investigation was to labeling somatostatin analogs with 99 m Tc and evaluate their suitability as an agents for in vivo use. Octreotide and Tyr-3-Octreotide were labeled by 99 mTc with direct and indirect methods. Sodium ascorbate and sodium dithionite were used for reduction of cystine bridge and HYNIC was used as bifunctional agents and different co ligands used for labeling by 99 mTc. Yield of labeling, purity, stability, internalisation, binding affinity and biodistribution of peptide conjugates were studied. Direct labeling of octreotide was simple, rapid, efficient and yield was good (%60). K d for binding affinity as high (10 -9 ) but stability was low. Labeling for HYNIC-Tyr-Octreotide had a high yield (>%90), good stability, internalisation and biodistribution. with more experimental work and some improve this peptide-based radiopharmaceuticals can be employed in all nuclear medicine centers as a useful agent for imaging of tumors

  13. Distinction between infection and inflammation by a 99mTc-labeled anti (1→3) – β - D - glucans aptamer

    International Nuclear Information System (INIS)

    Lacerda, Camila M.S.; Ferreira, Ieda M.; Andrade, S.R.; Barros, Andre L.B.; Fernandes, Simone O.A.; Cardoso, Valbert N.

    2015-01-01

    The difficulty in the early diagnosis of infectious foci, whether caused by fungus or bacteria has raised the need to research new methods for this purpose. The distinction between inflammation and infection as well as the pathogen identification in cases of infection are of great relevance to decision-making in therapy and follow-up treatments. The aim of this study was to evaluate the anti (1→3) – β - D - glucans aptamer Seq6, labeled with 99m Tc , to distinguish between infection and inflammation. Firstly, in vitro studies were carried out by labeling the aptamer with 32 P to evaluate its binding capacity for (1→3) – β - D - glucans (main fungal cell wall polysaccharide), peptidoglycan (polysaccharide of bacterial cell wall) and also for Candida albicans and Staphylococcus aureus cells. The aptamers were labeled with 99m Tc by the direct labeling method. The stability of the 99m Tc -labeled aptamer was evaluated in saline, plasma, and cysteine excess. The biodistribution studies were approved by the Ethics Committee for Animal Experimentation of the Federal University of Minas Gerais (CETEA/UFMG), protocol. 143/2013. The aptamer labeled with 99m Tc was intravenously administered in three groups (n=6) of male Swiss mice (weight: 25-30g): infected with S. aureus or C. albicans, or with experimental inflammation induced by zymosan. The 32 P aptamer showed high binding affinity for beta-glucan and peptidoglycan. Binding to C. albicans and S. aureus cells also occurred. The radiolabel yield for the aptamer labeling with 99m Tc was higher than 90%. Stability tests in saline, plasma and excess of cysteine provided satisfactory results, since no significant variation in the radiolabel yield percentage was verified up to 24 hours, even increasing the cysteine concentration. In the biodistribution studies was analyzed the radiolabeled aptamer uptake by the animal infected thigh relative to the uninfected one. The animals infected with C. albicans presented a

  14. Radionuclide imaging of small-cell lung cancer (SCLC) using 99mTc-labeled neurotensin peptide 8-13

    International Nuclear Information System (INIS)

    Zhang Kaijun; An Rui; Gao Zairong; Zhang Yongxue; Aruva, Mohan R.

    2006-01-01

    Objectives: To prepare 99m technetium ( 99m Tc)-labeled neurotensin (NT) peptide and to evaluate the feasibility of imaging oncogene NT receptors overexpressed in human small-cell lung cancer (SCLC) cells. Methods: The NT analogue (Nα-His)Ac-NT(8-13) was synthesized such that histidine was attached at the N-terminus. The analogue was labeled with [ 99m Tc(H 2 O) 3 (CO) 3 ] at pH 7. 99m Tc-(Nα-His)Ac-NT(8-13) in vitro stability was determined by challenging it with 100 times the molar excess of DTPA, human serum albumin (HSA) and cysteine. The affinity, 99m Tc-(Nα-His)Ac-NT(8-13) binding to SCLC cell line NCI-H446, was studied in vitro. Biodistribution and imaging with 99m Tc-(Nα-His)Ac-NT(8-13) were performed at 4 and 12 h postinjection, and tissue distribution and imaging after receptor blocking were carried out at 4 h in nude mice bearing human SCLC tumor. Blood clearance was determined in normal mice. Results: The affinity constant (K d ) of 99m Tc-(Nα-His)Ac-NT(8-13) to SCLC cells was 0.56 nmol/L. When challenged with 100 times the molar excess of DTPA, HSA or cysteine, more than 97±1.8% radioactivity remained as 99m Tc-(Nα-His)Ac-NT(8-13). Tumor-to-muscle ratio was 3.35±1.01 at 4 h and 4.20±1.35 at 12 h postinjection. The excretory route of 99m Tc-(Nα-His)Ac-NT(8-13) was chiefly through the renal pathway. In the receptor-blocking group treated with unlabeled (Nα-His)Ac-NT(8-13), tumor-to-muscle ratio at 4 h was 1.25±0.55. Conclusion: The results suggest that 99m Tc-(Nα-His)Ac-NT(8-13) specifically binds to the SCLC cells and made 99m Tc-(Nα-His)Ac-NT(8-13) a desirable compound for further studies in planar or SPECT imaging of oncogene receptors overexpressed in SCLC cells

  15. Development of a Tc-99m labeled sigma-2 receptor-specific ligand as a potential breast tumor imaging agent

    International Nuclear Information System (INIS)

    Choi, Seok-Rye; Yang, Biao; Ploessl, Karl; Chumpradit, Sumalee; Wey, Shiaw-Pyng; Acton, Paul D.; Wheeler, Kenneth; Mach, Robert H.; Kung, Hank F.

    2001-01-01

    A novel in vivo imaging agent, 99m Tc labeled [(N-[2-((3'-N'-propyl-[3,3,1]aza-bicyclononan-3α-yl)(2''-methoxy-5- methyl-phenylcarbamate) (2-mercaptoethyl)amino)acetyl]-2-aminoethanethiolato] technetium(V) oxide), [ 99m Tc]2, displaying specific binding towards sigma-2 receptors was prepared and characterized. In vitro binding assays showed that the rhenium surrogate of [ 99m Tc]2, Re-2, displayed excellent binding affinity and selectivity towards sigma-2 receptors (K i = 2,723 and 22 nM for sigma-1 and sigma-2 receptor, respectively). Preparation of [ 99m Tc]2 was achieved by heating the S-protected starting material, 1, in the presence of acid, reducing agent (stannous glucoheptonate) and sodium [ 99m Tc]pertechnetate. The lipophilic racemic mixture was successfully prepared in 10 to 50% yield and the radiochemical purity was >98%. Separation of the isomers, peak A and peak B, was successfully achieved by using a chiralpak AD column eluted with an isocratic solvent (n-hexane/isopropanol; 3:1; v/v). The peak A and peak B appear to co-elute with the isomers of the surrogate, Re-2, under the same HPLC condition. Biodistribution studies in tumor bearing mice (mouse mammary adenocarcinoma, cell line 66, which is known to over-express sigma-2 receptors) showed that the racemic [ 99m Tc]2 localized in the tumor. Uptake in the tumor was 2.11, 1.30 and 1.11 %dose/gram at 1, 4 and 8 hr post iv injection, respectively, suggesting good uptake and retention in the tumor cells. The tumor uptake was significantly, but incompletely, blocked (about 25-30% blockage) by co-injection of 'cold' (+)pentazocine or haloperidol (1 mg/Kg). A majority of the radioactivity localized in the tumor tissue was extractable (>60%), and the HPLC analysis showed that it is the original compound, racemic [ 99m Tc]2 (>98% pure). The distribution of the purified peak A and peak B was determined in the same tumor bearing mice at 4 hr post iv injection. The tumor uptake was similar for both isomers

  16. Homologous labelling of leukocytes with Tc 99m- dimeric ethylcysteinate (DEC): 'in vitro' and 'in vivo' tests; Marcacion leucocitaria homologa con Tc99m-Etilcisteinato dimero (ECD): pruebas 'in vitro' e 'in vivo'

    Energy Technology Data Exchange (ETDEWEB)

    Soroa, Victoria E [Hospital de Clinicas Jose de San Martin, Buenos Aires (Argentina). Centro de Medicina Nuclear; Ozker, K [Medical Coll. of Wisconsin, Milwaukee, WI (United States). Dept. of Radiology

    1999-07-01

    Preliminary tests have been carried out to validate the use of DEC -Tc 99m labelled leukocytes as a more stable substitute for Tc 99m-HMPAO in the diagnosis of infectious and inflammatory diseases. Although in all the patients the infectious focuses have been detected and the results are promissory, further studies with different infections /inflammations are needed to validate the procedure as an alternative routine technique.

  17. /sup 99m/Tc-labeled solid-phase meal: a quantitative clinical measurement of human gastric emptying

    Energy Technology Data Exchange (ETDEWEB)

    Martin, J.L.; Beck, W.J.; McDonald, A.P.; Carlson, G.M.; Mathias, J.R.

    1983-08-01

    A solid-phase meal labeled with /sup 99m/Tc-sulfur colloid provides an improved clinical test for the quantitative evaluation of human gastric emptying. We studied 12 healthy male controls and five male patients with known gastric stasis secondary to a vagotomy and drainage procedure. All subjects were fasted for 8 hours before the study, and each consumed an unbuttered biscuit and a poached egg white containing 1 mCi of /sup 99m/Tc-sulfur colloid. For 2 hours, 60-second counts were measured every 10 minutes by a Pho Gamma III scintillation camera. The t/sup 1///sup 2/ for control subjects was 60 minutes, at which time patients with gastric stasis had retained 98% of the test meal. At 120 minutes, control subjects and patients with gastric stasis had 4.7% and 89%, respectively, of the meal remaining in the stomach. The solid-phase test meal labeled with /sup 99m/Tc-sulfur colloid is easy to perform and can be used clinically to quantitatively measure gastric emptying in humans. This test can discriminate between control subjects and patients with known gastric stasis.

  18. /sup 99m/Tc-labeled solid-phase meal: a quantitative clinical measurement of human gastric emptying

    International Nuclear Information System (INIS)

    Martin, J.L.; Beck, W.J.; McDonald, A.P.; Carlson, G.M.; Mathias, J.R.

    1983-01-01

    A solid-phase meal labeled with /sup 99m/Tc-sulfur colloid provides an improved clinical test for the quantitative evaluation of human gastric emptying. We studied 12 healthy male controls and five male patients with known gastric stasis secondary to a vagotomy and drainage procedure. All subjects were fasted for 8 hours before the study, and each consumed an unbuttered biscuit and a poached egg white containing 1 mCi of /sup 99m/Tc-sulfur colloid. For 2 hours, 60-second counts were measured every 10 minutes by a Pho Gamma III scintillation camera. The t 1 / 2 for control subjects was 60 minutes, at which time patients with gastric stasis had retained 98% of the test meal. At 120 minutes, control subjects and patients with gastric stasis had 4.7% and 89%, respectively, of the meal remaining in the stomach. The solid-phase test meal labeled with /sup 99m/Tc-sulfur colloid is easy to perform and can be used clinically to quantitatively measure gastric emptying in humans. This test can discriminate between control subjects and patients with known gastric stasis

  19. Acetylsalicylic acid and labeling of blood constituents with technetium-99m

    Energy Technology Data Exchange (ETDEWEB)

    Fonseca, Adenilson de Souza da [Universidade do Estado, Rio de Janeiro, RJ (Brazil). Dept. de Farmacologia e Psicobiologia; Frydman, Jacques Natan Grinapel; Rocha, Vanessa Camara da; Bernardo-Filho, Mario [Universidade do Estado, Rio de Janeiro, RJ (Brazil). Inst. de Biologia Roberto Alcantara Gomes. Dept. de Biofisica e Biometria

    2005-10-15

    Acetylsalicylic acid is the drug most used an anti-inflammatory agent and for secondary prevention of thrombotic phenomenon. Drugs can modify the labeling of blood constituents with technetium-99m (99m Tc). The aim of this work was to evaluate the effect of in vitro or in vivo assays with acetylsalicylic acid on the labeling of the blood constituents with 99m Tc. In vitro assay was performed with samples of whole blood from Wistar rats incubated with acetylsalicylic acid (1.0 mg/ml) for one hour before the 99m Tc-labeling process. For in vivo assay, Wistar rats were treated with acetylsalicylic acid (1.5 mg/kg) during one hour, and the whole blood was withdrawn for the 99m Tc-labeling process. Saline was used in control groups. Data showed that the fixation of 99m Tc to the blood constituents was not significantly (p>0.05) modified in in vitro and in vivo assays with acetylsalicylic acid, at least not when the experiments were carried out with the doses normally used in human beings. (author)

  20. Technetium-99m labelled antimicrobial peptides discriminate between bacterial infections and sterile inflammations

    International Nuclear Information System (INIS)

    Welling, M.M.; Pauwels, E.K.J.; Paulusma-Annema, A.; Nibbering, P.H.; Balter, H.S.

    2000-01-01

    The aim of this study was to select technetium-99m labelled peptides that can discriminate between bacterial infections and sterile inflammations. For this purpose, we first assessed the binding of various 99m Tc-labelled natural or synthetic peptides, which are based on the sequence of the human antimicrobial peptide ubiquicidin (UBI) or human lactoferrin (hLF), to bacteria and to leucocytes in vitro. In order to select peptides that preferentially bind to bacteria over host cells, radiolabelled peptides were injected into mice intraperitoneally infected with Klebsiella pneumoniae (K. pneumoniae) and the amount of radioactivity associated with the bacteria and with the leucocytes was quantitated. The next phase focussed on discrimination between bacterial infections and sterile inflammatory processes using 99m Tc-labelled peptides in mice intramuscularly infected with various bacteria (e.g. multi-drug-resistant Staphylococcus aureus) and in animals that had been injected with lipopolysaccharides (LPS) of bacterial origin to create a sterile inflammatory process. Also, we studied the distribution of 99m Tc-labelled UBI 29-41 and UBI 18-35 in rabbits having an experimental thigh muscle infection with K. pneumoniae and in rabbits injected with LPS. Based on the results of our in vitro and in vivo binding assays, two peptides, i.e. UBI 29-41 and UBI 18-35, were selected as possible candidates for infection imaging. The radiolabelled peptides can detect infections with both gram-positive and gram-negative bacteria in mice as early as 5-30 min after injection, with a target-to-non-target (T/NT) ratio between 2 and 3; maximum T/NT ratios were seen within 1 h after injection. In rabbits, high T/NT ratios (>5) for 99m Tc-labelled UBI 29-41 were observed from 1 h after injection. No accumulation of the selected 99m Tc-labelled UBI-derived peptides was observed in thighs of mice and rabbits previously injected with LPS. Scintigraphic investigation into the biodistribution of

  1. Technetium-99m labelled antimicrobial peptides discriminate between bacterial infections and sterile inflammations

    Energy Technology Data Exchange (ETDEWEB)

    Welling, M.M.; Pauwels, E.K.J. [Dept. of Radiology, Leiden University Medical Center (LUMC) (Netherlands); Paulusma-Annema, A.; Nibbering, P.H. [Dept. of Infectious Diseases, Leiden University Medical Center (Netherlands); Balter, H.S. [Centro Investigaciones Nucleares, Univ. of the Republic Uruguay, Montevideo (Uruguay)

    2000-03-01

    The aim of this study was to select technetium-99m labelled peptides that can discriminate between bacterial infections and sterile inflammations. For this purpose, we first assessed the binding of various {sup 99m}Tc-labelled natural or synthetic peptides, which are based on the sequence of the human antimicrobial peptide ubiquicidin (UBI) or human lactoferrin (hLF), to bacteria and to leucocytes in vitro. In order to select peptides that preferentially bind to bacteria over host cells, radiolabelled peptides were injected into mice intraperitoneally infected with Klebsiella pneumoniae (K. pneumoniae) and the amount of radioactivity associated with the bacteria and with the leucocytes was quantitated. The next phase focussed on discrimination between bacterial infections and sterile inflammatory processes using {sup 99m}Tc-labelled peptides in mice intramuscularly infected with various bacteria (e.g. multi-drug-resistant Staphylococcus aureus) and in animals that had been injected with lipopolysaccharides (LPS) of bacterial origin to create a sterile inflammatory process. Also, we studied the distribution of {sup 99m}Tc-labelled UBI 29-41 and UBI 18-35 in rabbits having an experimental thigh muscle infection with K. pneumoniae and in rabbits injected with LPS. Based on the results of our in vitro and in vivo binding assays, two peptides, i.e. UBI 29-41 and UBI 18-35, were selected as possible candidates for infection imaging. The radiolabelled peptides can detect infections with both gram-positive and gram-negative bacteria in mice as early as 5-30 min after injection, with a target-to-non-target (T/NT) ratio between 2 and 3; maximum T/NT ratios were seen within 1 h after injection. In rabbits, high T/NT ratios (>5) for {sup 99m}Tc-labelled UBI 29-41 were observed from 1 h after injection. No accumulation of the selected {sup 99m}Tc-labelled UBI-derived peptides was observed in thighs of mice and rabbits previously injected with LPS. Scintigraphic investigation

  2. 99mTc-Dextran-70: preparation and quality control

    International Nuclear Information System (INIS)

    Herrerias, Rosana; Muramoto, Emiko; Hamada, Elena S.; Barboza, Marycel F. de; Silva, Constancia P.G. da

    1997-01-01

    Dextran-70 labelled with 99m Tc is used for lymphocintigraphy in Nuclear Medicine. The aims of this work were: the lyophilized kit formulation; the radiochemical quality control determination and the biodistribution studies in Wistar rats. Each lyophilized vial contains: 50 mg Dextran-70 (Sigma); 750 μg Sn Cl 2 . 2 H 2 O, pH = 4.0. For the radiochemical determination the following parameters were assayed: Chromatography systems (Whatman 3MM, TLC-SG (Silica-gel) e TLC-A1 (aluminium); the 99m Tc activities (37, 111 and 1850 MBq); the 99m Tc volumes (1,3,5 and 8 mL) and the stability after the lyophilization process (1, 3, 6, 12 and 24 months). The Whatman 3MM chromatography system using acetone as solvent presented a purity yield of 99.88; 99.70; 99.00 and 98.92% using 1, 3, 5 and 8 mL of 99m Tc, respectively. The yield of labelling showed 99.80 % of radiochemical purity using 1850 MBq of 99m Tc, after 24 months. The biological studies were performed in Wistar rats, average weight 250g, after intravenous administration of 99m Tc-Dextran-70 (2.96 MBq). A slow blood decrease with high hepatic uptake was mesured. The high kidney uptake observed, during the experiment, was due the experiment, was due the fact that the animals were kept under anaesthesic effect. (author). 4 refs., 2 figs., 4 tabs

  3. Myocardial uptake characteristics of three 99mTc-labeled tracers for myocardial perfusion imaging one hour after rest injection

    International Nuclear Information System (INIS)

    Manka-Waluch, A.; Palmedo, H.; Reinhardt, M.J.; Joe, A.Y.; Manka, C.; Guhlke, S.; Biersack, H.J.; Bucerius, J.

    2006-01-01

    99m Tc-tetrofosmin and 99m Tc-sestamibi are approved tracers for myocardial perfusion studies. Recently, a 99m Tc-methoxyisobutylisonitrile (MIBI) preparation from a different manufacturer ( 99m Tc-cardiospect-MIBI) has been introduced to the market. Therefore, the aim of this study was the evaluation of 99m Tc-tetrofosmin as well as of two different 99m Tc-labeled MIBI tracers with regard to differences in imaging quality under resting conditions. Sixty patients (mean age 63.8 years±1.25) with known or suspected coronary artery disease but without evidence of rest-ischemia were included. Twenty patients in each group were examined by a two-day-rest-stress protocol using the three 99m Tc-labeled tracers. Visual analysis of all images was performed by two experienced physicians blinded with regard to the applied tracer. Regions of interest (ROI) were defined over the heart, lung and whole body only in the rest imaging in order to calculate heart-to-lung, lung-to-whole body-, and heart-to-whole body-ratios. The heart-to-lung ratio was statistically significant higher for 99 m T c-cardiospect-MIBI as compared to 99m Tc-sestamibi as well as to 99m Tc-tetrofosmin. Furthermore, a significantly higher heart-to-lung ratio was found for 99m Tc-sestamibi as compared to 99m Tc-tetrofosmin. The heart-to-whole body-ratio and the lung-to-whole body-ratio were equivalent between all tracers. Visual analysis revealed only slight differences regarding image quality between all tracers. ROI analysis surprisingly revealed a significant higher myocardial uptake and consequently a higher heart-to-lung ratio for 99m Tc-cardiospect-MIBI. Whether this leads to a better visual image quality has to be evaluated in future studies with larger study populations as well as semiquantitative segmental analysis of the myocardial perfusion images. (author)

  4. Tumor VEGF-R2 imaging with Tc-99m DTPA-dextran-DC101

    International Nuclear Information System (INIS)

    Kim, E. M.; Jeong, H. J.; Kim, S. L.; Jeong, S. J.; Lee, C. M.; Kim, D. W.; Lim, S. T.; Sohn, M. H.

    2007-01-01

    Vascular endothelial growth factor (VEGF) and its receptor (fetal liver kinase 1/kinase insert domain-containing receptor) play an important role in vascular permeability and tumor angiogenesis. Here, we investigated the Tc-99m DC101-dextran for VEGF-R2 imaging in tumor xenografted mice. DTPA conjugated amino-dextran was synthesized and then this was reacted with sulfo-LC-SPDP. Synthesis was identified by 1H-NMR. DTPA-dextran-SPDP was reacted with DC101. Binding affinity was checked by ELISA assay. Female athymic nude mice bearing B16F10 tumors were each injected via the tail vein with about 18.5 MBq of the Tc-99m DTPA-dextran-DC101, Tc-99m DTPA-DC101 and I-131 DC101. Biodistribution was performed at 1, 6, and 24h. DTPA-dextran-DC101 bind to FLK-1 in a dose-dependent manner. And this was blocked by significantly by free DC101. Labeling efficiency was approximately above 99% at 24 hr. Tc-99m DTPA-DC101 and I-131 DC101 showed rapid liver uptake, whereas Tc-99m DTPA-dextran-DC101 weak liver uptake and kidney elimination. In biodistribution results, Tc-99m DTPA-dextran-DC101 showed rapid renal clearance, and increased tumor uptake according to the time. Conjugation of antibody with dextran polymer is responsible for the decreased liver uptake and increased tumor uptake

  5. Modification of PLGA nanoparticles for improved properties as a 99mTc-labeled agent in sentinel lymph node detection.

    Science.gov (United States)

    Subramanian, Suresh; Pandey, Usha; Gugulothu, Dalapathi; Patravale, Vandana; Samuel, Grace

    2013-10-01

    We have earlier reported on the possible application of poly [lactide (co-glycolide)] (PLGA) nanoparticles of suitable size to serve as a (99m)Tc-labeled diagnostic tracer in sentinel lymph node detection (SLND). Additional efforts have now been made to improve both the radiolabeling yield and the biological efficacy by modifying the PLGA particles. Two approaches were taken, one based on in situ loading of mebrofenin inside PLGA nanoparticles and the second one based on functionalization of existing terminal carboxylic acid groups on the nanoparticle surface with p-aminobenzyl diethylenetriamine pentaacetic acid (p-NH2-Bz-DTPA) for enhanced availability of functional groups suitable for (99m)Tc complexation. The modified PLGA derivatives were purified and characterized. Radiolabeling of the modified PLGA nanoparticles was carried out with (99m)Tc using stannous chloride as the reducing agent. Mebrofenin encapsulated PLGA nanoparticles (mebrofenin-PLGA) did not show any significant improvement in the radiolabeling yield in comparison to the earlier reported "plain" PLGA nanoparticles, probably due to inaccessibility of the mebrofenin moiety to (99m)Tc upon encapsulation. DTPA-conjugated PLGA nanoparticles (DTPA-PLGA) showed appreciable improvement in radiolabeling yield under more moderate reaction conditions and better stability. In the biological evaluation performed in Wistar rat model, (99m)Tc-DTPA-PLGA nanoparticles showed a considerable increase in uptake in the sentinel node and the percentage popliteal extraction of the preparation was also higher. (99m)Tc-mebrofenin-PLGA did not show any improvement in SLN uptake over plain PLGA nanoparticles. The above results suggest that surface modification of PLGA by covalently coupling DTPA to PLGA nanoparticles prior to (99m)Tc labeling appears to be a superior approach to achieve a suitable (99m)Tc-labeled PLGA nanoparticle preparation for SLND.

  6. Neutrophil labeling with [99mTc]-technetium stannous colloid is complement receptor 3-mediated and increases the neutrophil priming response to lipopolysaccharide

    International Nuclear Information System (INIS)

    Gallagher, Hayley; Ramsay, Stuart C.; Barnes, Jodie; Maggs, Jacqueline; Cassidy, Nathan; Ketheesan, Natkunam

    2006-01-01

    Introduction: [ 99m Tc]-technetium stannous colloid (TcSnC)-labeled white cells are used to image inflammation. Neutrophil labeling with TcSnC is probably phagocytic, but the phagocytic receptor involved is not known. We hypothesised that complement receptor 3 (CR3) plays a key role. Phagocytic labeling could theoretically result in neutrophil activation or priming, affecting the behaviour of labeled cells. Fluorescence-activated cell sorter (FACS) analysis side scatter measurements can assess neutrophil activation and priming. Methods: We tested whether TcSnC neutrophil labeling is CR3-mediated by assessing if neutrophil uptake of TcSnC was inhibited by a monoclonal antibody (mAb) directed at the CD11b component of CR3. We tested if TcSnC-labeled neutrophils show altered activation or priming status, comparing FACS side scatter in labeled and unlabeled neutrophils and examining the effect of lipopolysaccharide (LPS), a known priming agent. Results: Anti-CD11b mAb reduced neutrophil uptake of TcSnC in a dose-dependent fashion. Labeled neutrophils did not show significantly increased side scatter compared to controls. LPS significantly increased side scatter in control cells and labeled neutrophils. However, the increase was significantly greater in labeled neutrophils than unlabeled cells. Conclusions: Neutrophil labeling with TcSnC is related to the function of CR3, a receptor which plays a central role in phagocytosis. TcSnC labeling did not significantly activate or prime neutrophils. However, labeled neutrophils showed a greater priming response to LPS. This could result in labeled neutrophils demonstrating increased adhesion on activated endothelium at sites of infection

  7. Noninvasive evaluation of active lower gastrointestinal bleeding: comparison between contrast-enhanced MDCT and 99mTc-labeled RBC scintigraphy.

    Science.gov (United States)

    Zink, Stephen I; Ohki, Stephen K; Stein, Barry; Zambuto, Domenic A; Rosenberg, Ronald J; Choi, Jenny J; Tubbs, Daniel S

    2008-10-01

    The purpose of our study was to compare contrast-enhanced MDCT and (99m)Tc-labeled RBC scanning for the evaluation of active lower gastrointestinal bleeding. Over 17 months, 55 patients (32 men, 23 women; age range, 21-92 years) were evaluated prospectively with contrast-enhanced MDCT using 100 mL of iopromide 300 mg I/mL. Technetium-99m-labeled RBC scans were obtained on 41 of 55 patients and select patients underwent angiography for attempted embolization. Each imaging technique was reviewed in a blinded fashion for sensitivity for detection of active bleeding as well as the active lower gastrointestinal bleeding location. Findings were positive on both examinations in eight patients and negative on both examinations in 20 patients. Findings were positive on contrast-enhanced MDCT and negative on (99m)Tc-labeled RBC in two patients; findings were negative on contrast-enhanced MDCT and positive on (99m)Tc-labeled RBC in 11 patients. Statistics showed significant disagreement, with simple agreement = 68.3%, kappa = 0.341, and p = 0.014. Sixteen of 60 (26.7%) contrast-enhanced MDCT scans were positive prospectively, with all accurately localizing the site of bleeding and identification of the underlying lesion in eight of 16 (50%). Nineteen of 41 (46.3%) (99m)Tc-labeled RBC scans were positive. Eighteen of 41 matched patients went on to angiography. In four of these 18 (22.2%) patients, the site of bleeding was confirmed by angiography, but in 14 of 18 (77.8%), the findings were negative. Contrast-enhanced MDCT and (99m)Tc-labeled RBC scanning show significant disagreement for evaluation of active lower gastrointestinal bleeding. Contrast-enhanced MDCT appears effective for detection and localization in cases of active lower gastrointestinal bleeding in which hemorrhage is active at the time of CT.

  8. Radiolabelling of glycosylated MFE-23::CPG2 fusion protein (MFECP1) with 99mTc for quantitation of tumour antibody-enzyme localisation in antibody-directed enzyme pro-drug therapy (ADEPT).

    Science.gov (United States)

    Francis, R J; Mather, S J; Chester, K; Sharma, S K; Bhatia, J; Pedley, R B; Waibel, R; Green, A J; Begent, R H J

    2004-08-01

    MFECP1 is a glycosylated recombinant fusion protein composed of MFE-23, a high-affinity anti-carcinoembryonic antigen (CEA) single chain Fv (scFv), fused to the enzyme carboxypeptidase G2 (CPG2), and has been constructed for use in antibody-directed enzyme pro-drug therapy (ADEPT). Radiolabelling of glycosylated MFECP1 with technetium-99m was developed for the purpose of determining tumour localisation of MFECP1 in a phase I ADEPT clinical study. The method used was 99mTc-carbonyl [99mTc(H2O)3(CO)3]+ (abbreviated to TcCO) mediated labelling of 99mTc to the hexahistidine (His) tag of MFECP1. MFECP1 fusion protein was labelled with TcCO under a variety of conditions, and this was shown to be a relatively simple and robust method. Tissue biodistribution was assessed in a CEA-expressing LS174T (human colon carcinoma) nude mouse xenograft model. Tissues were taken at 1, 4 and 6 h for assessment of distribution of radioactivity and for measurement of CPG2 enzyme levels. The amount of radioactivity retained by the tumour proved to be an accurate estimation of actual measured enzyme activity, indicating that this radiolabelling method does not appear to damage the antibody-antigen binding or the enzyme activity of MFECP1. However, correlation between CPG2 enzyme activity and measured radioactivity in liver, spleen and kidney was poor, indicating retention of radioactivity in non-tumour sites but loss of enzyme activity. The high retention of technetium radioisotope in normal tissues may limit the clinical applicability of this radiolabelling method for MFECP1; however, these results suggest that this technique does have applicability for measuring the biodistribution of His-tagged recombinant proteins.

  9. Radiolabelling of glycosylated MFE-23::CPG2 fusion protein (MFECP1) with 99mTc for quantitation of tumour antibody-enzyme localisation in antibody-directed enzyme pro-drug therapy (ADEPT)

    International Nuclear Information System (INIS)

    Francis, R.J.; Chester, K.; Sharma, S.K.; Bhatia, J.; Pedley, R.B.; Green, A.J.; Begent, R.H.J.; Mather, S.J.; Waibel, R.

    2004-01-01

    MFECP1 is a glycosylated recombinant fusion protein composed of MFE-23, a high-affinity anti-carcinoembryonic antigen (CEA) single chain Fv (scFv), fused to the enzyme carboxypeptidase G2 (CPG2), and has been constructed for use in antibody-directed enzyme pro-drug therapy (ADEPT). Radiolabelling of glycosylated MFECP1 with technetium-99m was developed for the purpose of determining tumour localisation of MFECP1 in a phase I ADEPT clinical study. The method used was 99m Tc-carbonyl [ 99m Tc(H 2 O) 3 (CO) 3 ] + (abbreviated to TcCO) mediated labelling of 99m Tc to the hexahistidine (His) tag of MFECP1. MFECP1 fusion protein was labelled with TcCO under a variety of conditions, and this was shown to be a relatively simple and robust method. Tissue biodistribution was assessed in a CEA-expressing LS174T (human colon carcinoma) nude mouse xenograft model. Tissues were taken at 1, 4 and 6 h for assessment of distribution of radioactivity and for measurement of CPG2 enzyme levels. The amount of radioactivity retained by the tumour proved to be an accurate estimation of actual measured enzyme activity, indicating that this radiolabelling method does not appear to damage the antibody-antigen binding or the enzyme activity of MFECP1. However, correlation between CPG2 enzyme activity and measured radioactivity in liver, spleen and kidney was poor, indicating retention of radioactivity in non-tumour sites but loss of enzyme activity. The high retention of technetium radioisotope in normal tissues may limit the clinical applicability of this radiolabelling method for MFECP1; however, these results suggest that this technique does have applicability for measuring the biodistribution of His-tagged recombinant proteins. (orig.)

  10. Comparison of Tc-99m labeled liver and liver pate as markers for solid-phase gastric emptying

    International Nuclear Information System (INIS)

    Christian, P.E.; Moore, J.G.; Datz, F.L.

    1984-01-01

    A radionuclide marker for studies of solid-phase gastric emptying should have a high labeling efficiency and remain relatively stable during gastric emptying. The availability of materials and the ease of preparation are also considerations in selecting radionuclide markers. The stability of intracellularly labeled chicken liver, surface-labeled chicken liver, and labeled pureed meat (liver pate) incubated with hydrochloric acid solution or gastric juice have been compared. Intracellularly labeled chicken liver and labeled liver pate were also compared in gastric emptying studies in humans. In vitro results demonstrated labeling efficiencies greater than 92% for both intracellularly labeled liver and labeled liver pate. The pate labeled with Tc-99m sulfur colloid was more stable than Tc-99m surface-labeled liver in vitro and its prepartion was easier than with the intracellular labeling technique. Gastric emptying studies on normal subjects demonstrated equal performance of the intracellularly labeled liver and the labeled liver pate. Labeled liver pate is thus an alternative to intracellularly labeled chicken liver in measuring solid-phase gastric emptying

  11. Detection of gastritis by /sup 99m/Tc-labeled red-blood-cell scintigraphy

    International Nuclear Information System (INIS)

    Wilton, G.P.; Wahl, R.L.; Juni, J.E.; Froelich, J.W.

    1984-01-01

    Gastritis is a common condition, with a variety of causes, that is diagnosed most often by barium upper gastrointestinal tract series or endoscopy. The authors report a case in which gastritis without active bleeding was apparent in scintiscans obtained during the evaluation of GI bleeding using /sup 99m/Tc-labeled red blood cells (TcRBC). The scintigraphic findings that suggest gastritis are described

  12. Rapid radiochemical methods for preparation of sup(99m)Tc labelled compounds

    International Nuclear Information System (INIS)

    Narasimhan, D.V.S.; Banodkar, S.M.; Kothari, K.; Mani, R.S.

    1981-01-01

    Several inorganic and organic compounds incorporating sup( 99 m)Tc are being extensively used for imaging various body organs. The preparation of these sup( 99 m)Tc compounds with the necessary purity requirements is carried out by controlled reduction of sup( 99 m)Tc-pertechnetate using Sn(II) ions as the reducing agent followed by complexation with various active ingredients. The authors here present procedures developed at Radiopharmaceuticals Section of BARC for preparing sup( 99 m)Tc-diphosphonate, sup( 99 m)Tc-glucoheptonate, sup( 99 m)Tc-albumin microspheres and sup( 99 m)Tc-phytate with high radiochemical purity. The paper also describes procedures for the preparation of freeze-dried kits for single step preparation of these compounds. The paper also describes the authors' experience with various analytical procedures for the determination of radiochemical purity of these preparations. (author)

  13. Demonstration of 99mTc-labelled plasmin on the surface of ex vivo thrombi

    International Nuclear Information System (INIS)

    Tengborn, L.; Hedner, U.; Rohlin, M.; Stahlberg, F.

    1982-01-01

    In an vitro system using the Chandler model for the preparation of in vitro thrombi trace amounts of porcine or human 99mTc-labelled plasmin was found to adsorb to the surface of a preformed thrombus. A radioactive lining of the thrombus could be demonstrated using autoradiography after addition of 99mTc-labelled plasmin in concentrations of 0.04 - 0.07 or 0.4 - 0.7 CTA u/thrombus made from 2 ml whole blood (0.035 - 0.35 microM). The same pattern was found for porcine as for human plasmin. The presence of tranexamic acid in concentrations of 3 to 12 mM did not affect the binding of plasmin indicating that the plasmin binding to fibrin was independent of the lysine binding sites. Furthermore alpha 2-antiplasmin was demonstrated on/in the thrombus also when no plasmin was present indicating a binding of alpha 2-antiplasmin to the thrombus. The plasmin bound to the thrombus was proteolytically inactive. In order to obtain thrombolysis most of the alpha 2-antiplasmin in the surrounding medium had to be neutralized

  14. Instant thin layer chromatography (ITLC) - the most true and convenient method for the determination of radiochemical purity of Tc-99m Labeled radiopharmaceuticals

    International Nuclear Information System (INIS)

    Anwar-Ul-Azim, M.; Ansari, M.I.H.

    2007-01-01

    Full text: Determination of radiochemical purity usually involves paper chromatography method or some column chromatography such as ion exchange or gel filtration technique. In this study, a modified chromatography method with thin-layer support called instant thin Layer chromatography (ITLC) was used for the measurement of radiochemical purity. The aim of the study was to present instant thin layer chromatography-Silica-Gel (ITLC-SG) technique as a fairly rapid , convenient and inexpensive system for the screening of radiochemical impurities of 99mTc-labeled radiopharmaceuticals resulting from physical , chemical and/or radiation decomposition. Materials and Methods: The experiment was carried out at the Institute of Nuclear Medicine and Ultrasound, Dhaka for a period of 10 months from August '05 to May '06. Radiochemical purity of seven types of 99mTc-labeled radiopharmaceuticals, namely 99mTc-DTPA,99mTc- MI I, 99m Tc - HDP, 99m Tc - DMSA, 99m Tc - Tetofosmin, 99mTc-Fyton and 99mTc-ECD were measured by the use of two solvent dual-instant thin layer chromatography systems. Commercially available instant thin layer chromatography plate ( 20cm x20cm) impregnated with silica gel (ITLC-SG: Merck, Germany) was used as a stationary phase for the measurement of radiochemical impurities.Acetone, Ethyl methyl ketone, chloroform and methanol were used to measure the amount of free pertechnetate in the labelled radiopharmaceuticals and 0.9% saline was used in all cases as solvent (Mobile phase) to measure the amount of the hydrolyzed-reduced technetium colloid. Results: The results showed that the measured radiochemical purity of 99mTc-DTPA, 99mTc-MIBI, 99mTc-HDP, 99mTc-DMSA, 99mTc-Tetofosmin, 99mTc-Fyton and 99mTc-ECD were acceptable for all the studied samples except two samples of 99mTc-MIBI, one sample of 99mTc-Fyton and two samples of 99mTc-ECD, where the measured radiochemical purity were not within the acceptable RCP limits of commonly used radiopharmaceuticals (RCP

  15. Work in progress. Gastrointestinal ulcerations: detection using a technetium-99m-labeled ulcer-avid agent

    International Nuclear Information System (INIS)

    Vasquez, T.E.; Bridges, R.L.; Braunstein, P.; Jansholt, A.L.; Meshkinpour, H.

    1983-01-01

    Technetium-99m-labeled sucralfate, an ulcer-avid material, was shown in preliminary animal and human studies to be stable in vivo with good sensitivity. Eight experimentally produced discrete gastric ulcers in three rabbits were visualized using this material. Of seven human studies, four studies were true-positive and three were true-negative. It is suggested that Tc-99m-labeled sucralfate may prove to have significant clinical advantages for the evaluation of gastrointestinal ulcer disease and other diseases that are associated with loss of mucosal integrity. The method for labeling sucralfate with Tc-99m was developed by the authors

  16. Study on the preparation of methylene diphosphonate (MDP) labeling with 99mTc for bone scintigraphy

    International Nuclear Information System (INIS)

    Nguyen Thi Thu; Le Van So; Vo Thi Cam Hoa; Bui Van Cuong; Mai Phuoc Tho; Pham Ngoc Dien; Duong Van Dong; Chu Van Khoa

    2005-01-01

    The 99m Tc-MDP kit was prepared by using aseptic technique. The composition of MDP invivo kit including 5 mg MDP, 0.5 mg stannous chloride, 0.5 mg ascorbic acid and 5 mg sodium chloride. The kit produces 99m Tc-MDP with more than 95% labelling efficiency at pH 6-7 when mixed with requisite amount of 99m Tc-pertechnetate. The preparation has been found sterity, pyrogen free, to be sufficiency stable invitro as well as invivo, blood clearance. After intravenous administrations abound 50% of the dose is accumulated and retained by the skeleton. The kit provides quality product in high yield, more stable than other phosphonate kit, high bone uptake. High avidity of 99m Tc-MDP for bone imaging makes it a promising agent for the detection of bone diseases. (author)

  17. Preparation of 99mTc-EDTA-MN and Its Bioimaging in Mouse

    Directory of Open Access Journals (Sweden)

    Yongshuai QI

    2015-07-01

    Full Text Available Background and objective Hypoxia is an important biological characteristics of solid tumor, it is not sensitive to radiotherapy and chemotherapy for which is the presence of hypoxic cell, thus increasing their resistance to conventional radiotherapy and chemotherapy, therefore, the detection of hypoxia degree of tumor tissue is of great significance. The hypoxia imaging of nuclear medicine can reflect the degree of tissue hypoxia, which can selectively retained on the hypoxic cells or tissues, including nitroimidazole and non nitroimidazole; the nitroimidazole is widely and deeply researched as hypoxic celles developer in China and abroad at present. The research about application of radionuclide labelled technique has clinical application value to develop the hypoxia imaging agent EDTA-MN complexes which was labeled. To study the feasibility of 99mTc by direct labeling method, the radiochemical properties evaluation of 99mTc-EDTA-MN, and observe the distribution characteristics of 99mTc radiolabeled EDTA-MN in the xenograft lung cancer nude mice bearing non-small cell lung cancer cell (A549, and provide experimental evidence for its further research and application. Methods The radiolabeling of EDTA-MN with 99mTc was performed with direct labeling method, respectively, on the reaction dosage (10 mg, 5 mg, 2 mg, stannous chloride dosage (8 mg/mL, 4 mg/mL, 2 mg/mL, mark system pH (2, 4, 5, 6 one by one test, using orthogonal design analysis, to find the optimal labeling conditions. Labelling rate, radiochemical purity, lipid-water partition coefficient and in vitro stability in normal saline (NS were determined by TLC and HPLC, and the preliminary study on the distribution of 99mTc-EDTA-MN in nude mice. Results The labeling rate of 99mTc-EDTA-MN with the best labeling conditions was (84.11±2.83%, and the radiochemical purity was higher than 90% by HPLC purification, without any notable decomposition at room temperature over a period of 12 h. The

  18. The preparation for an instant kit of 99mTc(V) DMSA as a tumor-seeking imaging agent and animal experimentation

    International Nuclear Information System (INIS)

    Li Yunlong; Li Hongyu; Jing Hui; Guo Hongyuan; Liu Yingmei; Zhao Hui

    1997-10-01

    A method for preparing an instant kit of 99m Tc(V) DMSA was described. The effect of pH on labelling efficiency of the kit was investigated. 99m Tc(V) DMSA was characterized by TLC on silica-gel sheets, eluting with n-butanol: acetic acid: water = 3:2:3 (volume ratio). Radiochemical purity and stability of 99m Tc(V) DMSA in vitro were studied. The results clearly demonstrated that the yield of 99m Tc(V) DMSA was more than 95% at pH 8∼8.5 and the agent was stable in 3 h at room temperature. Effect of temperature, moisture and luminosity on the stability of the freeze-dried kit were considered. The biological distributions of 99m Tc(V) DMSA were measured in mice bearing tumor S180. The results indicated that during 1∼6 h after i.v. injection, 99m Tc(V) DMSA was highly up taken in tumor tissue, the ratios of tumor: muscle and tumor: bone were in the ranges of 1.4∼2.4 and 1.2∼1.8, respectively. This peculiarity indicated that 99m Tc(V) DMSA has tumor-seeking property and could be used as a tumor-seeking imaging agent. (9 refs., 11 tabs.)

  19. In vivo/in vitro labeling of red blood cells with sup(99m)Tc and clinical applications

    International Nuclear Information System (INIS)

    Bauer, R.; Langhammer, H.; Pabst, H.W.; Bauer, U.; Sauer, E.

    1981-01-01

    A reliable and stabile in vivo/in vitro labeling technique of red blood cells (RBC) is described. The patients are injected 20% of the content of an unlabeled kit used for bone scintigraphy (TechneScan PYP, Byk-Mallinckrodt). 15 minutes later 3 ml blood are sampled in a heparinized syringe. The blood is incubated together with 30-40 mCi (1-1.5 GBq) sup(99m)Tc for 10 minutes in a water bath at 35-37 0 C. After centrifugation at 500 g a dose of 15-25 mCi (0.6-1 GBq) sup(99m)Tc labeled RBC may be withdrawn in a volume of 1-1.5 ml. Mean labeling efficiency is 88%, without using the first eluat of a Tc-generator the yield is as high as 92%. Due to the small volume, the labeled RBC may be reinjected as bolus and first pass radionuclide angiocardiography can be performed. Using labeled RBC, scintigraphy of the intravasal space is possible up to 20 hours without deterioration in contrast or accumulation of radioactivity in the extravasal space or in other organs. Evaluation of heart function can be performed up to 10 hours. In addition, labeled RBC are useful in detecting unknown gastrointestinal bleeding. (orig.) [de

  20. Evaluation of the absorbed dose to the kidneys due to Tc99m (DTPA) / Tc99m (Mag3) and Tc99m (Dmsa)

    International Nuclear Information System (INIS)

    Vasquez A, M.; Murillo C, F.; Castillo D, C.; Rocha J, J.; Sifuentes D, Y.; Sanchez S, P.; Idrogo C, J.; Marquez P, F.

    2015-10-01

    The absorbed dose in the kidneys of adult patients has been assessed using the biokinetics of radiopharmaceuticals containing Tc 99m (DTPA) / Tc 99m (Mag3) or Tc 99m (Dmsa).The absorbed dose was calculated using the formalism MIRD and the Cristy-Eckerman representation for the kidneys. The absorbed dose to the kidneys due to Tc 99m (DTPA) / Tc 99m (Mag3), are given by 0.00466 mGy.MBq -1 / 0.00339 mGy.MBq -1 . Approximately 21.2% of the absorbed dose is due to the bladder (content) and the remaining tissue, included in biokinetics of Tc 99m (DTPA) / Tc 99m (Mag3). The absorbed dose to the kidneys due to Tc 99m (Dmsa) is 0.17881 mGy.MBq -1 . Here, 1.7% of the absorbed dose is due to the bladder, spleen, liver and the remaining tissue, included in biokinetics of Tc 99m (Dmsa). (Author)

  1. Studies of techniques for the post-elution concentration of 99mTc obtained from gel type 99Mo/99mTc generators

    International Nuclear Information System (INIS)

    Suzuki, Katia Noriko

    2009-01-01

    On average 80% of the radiopharmaceuticals used in Nuclear Medicine are labeled with 99 mTc due to its physical properties and easy attainment through of 99 Mo/ 99 mTc generators. The Directory of Radiopharmacy (DIRF) of IPEN-CNEN/SP developed a gel type chromatographic generator of MoZr with 99 Mo produced by 98 Mo(n,γ) 99 Mo reaction that occurs at the IEA-R1 Nuclear Reactor. The gel is composed of zirconium molybdate with elution volume of 12 mL with an activity of 11100 MBq (300 mCi) producing a radioactive concentration of 925 MBq (25 mCi)/mL. The fission generator gives a higher radioactive concentration around 1850 MBq (50 mCi)/mL. The aim of this work is to study a system of post-elution concentration of 99 mTc for the attainment of a high enough radioactive concentration to meet the demands of the market, with a proved quality. Two types of systems of post-elution concentration were developed: the single and the tandem. The most appropriate system for the gel generator of 99 Mo/ 99 mTc, being at the same time sterile and vacuum automated, was the tandem system using Dionex 2.5 cc/QMA cartridges. The gel generator is eluted with 10 mL of solution of 0.1% NaCl and the pertechnetate anion is retained in the QMA cartridge and further eluted with 4 mL of saline. The process takes no more than 30 minutes. The elution efficiency of the system of concentration was 90 %. At the beginning of 2009 a global crisis in the supply of 99 Mo took place making it necessary the development of alternative technologies for the production of 99 Mo/ 99 mTc generators using fission produced 99 Mo and the development of an appropriate method to extend the useful life of this generator. The results of this study showed that the same system developed for the post- concentration of the gel generator can be employed for the fission generator, using the tandem system, giving a concentration factor of 3 for the elution of 99 mTc. (author)

  2. Radioimmunoscintigraphy with 99mTc-labelled anti-CEA monoclonal antibodies in colorectal carcinoma patients

    International Nuclear Information System (INIS)

    Sergieva, S.; Baychev, G.; Tzingilev, D.; Delijski, T.; Kirova, G.; Kirilova, B.; Nenovska, M.

    1998-01-01

    Sixteen patients (2 female and 14 male, aged 42-75) were given intravenous injections with 99m Tc (555-740 MBq)-labelled anti-CEA MAb (CEA-Scan, Mallinckrodt Medical and M-CEATEC, Sorin Biomedica). Five of them were with duly established or established or suspected primary colorectal carcinoma, and eleven were studied postoperatively after recording an increase CEA levels in serum. The patients were scanned within 4-24 h of infusion using planar and tomographic imaging in rotation gamma-camera DIACAM (Siemens). At all 16 patients 27 true positive results were obtained: in 7 primary colorectal carcinomas, 5 locally recurrent tumors, 7 liver metastases, 6 lymphogeneous lesions and two - in the ureteral region. True negative results were established at three patients, false positive - in one patient with chronic inflammation, and false negative results - in 3 cases with liver metastases foci < 8 mm. Having 90 % sensitivity, 75 % specificity and 82.3 % accuracy, radioimmunoscintigraphy is a highly informative and sensitive imaging method for diagnosing and following up of primary, recurrent and metastatic foci in colorectal carcinoma patients. (author)

  3. In-house cyclotron production of high-purity Tc-99m and Tc-99m radiopharmaceuticals.

    Science.gov (United States)

    Martini, Petra; Boschi, Alessandra; Cicoria, Gianfranco; Zagni, Federico; Corazza, Andrea; Uccelli, Licia; Pasquali, Micòl; Pupillo, Gaia; Marengo, Mario; Loriggiola, Massimo; Skliarova, Hanna; Mou, Liliana; Cisternino, Sara; Carturan, Sara; Melendez-Alafort, Laura; Uzunov, Nikolay M; Bello, Michele; Alvarez, Carlos Rossi; Esposito, Juan; Duatti, Adriano

    2018-05-30

    In the last years, the technology for producing the important medical radionuclide technetium-99m by cyclotrons has become sufficiently mature to justify its introduction as an alternative source of the starting precursor [ 99m Tc][TcO 4 ] - ubiquitously employed for the production of 99m Tc-radiopharmaceuticals in hospitals. These technologies make use almost exclusively of the nuclear reaction 100 Mo(p,2n) 99m Tc that allows direct production of Tc-99m. In this study, it is conjectured that this alternative production route will not replace the current supply chain based on the distribution of 99 Mo/ 99m Tc generators, but could become a convenient emergency source of Tc-99m only for in-house hospitals equipped with a conventional, low-energy, medical cyclotron. On this ground, an outline of the essential steps that should be implemented for setting up a hospital radiopharmacy aimed at the occasional production of Tc-99m by a small cyclotron is discussed. These include (1) target production, (2) irradiation conditions, (3) separation/purification procedures, (4) terminal sterilization, (5) quality control, and (6) Mo-100 recovery. To address these issues, a comprehensive technology for cyclotron-production of Tc-99m, developed at the Legnaro National Laboratories of the Italian National Institute of Nuclear Physics (LNL-INFN), will be used as a reference example. Copyright © 2018 Elsevier Ltd. All rights reserved.

  4. Production of the antimicrobial peptide UBI 29-41 labelled with 99mTc by an indirect method; Obtencion del peptido antimicrobiano UBI 29-41 marcado con 99mTc empleando un metodo indirecto

    Energy Technology Data Exchange (ETDEWEB)

    Nevares, Noemi; Crudo, Jose L; Zapata, Miguel; Castiglia, Silvia G. de [Comision Nacional de Energia Atomica, Ezeiza (Argentina). Dept. de Radioquimica

    2003-07-01

    The infection processes are a major problem in human health causing a high number of human deaths all around the world. Diagnostic imaging in nuclear medicine is an attractive option in the detection of infection processes due to its sensitivity. The antimicrobial peptides are very important in the development of new radiopharmaceuticals, since their antimicrobial activity towards a great variety of microorganisms have been proven. The aim of this work was to obtain the antimicrobial peptide UBI 29-41 labelled with technetium 99 m, by an indirect method via NHS-Hynic and tricine as a coligand, and evaluate its stability and its ability to discriminate between infection and inflammation sites. The radiochemical purity of the labeling procedure was 95.5{+-}1,2 %. The cysteine challenge showed a great stability of the 99mTc UBI-Hynic, and the stability in human serum showed that the 81% of the radioactivity remained bounded to UBI-Hynic at 48 hs of incubation. The bio distribution's studies showed main elimination via kidney of 99mTc UBI-Hynic and the target/non target ratio was 1,81 for infected mice and 1,16 for inflamed mice. (author)

  5. Technetium-99m direct radiolabeling of monoclonal antibody ior egf/r3

    Energy Technology Data Exchange (ETDEWEB)

    Morales, Alejo A. Morales; Crespo, Francisco Zayas; Gandolff, Gilda Nunez; Escobar, Normando Iznaga; Perez, Niuvis Perez; Hernandez, Juan C. Izquierdo

    1998-01-01

    Monoclonal antibodies (MAbs) are being widely used for imaging studies, coupled mainly with {sup 99m}Tc. The antibody ior egf/r3 is a MAb against human epidermal growth factor receptor (hEGF-r), and we have developed a method for optimum labeling of this MAb with {sup 99m}Tc. The reduction was performed with 2-mercaptoethanol (2-ME) at a molar ratio of 2000:1 (2-ME:MAb) and methylene diphosphonate as transchelant. The integrity of reduced MAb was checked by mean of native polyacrylamide gel electrophoresis (PAGE) and gel filtration chromatography on Superose 12 (purity >99%). Radio colloids remained lower than 2%, and the labeling efficiency was 98.5%. The number of sulfhydryl groups generated was quantified using Ellman's reagent and was found to be 6.65 {+-} 0.69 per antibody molecule. In vitro stability studies in several challenging conditions (DTPA, human serum albumin and human serum) were performed, and no significant loss in binding percentage was seen. Radio receptor assay was used to test immunoreactivity of the reduced MAb. Both labeled and unlabeled MAbs were able to compete for binding to the hEGF-r with radioiodinated EGF. Biodistribution studies in BALB/c mice are reported.

  6. Technetium-99m direct radiolabeling of monoclonal antibody ior egf/r3

    International Nuclear Information System (INIS)

    Morales, Alejo A. Morales; Crespo, Francisco Zayas; Gandolff, Gilda Nunez; Escobar, Normando Iznaga; Perez, Niuvis Perez; Hernandez, Juan C. Izquierdo

    1998-01-01

    Monoclonal antibodies (MAbs) are being widely used for imaging studies, coupled mainly with 99m Tc. The antibody ior egf/r3 is a MAb against human epidermal growth factor receptor (hEGF-r), and we have developed a method for optimum labeling of this MAb with 99m Tc. The reduction was performed with 2-mercaptoethanol (2-ME) at a molar ratio of 2000:1 (2-ME:MAb) and methylene diphosphonate as transchelant. The integrity of reduced MAb was checked by mean of native polyacrylamide gel electrophoresis (PAGE) and gel filtration chromatography on Superose 12 (purity >99%). Radio colloids remained lower than 2%, and the labeling efficiency was 98.5%. The number of sulfhydryl groups generated was quantified using Ellman's reagent and was found to be 6.65 ± 0.69 per antibody molecule. In vitro stability studies in several challenging conditions (DTPA, human serum albumin and human serum) were performed, and no significant loss in binding percentage was seen. Radio receptor assay was used to test immunoreactivity of the reduced MAb. Both labeled and unlabeled MAbs were able to compete for binding to the hEGF-r with radioiodinated EGF. Biodistribution studies in BALB/c mice are reported

  7. Production and clinical evaluation of 99mTc-octreotide

    International Nuclear Information System (INIS)

    Fettich, J.; Kolenc-Peitl, P.

    2004-01-01

    Full text: Due to advantages of 99m-Tc labelled radiopharmaceuticals we examined the feasibility of producing 99m-Tcoctreotide in our laboratory and compare the results with 111-In-octreotide in the same patients. Keeping constant amount of components without exceeding amount of the peptide used, preparation of 99m-Tc-ethylendiaminediacetic- acidhydrazinonicotinamide-D-Phe1,Tyr3-octreotide (99m-Tc EDDA/HYNIC-TOC) was achieved. Radiochemical purity was tested using high-pressure liquid chromatography for 24 hours. In vitro stability testing of the product showed that radiochemical purity remained above 95% for 24 hours and the radiopharmaceutical was found suitable for human use. 5 - 10 μg of the peptide labelled with 550-650 MBq of 99m-Tc was prepared for each patient. 32 patients with clinically suspicious or confirmed carcinoid were investigated with 550 - 650 MBq 99m-Tcoctreotide prepared in our laboratory followed by 110 MBq 111-In-octreotide (Octreoscan, Mallinkrodt). Whole body scintigraphy and abdominal SPECT were performed 4 and 20 hrs after injection of respective radiopharmaceutical. In all patients both studies were acquired within 5 days. All patients gave informed consent for the study as required by Ethics committee. No abnormal tracer uptake was seen anywhere in the body in 12 patient with either of the radiopharmaceuticals. These were used to assess normal distribution of both radiopharmaceuticals. Normal accumulation was seen in case of both radiopharmaceuticals in the spleen, kidneys, liver and gallbladder. Biliary activity was seen in the gut in patients that were not well prepared for the study. There was significantly less activity seen in the kidneys in case of 99m-Tc-octreotide. This could be explained by higher hydrophilicity of the 99m-Tc-EDDA/HYNEC-TOC molecules as compared with 111-In-DTPA-octreotide. 20 patients with confirmed carcinoids showed abnormal uptake but without any difference in distribution of the two radiopharmaceuticals

  8. Determination of Cyclam as Impurity in 99mTc-CTMP Using Radio electrophoresis Method

    International Nuclear Information System (INIS)

    Isti Daruwati; Misyetti; Maula Eka Sriyani; Teguh Hafiz AW

    2009-01-01

    Labelled compound of CTMP that are used for bone seeking radiopharmaceuticals must have to fulfill the standard requirements, such as have high radiochemical purity. CTMP compounds was in house synthesized from cyclam and formaldehyde in an acidic condition (conc. HCl) using Mannich methods. Impurities in CTMP product are the residue of cyclam, phosphoric acid, formaldehyde and hydrochloric acid. Formaldehyde and hydrochloride acid in the aqueous form is easily removed through the rinse process in the synthesis, while cyclam in the solid phase could be mix with CTMP. Therefore the impurities of cyclam in 99m Tc-CTMP must be determined. With nuclear technique, the determination of cyclam could be assessed simultaneously with labelled of CTMP with technetium-99m. Separation of 99m Tc-CTMP and 99m Tc-cyclam in solution was conducted with radio-electrophoresis method simultaneously. The radiochemical purity for both radiolabelled compound was determined by paper chromatography. The purity of radiolabelled 99m Tc-CTMP from cyclam was determined using electrophoresis method. The result show that the amount of cyclam in CTMP can be determined simultaneously using nuclear techniques with the labeling of 99m Tc-CTMP. Electrophoresis method can separated 99m Tc-cyclam, 99m Tc-CTMP, 99m TcO4 and 99m Tc-reduced with limit quantitation of cyclam until 0,4% w/w. (author)

  9. Radiolabeling of human platelets using four radiopharmaceuticals with Tc-99m

    International Nuclear Information System (INIS)

    Portillo L, M.C.; Godoy, C.

    1991-01-01

    The present investigation work has been done in an evaluation of four different radiopharmaceuticals with Tin II (Glucoheptonate, Pyrophosphate, Citrate and DTPA), with the purpose of determining which one of the four would be obtained a higher rate of radiolabeling of platelets with Tc-99m. In order to evaluate the four radiopharmaceuticals it was procede to the separation and labeling of the human platelets. It was worked with samples of blood from five pacients, and the platelets from each one of them were labeled with the radiopharmaceuticals-Tc-99m. Then was observed a significant difference among the four radiopharmaceuticals studied, with a reliable level of 0.05 being the Glucoheptonate-Tc-99m the best to label platelets, obtaining with the same 50.23% of labeling efficiency, while for DTPA, Pyrophosphate and Citrate, It was obtained 33.42%, 29.82% and |2.62% respectively. Also, it was studied the biodistribution of the labeled platelets, using Glucoheptonate-Tc-99m as a radiopharamceutical. The biodistribution was studied in white mice at different times and it was founded that the place of biodistribution of the labeled platelets is given in greater percentage in the liver, spleen, lungs and kydneis. (Author)

  10. Biological evaluation of 99m Tc-N-(3-bromo-trimethyl-acetanilide)-iminodiacetic acid (99mTc mebrofenin) as hepatobiliary radiopharmaceutical

    International Nuclear Information System (INIS)

    Hamada, E.S.

    1994-01-01

    Technetium-99 m-N-(3-bromo-2,4,6-trimethyl acetanilide) iminodiacetic acid ( 99m Tc-Mebrofenin) has been described as having optimal properties as hepatobiliary radiopharmaceutical. This paper describes the synthesis, radiopharmaceutical preparation and biological distribution of new labeled compound. The biodistribution study of 99m Tc-Mebrofenin- was carried out in normal mice. The specificity for hepatobiliary excretion blood clearance and cumulative biliary excretion were evaluated in normal and cirrhotic rats. (author). 5 refs, 3 figs, 3 tabs

  11. Radioimmunoscintigraphy with technetium-99m labelled monoclonal antibody, 1A3, in colorectal cancer

    International Nuclear Information System (INIS)

    Granowska, M.; Britton, K.E.; Mather, S.J.; Morris, G.; Ellison, D.; Soobramoney, S.; Talbot, I.C.; Northover, J.M.A.

    1993-01-01

    This study of radioimmunoscintigraphy (RIS) was primarily undertaken to determine how the imaging results related to surgical findings. Technetium-99m radiolabelled 1A3, a monoclonal antibody against a columnar cell surface antigen, was used. No adverse effects or thyroid uptake was observed in 127 studies. The 85 primary colorectal cancers were all image positive. In the assessment of recurrent tumour in the abdomen or pelvis, the accuracy was 33/35 (94%), including true-positive findings in some whose serum carcinoembryonic antigen was normal. There was a positive predictive value for abdominal or pelvic recurrence of 92% and a negative predictive value of 100%, at a prevalence of 66%. In those patients whose liver was able to be evaluated, the accuracy was 72/79 (91%). There was a positive predictive value for liver metastases of 88% and a negative predictive value of 93%, at a prelavence of 32%. The simple procedure for labelling antibody with 99m Tc and its ready availability allow a completed report to be given within 24 h of the request. (orig.)

  12. Further optimisation of 99mTc-Nanocoll sentinel node localisation in carcinoma of the breast by improved labelling

    International Nuclear Information System (INIS)

    Gommans, G.M.M.; Dongen, A. van; Schors, T.G. van der; Boer, R.O.; Gommans, E.; Visser, J.F.M.; Waard, J.W.D. de; Clarijs, W.W.J.; Bos, J. van de

    2001-01-01

    The sentinel node (SLN) procedure has gained widespread acceptance for the axillary staging of patients who present with carcinoma of the breast. A first series of 21 patients were imaged 2 and 4 h after the injection of technetium-99m colloidal albumin. Preoperatively, axillary foci were located scintigraphically and with a hand-held gamma probe that was also used to detect the radiolabelled nodes 22 h later in the operating theatre. In a high percentage of our first series it was difficult to localise the sentinel node owing to a low count rate ex vivo. The aim of this study was to facilitate the detection of sentinel nodes by improving the count rate by the use of higher specific concentrations of 99m Tc-colloidal albumin, with increased radiochemical labelling efficiency and stability. In vitro tests were performed to establish the radiochemical labelling efficiency and stability of different concentrations of 99m Tc-colloidal albumin. Concentrations of 2.5, 10, 20, 25, 30, 37 and 50 MBq 99m Tc/μg colloidal albumin (Nanocoll) were prepared under nitrogen and in vacuum. The quality of the solutions was assessed by testing the radiochemical labelling efficiency and stability after 0.5, 2, 5, 8 and 24 h. The particle size of colloidal albumin was tested by dynamic light scattering at 30.2 , 62.6 and 90.0 angles. Following the results of the in vitro studies, higher concentrations of 99m Tc-colloidal albumin were used in vivo in a further series of 98 patients. For labelling under nitrogen, a maximum acceptable concentration of 10 MBq/μg was found, which complies with the specifications of the manufacturer. By preparing the labelling in vacuum vials, a 2.5 times greater radiochemical labelling efficiency over the entire period was achieved, and a significant improvement (P 99m Tc-colloidal albumin, which facilitated the detection of the SLN by the gamma probe during surgery. (orig.)

  13. Evaluation of labelling conditions, quality control and biodistribution study of 99mTc-5-aminolevulinic acid (5-ALA). A potential liver imaging agent

    International Nuclear Information System (INIS)

    Kalim Ullah Khan; Mohammad Rafi; Samina Roohi; Rizwana Zahoor; Zafar Iqbal; Mushtaq Ahmad

    2014-01-01

    Labelling of 5-aminolevulinic acid (5-ALA) with 99m Tc was achieved by using SnCl 2 ·2H 2 O as reducing agent. Radiochemical purity and labelling efficiency was determined by instant thin layer chromatography/paper chromatography. Efficiency of labelling was dependent on many parameters such as amount of ligand, reducing agent, pH, and time of incubation. 99m Tc labelled 5-ALA remained stable for 24 h in human serum. Tissue biodistribution of 99m Tc-5-ALA was evaluated in Sprague-Dawley rats. Biodistribution study (% ID/g) in rats revealed that 99m Tc-5-ALA was accumulated significantly in liver, spleen, stomach and intestine after half hour, 4 and 24 h. Significant activity was noted in bladder and urine at 4 h. High liver uptake of 99m Tc-5-ALA makes it a promising liver imaging agent. (author)

  14. Development of Tc-99m-DTPA-HSA as a new blood pool scanning agent

    Energy Technology Data Exchange (ETDEWEB)

    Shirakami, Y; Matsumoto, Y; Yamauchi, Y; Kurami, M; Ueda, N; Hazue, M

    1987-04-01

    A new HSA preparation, Tc-99m-DTPA-HSA, was developed as a blood pool scanning agent. It shows higher labeling yield (more than 95 %) and higher blood retention (74.7 % I.D. at 1 hour post-injection) than Tc-99m-HSA prepared by directly labeling of HSA with Tc-99m. The introduction of DTPA, a strong bifunctional chelating agent, to HSA provides sites for the stable binding of Tc-99m. The preparation composed of 20 mCi of Tc-99m at calibration time and 10 mg of DTPA-HSA in a vial. After labeling, it had been stable for 24 hours at room temperature. In rats, most of Tc-99m-DTPA-HSA injected was metabolized and excreted in urine and feces. The cumulative radioactivity in urine and feces were 56.0 % and 13.7 % of injected dose, respectively, at 48 hours after injection. Metabolites observed in urine were Tc-99m-urea, Tc-99m-DTPA, reduced Tc-99m and so on. Tc-99m-DTPA-HSA proved, thus, a desirable feature for the blood pool scanning agent.

  15. Distinction between infection and inflammation by a {sup 99m}Tc-labeled anti (1→3) – β - D - glucans aptamer

    Energy Technology Data Exchange (ETDEWEB)

    Lacerda, Camila M.S.; Ferreira, Ieda M.; Andrade, S.R., E-mail: cmslacerda@gmail.com.br [Centro de Desenvolvimento da Tecnologia Nuclear (CDTN/CNEN-MG), Belo Horizonte, MG (Brazil); Barros, Andre L.B.; Fernandes, Simone O.A.; Cardoso, Valbert N., E-mail: valbertcardoso@yahoo.com.br [Universidade Federal de Minas Gerais (UFMG), Belo Horizonte, MG (Brazil). Faculdade de Farmacia. Departamento de Analises Clinicas e Toxicologicas

    2015-07-01

    The difficulty in the early diagnosis of infectious foci, whether caused by fungus or bacteria has raised the need to research new methods for this purpose. The distinction between inflammation and infection as well as the pathogen identification in cases of infection are of great relevance to decision-making in therapy and follow-up treatments. The aim of this study was to evaluate the anti (1→3) – β - D - glucans aptamer Seq6, labeled with {sup 99m}Tc , to distinguish between infection and inflammation. Firstly, in vitro studies were carried out by labeling the aptamer with {sup 32}P to evaluate its binding capacity for (1→3) – β - D - glucans (main fungal cell wall polysaccharide), peptidoglycan (polysaccharide of bacterial cell wall) and also for Candida albicans and Staphylococcus aureus cells. The aptamers were labeled with {sup 99m}Tc by the direct labeling method. The stability of the {sup 99m}Tc -labeled aptamer was evaluated in saline, plasma, and cysteine excess. The biodistribution studies were approved by the Ethics Committee for Animal Experimentation of the Federal University of Minas Gerais (CETEA/UFMG), protocol. 143/2013. The aptamer labeled with {sup 99m}Tc was intravenously administered in three groups (n=6) of male Swiss mice (weight: 25-30g): infected with S. aureus or C. albicans, or with experimental inflammation induced by zymosan. The {sup 32}P aptamer showed high binding affinity for beta-glucan and peptidoglycan. Binding to C. albicans and S. aureus cells also occurred. The radiolabel yield for the aptamer labeling with {sup 99m}Tc was higher than 90%. Stability tests in saline, plasma and excess of cysteine provided satisfactory results, since no significant variation in the radiolabel yield percentage was verified up to 24 hours, even increasing the cysteine concentration. In the biodistribution studies was analyzed the radiolabeled aptamer uptake by the animal infected thigh relative to the uninfected one. The animals

  16. Predictable efficacy for splenic artery embolization with sites of sequestration using 99mTc labeled platelets in immunogenic idiopathic thrombocytopenic purpura

    International Nuclear Information System (INIS)

    Tian Aiping

    1992-01-01

    28 patients with chronic Immunogenic (Idiopathic) Thrombocytopenic purpura (ITP) were determined of the site of sequestration using 99m Tc labeled platelets. Among them, partial splenic artery embolization were done in 20 patients. 7/8 spleen type cases and 1/6 hepato-spleen hepatic type cases have their platelets counts raised above 100 x 10 9 /L. The separation of platelets and its 99m Tc labelling method were also discussed. Above results suggested that the determination of sequestration site of the 99m Tc labelled platelets have some help for the splenic artery embolization therapy in ITP

  17. Csintigraphic imaging of experimental cardiomyopathy in dogs using /sup 99m/Tc-hexylidene aminodiphosphonate (/sup 99m/Tc-AHDP)

    Energy Technology Data Exchange (ETDEWEB)

    Duska, F; Vizda, J; Kafka, P; Kubicek, J; Mazurova, Y; Palicka, V; Grossmann, V

    1987-11-01

    Scintiscanning of the myocardium using /sup 99m/Tc-AHDP (hexylidene aminodiphosphonate) was performed in 12 dogs with experimental cardiomyopathy, induced by a large intravenous dose of theophylline and adrenaline. A marked positivity of the scan was determined in animals with 4 and 24 hours-old lesions. The scans proved to be negative after 7 days. The scintigraphic examinations yielded results which were in agreement with the plasma level of creatine kinase, a comparison with histological examination revealed that the maximum accumulation of the radiopharmaceutical occurred at the time the myocardium damage reached the stage of myocytolysis. /sup 99m/Tc-AHDP is therefore suitable for the detection of mild myocardium damage at its early stages. (author). 1 fig., 1 tab., 20 refs.

  18. 99mTc labelled peptides for imaging peripheral receptors

    International Nuclear Information System (INIS)

    Gil, M.C.; Chandia, V.M.; Errazu, X.

    2001-01-01

    Radiolabelling of somatostatin analogues as RC-160 and TOC with 99m Tc, using direct and bifunctional chelating methods as well as quality control and evaluation methods, has been accomplished following the techniques and recommendation of the first and second RCMs. Synthesis of bifunctional chelating agents, such as Bz-MAG-3, is routinely produced in our laboratory. Synthesis of HYNIC and HYNIC-MAG-3 is in progress. Radioiodination of RC-160 using chloramine-T and iodogen methods were also studied in order to get experience with the different techniques used to evaluate the labelled peptides. (author)

  19. Tc-99m imaging agents

    International Nuclear Information System (INIS)

    Weininger, J.; Trumper, J.

    1984-01-01

    A wide range of pharmaceuticals for labeling with Tc-99m, developed by the Soreq Radiopharmaceuticals Department, is described. Details of the production and quality control of 13 kits are given, as well as the range of results required for consistently high quality imaging agents

  20. Study of technetium behaviour in radiopharmaceuticals. Characterization of sup(99m)Tc-pyrophosphate, sup(99m)Tc-dimercaptosuccinate, sup(99m)Tc-diethylenetriaminepentaacetate complexes and sup(99m)Tc-colloidal rhenium sulphide

    International Nuclear Information System (INIS)

    Saccavini, J.-C.

    1980-12-01

    The chemistry of technetium in extremely dilute solution was approached through the study of three complexing agents and a colloid. By the application of high-performance chromatographic techniques to the analysis of (Tc-pyro), (Tc-DTPA), (Tc-DMSA) complexes it was possible to isolate one or more chelates from a single complexing agent. Addition of pertechnetates to a solution of sodium pyrophosphates and stannous chloride at neutral pH leads to the formation of two complexes, both highly osteotropic. By the use of sup(117m)Sn it was shown that tin employed as reducing agent enters into the composition of one of the two complexes, either of which may be obtained preferentially by varying the (Sn)/(pyro) ratio. With technetium at acid pH (2.5) DMSA gives one or more chelates according to the concentration of the reagents present. DTPA with technetium at neutral pH gives a single complex for which a structure is proposed. The addition of calcium, indispensable for DTPA injection, leads to the appearance of a second bimetallic complex in very much smaller proportions than the first. The size distribution of some colloids was studied by ultrafiltration and permeation on gel. The preparation of colloidal rhenium sulphide and the technetium labelling conditions needed to obtain a very fine colloid were developed. The behaviour of technetium in the presence of colloidal rhenium sulphide and tin pyrophosphate was followed by sup(99m)Tc - sup(186)Re and sup(99m)Tc - sup(117m)Sn double-labelling tests. One reduced technetium fraction associates with the hydrolysed tin, the other follows the rhenium sulphide [fr

  1. Neutrophil labeling with [{sup 99m}Tc]-technetium stannous colloid is complement receptor 3-mediated and increases the neutrophil priming response to lipopolysaccharide

    Energy Technology Data Exchange (ETDEWEB)

    Gallagher, Hayley [School of Veterinary and Biomedical Sciences, James Cook University, Townsville, Queensland 4811 (Australia); Ramsay, Stuart C. [School of Medicine, James Cook University, Townsville, Queensland (Australia) and Townsville Nuclear Medicine, Mater Hospital, Townsville, Queensland 4812 (Australia)]. E-mail: stuart.ramsey@jcu.edu.au; Barnes, Jodie [School of Veterinary and Biomedical Sciences, James Cook University, Townsville, Queensland 4811 (Australia); Maggs, Jacqueline [Department of Nuclear Medicine, Townsville Hospital, Townsville, Queensland 4814 (Australia); Cassidy, Nathan [Townsville Nuclear Medicine, Mater Hospital, Townsville, Queensland 4812 (Australia); Ketheesan, Natkunam [School of Veterinary and Biomedical Sciences, James Cook University, Townsville, Queensland 4811 (Australia); School of Medicine, James Cook University, Townsville, Queensland (Australia)

    2006-04-15

    Introduction: [{sup 99m}Tc]-technetium stannous colloid (TcSnC)-labeled white cells are used to image inflammation. Neutrophil labeling with TcSnC is probably phagocytic, but the phagocytic receptor involved is not known. We hypothesised that complement receptor 3 (CR3) plays a key role. Phagocytic labeling could theoretically result in neutrophil activation or priming, affecting the behaviour of labeled cells. Fluorescence-activated cell sorter (FACS) analysis side scatter measurements can assess neutrophil activation and priming. Methods: We tested whether TcSnC neutrophil labeling is CR3-mediated by assessing if neutrophil uptake of TcSnC was inhibited by a monoclonal antibody (mAb) directed at the CD11b component of CR3. We tested if TcSnC-labeled neutrophils show altered activation or priming status, comparing FACS side scatter in labeled and unlabeled neutrophils and examining the effect of lipopolysaccharide (LPS), a known priming agent. Results: Anti-CD11b mAb reduced neutrophil uptake of TcSnC in a dose-dependent fashion. Labeled neutrophils did not show significantly increased side scatter compared to controls. LPS significantly increased side scatter in control cells and labeled neutrophils. However, the increase was significantly greater in labeled neutrophils than unlabeled cells. Conclusions: Neutrophil labeling with TcSnC is related to the function of CR3, a receptor which plays a central role in phagocytosis. TcSnC labeling did not significantly activate or prime neutrophils. However, labeled neutrophils showed a greater priming response to LPS. This could result in labeled neutrophils demonstrating increased adhesion on activated endothelium at sites of infection.

  2. Influence of Momordica charantia L. on the red and white blood cells labeling with 99mTc

    International Nuclear Information System (INIS)

    Brandao, Jose Odinilson de Caldas; Souza, Grace M. Lima de; Catanho, Maria T. Jansem de Almeida

    2008-01-01

    Full text: Momordica charantia L. is popularly known in Brazil as bitter melon and it's commonly used to treat several diseases as cancer, diabetes and to heal skin injuries. Many papers have been published showing the potential radio pharmacological activity of this plant due to its linkage with 99m Tc through some protein fractions of the extract. In this study, it was evaluated the influence of Momordica charantia L extract , labeling ( in vitro) of blood elements with sodium pertechnetate (Na 99m TcO 4 ). In the labeling of red blood cells (in vitro), blood samples were obtained from Wistar rats and incubated with different concentrations of M. charantia, for control group was used NaCl 0.9% and added stannous chloride (SnCl 2 ) and 99m Tc. The plasma fractions (P) and the cells (C) were separated and, also, precipitated with trichloroacetic acid at 5%, obtaining the soluble (SF) and insoluble (IF) fractions. The radioactivity rate (%ATl) of each fraction was calculated. The same methodology was applied for white blood cells but these cells were separated in advance by centrifugation at 1800 rpm during 15 minutes. There weren't alterations in the labeling of red blood cells in the concentrations tested of the extract when compared with the rate of the control group neither in the insoluble fractions. However, on the white blood cells it was noticed an increase in 99m Tc uptake in the presence of M. charantia extract. So its possible to conclude, based on previous results obtained by our group, that the M. charantia L. could be used to evaluate inflammatory processes. (author)

  3. An aqueous extract of Vitex agnus castus alters the labeling of blood constituents with technetium-99m

    Energy Technology Data Exchange (ETDEWEB)

    Costa, Maria Regina de Macedo; Ribeiro, Camila Godinho; Santos-Filho, Sebastiao David; Neves, Rosane de Figueiredo; Catanho, Maria Teresa Jansem de Almeida [Universidade Federal do Rio Grande do Norte, Natal, RN (Brazil). Centro de Ciencias da Saude]. E-mail: mariaregina.mr@terra.com.br; Fonseca, Adenilson de Souza da; Bernardo-Filho, Mario [Universidade do Estado do Rio de Janeiro (UERJ), Rio de Janeiro, RJ (Brazil). Inst. de Biologia Roberto Alcantara Gomes. Dept. de Biofisica e Biometria

    2007-09-15

    The development of experimental assays to study properties of herbal medicine is worthwhile. Vitex agnus castus (VAC) is utilized in popular medicine and some actions have been attributed to its extract. Blood cells (BC) and plasma proteins are labeled with technetium-99m (Tc-99m) and have been used in nuclear medicine, as in basic research. This procedure uses a reducing agent and stannous ion is utilized. There are reports that drugs can alter this labeling process. The aim of this work was to evaluate the influence of an aqueous extract of VAC on the labeling of blood constituents with Tc-99m. Blood was incubated with VAC, stannous chloride and Tc-99m, as sodium pertechnetate, and centrifuged. Samples of BC and plasma were separated, aliquots of BC and plasma were also precipitated with trichloroacetic acid to obtain soluble and insoluble fractions and the percentage of radioactivity (%ATI) was determined. The results show a statistical (p<0.05) alteration in the %ATI on blood compartments and on the insoluble fractions of plasma and BC. Probably, this extract would have chemical compounds with oxidant properties. (author)

  4. An aqueous extract of Vitex agnus castus alters the labeling of blood constituents with technetium-99m

    International Nuclear Information System (INIS)

    Costa, Maria Regina de Macedo; Ribeiro, Camila Godinho; Santos-Filho, Sebastiao David; Neves, Rosane de Figueiredo; Catanho, Maria Teresa Jansem de Almeida; Fonseca, Adenilson de Souza da; Bernardo-Filho, Mario

    2007-01-01

    The development of experimental assays to study properties of herbal medicine is worthwhile. Vitex agnus castus (VAC) is utilized in popular medicine and some actions have been attributed to its extract. Blood cells (BC) and plasma proteins are labeled with technetium-99m (Tc-99m) and have been used in nuclear medicine, as in basic research. This procedure uses a reducing agent and stannous ion is utilized. There are reports that drugs can alter this labeling process. The aim of this work was to evaluate the influence of an aqueous extract of VAC on the labeling of blood constituents with Tc-99m. Blood was incubated with VAC, stannous chloride and Tc-99m, as sodium pertechnetate, and centrifuged. Samples of BC and plasma were separated, aliquots of BC and plasma were also precipitated with trichloroacetic acid to obtain soluble and insoluble fractions and the percentage of radioactivity (%ATI) was determined. The results show a statistical (p<0.05) alteration in the %ATI on blood compartments and on the insoluble fractions of plasma and BC. Probably, this extract would have chemical compounds with oxidant properties. (author)

  5. Preoperative radiological diagnosis by 99mTc·MIBI-99mTc subtraction scintigraphy for primary hyperparathyroidism

    International Nuclear Information System (INIS)

    Inouye, Takahiro; Tomita, Toshiki; Shinden, Seiichi; Takagi, Hitoshi; Kano, Shigeru.

    1996-01-01

    Preoperative radiological diagnosis constitutes the most important factor for the surgical treatment of hyperparathyroidism. In this regard, MRI is useful for detecting the abnormal parathyroid, but it is often difficult to localize it using MRI only. It is thus necessary to combine this procedure with excellent subtraction scintigraphy. We performed both 201 Tl- 99m Tc and 99m Tc·MIBI- 99m Tc subtraction scintigraphy in seven patients with primary hyperparathyroidism and compared them the radiological results. Five patients presented parathyroid adenomas and the rest hypertrophy of the parathyroid. We could detect the abnormal parathyroid in four patients (57.1%) by 201 Tl- 99m Tc subtraction scintigraphy and in six patients (85.7%) by 99m Tc·MIBI- 99m Tc subtraction scintigraphy. We therefore believe that 99m Tc·MIBI- 99m Tc subtraction scintigraphy will become an essential examination for primary hyperparathyroidism rather than the presently employed 201 Tl- 99m Tc subtraction scintigraphy. (author)

  6. Evaluation of tricine and EDDA as Co-ligands for 99mTc-labeled HYNIC-MSH analogs for melanoma imaging.

    Science.gov (United States)

    Garcia, Maria Fernanda; Zhang, Xiuli; Gallazzi, Fabio; Fernandez, Marcelo; Moreno, Maria; Gambini, Juan Pablo; Porcal, Williams; Cabral, Pablo; Quinn, Thomas P

    2015-01-01

    Several radiolabeled alpha-melanocyte stimulating hormone (α-MSH) analogs have been studied for their abilities to target melanoma tumor cells through specific recognition and binding to the melanocortin receptor 1 (MCR1). In this work, a lactam bridgecyclized α-MSH analog was labeled with (99m) via the hydrazinonicotinamide (HYNIC) chelator and characterized for its melanoma tumor targeting properties. The bifunctional chelating agent HYNIC-Boc was attached to the N-terminus of the MSH peptide followed by the lactam cyclization, resulting in the HYNIC-cyc-MSH analog. The lactam cyclized peptide displayed high affinity and specificity for MC1-receptors present on B16/F1 melanoma tumor cells, exhibiting an IC50 of 6.48 nM. HYNIC-cyc-MSH was radiolabeled with (99m)Tc using two common co-ligands, tricine and EDDA. In vitro, the radiochemical stability, cell binding and efflux properties were similar between the peptides radiolabeled with tricine and EDDA as co-ligands. In vivo, biodistribution studies (n=4) demonstrated that (99m)Tc- HYNIC-cyc-MSH/tricine had superior tumor to muscle and tumor to blood ratios than (99m)Tc-HYNIC-cyc-MSH/EDDA at early time points. Planar gamma imaging of melanoma bearing mice showed that 99mTc-HYNIC-cyc-MSH/tricine was able to clearly visualize tumors, underscoring the potential utility of (99m)Tc labeled lactam cyclized MSH molecules as melanoma imaging agents.

  7. Evaluation of the absorbed dose to the kidneys due to Tc{sup 99m} (DTPA) / Tc{sup 99m} (Mag3) and Tc{sup 99m} (Dmsa); Evaluacion de la dosis absorbida en los rinones debido al Tc{sup 99m} (DTPA) / Tc{sup 99m} (MAG3) y Tc{sup 99m} (DMSA)

    Energy Technology Data Exchange (ETDEWEB)

    Vasquez A, M.; Murillo C, F.; Castillo D, C.; Rocha J, J.; Sifuentes D, Y.; Sanchez S, P. [Universidad Nacional de Trujillo, Av. Juan Pablo II s/n, Trujillo (Peru); Idrogo C, J.; Marquez P, F., E-mail: marvva@hotmail.com [Instituto Nacional de Enfermedades Neoplasicas, Av. Angamos 2520, Lima (Peru)

    2015-10-15

    The absorbed dose in the kidneys of adult patients has been assessed using the biokinetics of radiopharmaceuticals containing Tc{sup 99m} (DTPA) / Tc{sup 99m} (Mag3) or Tc{sup 99m} (Dmsa).The absorbed dose was calculated using the formalism MIRD and the Cristy-Eckerman representation for the kidneys. The absorbed dose to the kidneys due to Tc{sup 99m} (DTPA) / Tc{sup 99m} (Mag3), are given by 0.00466 mGy.MBq{sup -1} / 0.00339 mGy.MBq{sup -1}. Approximately 21.2% of the absorbed dose is due to the bladder (content) and the remaining tissue, included in biokinetics of Tc{sup 99m} (DTPA) / Tc{sup 99m} (Mag3). The absorbed dose to the kidneys due to Tc{sup 99m} (Dmsa) is 0.17881 mGy.MBq{sup -1}. Here, 1.7% of the absorbed dose is due to the bladder, spleen, liver and the remaining tissue, included in biokinetics of Tc{sup 99m} (Dmsa). (Author)

  8. Tc-99m Glu-Cys-Gly-His-Gly-Lys (ECG-HGK), a novel Tc-99m labeled hexapeptide for molecular tumor imaging.

    Science.gov (United States)

    Kim, Dae-Weung; Kim, Myoung Hyoun; Kim, Chang Guhn

    2016-03-01

    Domain 5 of kinin-free high molecular weight kininogen inhibits the adhesion of many tumor cell lines, and it has been reported that the histidine-glycine-lysine (HGK)-rich region might be responsible for inhibition of cell adhesion. The authors developed HGK-containing hexapeptide, glutamic acid-cysteine-glycine (ECG)-HGK, and evaluated the utility of Tc-99m ECG-HGK for tumor imaging. Hexapeptide, ECG-HGK was synthesized using Fmoc solid-phase peptide synthesis. Radiolabeling efficiency was evaluated. The uptake of Tc-99m ECG-HGK within HT-1080 cells was evaluated in vitro. In HT-1080 tumor-bearing mice, gamma imaging and biodistribution studies were performed. The complexes Tc-99m ECG-HGK was prepared in high yield. The uptake of Tc-99m ECG-HGK within the HT-1080 tumor cells had been demonstrated by in vitro studies. The gamma camera imaging in the murine model showed that Tc-99m ECG-HGK was accumulated substantially in the HT-1080 tumor (tumor-to-muscle ratio = 5.7 ± 1.4 at 4 h), and the tumoral uptake was blocked by the co-injection of excess HGK (tumor-to-muscle ratio = 2.8 ± 0.6 at 4 h). In the present study, Tc-99m ECG-HGK was developed as a new tumor imaging agents. Our in vitro and in vivo studies revealed specific function of Tc-99m ECG-HGK for tumor imaging. Copyright © 2016 John Wiley & Sons, Ltd.

  9. Synthesis, Characterization, and Preclinical Evaluation of (99m)Tc-Labeled Macrobicyclic and Tricyclic Chelators as Single Photon Emission Computed Tomography Tracer.

    Science.gov (United States)

    Yadav, Neelam; Chuttani, Krishna; Mishra, Anil K; Singh, Bachcha

    2016-05-01

    The novel tetraaza macrobicyclic chelator 3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene-2,10-dione (TBPD) and pentaaza macrotricyclic chelator 9-oxa-3,6,12,15,21-pentaazatricyclo[15,3,2,1]trieicos-1(21),17,19-triene-2,7,11,16-tetradione (OPTT) were synthesized, characterized, and radiolabeled with (99m)Tc to produce (99m)Tc-TBPD and (99m)Tc-OPTT. These radiolabeled complexes were prepared with high radiolabeling yield, radiochemical purity, and good in vitro stability up to 24 h. The labeling efficiency of (99m)Tc-TBPD and (99m)Tc-OPTT was found 98% and 97%. In vitro serum stability of (99m)Tc-TBPD was found to be 95.2%, while that of (99m)Tc-OPTT 94.2% up to 24 h. Blood kinetics experiments of (99m)Tc-labeled complexes showed biphasic pattern of blood clearance. About 99.57 ± 0.89% activity of (99m)Tc-TBPD and 99.42 ± 0.88% activity of (9m)Tc-OPTT were cleared off blood stream at 24 h postadministration. The biological half-life of (99m) Tc-TBPD was observed: t1/2(F) 1 h 5 min and t1/2(S) 12 h and biological half-life of (99m)Tc-OPTT was observed: t1/2(F) 1 h 10 min and t1/2(S) 9 h 50 min, respectively. The biodistribution studies revealed that maximum uptake of (99m)Tc-TBPD was found in liver, concluded that excretory pathway is hepatobiliary, while that of (99m)Tc-OPTT was renal as well as hepatobiliary. The negligible activity observed in stomach confirming the stability of radiolabeled complex in biological milieu. In vitro cytotoxicity study of TBPD and OPTT did not show any considerable antiproliferative activity against cancer cells of human cervical SW756, HeLa, and glioblastoma U-87, U373 cell lines. © 2015 John Wiley & Sons A/S.

  10. The preparation and biodistribution of 99mTc-cyclohexanedione dioxime and its methaneboronic acid adduct

    International Nuclear Information System (INIS)

    Luo Shineng; Xie Minhao; Xi Yuefen; Feng Yingying; Guo Yuzhi

    1993-01-01

    The preparation and biodistribution of 99m Tc-cyclohexanedione dioxime ( 99m Tc-CDO) and its methaneboronic acid adduct ( 99m Tc-CDO-MeB) are reported. The result shows that pH value exerts greater effect on the labelling yield of 99m Tc-CDO-MeB than that of 99m Tc-CDO. When pH value was 3.5-4.0, the labelling yield of 99m Tc-CDO-MeB was higher than 90%. Biodistribution experiment showed that 99m Tc-CDO-MeB was taken by heart and brain in the first few minutes after intravenous injection. The uptakes of 99m Tc-CDO-MeB by heart and brain were higher than those of 99m Tc-CDO

  11. Development of a formulation lyophilized for the obtention of a antimicrobial peptide Ubiquicidine labelled with {sup 99m} Tc; Desarrollo de una formulacion liofilizada para la obtencion del peptido antimicrobiano Ubiquicidina marcado con Tc-99m

    Energy Technology Data Exchange (ETDEWEB)

    Palomares R, P; Hernandez B, C A; Contreras N, G; Garcia P, M L; Pantoja H, I E [UAEM, Toluca (Mexico); Ferro F, G [ININ, A.P. 18-1027, 11801 Mexico D.F. (Mexico)

    2004-07-01

    The {sup 99m} Tc-UBI 29-41 are a labelled fragment of the antimicrobial human peptide Ubiquicidine proposed as a new radiopharmaceutical able to differentiate an infectious process of an inflammatory one through the gamma graphic image. It has been demonstrated that the {sup 99m} Tc-UBI 29-41 unite to bacteria in vitro and that accumulates in infection sites in human with minimum captivation in inflammation sites. In this work the development of a pharmaceutical lyophilized formulation is presented for the instantaneous marked one of the UBI 29-41 with {sup 99m} Tc. The selection of the components of the formulation settled down by means of the employment of an experimental design of 3 factors with mixed levels, evaluating the effect of the diluent type, concentration of tinny chloride and the reaction volume. The obtained formulations showed to be stable until for 6 months, being obtained complexes of the radiolabelled peptide with radiochemical purity > 95 % in sterile form and apirogen. The developed pharmaceutical form, will facilitate the routinary use of this new radiopharmaceutical in the diverse hospital departments of nuclear medicine. (Author)

  12. 99mTc-labelled HYNIC-minigastrin with reduced kidney uptake for targeting of CCK-2 receptor-positive tumours

    International Nuclear Information System (INIS)

    Guggenberg, E. von; Gabriel, M.; Virgolini, I.J.; Decristoforo, C.; Dietrich, H.; Skvortsova, I.

    2007-01-01

    Different attempts have been made to develop a suitable radioligand for targeting CCK-2 receptors in vivo, for staging of medullary thyroid carcinoma (MTC) and other receptor-expressing tumours. After initial successful clinical studies with [DTPA 0 ,DGlu 1 ]minigastrin (DTPA-MG0) radiolabelled with 111 In and 90 Y, our group developed a 99m Tc-labelled radioligand, based on HYNIC-MG0. A major drawback observed with these derivatives is their high uptake by the kidneys. In this study we describe the preclinical evaluation of the optimised shortened peptide analogue, [HYNIC 0 ,DGlu 1 ,desGlu 2-6 ]minigastrin (HYNIC-MG11). 99m Tc labelling of HYNIC-MG11 was performed using tricine and EDDA as coligands. Stability experiments were carried out by reversed phase HPLC analysis in PBS, PBS/cysteine and plasma as well as rat liver and kidney homogenates. Receptor binding and cell uptake experiments were performed using AR4-2J rat pancreatic tumour cells. Animal biodistribution was studied in AR4-2J tumour-bearing nude mice. Radiolabelling was performed at high specific activities and radiochemical purity was >90%. 99m Tc-EDDA-HYNIC-MG11 showed high affinity for the CCK-2 receptor and cell internalisation comparable to that of 99m Tc-EDDA-HYNIC-MG0. Despite high stability in solution, a low metabolic stability in rat tissue homogenates was found. In a nude mouse tumour model, very low unspecific retention in most organs, rapid renal excretion with reduced renal retention and high tumour uptake were observed. 99m Tc-EDDA-HYNIC-MG11 shows advantages over 99m Tc-EDDA-HYNIC-MG0 in terms of lower kidney retention with unchanged uptake in tumours and CCK-2 receptor-positive tissue. However, the lower metabolic stability and impurities formed in the labelling process still leave room for further improvement. (orig.)

  13. Solid phase reduction of 99mTcO4radical with zinc: a method for the preparation of difficult 99mTc complexes

    International Nuclear Information System (INIS)

    Kremer, C.; Leon, A.; Gambino, D.; Cartesio, S.; Ures, C.; Savio, E.; Campos, E.; Kremer, E.

    1989-01-01

    Two groups of compounds: aminoacids (glutamic acid, glutamine, glycine, lysine) and amines (ethylenediamine, diethylenetriamine, o-phenantroline, o-phenylenediamine) have been labelled with 99m Tc by means of a solid phase reduction using fine powdered zinc as reducing agent. In all cases radiochemical purity in excess of 90% was obtained, with no evidence of colloid formation. Labelling yields were variable depending on the ligand used. The results show that the method presented allows labelling some molecules with 99m Tc for which the use of conventional techniques are not feasible. (author)

  14. Preparation of 99mTc-thiourea complex as a precursor for Tc(III) labeled compounds

    International Nuclear Information System (INIS)

    Rey, A.; Teran, M.; Molina, S.; Leon, A.; Kremer, C.; Gambino, D.; Kremer, E.

    1996-01-01

    Ligand exchange is one of the possible synthetic routes to obtain 99m Tc coordination compounds. However, the success of this route depends on the availability of good precursors. The objective of this work is the preparation of the complex [ 99m Tc (tu) 6 ] 3+ (tu = thiourea), as a potential precursor for 99m Tc(III) coordination compounds. The preparation was successfully performed in acidic conditions, the excess of tu serving as reducing agent. At pH values higher than 3, the compound becomes unstable and on addition of polydentate ligands new Tc(III) complexes are formed. With edta, the complex 99m Tc(III)-edta was obtained in high yield. (author). 13 refs., 3 tabs

  15. Scintigraphy with 99mTc labelled polyclonal human IgG in rheumatoid arthritis patients

    International Nuclear Information System (INIS)

    Stanchev, V.; Batalov, A.; Atanasov, A.

    1999-01-01

    The study design to assess the diagnostic relevance of scintigraphy with 99m Tc labelled polyclonal human IgG (HIG) for detecting active synovitis in rheumatoid arthritis patients. Fifteen patients presenting rheumatoid arthritis and 3 healthy volunteers are studied on digital camera (Diacam, Siemens). Following iv injection of 500 MBq 99m Tc - HIG, a 3- phase scintigraphy of the knee joints is performed and 4 hours later multiple planar views of the peripheral joint are recorded. Scintigraphic data are comparatively studied with the clinical indicators pointing to active synovitis - joint swellings and pain. Markedly expressed 99m Tc - HIG uptake is noted in joints apparently the most actively involved in the arthritis process clinically, whereas most of the joints without evidence of active synovitis revealed background activity only. The obtained scintigraphic results correlate strongly with the clinical indicator joint swelling (93.2%), and somewhat less with the presence of pain (81.5%). 13.5 per cent of the joints without clinically detectable swelling and 25.6% those free of pain are HIG-positive. 99m Tc - HIG scintigraphy is a highly sensitive noninvasive method of detecting active synovitis, promoting objective assessment of the joint inflammatory process in the course of treatment and follow-up study of rheumatoid arthritis patients

  16. Experimental study of per-rectal portal scintigraphy using 99mTc-EHIDA

    International Nuclear Information System (INIS)

    Tamaki, Satoshi; Shinotsuka, Akira; Takenaka, Hiroki

    1991-01-01

    We discovered that 99m Tc-diethyl iminodiacetic acid ( 99m Tc-EHIDA) commonly used for hepatobiliary scintigraphy could also be administered per-rectally, with adequate absorption and optimal visualization of the portal system. To evaluate its usefulness, we experimented on rabbits using the method. Portal scintigraphy with rectal administration of 99m Tc-EHIDA, 123 I-N-isopropyl-p-iodoamphetamine ( 123 I-IMP) and 99m Tc-red blood cell ( 99m Tc-RBC) were performed in normal rabbits and in extrahepatic portal shunt model rabbits. Images of the liver and thorax were obtained and shunt indices were calculated from the count values of liver and lung or heart. Then the shunt indices were compared with shunt rate derived from direct injection of 99m Tc-macroaglutinated albumin ( 99m Tc-MAA) into inferior mesenteric vein. Correlation between shunt rate of 99m Tc-MAA and shunt indices of 99m Tc-RBC, 123 I-IMP and 99m Tc-EHIDA were 0.64, 0.75 and 0.78, respectively, with 99m Tc-EHIDA having the most favorable results. We concluded that 99m Tc-EHIDA per-rectal portal scintigraphy is a noninvasive, quantitative, inexpensive and simple method for evaluation of portal circulation system. Also, we think that this method would be applicable to human usage from our experience with normal volunteers. (author)

  17. Nuclear medicine: Monoclonal antibodies

    International Nuclear Information System (INIS)

    Endo, K.; Sakahara, H.; Koizumi, M.; Kawamura, Y.; Torizuka, K.; Yokoyama, A.

    1986-01-01

    Antitumor monoclonal antibody was successfully labeled with Tc-99m by using dithiosemicarbazone (DTS) as a bifunctional chelating agent. In the first step, DTS was coupled to antibody without loss of immunoreactivity; the compound then efficiently formed a neutral 1:1 chelate with pentavalent or tetravalent Tc-99m. Imaging with Tc-99m-labeled monoclonal antibody to human osteosarcoma (OST-7) clearly displayed a small tumor in nude mice at 6 and 24 hours after intravenous administration. The tumor-to-blood ratio of the Tc-99m-labeled monoclonal antibody was higher than that of a radioiodinated antibody and similar to that of an In-111-labeled antibody. Thus, conjugation of DTS to monoclonal antibody followed by radiometalation is a simple and efficient method of preparing Tc-99m-labeled monoclonal antibody

  18. {sup 99} {sup m}Tc-sulphur-colloid and heat-denatured {sup 99} {sup m}Tc-labelled red cell scans demonstrating a giant intrapelvic spleen in a girl after splenectomy

    Energy Technology Data Exchange (ETDEWEB)

    Kao, P.F. [Dept. of Nuclear Medicine, Chang Gung Memorial Hospital and Chang Gung University School of Medicine, Tauyuan, Taiwan (Taiwan); Dept. of Nuclear Medicine, Chang Gung Memorial Hospital, Taipei, Taiwan (Taiwan); Tzen, K.Y.; Tsai, M.F. [Dept. of Nuclear Medicine, Chang Gung Memorial Hospital and Chang Gung University School of Medicine, Tauyuan, Taiwan (Taiwan); Lin, J.N. [Dept. of Paediatric Surgery, Chang Gung Childrens Hospital and Chang Gung University School of Medicine, Tauyuan, Taiwan (Taiwan)

    2001-04-01

    A 17 x 12 x 5-cm giant intrapelvic mass in a 14-year-old girl is reported. This mass developed 6 years after a splenectomy for splenic torsion. The heat-denatured {sup 99} {sup m}Tc-labelled red cell scan and {sup 99} {sup m}Tc- sulphur-colloid scan confirmed the specific red cell sequestration function and reticuloendothelial activity in the giant intrapelvic spleen. The size and development of the giant intrapelvic spleen are unusual. The usefulness of functional images to diagnosis the nature of the intrapelvic mass is well demonstrated. (orig.)

  19. Safety, biodistribution, pharmacokinetics, and immunogenicity of 99mTc-labeled humanized monoclonal antibody BIWA 4 (bivatuzumab) in patients with squamous cell carcinoma of the head and neck.

    Science.gov (United States)

    Colnot, David R; Roos, Jan C; de Bree, Remco; Wilhelm, Abraham J; Kummer, J Alain; Hanft, Gertraud; Heider, Karl-Heinz; Stehle, Gerd; Snow, Gordon B; van Dongen, Guus A M S

    2003-09-01

    Previous studies have shown the potential of murine and chimeric anti-CD44v6 monoclonal antibodies (MAbs) for radioimmunotherapy (RIT) of head and neck squamous cell carcinoma (HNSCC). A limitation of these MAbs, however, appeared to be their immunogenicity. Therefore, humanized monoclonal antibody BIWA 4 (bivatuzumab), with an intermediate affinity for CD44v6, was recently selected. As a prelude to RIT, we evaluated the safety, tumor-targeting potential, pharmacokinetics, and immunogenicity of technetium-99m-labeled BIWA 4 in patients undergoing operations for primary HNSCC in this study. Ten patients were treated at BIWA 4 dose levels of 25 mg (n=3), 50 mg (n=4), and 100 mg (n=3). Patients received 2 mg of 750 MBq 99mTc-BIWA 4, together with 23-, 48-, and 98-mg unlabeled BIWA 4, respectively. Radioimmunoscintigraphy (RIS) was performed within 1 h and after 21 h, and patients underwent surgery at 48 h after injection. Biodistribution of 99mTc-BIWA 4 was evaluated by radioactivity measurements in blood, bone marrow, and in biopsies of a surgical specimen obtained 48 h after injection. BIWA 4 concentration in blood was assessed by ELISA and high performance liquid chromatography and related to soluble CD44v6 levels in serum samples. The development of human anti-human antibody (HAHA) responses was determined. Administration of 99mTc-BIWA 4 was well tolerated by all patients and no HAHA responses were observed. A mean t1/2 in plasma of 54.8 +/- 11.5 h, 76.1 +/- 21.8 h, and 68.5 +/- 21.2 h was found for the 25-, 50-, and 100-mg dose group, respectively. No complex formation of BIWA 4 with soluble CD44v6 in blood was observed. RIS showed targeting of primary tumors and lymph node metastases in 8 of 10 and 1 of 5 patients, respectively. The highest tumor uptake and tumor to nontumor ratios were observed for the 50-mg dose group. Tumor uptake was 12.9 +/- 5.9, 26.2 +/- 3.1, and 15.4 +/- 1.9% of the injected dose (ID)/kg for the 25-, 50-, and 100-mg dose group

  20. 99mTc ovalbumin labelled eggs for gastric emptying scintigraphy: in-vitro comparison of solid food markers.

    Science.gov (United States)

    Blanc, Frédérique; Salaun, Pierre Y; Couturier, Olivier; Querellou, Solène; Le Duc-Pennec, Alexandra; Mougin-Degraef, Marie; Bizais, Yves; Legendre, Jean M

    2005-11-01

    The reliability of solid phase gastric emptying measurements by scintigraphy requires a marker that remains within the solid component of the test meal, and which is not degraded by the gastric juice throughout the scintigraphic procedure. In Europe, foods are most often labelled with 99mTc rhenium sulfide macrocolloid (RSMC) but this solid phase marker was withdrawn from the market in January 2004. To test other potential solid phase markers and to compare them to the reference marker RSMC. These markers were rhenium sulfide nanocolloid (RSNC), tin fluoride colloid (TFC), phytates and two albumins (Alb and AlbC). All were radiolabelled with 99mTc. After quality control, each 99mTc marker was incorporated into the albumin of one egg. Then, egg white and yolk were mixed together, and a well-cooked omelette was prepared. Aliquots of the omelette were incubated with an acidic solution of pepsin at 37 degrees C which mimicked gastric juice. Unbound radioactivity in the supernatant fraction was measured at various times up to 3 h. The radiochemical purity was > 95% for all radiopharmaceuticals. During the in-vitro incubation, the percentage of 99mTc labelled colloids released from the omelette increased continuously: after 3 h, 5% for TFC and RSMC, 8% for phytates, and > 9% for the two albumins and RSNC. Considering quality controls and release of 99mTc during in-vitro incubation of the omelette, TFC showed the same behaviour as the reference marker RSMC. Thus, TFC seems to be the best candidate to replace RSMC for the radiolabelling of the solid phase of the gastric emptying test meal.

  1. Preparation of 99mTc-Ancitabine as a Possible Tumor Imaging Agent

    International Nuclear Information System (INIS)

    Ibrahim, I.T.; Attallah, K.M.

    2010-01-01

    Ancitabine is one of the potent chemotherapeutic anticancer drugs. Tc-Ancitabine ( 99m Tc-ANC) was prepared using stannous chloride as reducing agent, which produced yield above 90% at ph 4 at room temperature within 1-5 min as reaction time. The labeled drug was stable for more than 8 h post labeling. Biodistribution study of 99m Tc-ANC in normal mice reflected that its uptake was increased in organ of high proliferation like stomach. In solid tumor bearing mice 99m Tc-ANC was incorporated rapidly in tumor site and declined slowly, while it was declined rapidly from other tissues. Biodistribution of 99m Tc-ANC in solid tumor presented a possible model for imaging of tumors.

  2. EGF receptor targeted tumor imaging with biotin-PEG-EGF linked to 99mTc-HYNIC labeled avidin and streptavidin

    International Nuclear Information System (INIS)

    Jung, Kyung-Ho; Park, Jin Won; Paik, Jin-Young; Quach, Cung Hoa Thien; Choe, Yearn Seong; Lee, Kyung-Han

    2012-01-01

    Introduction: As direct radiolabeled peptides suffer limitations for in vivo imaging, we investigated the usefulness of radioloabeled avidin and streptavidin as cores to link peptide ligands for targeted tumor imaging. Methods: Human epidermal growth factor (EGF) was site specifically conjugated with a single PEG-biotin molecule and linked to 99m Tc-HYNIC labeled avidin-FITC (Av) or streptavidin-Cy5.5 (Sav). Receptor targeting was verified in vitro, and in vivo pharmacokinetic and biodistribution profiles were studied in normal mice. Scintigraphic imaging was performed in MDA-MB-468 breast tumor xenografted nude mice. Results: Whereas both 99m Tc-Av-EGF and 99m Tc-Sav-EGF retained receptor-specific binding in vitro, the two probes substantially diverged in pharmacokinetic and biodistribution behavior in vivo. 99m Tc-Av-EGF was rapidly eliminated from the circulation with a T1/2 of 4.3 min, and showed intense hepatic accumulation but poor tumor uptake (0.6%ID/gm at 4 h). 99m Tc-Sav-EGF displayed favorable in vivo profiles of longer circulation (T1/2β, 51.5 min) and lower nonspecific uptake that resulted in higher tumor uptake (3.8 %ID/gm) and clear tumor visualization at 15 h. Conclusion: 99m Tc-HYNIC labeled streptavidin linked with growth factor peptides may be useful as a protein-ligand complex for targeted imaging of tumor receptors.

  3. Technetium-99m labelled fluconazole and antimicrobial peptides for imaging of Candida albicans and Aspergillus fumigatus infections

    Energy Technology Data Exchange (ETDEWEB)

    Lupetti, Antonella [Department of Infectious Diseases, Leiden University Medical Center (LUMC), Leiden (Netherlands); Dipartimento di Patologia Sperimentale, Biotecnologie Mediche, Univ. di Pisa (Italy); Welling, Mick M. [Department of Radiology, Division of Nuclear Medicine, LUMC, Leiden (Netherlands); Mazzi, Ulderico [Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Padova (Italy); Nibbering, Peter H. [Department of Infectious Diseases, Leiden University Medical Center (LUMC), Leiden (Netherlands); Pauwels, Ernest K.J. [Department of Radiology, Division of Nuclear Medicine, LUMC, Leiden (Netherlands); Department of Radiology, Leiden University Medical Center (LUMC) (Netherlands)

    2002-05-01

    The aim of this study was to investigate whether technetium-99m labelled fluconazole can distinguish fungal from bacterial infections. Fluconazole was labelled with {sup 99m}Tc and radiochemical analysis showed less than 5% impurities. The labelling solution was injected into animals with experimental infections. For comparison, we used two peptides for infection detection, i.e. UBI 29-41 and hLF 1-11, and human IgG, all labelled with {sup 99m}Tc. Mice were infected with Candida albicans or injected with heat-killed C. albicans or lipopolysaccharides to induce sterile inflammation. Also, mice were infected with Staphylococcus aureus or Klebsiella pneumoniae. Next, accumulation of {sup 99m}Tc-fluconazole and {sup 99m}Tc-labelled peptides/IgG at affected sites was determined scintigraphically. {sup 99m}Tc-fluconazole detected C. albicans infections (T/NT ratio=3.6{+-}0.47) without visualising bacterial infections (T/NT ratio=1.3{+-}0.04) or sterile inflammatory processes (heat-killed C. albicans: T/NT ratio=1.3{+-}0.2; lipopolysaccharide: T/NT ratio=1.4{+-}0.1). C. albicans infections were already seen within the first hour after injection of {sup 99m}Tc-fluconazole (T/NT ratio=3.1{+-}0.2). A good correlation (R{sup 2}=0.864; P<0.05) between T/NT ratios for this tracer and the number of viable C. albicans was found. Although {sup 99m}Tc-UBI 29-41 and {sup 99m}Tc-hLF 1-11 were able to distinguish C. albicans infections from sterile inflammatory processes in mice, these {sup 99m}Tc-labelled peptides did not distinguish these fungal infections from bacterial infections. It is concluded that {sup 99m}Tc-fluconazole distinguishes infections with C. albicans from bacterial infections and sterile inflammations. (orig.)

  4. Development of instant kits 99Tcm-labelling of anti-CEA antibody and hIgG for scintigraphy

    International Nuclear Information System (INIS)

    Boonkittcharoen, V.

    1998-01-01

    99 Tc m -labelled monoclonal antibodies (MAbs) and human immunoglobulins (hIgG) have recently emerged as a new class of site specific radiopharmaceuticals. The role of 99 Tc m -labelled MAbs particularly anti-CEA IgG in tumour imaging has essentially established for early revealing of occult lesions in patients. Superiority of the method over X ray CT has been addressed for its capability in differentiating post-operation fibrosis from viable tumour. At present data, instant kits for preparation of this particular class of radiopharmaceuticals can be obtained from commercial sources but unfortunately at high prices. This prohibits the use of these promising diagnostic agents in developing country like Thailand. Under the assistance from IAEA through a research coordinating program, we worked on the 99 Tc m -radiochemistry in immunoglobulin labelling to establish the knowledge and acquire the know how in the development of in-house instant kits at low cost to serve the local nuclear medicine clinics in diagnosis of infectious and neoplastic diseases

  5. [99mTc[TRODAT-1: a novel technetium-99m complex as a dopamine transporter imaging agent

    International Nuclear Information System (INIS)

    Kung Meiping; Stevenson, D.A.; Ploessl, K.; Meegalla, S.K.; Beckwith, A.; Essman, W.D.; Mu, M.; Lucki, I.; Kung, H.F.

    1997-01-01

    Technetium-99m is the most commonly used radionuclide in routine nuclear medicine imaging procedures. Development of 99m Tc-labeled receptor-specific imaging agents for studying the central nervous system is potentially useful for evaluation of brain function in normal and disease states. A novel 99m Tc-labeled tropane derivative, [ 99m Tc[TRODAT-1, which is useful as a potential CNS dopamine transporter imaging agent, was evaluated and characterized. After i.v. injection into rats, [ 99m Tc[TRODAT-1 displayed specific brain uptake in the rat striatal region (striatum-cerebellum/cerebellum ratio 1.8 at 60 min), where dopamine neurons are concentrated. The specific striatal uptake could be blocked by pretreating rats with a dose of competing dopamine transporter ligand, β-CIT (or RTI-55, i.v., 1 mg/kg). However, the specific striatal uptake of [ 99m Tc[TRODAT-1 was not affected by co-injection of excess free ligand (TRODAT-1, up to 200 μg per rat) or by pretreating the rats with haloperidol (i.v., 1 mg/kg). The specific uptake in striatal regions of rats that had prior 6-hydroxydopamine lesion in the substantia nigra area showed a dramatic reduction. The radioactive material recovered from the rat striatal homogenates at 60 min after i.v. injection of [ 99m Tc[TRODAT-1 showed primarily the original compound (>95%), a good indication of in vivo stability in brain tissue. Similar and comparable organ distribution patterns and brain regional uptakes of [ 99m Tc[TRODAT-1 were obtained for male and female rats. (orig./AJ). With 4 figs., 6 tabs

  6. Technetium 99m-labeled annexin v scintigraphy of platelet activation in vegetations of experimental endocarditis

    International Nuclear Information System (INIS)

    Rouzet, F.; Sarda-Mantel, L.; Le Guludec, D.; Rouzet, F.; Sarda-Mantel, L.; LeGuludec, D.; Rouzet, F.; Sarda-Mantel, L.; Le Guludec, D.; Hernandez, M.D.; Louedec, L.; Michel, J.B.; Hervatin, F.; Lefort, A.; Fantin, B.; Duval, X.; Duval, X.; Hernandez, M.D.

    2008-01-01

    Background: The pathophysiology of infective endocarditis involves a pathogen/host tissue interaction, leading to formation of infected thrombotic vegetations. Annexin V is a ligand of phosphatidyl-serines exposed by activated platelets and apoptotic cells. Because vegetations are platelet-fibrin clots in which platelet pro-aggregant activity is enhanced by bacterial colonization, we investigated the ability of annexin V labeled with technetium 99m Tc ( 99m Tc-ANX) to provide functional imaging of these vegetations in experimental models of infective endocarditis. This ability was assessed in rabbits and rats because of the different interest of these 2 species in preclinical analysis. Methods and Results: Non-bacterial thrombotic endocarditis was induced with the use of a catheter left indwelling through the aortic or tricuspid valve, and animals were injected with either a bacterial inoculum or saline. Scintigraphic investigations were performed 5 days later and showed a higher 99m Tc-ANX uptake by vegetations in infected versus non-infected animals (ratio,1.3 for in vivo acquisitions and 2 for autoradiography; P ≤ 0.0001 for all), whereas no significant uptake was present in controls. Right-sided endocarditis was associated with pulmonary uptake foci corresponding to emboli. Histological analysis of vegetations showed a specific uptake of 99m Tc-ANX at the interface between circulating blood and vegetation. In parallel, underlying myocardial tissue showed myocyte apoptosis and mucoid degeneration, without extracellular matrix degradation at this stage. Conclusions: 99m Tc-ANX is suitable for functional imaging of platelet-fibrin vegetations in endocarditis, as well as embolic events. 99m Tc-ANX uptake reflects mainly platelet activation in the luminal layer of vegetations. This uptake is enhanced by bacterial colonization. (authors)

  7. Design and evaluation of new Tc-99m-labeled lactam bridge-cyclized alpha-MSH peptides for melanoma imaging.

    Science.gov (United States)

    Guo, Haixun; Gallazzi, Fabio; Miao, Yubin

    2013-04-01

    The purpose of this study was to examine the melanoma targeting and imaging properties of new (99m)Tc-labeled lactam bridge-cyclized alpha-melanocyte stimulating hormone (α-MSH) peptides using bifunctional chelating agents. MAG3-GGNle-CycMSH(hex), AcCG3-GGNle-CycMSH(hex), and HYNIC-GGNle-CycMSH(hex) peptides were synthesized, and their melanocortin-1 (MC1) receptor binding affinities were determined in B16/F1 melanoma cells. The biodistribution of (99m)Tc-MAG3-GGNle-CycMSH(hex), (99m)Tc-AcCG3-GGNle-CycMSH(hex), (99m)Tc(CO)3-HYNIC-GGNle-CycMSH(hex), and (99m)Tc(EDDA)-HYNIC-GGNle-CycMSH(hex) were determined in B16/F1 melanoma-bearing C57 mice at 2 h postinjection to select a lead peptide for further evaluation. The melanoma targeting and imaging properties of (99m)Tc(EDDA)-HYNIC-GGNle-CycMSH(hex) were further examined because of its high melanoma uptake and fast urinary clearance. The IC50 values of MAG3-GGNle-CycMSH(hex), AcCG3-GGNle-CycMSH(hex), and HYNIC-GGNle-CycMSH(hex) were 1.0 ± 0.05, 1.2 ± 0.19, and 0.6 ± 0.04 nM in B16/F1 melanoma cells, respectively. Among these four (99m)Tc-peptides, (99m)Tc(EDDA)-HYNIC-GGNle-CycMSH(hex) exhibited the highest melanoma uptake (14.14 ± 4.90% ID/g) and fastest urinary clearance (91.26 ± 1.96% ID) at 2 h postinjection. (99m)Tc(EDDA)-HYNIC-GGNle-CycMSH(hex) showed high tumor to normal organ uptake ratios except for the kidneys. The tumor/kidney uptake ratios of (99m)Tc(EDDA)-HYNIC-GGNle-CycMSH(hex) were 2.50 and 3.55 at 4 and 24 h postinjection. The melanoma lesions were clearly visualized by SPECT/CT using (99m)Tc(EDDA)-HYNIC-GGNle-CycMSH(hex) as an imaging probe at 2 h postinjection. Overall, high melanoma uptake coupled with fast urinary clearance of (99m)Tc(EDDA)-HYNIC-GGNle-CycMSH(hex) highlighted its potential for metastatic melanoma detection in the future.

  8. Regional differences between 99mTc-ECD and 99mTc-HMPAO SPET in perfusion changes with age and gender in healthy adults

    International Nuclear Information System (INIS)

    Inoue, Kentaro; Nakagawa, Manabu; Goto, Ryoi; Kinomura, Shigeo; Sato, Tachio; Sato, Kazunori; Fukuda, Hiroshi

    2003-01-01

    A number of studies using single-photon emission tomography (SPET) have shown perfusion changes with age in several cortical and subcortical areas, which might distort the results of perfusion imaging studies of neuropsychiatric disorders. Technetium-99m labelled ethyl cysteinate dimer (ECD) and hexamethylpropylene amine oxime (HMPAO) are both used as markers of cerebral perfusion, but have different pharmacokinetics and retention patterns. The aim of this study was to determine whether age and gender effects on perfusion SPET differ depending on whether 99m Tc-HMPAO or 99m Tc-ECD is used. Forty-five subjects (20 male and 25 female, mean age 52.8±6.6 years) were assigned to 99m Tc-HMPAO SPET (HMPAO group), and 39 subjects (24 male and 15 female, mean age 52.6±6.7 years) to 99m Tc-ECD SPET (ECD group). SPET images were obtained about 10 min after intravenous injection of approximately 800 MBq 99m Tc-HMPAO or 99m Tc-ECD using the same SPET scanner. Three-dimensional volumetric magnetic resonance imaging was performed to as7sess morphological changes in the grey matter. All image processing and statistical analyses were performed using SPM99 software. An area in the right anterior frontal lobe showed an increase in perfusion with age only in the HMPAO group, whereas areas in the bilateral retrosplenial cortex showed decreases in perfusion with age only in the ECD group; neither group showed corresponding changes in the grey matter. The present study shows that different effects of age on perfusion are observed depending on whether 99m Tc-HMPAO and 99m Tc-ECD is used. This suggests that the results of perfusion SPET are differently confounded depending on the tracer used, and that perfusion SPET with these tracers has limitations when used in research on subtle perfusion changes. (orig.)

  9. Quality control and testing of 99 sup (m) Tc-macroaggregated albumin

    International Nuclear Information System (INIS)

    Darte, L.; Persson, B.R.R.

    1975-06-01

    33 sup(m)Tc-labelled macroaggregated albumin particles prepared from a commercial 'kit' have been tested in detail. With the introduction of the method of gel chromatography column scanning it became possible to make fast and simple quantitative measurements of the radiochemical purity. This was found to be the only reliable method for quantitative determination of non-aggregated sup(99m)Tc-labelled albumin. The measuring results of the kit in question have shown a labelling efficiency of about 97-99 %. In addition to a few percent of sup(99m)Tc-pertechnetate less than 0.5 % of disturbing radioactivity was found. The labelling was stable for at least 5-6 h. About 80 % of the particles are in the size-range of 10-80 μm. A rough estimation of the number of particles in the solution resulted in 0.5 x 10 6 per mg of MAA. The dynamic studies of the lung uptake and the elimination of sup(99m)Tc-MAA in man resulted in a biological half-time in the lungs of about 1-2 h. The radiation absorbed dose to the lungs per mCi administrered sup(99m)Tc-MAA was estimated to 0.1 rad. Less than 1 % of the radioactivity was accumulated in liver, spleen or kidneys during the first 25 minutes after injection. (author)

  10. Molecular imaging of atherosclerotic plaques with technetium-99m-labelled antisense oligonucleotides

    International Nuclear Information System (INIS)

    Qin Guangming; Zhang Yongxue; Cao Wei; An Rui; Gao Zairong; Xu Wendai; Zhang Kaijun; Li Guiling; Li Shuren

    2005-01-01

    The purpose of this study was to visualise experimental atherosclerotic lesions using radiolabelled antisense oligonucleotides (ASONs). Atherosclerosis was induced in New Zealand White rabbits fed 1% cholesterol for approximately 60 days. In vivo and ex vivo imaging was performed in atherosclerotic rabbits and normal control rabbits after i.v. injection of 92.5±18.5 MBq 99m Tc-labelled ASON or 99m Tc-labelled sense oligonucleotides. Immediately after the in vivo imaging, the animals were sacrificed and ex vivo imaging of the aortic specimens was performed. Biodistribution of radiolabelled c-mycASON was evaluated in vivo in atherosclerotic rabbits. Planar imaging revealed accumulation of 99m Tc-labelled c-mycASON in atherosclerotic lesions along the artery wall. Ex vivo imaging further demonstrated that the area of activity accumulation matched the area of atherosclerotic lesions. In contrast, no atherosclerotic lesions were found in the vessel wall and no positive imaging results were obtained in animals of the control group. This molecular imaging approach has potential for non-invasive imaging of atherosclerotic plaques at an early stage. (orig.)

  11. Pharmacokinetics of the FO23C5 anti-CEA antibody fragment labelled with 99Tcm and 111In: a comparison in patients

    International Nuclear Information System (INIS)

    Hnatowich, D.J.; Mardirossian, G.; Rusckowski, M.; Roy, S.; Busche, H.; Griffin, T.W.; Brill, A.B.

    1993-01-01

    The FO23C5 anti-carcinoembryonic antigen (CEA) F(ab') 2 antibody was radiolabelled with sup(111)In via diethylenetriaminepentaacetic acid (DTPA) and directly with 99 Tc m by stannous ion and mercaptoethanol antibody reduction to compare the pharmacokinetics of these three agents. Four patients received 15 mCi 99 Tc m -Fab' 1 week before receiving 1 mCi 111 In-F(ab') 2 . Five additional patients received only the 99 Tc m -Fab'. The biodistribution of 99 Tc m was as expected for a labelled Fab' fragment: relative to 111 In, 99 Tc m cleared rapidly from circulation and into kidneys and urine. Liver levels of 111 In and 99 Tc m were surprisingly similar at 1 day although initial 111 In levels were lower and increased while 99 Tc m levels were higher and decreased. Spleen levels were also similar. In 4/9 patients receiving 99 Tc m , hepatobiliary clearance was observed at levels which could confuse interpretation whereas this mode of clearance was observed in only 1/4 patients receiving 111 In. Image quality was superior with 111 In versus 99 Tc m at 1 day postadministration as judged by counting rates and background activity whereas the opposite was true at 2-3 h postadministration. (author)

  12. Pharmaceutical grade sodium (99mTc) pertechnetate from 99Mo/99mTc-TCM-Autosolex generator

    International Nuclear Information System (INIS)

    Chattopadhyay, Sankha; Barua, Luna; Das, Sujata Saha

    2014-01-01

    Technetium-99m (T 1/2 = 6.02h; 140.51 keV (89%)) is the most useful radioisotope in diagnostic nuclear medicine. More than 80% of all diagnostic procedures done worldwide in nuclear medicine centre are performed with 99m Tc. Worldwide crisis of fission 99 Mo based generator in recent past had put the nuclear medicine fraternity in very harsh situation. In order to have an indigenous solution of this problem, we tried to develop a computer controlled semi automated 99 Mo/ 99m Tc generator using MEK solvent extraction technique, which utilizes abundantly available 99 Mo produced by (n,γ) reaction in BARC reactors. The aim of this work is to provide a more reliable, computer controlled module (TCM- AUTOSOLEX) for the recovery of pharmaceutical grade 99m Tc from low specific activity 99 Mo based on solvent extraction methodology

  13. Radiolabeling of rituximab with {sup 188}Re and {sup 99m}Tc using the tricarbonyl technology

    Energy Technology Data Exchange (ETDEWEB)

    Dias, Carla Roberta [Instituto de Pesquisas Energeticas e Nucleares, Av. Professor Lineu Prestes 2242, 05508-000 Sao Paulo (Brazil); Jeger, Simone [Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Paul Scherrer Institute, 5232 Villigen-PSI (Switzerland); Osso, Joao Alberto [Instituto de Pesquisas Energeticas e Nucleares, Av. Professor Lineu Prestes 2242, 05508-000 Sao Paulo (Brazil); Mueller, Cristina; De Pasquale, Christine; Hohn, Alexander; Waibel, Robert [Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Paul Scherrer Institute, 5232 Villigen-PSI (Switzerland); Schibli, Roger, E-mail: roger.schibli@psi.c [Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Paul Scherrer Institute, 5232 Villigen-PSI (Switzerland); Department of Chemistry and Applied Biosciences of the ETH, 8093 Zurich (Switzerland)

    2011-01-15

    Introduction: The most successful clinical studies of immunotherapy in patients with non-Hodgkin's lymphoma (NHL) use the antibody rituximab (RTX) targeting CD20{sup +} B-cell tumors. Rituximab radiolabeled with {beta}{sup -} emitters could potentiate the therapeutic efficacy of the antibody by virtue of the particle radiation. Here, we report on a direct radiolabeling approach of rituximab with the {sup 99m}Tc- and {sup 188}Re-tricarbonyl core (IsoLink technology). Methods: The native format of the antibody (RTX{sub wt}) as well as a reduced form (RTX{sub red}) was labeled with {sup 99m}Tc/{sup 188}Re(CO){sub 3}. The partial reduction of the disulfide bonds to produce free sulfhydryl groups (-SH) was achieved with 2-mercaptoethanol. Radiolabeling efficiency, in vitro human plasma stability as well as transchelation toward cysteine and histidine was investigated. The immunoreactivity and binding affinity were determined on Ramos and/or Raji cells expressing CD20. Biodistribution was performed in mice bearing subcutaneous Ramos lymphoma xenografts. Results: The radiolabeling efficiency and kinetics of RTX{sub red} were superior to that of RTX{sub wt} ({sup 99m}Tc: 98% after 3 h for RTX{sub red} vs. 70% after 24 h for RTX{sub wt}). {sup 99m}Tc(CO){sub 3}-RTX{sub red} was used without purification for in vitro and in vivo studies whereas {sup 188}Re(CO){sub 3}-RTX{sub red} was purified to eliminate free {sup 188}Re-precursor. Both radioimmunoconjugates were stable in human plasma for 24 h at 37{sup o}C. In contrast, displacement experiments with excess cysteine/histidine showed significant transchelation in the case of {sup 99m}Tc(CO){sub 3}-RTX{sub red} but not with pre-purified {sup 188}Re(CO){sub 3}-RTX{sub red}. Both conjugates revealed high binding affinity to the CD20 antigen (K{sub d}=5-6 nM). Tumor uptake of {sup 188}Re(CO){sub 3}-RTX{sub red} was 2.5 %ID/g and 0.8 %ID/g for {sup 99m}Tc(CO){sub 3}-RTX{sub red} 48 h after injection. The values for other

  14. Liver scanning with sup(99m)Tc-phytate

    Energy Technology Data Exchange (ETDEWEB)

    Kubo, A; Isobe, Y; Kobayashi, T; (Keio Univ., Tokyo (Japan). School of Medicine); Kinoshita, Fumio; Shibata, Masayoshi

    1975-03-01

    /sup 198/Au-colloid has been widely used for liver scanning in Japan but it is not the best scanning agent because of the large exposure dose to the patient. The authors performed a few basic experiments with sup(99m)Tc-phytate, the preparation of which is very easy. The labeling efficiency was found to be 97.5% immediately after preparation and it remained fairly stable for a period of time. As a result, the compound can be used up to 6 hours after preparation without fear of chemical instability. Liver scanning with sup(99m)Tc-phytate was done on 116 patients and was compared with /sup 198/Au-colloid liver-scanning. Scans made with sup(99m)Tc were found to be superior to those made with /sup 198/Au in the resolution of surface defects in the liver, while at increasing depths the resolution with sup(99m)Tc dropped rapidly, apparently due to absorption of its relatively low energy photon. This indicates the importance of taking multidirectional views. The degrees of splenic concentration of sup(99m)Tc-phytate were fairly close to those of /sup 198/Au-colloid. Therefore, liver scanning with sup(99m)Tc-phytate is useful in the diagnostic evaluation of diffuse parenchymal liver disease.

  15. Liver scanning with sup(99m)Tc-phytate

    International Nuclear Information System (INIS)

    Kubo, Atsushi; Isobe, Yoshinori; Kobayashi, Takeshi; Kinoshita, Fumio; Shibata, Masayoshi.

    1975-01-01

    198 Au-colloid has been widely used for liver scanning in Japan but it is not the best scanning agent because of the large exposure dose to the patient. The authors performed a few basic experiments with sup(99m)Tc-phytate, the preparation of which is very easy. The labeling efficiency was found to be 97.5% immediately after preparation and it remained fairly stable for a period of time. As a result, the compound can be used up to 6 hours after preparation without fear of chemical instability. Liver scanning with sup(99m)Tc-phytate was done on 116 patients and was compared with 198 Au-colloid liver-scanning. Scans made with sup(99m)Tc were found to be superior to those made with 198 Au in the resolution of surface defects in the liver, while at increasing depths the resolution with sup(99m)Tc dropped rapidly, apparently due to absorption of its relatively low energy photon. This indicates the importance of taking multidirectional views. The degrees of splenic concentration of sup(99m)Tc-phytate were fairly close to those of 198 Au-colloid. Therefore, liver scanning with sup(99m)Tc-phytate is useful in the diagnostic evaluation of diffuse parenchymal liver disease. (auth.)

  16. Preparation, quality control and biological characterization of 99mTc-vincristine

    International Nuclear Information System (INIS)

    Saira Hina; Muhammad Ibrahim Rajoka; Asma Haque

    2015-01-01

    In present study it is aimed to radiolabel vincristine with 99m Tc and to evaluate bioaffinity of 99m Tc labeled vinc. The optimum conditions required to obtain 99.6 ± 0.4 %, (n = 5) radiolabeling yield of 99m Tc-vincristine ( 99m Tc-vinc) were as follows: pH 4, 5 µg of vincristine sulphate, 6 µg SnCl 2 ·2H 2 O as a reducing agent and 10 min incubation time at room temperature. Quality control of 99m Tc-vinc was done by using paper electrophoresis and thin layer chromatography. The radiolabeling yield was confirmed by High performance liquid chromatography using radioactive and UV detector operating at 230 nm. 99m Tc-vinc was stable in vitro for 5 h. Biodistribution and scintigraphy of 99m Tc-vinc was performed in mice and rabbits respectively and that 99m Tc-vinc showed high uptake of it in liver and spleen. Finally 99m Tc-vinc may be the potential imaging agent for liver and spleen. (author)

  17. Leukocyte scintigraphy with 99mTc-exametazime-labeled leukocytes is not useful for follow-up of systemic vasculitis

    International Nuclear Information System (INIS)

    Staudenherz, A.; Kletter, K.; Deicher, R.; Haas, M.; Hoerl, W.H.; Jilma, B.; Becherer, A.; Dudczak, R.

    2002-01-01

    Background: The prognosis of systemic vasculitis, for instance Wegener's granulomatosis (WG), was greatly improved by the introduction of immunosuppressive treatment. However, relapses are frequent and predictors are scarce. 111 In-leukocytes have been found to indicate unknown manifestations of WG and to predict later relapse. We prospectively investigated the value of 99m Tc-Exametazime ( 99m Tc-HMPAO)-labeled leukocytes with regard to specific patterns and for their usefulness in the follow-up of patients with WG. Methods: The vasculitis group consisted of 8 patients with WG and 2 with idiopathic necrotizing glomerulonephritis (ING). Seven patients with different inflammatory diseases served as controls. Leukocyte labeling with 99m Tc-HMPAO was done using a slightly modified Hammersmith protocol. Cell viability after labeling was verified in vivo by the exclusion of early lung and splenic uptake and in vitro by means of propidium iodide and FACS analysis. Static gamma camera images from the head, chest, abdomen, and pelvis were obtained up to 18 hours after injection of approximately 300 MBq 99m Tc-HMPAO-labeled leukocytes. Scintigrams were analyzed visually; for semiquantitative analysis ROIs were drawn over the nasal region, the right lung, kidneys, and liver. Results: Increased nasal leukocyte accumulation was found in 7/8 patients with WG and in 2/2 patients with ING. Of 2 patients who had a relapse 6 months later, one presented with, and one without nasal uptake. The kidney/liver ratio was higher in controls (0.24 ± 0.07 vs. 0.37 ± 0.11, p 99m Tc-HMPAO leukocyte scintigraphy failed to indicate or exclude a later relapse and is therefore not suitable as a diagnostic tool in the management of patients with systemic vasculitis. (author)

  18. Leukocyte scintigraphy with 99mTc-exametazime-labeled leukocytes is not useful for follow-up of systemic vasculitis

    International Nuclear Information System (INIS)

    Becherer, A.; Dudczak, R.; Deicher, R.; Haas, M.; Hoerl, W.H.; Jilma, B.; Staudenherz, A.; Kletter, K.

    2002-01-01

    The prognosis of systemic vasculitis, for instance Wegener's granulomatosis (WG), was greatly improved by the introduction of immunosuppressive treatment. However, relapses are frequent and predictors are scarce. 111 In-leukocytes have been found to indicate unknown manifestations of WG and to predict later relapse. We prospectively investigated the value of 99m Tc-Exametazime ( 99m Tc-HMPAO)-labeled leukocytes with regard to specific patterns and for their usefulness in the follow-up of patients with WG. The vasculitis group consisted of 8 patients with WG and 2 with idiopathic necrotizing glomerulonephritis (ING). Seven patients with different inflammatory diseases served as controls. Leukocyte labeling with 99m Tc-HMPAO was done using a slightly modified Hammersmith protocol. Cell viability after labeling was verified in vivo by the exclusion of early lung and splenic uptake and in vitro by means of propidium iodide and FACS analysis. Static gamma camera images from the head, chest, abdomen, and pelvis were obtained up to 18 hours after injection of approximately 300 MBq 99m Tc-HMPAO-labeled leukocytes. Scintigrams were analyzed visually; for semiquantitative analysis ROls were drawn over the nasal region, the right lung, kidneys, and liver. Increased nasal leukocyte accumulation was found in 7/8 patients with WG and in 2/2 patients with ING. Of 2 patients who had a relapse 6 months later, one presented with, and one without nasal uptake. The kidney/liver ratio was higher in controls (0.24 ± 0.07 vs. 0.37 ± 0.11, p 99m Tc-HMPAO leukocyte scintigraphy failed to indicate or exclude a later relapse and is therefore not suitable as a diagnostic tool in the management of patients with systemic vasculitis. (author)

  19. Influence of antiseptic on the impurities in the preparation of dimercaptosuccinic labelled with {sup 99m}Tc; Influence des antiseptiques sur la presence d'impuretes dans la preparation de l'acide dimercaptosuccinique marque au 99mTc

    Energy Technology Data Exchange (ETDEWEB)

    Metaye, T.; Rosenberg, T.; Perdrisot, R. [CHU de Poitiers, Service de medecine nucleaire et biophysique, 86 (France)

    2010-07-01

    Purpose: antiseptic solutions are used to disinfect the rubber stoppers on the bottles of radiopharmaceutical. Small amounts of these solutions can pass into the bottle when the cap is pricked to inject the {sup 99m}Tc. After finding in a patient a suboptimal labelling using biseptin, we studied the effect of various antiseptics on the presence of impurities in the preparation of the dimercaptosuccinic acid labelled with {sup 99m}Tc ({sup 99m}Tc-D.M.S.A.). Conclusions: We recommend using 70% isopropanol or modified alcohol Cooper instead of biseptin to disinfect the D.M.S.A. bottles caps. (N.C.)

  20. Labeling of ursodeoxycholic acid with technetium-99m for hepatobiliary imaging

    International Nuclear Information System (INIS)

    Sanad, M.H.; El-Tawoosy, M.

    2013-01-01

    An adopted method for the preparation of high radiochemical purity 99m Tc-ursodeoxycholic acid (UDCA) was conducted with a high radiochemical yield up to 97.5 %. The reaction proceeds well using 2 mg UDCA, 50 μg tin chloride in solution of pH 8 at room temperature for 30 min. The radiochemical yield was up to 97.5 % as pure as 99m Tc-UDCA. Different chromatographic techniques (paper chromatography and electrophoresis) were used to evaluate the radiochemical yield and purity of the labeled product. Biodistribution studies were carried out in Albino Swiss mice at different time intervals after administration of 99m Tc-UDCA. The uptake of 99m Tc-UDCA in the liver gave the chance to diagnose it. The results indicate that the labeled compound cleared from the systematic circulation within 2 h after administration and majority of organs showed significant decrease in uptake of 99m Tc-UDCA. Finally, the liver uptake was high and the results indicate the possibility of using 99m Tc-UDCA for hepatobiliary imaging.

  1. Evaluation of sup(99m)Tc labeled amino acids as radiopharmaceuticals, 4. S-substituted cysteines and N-substituted iminodiacetic acids

    Energy Technology Data Exchange (ETDEWEB)

    Karube, Yoshiharu; Maeda, Tatsuo; Ohya, Masato; Sugata, Setsuro; Kono, Akira (Kyushu Cancer Center Research Inst., Fukuoka (Japan)); Matsushima, Yoshikazu

    1982-06-01

    Sixteen sup(99m)Tc labeled ligands were evaluated as scintigraphic agents. The ligands studied were cysteine, glutathione, their S-substituted derivatives, lysine-N sup(epsilon), N sup(epsilon)-diacetic acid, glycylglycine-N,N-diacetic acid, glycylglycylglycine-N,N-diacetic acid, taurine-N,N-diacetic acid, hydrazine-N,N-diacetic acid, ethylenediamine-N,N-diacetic acid, and propylne-1,3-diamine-N/sup 1/-,N/sup 1/-diacetic acid. The ligands were labeled with sup(99m)Tc by the SnCl/sub 2/ method with more than 95% yield. The in vivo behavior of the sup(99m)Tc labeled ligands were studied in golden hamsters and dogs. The organ distribution in golden hamsters indicated clearance both by hepatobiliary and renal systems. The pancreas/blood ratios were much lower in the sup(99m)Tc ligands than in /sup 75/Se-selenomethionine. Scintigraphic studies in dogs showed that the liver and kidneys were well visualized but the accumulation by the pancreas was not sufficient for clear visualization.

  2. 99mTc-Tetrofosmin scintimammography in suspected breast cancer patients: comparison with 99mTc-MIBI

    International Nuclear Information System (INIS)

    Kim, Seong Jang; Kim, In Ju; Kim, Yong Ki; Bae, Young Tae

    2000-01-01

    The aim of this study was to investigate the diagnostic role of 99m Tc-Tetrofosmin in detection of breast cancer and compared with that of 99m Tc-MIBI. Forty-eight patients with a clinically palpable mass or abnormal mammographic or ultrasonographic findings had 99m Tc-MIBI and 99m Tc-Tetrofosmin scintimammographies after intravenous injection of 925 MBq of radiopharmaceuticals. The scintimammographs were correlated with histopathologic findings. Thirty-three patients were diagnosed with breast cancer and 15 patients with benign breast diseases. The numbers of true positive, true negative, false positive, and false negative cases of 99m Tc-MIBI scintimammography were 29, 10, 5, and 4 respectively. The sensitivity, specificity, positive predictive value, and negative predictive value of 99m Tc-MIBI scintimammographies were 87.8%, 66.7%, 85.3%, and 71.4% respectively. The numbers of true positive, true negative, false positive, and false negative cases of 99m Tc-Tetrofosmin were 31, 10, 5, and 2 respectively. The sensitivity, specificity, positive predictive value, negative predictive value of 99m Tc-Tetrofosmin were 93.9%, 66.7%, 86.1%, and 73.3% respectively. One patient was false negative in both 99m Tc-Tetrofosmin scintimammographies and its size was 0.5cm. 99m Tc-Tetrofosmin and 99m Tc-MIBI were non-invasive and useful in detection of breast cancer and 99m Tc-Tetrofosmin was comparable to the 99m Tc-MIBI in detection of primary breast cancer.=20

  3. Studies of labelling conditions for gentamicin with sup(99m)Tc. Complexation with ruthexium. Establishment of pharmacokinetics parameters through compartmental analysis

    International Nuclear Information System (INIS)

    Carvalho, O.G. de.

    1988-01-01

    Gentamicin sulphate is an aminoglycoside antibiotic type specifically used for treatment of infections produced by Gram-negative bacterias but at the other hand it presents ototoxic reactions as a serious side effect. The main purpose of labelling gentamicin with sup(99m)Tc was to obtain a radioactive tracer to carry out biological studies and compartmental analysis of this antibiotic. The optimal labelling conditions of gentamicin sulphate with sup(99m)Tc, using sodium pertechnetate solution eluted from a sup(99)Mo- sup(99m)Tc generator, were stablished by testing different masses of antibiotic, and reduction agent (SnCl sub(2).2H sub(2)O), and also different reaction time and final labelling PH. The same labelling procedure was used with Re (amonium perrenate) in order to obtain some semi-quantitative approximations of the chemical structure of the complex formed, since Re and Tc present similar chemical characteristics. In this way it is possible to suggest the role that the groups NH2 and C-O bonding of the gentamicin play in the complexation process. From the studies of the biological uptake of sup(99m)Tc-gentamicin sulphate in rats, the kidneys showed the highest affinity for the antibiotic. The maximum uptake was observed in 180 to 240 minutes followed by a decrease of it afterwards. For the dose and time used, no significative uptake by the auricular region was detected. Curve of plasma decay of sup(99m)Tc-gentamicin was obtained, and from the exponentials of each beanch of this curve respective half-lives were calculated. Furthermore the apparent volume of distribution was determined, and with the residual radioactivity in the body, the biological half-life and total clearance were obtained. The distribution of sup(99m)Tc-gentamicin in rats was set in a bi-compartments in addition to a retention one for the 24 hours time interval studied. (author)

  4. Effects of broccoli extract on biodistribution and labeling blood components with 99mTc-GH

    International Nuclear Information System (INIS)

    Cekic, Betul; Muftuler, Fazilet Zumrut Biber; Kilcar, Ayfer Yurt; Ichedef, Cigdem; Unak, Perihan

    2011-01-01

    Purpose: people consume vegetables without the knowledge of the side effects of the biological and chemical contents and interactions between radiopharmaceuticals and herbal extract. To this end, current study is focused on the effects of broccoli extract on biodistribution of radiolabeled glucoheptonate ( 99m Tc-GH) and radiolabeling of blood components. Methods: GH was labeled with 99m Tc. Quality control studies were done utilizing TLC method. Biodistribution studies were performed on male rats which were treated via gavage with either broccoli extract or SF as control group for 15 days. Blood samples were withdrawn from rats' heart. Radiolabeling of blood constituents performed incubating with GH, SnCl 2 and 99m Tc. Results: radiochemical yield of 99m Tc-GH is 98.46±1.48 % (n=8). Biodistribution studies have shown that according to the control, the treated group with broccoli has approximately 10 times less uptake in kidney. The percentage of the radioactivity ratios of the blood components is found to be same in both groups. Conclusions: although there is no considerable effect on the radiolabeling of blood components, there is an outstanding change on the biodistribution studies especially on kidneys. The knowledge of this change on kidney uptake may contribute to reduce the risk of misdiagnosis and/or repetition of the examinations in Nuclear Medicine. (author)

  5. Technetium-99m somatostatin analogues: effect of labelling methods and peptide sequence

    International Nuclear Information System (INIS)

    Decristoforo, C.; Mather, S.J.

    1999-01-01

    In this paper the preclinical evaluation of the somatostatin analogue RC160 labelled with technetium-99m using bifunctional chelators (BFCs) based on the hydrazinonicotinamide (HYNIC) and N 3 S system is described and a comparison made with [Tyr 3 ]-octreotide (TOC). Conjugates of both peptides with HYNIC, and of RC160 with benzoyl-MAG 3 and an N 3 S-adipate derivative were prepared and radiolabelling performed at high specific activities using tricine, tricine/nicotinic acid and ethylenediamine-N,N'-diacetic adic (EDDA) as co-ligands for HYNIC conjugates. All conjugates and 99m Tc-labelled peptides showed preserved binding affinity for the somatostatin receptor (IC50, Kd 99m Tc-RC160 derivatives compared with 99m Tc-EDDA/HYNIC-[Tyr 3 ]-octreotide (0.2%-3.5%ID/g vs 9.7%ID/g) and correlated well with the reduced internalisation rate for RC160 derivatives. Our results show that the selection of the labelling approach as well as the right choice of the peptide structure are crucial for labelling peptides with 99m Tc to achieve complexes with favourable biodistribution. Despite the relatively low tumour uptake compared with 99m Tc-EDDA/HYNIC-[Tyr 3 ]-octreotide, 99m Tc-RC160 could play a role in imaging tumours that do not bind octreotide derivatives. (orig.)

  6. Kit formulation for 99mTc-labeling of recombinant Annexin V molecule with a C-terminally engineered cysteine

    International Nuclear Information System (INIS)

    Chunxiong Lu; Quanfu Jiang; Cheng Tan; Huixin Yu; Minjin Hu; Zichun Hua; Nanjing University, Nanjing

    2015-01-01

    A new formulation of a freeze-dried kit for the labeling of a novel recombinant Annexin V molecules (with a single cysteine residue at its C-terminal, Cys-Annexin V) with technetium-99m has been developed. Effects of the amount range of Cys-Annexin V, stannous chloride, glucoheptonate and disodium edetate on the radiolabeling yield were studied in details. The stabilities of 99m Tc-Cys-Annexin V and freeze-dried kits were performed, respectively. In vitro cell uptake studies showed the binding of 99m Tc-Cys-Annexin V was specific on testing with apoptotic H446 cells. Therefore, 99m Tc-Cys-Annexin V is a potential apoptosis imaging agent and further study is needed. (author)

  7. In Vitro Evaluation of Tc-99m Radiopharmaceuticals for Gastric Emptying Studies

    Directory of Open Access Journals (Sweden)

    Türkan Ertay

    2014-02-01

    Full Text Available Objective: Gastrointestinal motility and functional motility disorders causing either delayed or accelerated gastric emptying (GE may result in similar symptoms including nausea, vomiting, early satiety, fullness, bloating, and abdominal discomfort or pain. Hence, it is important to evaluate patients for both rapid and delayed GE in the same test. The gold standard technique to measure GE is scintigraphy by radiolabeled test meals. The aim of this study was to test alternative Tc-99m agents to label eggs as the solid meal and compare to Tc-99m sulfur colloid (SC for gastric emptying studies. Methods: In search of alternative agents for gastric emptying studies, we mixed and fried eggs with four different particulate compounds (Tc-99m labeled SC, tin colloid, nanocolloid and MAA, as well as with free pertechnetate and Tc-99m DTPA. We then measured the stability of these compounds in simulated gastric juice. Results: Our experiments demonstrated that in addition to Tc-99m sulfur colloid;Tc-99m MAA, Tc-99m nanocolloid and Tc-99m tin colloid also appear to make stable complexes with eggs in acidic environment. Conclusion: Therefore, these agents may be used for gastric emptying studies which could be more practical in routine conditions.

  8. Development of 99mTc-DMSA for kidney imaging

    International Nuclear Information System (INIS)

    Shafii Khamis; Nurshuhadah Mohd Yusof

    2006-01-01

    In nuclear medicine studies, 99m Tc-Dimercaptosuccinic acid ( 99m Tc-DMSA) has been shown to be an excellent radiopharmaceutical agent for detecting focal abnormalities of the renal cortex in patients. The agent, however, oxidizes readily and must be used within 30 minutes of preparation. The instability of the radiopharmaceutical renders the kit less economical to use. Several factors affecting the labeling yield such as the kit formulation, stannous and stabilizer content were investigated. The radiochemical determination of the radiolabelled product was analyzed using I TLC-SG system developed in methyl ethyl ketone and the radiolabelled 99m Tc-DMSA biological distributions were carried out in female rats. Stability study of the radiolabelled 99m Tc-DMSA was carried out using ascorbic acid as stabilizer. Comparative study was also carried out on both the prepared kit and those obtained commercially. The DMSA kit was successfully developed and the result obtained was found to be comparable to that of the commercially available kit. (Author)

  9. Assessment of inflammatory bowel disease with two different 99mTc-leucocytes labelling methods

    International Nuclear Information System (INIS)

    Cardoso, V.N.; Plaza, P.J.L.; Roca, M.; Armero, F.; Martin-Comin, J.

    2002-01-01

    Aim of this study was to retrospectively compare the diagnostic accuracy of 99mTc-HMPAO white blood cell scintigraphy using two different cell suspension mediums: leukocyte poor plasma (LPP) and Hanks' Balanced Salt Solution (HBSS) in patients with suspicion of active inflammatory bowel disease. Materials and Methods: Leukocytes from 30 patients were labelled using LPP and in 28 using HBSS . In LPP method the leukocytes were resuspended in 0,5 ml cell-free plasma while in HBSS method the cells were resuspended in 0,5 ml HBSS. Scintigraphic images were obtained at 30 min and 2 h after injection of 185-200 MBq 99mTc-HMPAO leukocytes. Results: Leukocytes labelling efficiency were 65,5%, and 89,0%, respectively for LPP and HBSS methods. There were 22 true-positive, 7 true-negative and 1 false-negative results in the LPP group, while in the HBSS group results were 18, 10 and 0, respectively. Diagnostic accuracy was similar with both methods though sensitivity was slightly higher in the HBSS group. Conclusion These date indicate that leukocytes scintigraphy labelled using HBSS as resuspension medium should be used as first option method for WBC labelling and diagnosis of inflammatory bowel disease

  10. On the organ distribution of a selection of 99mTc-tagged tetracyclines

    International Nuclear Information System (INIS)

    Weinhold, S.E.M.

    1983-01-01

    During this study the time course of organ concentrations of 99mTc-tagged tetracycline and of 99mTc-rolitetracycline that had been labeled according to two different methods was investigated with reference to that of two standard preparations, 99mTcO 4 and 3 H-labeled tetracycline, which differ from the test substances in their chemical structures (lipohilia - hydrophilia). As the substances to be investigated here are chemically related, they showed mostly consistent organ concentrations and great vivo stability. The concentrations measured in the organs examined (particularly the lungs) followed the same pattern as the concentrations in the blood and were thus regarded as being primarily the result of convection processes, whereas the concentrations seen in some other organs (especially the kidneys and, to a lesser extent, the liver) rather appeared to be determined by invasion and evasion processes; this held true for 99mTc-labeled tetracyclines as well as for pertechnetate. None of the five substances tested during this study appeared to be able to pass the blood-brain barrier. As regards solubility in water, the 99mTc-labeled tetracyclines occupy an intermediate position between pertechnetate (extremely water-soluble) and 3 H-labeled tetracyclines (extremely lipophil), which can be seen from the moderately high blood concentrations of these preparations. In view of the high organ concentrations that are observed particularly in the kidneys following administration of 99mTc-labeled tetracycline and rolitetracycline, the use of these substances for renal scintiscanning appears worth considering, as only approx. one tenth of the dose of pertechnetate would be required for this purpose. (TRV) [de

  11. Labelled Preformed liposomes with 99MTC-DTPA, 99 MTC-ECD, 99MTC-MDP and 99MTC-MIBI : Labelling procedures and stability studies

    International Nuclear Information System (INIS)

    Savio, E.O.; Teran, M.A.; Vales, M.E.; Frier, M.

    2004-01-01

    Liposomes labelled with gamma e miters like 99mTc, can be used for scintigraphic imaging to non-invasively track and quantify the distribution of liposomes in the body. In vitro studies were done to choose a suitable radiopharmaceutical (RF) to be attached to performed liposomes. 99mTc-Complexes (DTPA, ECD, MDP, MIBI) were used to label collagen liposomes. Commercial kits were labelled with 99mTc04-(TechnoNuclear). Quality controls of the RF were performed. Collagen liposomes suspended in saline 0.9% were incubated at 4.25.37 and 60 for 30 min. Efficiency of the labelling procedure was determined by gel filtration using Sephadex G25 (Pharmacia) and NaC10.9%. Samples of 100mL (74MBq), were seeded and fractions of 0.5mL were colleted and measured in an ionisation chamber (Capintec CRC). Stability of the labelled liposomes was assessed incubating 0.5mL, of the suspension with 1mL of human serum during 30 min at 37 . Dialysis was performed using dialysis bags of 64 K pore size and NaCI 0.9% at room temperature. Samples of the saline bath were collected at 30.60 and 90 min. and measured in a solid scintillation counter Ortec.Liposomes labelled with 99mTc-DTPA and 99mTcMIBI showed a labelling efficiency of 80%; liposomes incubated with 99mTc-MDP were labelled in a 50% and 99mTc-ECD did not bind to liposomes in the conditions of study. Incubation of labelled liposomes with human serum showed 50% of strong binding to the plasmatic proteins for 99mTc-DTPA but low values (5%) for the other specimens. Labelled liposomes were achieved, with different RF, showing a suitable in vitro stability to perform in vivo studies

  12. Localization of the acute lower gastrointestinal hemorrhage in vivo-in vitro labeling of red blood cells with sup(99m)Tc

    International Nuclear Information System (INIS)

    Noguera, E.; Mothe, G.; Wyse, E.

    1984-01-01

    For the detection and localization of acute lower gastrointestinal hemorrhage in vivo-in vitro labeling of red blood cells with sup(99m)Tc and sup(99m)Tc sulfur colloid has been sugested. The procedure for labeling RBC with sup(99m)Tc consisted in injecting IV 1 mg of ClSn; 20 minutes after injection of tin 10 cc of blood were withdrawn in a syringe containing 20 mCi of sup(99m)Tc; this was incubated for 10 minutes and then injected IV. Scintigraphy of the abdominal cavity was done in supine position and performed with a large field gamma camera with a parallel hole-low energy colimator. Computer adquisition of images was started 5 minutes after RBC injection and made at the rate of one enery 5 minutes for 45 minutes. 14 patients were studied divided in: a) control: 6 patients. b) with active gastrointestinal hemorrhage: 4 patients had positive scintigraphy. The hemorrhage was documented with superior mesenteric arteriography, endoscopy and/or necropsy. The sensitivity was 100%. In 4 out of 14 patients scintigraphy with sup(99m)Tc RBC compared with simultaneous sup(99m)Tc sulfur colloid demonstrated that all patients with positive sup(99m)Tc RBC had also positive sup(99m)Tc sulfur colloid scintigraphy. c) without active gastrointestinal hemorrhage: all of them had negative scintigraphy (specificity 100%). Abdominal scintigraphy with sup(99m)Tc RBC or sulfur colloid are both sensitive for detection and localization of lower gastrointestinal bleeding and the negative study suggests the absence of active hemorrhage. It is suggested that the sup(99m)Tc sulfur colloid scintigraphy should be the initial procedure to study these patients and abdominal arteriography should be performed only in patients with positive abdominal scintigraphy. (M.E.L.) [es

  13. Breast-milk radioactivity after a Tc-99m DTPA aerosol/Tc-99m MAA lung study

    International Nuclear Information System (INIS)

    Mountford, P.J.; Hall, F.M.; Wells, C.P.; Coakley, A.J.

    1984-01-01

    Measurements were made of the concentration of Tc-99m activity in samples of breast milk following an administration of Tc-99m DTPA aerosol for a lung ventilation image and one of Tc-99m MAA for lung perfusion. The activity was 222 nCi/ml of milk (8.2 kBq/ml) at 2 hr after the MAA injection, and it was found to be excreted exponentially with an effective half-life of 4.6 hr. There was a small incorporation of Tc-99m into breast-milk protein. The authors conclude that the combined use of these two Tc-99m agents did not indicate the interruption of breast feeding beyond 24 hr after administration of the MAA, and that for an aerosol ventiliation study alone, breast feeding need not be interrupted for more than 4 hr after the test

  14. Quantitative assessment of limb blood flow using Tc-99m labeled red blood cells

    International Nuclear Information System (INIS)

    Itoh, Kazuo; Shougase, Takashi; Kawamura, Naoyuki; Tsukamoto, Eriko; Nakada, Kunihiro; Sakuma, Makoto; Furudate, Masayori

    1987-01-01

    A quantitative assessment of limb blood flow using a non-diffusible radioindicator, Tc-99m labeled red blood cells, was reported. This was an application of venous occlusion plethysmography using radionuclide which was originally proposed by M. Fukuoka et al. The peripheral blood flow (mean ± s.e.) of 30 legs in a normal control group was 1.87 ± 0.08 ml/100 ml/min. In heart diseases (46 legs), it was 1.49 ± 0.13 ml/100 ml/min. The limb blood flow between a control group and heart diseases was statistically significant (p < 0.01) in the t-test. The peripheral blood flow at rest between diseased legs and normal legs in occlusive arterial disorders was also statistically significant (p < 0.01) in a paired t-test. RAVOP was done after the completion of objective studies such as radionuclide angiography or ventriculography. Technique and calculation of a blood flow were very easy and simple. RAVOP study which was originally proposed by Fukuoka et al. was reappraised to be hopeful for quantitative measurement of limb blood flow as a non-invasive technique using Tc-99m labeled red blood cells. (author)

  15. Use of 99mTc-HMPAO-leucocyte scintigraphy coupled to 99mTc-colloid scintigraphy in diagnosing the osteo-articular sepsis

    International Nuclear Information System (INIS)

    Darlas, Y.; Pegoix, M.; Filmont, J.E.; Leclercq, S.; Rosas, M.H.; Agostini, D.; Aubriot, J.H.; Bouvard, G.

    1997-01-01

    The object of this study was the scintigraphic diagnosis of osseous sepsis based on the absence of congruence between leucocytic and colloidal fixations and the evaluation of the effect of coupling between the scintigraphies (sc) with leucocytes (A) and colloids (B) on the diagnosis feasibility index of this technique. Seventy four patients, 97 sc were divided into two groups according to the scintigraphic technique [(A) only]: 35 sc; [(A) and (B)]: 62 sc. [Prosthesis: 48 patients, 68 sc. Osteitis: 26 patients, 29 sc]. The scintigraphies were performed as follows: (A) autologous leucocytes labelled by 250 - 300 MBq of 99m Tc-HMPAO, with planar incidences (15 min), 3 - 4 hours after injection and (B) Labelled nano-colloids labelled by 180 - 200 MBq of 99m Tc, the same incidences, 30 min after injection. The delay between (A) and (B): 48 hours. The final diagnosis of sepsis: bacteriological and histologic criteria after biopsies and/or clinical, biological and radiological evolution. The comparison between the two groups is given in a table in terms of prevalence, sensitivity and specificity, using the χ2 and Fisher tests. In conclusion, the scintigraphy by 99m Tc-HMPAO-leucocyte is a sensitive method (Se ∼ 90%) for the diagnosis of osseous sepsis and coupled to the scintigraphy by 99m Tc-colloids allow obtaining a high specificity (Sp ≥ 90%) by reducing the number of falsely positive diagnoses

  16. Technetium-99m-human fibrinogen

    International Nuclear Information System (INIS)

    Wong, D.W.; Mishkin, F.S.

    1975-01-01

    Exogenous fibrinogen has been successfully labeled with /sup 99m/Tc using a modified electrolytic method. The exact labeling mechanism has not been determined. Experimental data suggest that the labeling process of /99m/Tc-fibrinogen is quite similar to that of /sup 99m/Tc-human serum albumin as reported earlier by Benjamin. Technetium-99m-fibrinogen is stable in human plasma or in 1 percent buffered human serum albumin. A binding efficiency of 76 percent has been achieved with approximately 25 percent clottable protein. The entire labeling procedure requires less than 1 hr of preparation time. This short labeling time in a closed system may allow development of a practical method for labeling autologous fibrinogen, thus eliminating the risk of hepatitis transmission. (U.S.)

  17. Scintigraphic detection of acute experimental endocarditis with the technetium-99m labelled glycoprotein IIb/IIIa receptor antagonist DMP444

    Energy Technology Data Exchange (ETDEWEB)

    Oyen, W.J.G.; Boerman, O.C.; Corstens, F.H.M. [Department of Nuclear Medicine, University Hospital Nijmegen, Nijmegen (Netherlands); Brouwers, F.M. [Department of Nuclear Medicine, University Hospital Nijmegen, Nijmegen (Netherlands); Department of Internal Medicine, University Hospital Nijmegen, Nijmegen (Netherlands); Barrett, J.A. [DuPont Pharmaceutical Company, Radiopharmaceutical Division, North Billerica, MA (United States); Verheugt, F.W.A. [Department of Cardiology, University Hospital Nijmegen, Nijmegen (Netherlands); Ruiter, D.J. [Department of Pathology, University Hospital Nijmegen, Nijmegen (Netherlands); Meer, J.W.M. van der [Department of Internal Medicine, University Hospital Nijmegen, Nijmegen (Netherlands)

    2000-04-01

    Bacterial endocarditis is an important clinical problem that may result in persistent bacteraemia and irreversible cardiac damage. Since endocarditis is characterized by aggregation of activated platelets, fibrin and bacteria, we studied DMP444, a technetium-99m labelled high-affinity antagonist of the GP IIb/IIIa receptor that is expressed on activated platelets. In seven Beagle dogs (11-15 kg), the left ventricle was catheterized via the right carotid artery. One hour later, 5 x 10{sup 7} colony forming units of Staphylococcus aureus were injected intracardially. Half an hour later, the catheter was removed. Two extra dogs underwent a complete sham procedure. One day after the intervention, five infected and the two non-infected dogs were injected with 37 MBq/kg {sup 99m}Tc-DMP444 and two infected dogs with 37 MBq/kg {sup 99m}Tc-IgG (used as a non-specific control agent) and imaged up to 4 h after injection. Samples were obtained for tissue counting, microbiology and histology. From 1 to 2 h post injection onward, there was clear focal accumulation of DMP444 in the aortic valve region when endocarditis was present, and this accumulation increased with time. The non-infected and the {sup 99m}Tc-IgG injected dogs showed only persisting blood pool activity without any focal abnormality. At 4 h post injection, the in vivo valve-to-blood pool ratios were 1.87{+-}0.18 in endocarditis, 1.01{+-}0.05 in non-infected controls and 1.09{+-}0.02 in {sup 99m}Tc-IgG injected dogs (P<0.05). It is concluded that targeting activated platelets with the {sup 99m}Tc-labelled GP IIb/IIIa antagonist DMP444 allows a final diagnosis of experimental bacterial endocarditis within 4 h owing to high, specific and fast in vivo uptake. (orig.)

  18. Scintigraphic detection of acute experimental endocarditis with the technetium-99m labelled glycoprotein IIb/IIIa receptor antagonist DMP444

    International Nuclear Information System (INIS)

    Oyen, W.J.G.; Boerman, O.C.; Corstens, F.H.M.; Brouwers, F.M.; Barrett, J.A.; Verheugt, F.W.A.; Ruiter, D.J.; Meer, J.W.M. van der

    2000-01-01

    Bacterial endocarditis is an important clinical problem that may result in persistent bacteraemia and irreversible cardiac damage. Since endocarditis is characterized by aggregation of activated platelets, fibrin and bacteria, we studied DMP444, a technetium-99m labelled high-affinity antagonist of the GP IIb/IIIa receptor that is expressed on activated platelets. In seven Beagle dogs (11-15 kg), the left ventricle was catheterized via the right carotid artery. One hour later, 5 x 10 7 colony forming units of Staphylococcus aureus were injected intracardially. Half an hour later, the catheter was removed. Two extra dogs underwent a complete sham procedure. One day after the intervention, five infected and the two non-infected dogs were injected with 37 MBq/kg 99m Tc-DMP444 and two infected dogs with 37 MBq/kg 99m Tc-IgG (used as a non-specific control agent) and imaged up to 4 h after injection. Samples were obtained for tissue counting, microbiology and histology. From 1 to 2 h post injection onward, there was clear focal accumulation of DMP444 in the aortic valve region when endocarditis was present, and this accumulation increased with time. The non-infected and the 99m Tc-IgG injected dogs showed only persisting blood pool activity without any focal abnormality. At 4 h post injection, the in vivo valve-to-blood pool ratios were 1.87±0.18 in endocarditis, 1.01±0.05 in non-infected controls and 1.09±0.02 in 99m Tc-IgG injected dogs (P 99m Tc-labelled GP IIb/IIIa antagonist DMP444 allows a final diagnosis of experimental bacterial endocarditis within 4 h owing to high, specific and fast in vivo uptake. (orig.)

  19. Effect of iron deficiency anemia on the biodistribution of 99mTc radiopharmaceuticals

    International Nuclear Information System (INIS)

    Calmanovici, Gabriela P.; Salgueiro, Maria J.; Janjetic, Mariana A.; Leonardi, Natalia M.; Boccio, Jose R.; Zubillaga, Marcela B.

    2006-01-01

    The distribution of colloids and labeled cells in organs is influenced by their intrinsic properties and by the state of the investigated subject. Iron deficiency remains an unsolved nutritional problem all over the world; one of its severe consequences is anemia. Because iron metabolism principally takes place in the liver, spleen, bone marrow, skeletal muscle and blood, we studied the effect of iron deficiency anemia on the biodistribution of 99m Tc phytate, 99m Tc gelatin colloid and 99m Tc RBC (red blood cells labeled with 99m Tc). Our results show that iron deficiency anemia modifies the pattern of biodistribution of the two colloids assayed. However, this behavior is different for both of them. This work contributes to studies that kinetically and statistically establish that iron deficiency anemia induces a significant inversion in the spleen-liver activity relationship when centellographic studies are performed with colloids such as 99m Tc phytate

  20. Receptor imaging with a new Tc-99m labelled somatostatin analogue (Tc-99m EDDA-TRYCINE-HYNIC-TOC): first clinical results and comparison with In-111 Dotatoc during radioreceptor therapy with Y-90 Dotatoc

    International Nuclear Information System (INIS)

    Baum, R.P.; Schmuecking, M.; Fischer, S.; Przetak, C.; Niesen, A.; Maecke, H.R.

    2002-01-01

    Full text: To evaluate Tc-99m EDDA-TRYCINE-HYNIC-TOC (TET-H-TOC) in patients with somatostatin receptor (SSTR)-positive tumors (staging, pretherapeutic indication for radioreceptor therapy and restaging after therapy) in comparison with In-111 DOTATOC. The Tc-99m labelled somatostatin analogue was synthesized by an optimized procedure in our pharmaceutical lab using lyophilized kits (radiochemical purity by HPLC, TLC > 95 %, product stability in vitro 4 to 6 h). So far, 46 patients (53 examinations) were studied after injection of 580-890 MBq (median 673 MBq) TET-H-TOC. The histologically proven tumors were endocrine neoplasias, renal carcinomas, bronchial carcinoma, mesothelioma and malignant fibrous histiocytoma. The imaging protocol consisted of whole-body scans and planar images of the tumor region (15 min, 1 h, 2 h, 4 h, 8 h, 24 h p.i.) and additionally SPECT-images (1 h and 4 h p.i.). For semi-quantitative assessment, individual regions of interest (ROI) were drawn in order to generate time-activity curves and to calculate tumor-to-tissue/background ratios which were compared by visual grading (scale 0 to 3+). Furthermore, pharmacokinetic analyses were carried out (radioactivity kinetics in plasma and urine). In some selected patients, image fusion of the whole-body scans was performed with CT and/or MRT and/or PET using a HERMES computer. 7 out of 46 patients showed an intense tracer accumulation in the SSTR-positive tumors (visual 3+, tumor / background ratio >2,5). In these patients, radioreceptor therapy was carried out using Y-90 DOTATOC (simultaneous injection of 150 MBq In-111 DOTATOC). All pretherapeutic scans with the Tc-99m labelled ligand (4 h p.i.) showed a similar overall pattern of biodistribution and tumor uptake in comparison to the therapy scans with In-111 / Y-90 DOTATOC 24 h p.i. The Tc-99m EDDA-HYNIC-TOC scans (incl. SPECT) offered superior imaging properties with earlier tumor visualization (all lesions were detected 1 h p.i.) as compared

  1. Comparison of relative renal function measured with either 99m Tc-DTPA or 99m Tc-EC dynamic scintigraphies with that measured with 99m Tc-DMSA static scintigraphy

    Energy Technology Data Exchange (ETDEWEB)

    Domingues, F.C.; Fujikawa, G.Y.; Decker, H.; Alonso, G.; Pereira, J.C.; Duarte, P.S. [Centro de Diagnostico Fleury, Sao Paulo, SP (Brazil). Secao de Medicina Nuclear; Sao Paulo Univ. (USP), SP (Brazil). Escola de Saude Publica. Dept. de Epidemiologia]. E-mail: paulo.duarte@fleury.com.br

    2006-07-15

    Objective: The aim of this study was to compare the renal function measured with either {sup 99m}Tc-DTPA or {sup 99m}Tc-EC dynamic scintigraphies with that measured using {sup 99m}Tc-DMSA static scintigraphy. Methods: the values of relative renal function measured in 111 renal dynamic scintigraphies performed either with {sup 99m}Tc-DTPA (55 studies) or with {sup 99m}Tc-EC (56 studies) were compared with the relative function measured using {sup 99m}Tc-DMSA static scintigraphy performed within a 1-month period. The comparisons were performed using Wilcoxon signed rank test. The number of {sup 99m}Tc-DTPA and {sup 99m}Tc-EC studies that presented relative renal function different by more than 5% from that measured with {sup 99m}Tc-DMSA, using chi square test were also compared. Results: the relative renal function measured with {sup 99m}Tc-EC is not statistically different from that measured with {sup 99m}Tc-DMSA (p = 0.97). The relative renal function measured with {sup 99m}Tc-DTPA was statistically different from that measured using {sup 99m}Tc-DMSA, but with a borderline statistical significance (p = 0.05). The number of studies with relative renal function different by more than 5% from that measured with {sup 99m}Tc-DMSA is higher for the {sup 99m}Tc-DTPA scintigraphy (p 0.04) than for {sup 99m}Tc-EC. Conclusion: the relative renal function measured with {sup 99m}Tc-EC dynamic scintigraphy is comparable with that measured with {sup 99m}Tc-DMSA static scintigraphy, while the relative renal function measured with {sup 99m}Tc-DTPA dynamic scintigraphy presents a significant statistical difference from that measured with {sup 99m}Tc-DMSA static scintigraphy. (author)

  2. Comparison of relative renal function measured with either 99m Tc-DTPA or 99m Tc-EC dynamic scintigraphies with that measured with 99m Tc-DMSA static scintigraphy

    International Nuclear Information System (INIS)

    Domingues, F.C.; Fujikawa, G.Y.; Decker, H.; Alonso, G.; Pereira, J.C.; Duarte, P.S.; Sao Paulo Univ.

    2006-01-01

    Objective: The aim of this study was to compare the renal function measured with either 99m Tc-DTPA or 99m Tc-EC dynamic scintigraphies with that measured using 99m Tc-DMSA static scintigraphy. Methods: the values of relative renal function measured in 111 renal dynamic scintigraphies performed either with 99m Tc-DTPA (55 studies) or with 99m Tc-EC (56 studies) were compared with the relative function measured using 99m Tc-DMSA static scintigraphy performed within a 1-month period. The comparisons were performed using Wilcoxon signed rank test. The number of 99m Tc-DTPA and 99m Tc-EC studies that presented relative renal function different by more than 5% from that measured with 99m Tc-DMSA, using chi square test were also compared. Results: the relative renal function measured with 99m Tc-EC is not statistically different from that measured with 99m Tc-DMSA (p = 0.97). The relative renal function measured with 99m Tc-DTPA was statistically different from that measured using 99m Tc-DMSA, but with a borderline statistical significance (p = 0.05). The number of studies with relative renal function different by more than 5% from that measured with 99m Tc-DMSA is higher for the 99m Tc-DTPA scintigraphy (p 0.04) than for 99m Tc-EC. Conclusion: the relative renal function measured with 99m Tc-EC dynamic scintigraphy is comparable with that measured with 99m Tc-DMSA static scintigraphy, while the relative renal function measured with 99m Tc-DTPA dynamic scintigraphy presents a significant statistical difference from that measured with 99m Tc-DMSA static scintigraphy. (author)

  3. Synthesis and formulation of {sup 99m} Tc-ECD radiopharmaceutical; Sintesis y formulacion del radiofarmaco {sup 99m} Tc-ECD

    Energy Technology Data Exchange (ETDEWEB)

    Ocampo G, B E

    1998-06-01

    Nuclear medicine is a medical specialty which uses radioactive compounds (radionuclides) for diagnostic and therapeutic purposes. {sup 99m} Tc is the more common radionuclide used in many studies in nuclear medicine because its advantages: it has a photopeak of 140 KeV and a half-life of 6 hours; it can be eluted from a Molybdenum 99 generator, so radiopharmaceuticals can be prepared on site. Ethyl cysteine dimer (ECD) labelled with reduced Technetium 99m has been purposed recently as a promising radiopharmaceutical for brain perfusion imaging {sup 99m} Tc-ECD is a lipophilic neutral complex which cross the brain blood barrier and show high brain uptake. The objective of this work was synthesize and to design a freeze dried formulation for the instant preparation of {sup 99m} Tc-ECD complex useful for brain perfusion imaging. We obtained a freeze dried stable formulation for the preparation of {sup 99m} Tc-ECD kit with a radiochemical purity higher than 90 %, which fulfills with the quality control of radiopharmaceuticals. Furthermore, we developed analytic techniques for the determination of the different chemical compounds into the lyophilized kit. (Author).

  4. Apoptotic abscess imaging with {sup 99m}Tc-HYNIC-rh-Annexin-V

    Energy Technology Data Exchange (ETDEWEB)

    Penn, David L.; Kim, Christopher; Zhang, Kaijun; Mukherjee, Archana; Devakumar, Devadhas; Jungkind, Donald [Department of Radiology, Thomas Jefferson University, Philadelphia, PA 19107 (United States); Thakur, Mathew L. [Department of Radiology, Thomas Jefferson University, Philadelphia, PA 19107 (United States)], E-mail: mathew.thakur@jefferson.edu

    2010-01-15

    Abscess formation causes systemic and localized up-regulation of neutrophil [polymorphonuclear leukocytes (PMNs)] signaling pathways. In the abscess, following bacterial ingestion or PMN activation by inflammatory mediators, PMN apoptosis is elevated and leads to the externalization of phosphatidylserine. Annexin-V (AnxV) has been shown to have high affinity to externalized phosphatidylserine. We hypothesized that {sup 99m}Tc-AnxV will target high densities of apoptotic PMNs and image abscesses. AnxV, conjugated with hydrazinenicaotinamide (HYNIC), was labeled with reduced {sup 99m}TcO{sub 4}{sup -} and its purity was determined by instant thin-layer chromatography. Apoptosis was induced in isolated human PMNs by incubation in 2% saline for 17 and 22 h at 37 deg. C. PMNs were then incubated with {sup 99m}Tc-HYNIC-AnxV and associated {sup 99m}Tc was determined. Abscesses were induced in mice by intramuscular injection of bacteria or turpentine. Following intravenous administration of {sup 99m}Tc-HYNIC-AnxV, mice were imaged and tissue distribution studied at 4 and 24 h. Radiochemical purity of {sup 99m}Tc-HYNIC-AnxV was 84.9{+-}8.11%. At 17 h, {sup 99m}Tc-HYNIC-AnxV bound to apoptotic PMNs was 71.6{+-}0.01% and 48.6{+-}0.01% for experimental and control cells, respectively (P=.002). At 22 h, experimental cells retained 74.9{+-}0.02% and control cells retained 47.2{+-}0.02% (P=.005). {sup 99m}Tc-HYNIC-AnxV associated with bacterial abscesses was 1.25{+-}0.09 and 3.75{+-}0.83 percent injected dose per gram (%ID/g) at 4 and 24 h compared to turpentine abscesses which was 1.02{+-}0.16 and 0.72{+-}0.17 %ID/g at 4 (P{<=}.05) and 24 h (P{<=}.01). {sup 99m}Tc-HYNIC-AnxV represents a minimally invasive and promising agent to image and potentially distinguish between infectious and inflammatory abscesses.

  5. Evaluation of new Tc-99m-labeled Arg-X-Asp-conjugated α-melanocyte stimulating hormone peptides for melanoma imaging.

    Science.gov (United States)

    Flook, Adam M; Yang, Jianquan; Miao, Yubin

    2013-09-03

    The purpose of this study was to examine the melanoma targeting and imaging properties of two new (99m)Tc-labeled Arg-X-Asp-conjugated α-melanocyte stimulating hormone (α-MSH) peptides. RTD-Lys-(Arg(11))CCMSH {c[Asp-Arg-Thr-Asp-DTyr]-Lys-Cys-Cys-Glu-His-DPhe-Arg-Trp-Cys-Arg-Pro-Val-NH2} and RVD-Lys-(Arg(11))CCMSH peptides were synthesized, and their melanocortin-1 (MC1) receptor binding affinities were determined in B16/F1 melanoma cells. The biodistribution and melanoma imaging properties of (99m)Tc-RTD-Lys-(Arg(11))CCMSH and (99m)Tc-RVD-Lys-(Arg(11))CCMSH were determined in B16/F1 melanoma-bearing C57 mice. The IC50 values of RTD-Lys-(Arg(11))CCMSH and RVD-Lys-(Arg(11))CCMSH were 0.7 ± 0.07 and 1.0 ± 0.3 nM in B16/F1 melanoma cells. Both (99m)Tc-RTD-Lys-(Arg(11))CCMSH and (99m)Tc-RVD-Lys-(Arg(11))CCMSH displayed high melanoma uptake. (99m)Tc-RTD-Lys-(Arg(11))CCMSH exhibited the highest tumor uptake of 18.77 ± 5.13% ID/g at 2 h postinjection, whereas (99m)Tc-RVD-Lys-(Arg(11))CCMSH reached the highest tumor uptake of 19.63 ± 4.68% ID/g at 4 h postinjection. Both (99m)Tc-RTD-Lys-(Arg(11))CCMSH and (99m)Tc-RVD-Lys-(Arg(11))CCMSH showed low accumulation in normal organs (<1.7% ID/g) except for the kidneys at 2 h postinjection. The renal uptake of (99m)Tc-RTD-Lys-(Arg(11))CCMSH and (99m)Tc-RVD-Lys-(Arg(11))CCMSH was 135.14 ± 23.62 and 94.01 ± 18.31% ID/g at 2 h postinjection, respectively. The melanoma lesions were clearly visualized by single-photon emission computed tomography (SPECT)/CT using either (99m)Tc-RTD-Lys-(Arg(11))CCMSH or (99m)Tc-RVD-Lys-(Arg(11))CCMSH as an imaging probe at 2 h postinjection. Overall, the introduction of Thr or Val residue retained high melanoma uptake of (99m)Tc-RTD-Lys-(Arg(11))CCMSH and (99m)Tc-RVD-Lys-(Arg(11))CCMSH. However, high renal uptake of (99m)Tc-RTD-Lys-(Arg(11))CCMSH and (99m)Tc-RVD-Lys-(Arg(11))CCMSH need to be reduced to facilitate their future applications.

  6. Evaluation of New Tc-99m-Labeled Arg-X-Asp-Conjugated Alpha-Melanocyte Stimulating Hormone Peptides for Melanoma Imaging

    Science.gov (United States)

    Flook, Adam M.; Yang, Jianquan; Miao, Yubin

    2013-01-01

    The purpose of this study was to examine the melanoma targeting and imaging properties of two new 99mTc-labeled Arg-X-Asp-conjugated alpha-melanocyte stimulating hormone (α-MSH) peptides. RTD-Lys-(Arg11)CCMSH {c[Asp-Arg-Thr-Asp-DTyr]-Lys-Cys-Cys-Glu-His-DPhe-Arg-Trp-Cys-Arg-Pro-Val-NH2} and RVD-Lys-(Arg11)CCMSH peptides were synthesized and their melanocortin-1 (MC1) receptor binding affinities were determined in B16/F1 melanoma cells. The biodistribution and melanoma imaging properties of 99mTc-RTD-Lys-(Arg11)CCMSH and 99mTc-RVD-Lys-(Arg11)CCMSH were determined in B16/F1 melanoma-bearing C57 mice. The IC50 values of RTD-Lys-(Arg11)CCMSH and RVD-Lys-(Arg11)CCMSH were 0.7 ± 0.07 and 1.0 ± 0.3 nM in B16/F1 melanoma cells. Both 99mTc-RTD-Lys-(Arg11)CCMSH and 99mTc-RVD-Lys-(Arg11)CCMSH displayed high melanoma uptake. 99mTc-RTD-Lys-(Arg11)CCMSH exhibited the peak tumor uptake of 18.77 ± 5.13% ID/g at 2 h post-injection, whereas 99mTc-RVD-Lys-(Arg11)CCMSH reached the peak tumor uptake of 19.63 ± 4.68% ID/g at 4 h post-injection. Both 99mTc-RTD-Lys-(Arg11)CCMSH and 99mTc-RVD-Lys-(Arg11)CCMSH showed low accumulation in normal organs (<1.7% ID/g) except for the kidneys at 2 h post-injection. The renal uptake of 99mTc-RTD-Lys-(Arg11)CCMSH and 99mTc-RVD-Lys-(Arg11)CCMSH was 135.14 ± 23.62 and 94.01 ± 18.31% ID/g at 2 h post-injection, respectively. The melanoma lesions were clearly visualized by SPECT/CT using either 99mTc-RTD-Lys-(Arg11)CCMSH or 99mTc-RVD-Lys-(Arg11)CCMSH as an imaging probe at 2 h post-injection. Overall, the introduction of Thr or Val residue retained high melanoma uptake of 99mTc-RTD-Lys-(Arg11)CCMSH and 99mTc-RVD-Lys-(Arg11)CCMSH. However, high renal uptake of 99mTc-RTD-Lys-(Arg11)CCMSH and 99mTc-RVD-Lys-(Arg11)CCMSH need to be reduced to facilitate their future applications. PMID:23885640

  7. 99mTc-MIBI, 99mTc-tetrofosmin and 99mTc-Q12 in vitro and in vivo

    International Nuclear Information System (INIS)

    Bernard, Bert F.; Krenning, Eric P.; Breeman, Wout A. P.; Ensing, Geert; Benjamins, Harry; Bakker, Willem H.; Visser, Theo J.; Jong, Marion de

    1998-01-01

    The aim of this study was to compare uptake of 99m Tc-MIBI, 99m Tc-tetrofosmin and 99m Tc-Q12 in vitro and biodistribution in vivo in rats. In vitro, uptake decreased in the order MIBI→tetrofosmin→Q12. Uptake of MIBI and tetrofosmin, but not of Q12, in cultured tumor cells was dependent on the plasma membrane and mitochondrial potential. In vivo, heart uptake of all three compounds was high and stable. Tumor uptake decreased in the order MIBI→Q12→tetrofosmin and the tumor/blood ratio in the order MIBI→tetrofosmin→Q12

  8. 99mTc-labeling and evaluation of a HYNIC modified small-molecular inhibitor of prostate-specific membrane antigen

    International Nuclear Information System (INIS)

    Xu, Xiaoping; Zhang, Jianping; Hu, Silong; He, Simin; Bao, Xiao; Ma, Guang; Luo, Jianmin; Cheng, Jingyi; Zhang, Yingjian

    2017-01-01

    Introduction: Prostate-specific membrane antigen (PSMA) is a well-established target in the development of radiopharmaceuticals for the diagnosis and therapy of prostate cancer (PCa). In this study, we evaluated a novel 99m Tc-labeled small molecular inhibitor of PSMA. Methods: This new small-molecular inhibitor of PSMA, 6-hydrazinonicotinate-Aminocaproic acid-Lysine-Urea-Glutamate (HYNIC-ALUG) was radiolabeled by 99m Tc and was evaluated both in vitro and in vivo using PCa models (PC-3 and LNCaP). Radiation dosimetry was assessed in mice. Results: 99m Tc-HYNIC-ALUG showed excellent stability in different media. A cell assay preliminarily displayed its specificity for PSMA. The inhibitor showed good pharmacokinetics making it suitable for in vivo imaging. PC-3-derived tumors showed no obvious radioactive uptake; however, the LNCaP-derived tumors showed very high radioactive uptake which was significantly decreased by the selective PSMA inhibitor 2-PMPA. Biodistribution in LNCaP xenografts showed an optimum tumor-to-blood ratio of 24.23 ± 3.54 at 2 h. Tumor uptake was also decreased in the inhibition experiment with 2-PMPA (19.45 ± 2.14%ID/g versus 1.42 ± 0.15%ID/g at 2 h). The effective dose of the 99m Tc-HYNIC-ALUG was 8.4E-04 mSv/MBq. Conclusions: A new 99m Tc-labeled PSMA inhibitor with specific accumulation in PSMA-positive tumors and low background in other organs was synthesized. The radiopharmaceutical also showed very low radiation dosimetry. This agent may significantly improve the diagnosis, staging, and subsequent monitoring of therapeutic effects in PCa patients.

  9. Evaluation of six new /sup 99m/Tc-IDA agents for hepatobiliary imaging

    Energy Technology Data Exchange (ETDEWEB)

    Chervu, L.R.; Joseph, J.A.; Chun, S.B.; Rolleston, R.E.; Synnes, E.I.; Thompson, L.M.; Aldis, A.E.; Rosenthall, L.

    1988-10-01

    IDA derivatives of three substituted benzothiazol, and two substituted chlorophenyl and one substituted pyrazoline compounds have been labeled with /sup 99m/Tc and screened with four rat models with hepatocellular dysfunction manifesting varying degrees of change of liver architecture and hepatocellular damage associated with an active parenchymal destruction, fatty metamorphosis and cirrhosis. Organ distribution studies at 1 h postinjection have been compared in normal and diseased animal models for each agent labeled with /sup 99m/Tc and with /sup 99m/Tc-Disofenin (Disida) and Lidofenin (Hida) and /sup 131/I-Rose Bengal. From the data obtained with the six new IDA derivatives, the distribution kinetics of /sup 99m/Tc-Arclophenin, (N-N'-2-benzoyl-4-chlorophenyl)carbamoylmethyl) imino diacetic acid (Phenida), are closely comparable to /sup 99m/Tc-Disofenin in all animal models. Crossover patient studies (n = 14) for clinical evaluation of /sup 99m/Tc-Arclophenin vs /sup 99m/Tc-Disofenin indicate the close similarity of the 2 agents with regard to blood pool retention, gross liver/heart ratios and liver washout, suggesting Arclophenin as a suitable agent for hepatobiliary function studies. The impaired hepatocellular animal models presented should serve for fast screening of hepatobiliary agents and enable comparison of a series of closely related compounds.

  10. Studies of liver scintigram by sup(99m)Tc-sodium phytate

    International Nuclear Information System (INIS)

    Abe, Masahide; Matsui, Kengo; Chiba, Kazuo; Yamada, Hideo; Iio, Masahiro

    1974-01-01

    Inositol hexaphosphate occurs in nature either free or in compounds (phytic acid). It is soluble in water and becomes a microcolloid by chelating serum calcium after intravenous injection, and forming insoluble calcium phytate, which undergoes reticuloendothelial localization. Case reports were made on all patients who had liver scan studies between August and December, 1973. Eighty-eight patients were studied with a total of 96 liver scans with sup(99m)Tc-phytate. Among these, the hepatic blood flow of eighteen were studied with sup(99m)Tc-phytate and 198 Au-colloid simultaneously. Labeling of sup(99m)Tc-phytate was easy, it remained stable for a long time and only a few free technetium were revealed (labeling yield: average 93.6%). The blood clearance of sup(99m)Tc-phytate was slower than that of 198 Au-colloid. This suggests that the liver scan must begin more than twenty minutes after the injection. Comparing their affinities for the reticuloendothelial system, sup(99m)Tc-phytate shows a greater accumulation in the spleen than does 198 Au-colloid. sup(99m)Tc-phytate is a useful diagnostic scanning agent of the liver and spleen. Because of its superior physical characteristics excellent scans are readily obtained with minimal radiation to the patient and there have been no side effects who have received sup(99m)Tc-phytate. (author)

  11. Lymphoscintigraphy in melanoma patients using Tc-99m dextran

    International Nuclear Information System (INIS)

    Marciano, D.; Padgett, H.; Henze, E.; Carlson, C.; Bennett, L.R.

    1984-01-01

    Surgical removal of regional lymph nodes draining the site of a melanoma is a generally practiced procedure. It is often difficult in many cases of truncal melanomas near the midline or near the waistline to determine which group or groups of nodes to remove. Colloidal Au-198, Tc-99m sulfur colloid, and Tc-99m antimony sulfur colloid have all been used and have given useful clinical information. Objections, however, have been raised to the local radiation dose with these compounds. To reduce this problem while obtaining greater information on lymph flow, the authors have studied dextran, a macromolecule commonly used as plasma substitute. Dextran (average mol. wt. 72,000) labeled with Tc-99m has been used to study lymph drainage from the site of truncal melanoma in 29 patients. Serial images in the first hour following intradermal injection clearly demonstrate tracer in efferent lymphatics within 5 to 10 minutes, and brief pooling in the regional lymph nodes between 20 and 60 minutes. When compared with particulate tracers such as micro Tc-99m sulfur colloid, the Tc-99m dextran appears to move much faster through the lymphatics. Overall distribution of the Tc-99m dextran to lymph nodes is very similar to previous findings with micro Tc-99m sulfur colloid. Dextran drainage to more than one group of regional nodes was seen in 12/29 patients as compared with 17/50 patients using micro Tc-99m sulfur colloid. The superior images with Tc-99m dextran appear to make it the agent of choice

  12. Development of a kit for RBC labelling with 99mTc and its clinic evaluation

    International Nuclear Information System (INIS)

    Marafuschi, A.M.; Nowotny, G.A.; Palcos, M.C.; Rotta, M. del C.

    1980-01-01

    A kit for labelling red blood cells (RBC) with 99m Tc based on a Tin Pyrophosphate mixture freeze-dried and a saline solution saturated with nitrogen has been prepared for spleen and placenta scanning, circulatory studies and blood volume determinations. The stannous tin is intended to reduce the 99m Tc pertechnetate, obtained either from generators or from solvent extraction, to the appropriate valence state suitable for labelling. The technique is as follows: Add to the heparinized blood sample the Tin-Pyrophosphate mixture dissolved in the saline solution. After five minutes incubation time at room temperature the plasma is discarded by centrifugation. Following the addition of the tracer activity to the separated RBC, the supernatant is discarded after a second centrifugation. Depending on the test to be performed, the RBC are either resuspended in saline solution for blood pool or circulation studies or denaturalized at 49.5 deg C for spleen scanning. The labelling yield (95-88%) and its stability has been checked by in vitro measurements, up to four hours after labelling. The biological distribution and spleen uptake have been determined in rats and rabbits. The developed method proved to be adequate for labelling RBC with good labelling retention. An interesting application is shown in babies with congenital cardiac defects and suspected absence of the spleen, where the scan gave a good image of the existing spleen. (author) [es

  13. Technetium 99m-labeled annexin v scintigraphy of platelet activation in vegetations of experimental endocarditis

    Energy Technology Data Exchange (ETDEWEB)

    Rouzet, F.; Sarda-Mantel, L.; Le Guludec, D. [Nucl Med Serv, Grp Hosp Bichat Claude Bernard, AP-HP, Paris (France); Rouzet, F.; Sarda-Mantel, L.; LeGuludec, D. [Univ Denis Diderot Paris 7, UMR S773, Paris (France); Rouzet, F.; Sarda-Mantel, L.; Le Guludec, D. [INSERM, U773, Paris (France); Hernandez, M.D.; Louedec, L.; Michel, J.B. [Univ Paris 07, CHU Xavier Bichat, INSERM, U698, Paris (France); Hervatin, F. [CEA, DSV, DRM, SHFJ, Orsay (France); Lefort, A.; Fantin, B. [Univ Denis Diderot Paris 7, EA 3964, Paris (France); Duval, X. [Univ Denis Diderot Paris 7, INSERM, CIC 007, Paris (France); Duval, X. [Univ Denis Diderot Paris 7, AP-HP, Grp Hosp Bichat Claude Bernard, Ctr Invest Clin, Paris (France); Hernandez, M.D. [Univ Guadalajara, DeptPathol, Guadalajara 44430, Jalisco (Mexico)

    2008-07-01

    Background: The pathophysiology of infective endocarditis involves a pathogen/host tissue interaction, leading to formation of infected thrombotic vegetations. Annexin V is a ligand of phosphatidyl-serines exposed by activated platelets and apoptotic cells. Because vegetations are platelet-fibrin clots in which platelet pro-aggregant activity is enhanced by bacterial colonization, we investigated the ability of annexin V labeled with technetium {sup 99m}Tc ({sup 99m}Tc-ANX) to provide functional imaging of these vegetations in experimental models of infective endocarditis. This ability was assessed in rabbits and rats because of the different interest of these 2 species in preclinical analysis. Methods and Results: Non-bacterial thrombotic endocarditis was induced with the use of a catheter left indwelling through the aortic or tricuspid valve, and animals were injected with either a bacterial inoculum or saline. Scintigraphic investigations were performed 5 days later and showed a higher {sup 99m}Tc-ANX uptake by vegetations in infected versus non-infected animals (ratio,1.3 for in vivo acquisitions and 2 for autoradiography; P {<=} 0.0001 for all), whereas no significant uptake was present in controls. Right-sided endocarditis was associated with pulmonary uptake foci corresponding to emboli. Histological analysis of vegetations showed a specific uptake of {sup 99m}Tc-ANX at the interface between circulating blood and vegetation. In parallel, underlying myocardial tissue showed myocyte apoptosis and mucoid degeneration, without extracellular matrix degradation at this stage. Conclusions: {sup 99m}Tc-ANX is suitable for functional imaging of platelet-fibrin vegetations in endocarditis, as well as embolic events. {sup 99m}Tc-ANX uptake reflects mainly platelet activation in the luminal layer of vegetations. This uptake is enhanced by bacterial colonization. (authors)

  14. An expedient method for the preparation of 99mTc-MIBI and 99mTc-MAG3 using microwave and teflon 'bomb'

    International Nuclear Information System (INIS)

    Varelis, P.; Poot, M.T.

    1998-01-01

    Full text: The recommended method for the preparation of 99mTc-MIBI and 99mTc-MAG3 requires that they be heated in a boiling water bath for 10 minutes, after reconstitution with sodium pertechnetate. This method is both inconvenient and time consuming. A more rapid and convenient method for the preparation of these radiopharmaceuticals employs a conventional microwave oven. However, a serious limitation of this method is the hazard associated with an explosion of a vessel containing a radioactive substance. Traditionally, mixtures that can potentially explode are contained in a device called a 'bomb'. We have developed a method, utilising such a device, that allows us to rapidly and safely prepare 99mTc-MIBI and 99mTc-MAG3 using a microwave oven. This device is used in our department on a daily basis. Since using the teflon bomb, there has been one incidence of an explosion, which was successfully contained within the bomb. There was no statistically significant difference between the radiochemical purity (RCP) of the microwave prepared samples and those obtained using the recommended method. In conclusion, 99mTc-MIBI and 99mTc-MAG3 can be safely prepared and quality controlled in under ten minutes using a microwave oven and our teflon bomb. The average RCP for 99mTc-MIBI and 99mTc-MAG3 prepared using a microwave oven were 97.0+2.0% (n=19) and 99.8+0.2 (n=7) respectively

  15. An expedient method for the preparation of 99mTc-MIBI and 99mTc-MAG3 using microwave and teflon `bomb`

    Energy Technology Data Exchange (ETDEWEB)

    Varelis, P.; Poot, M.T. [St George Hospital, Sydney, NSW (Australia). Department of Nuclear Medicine

    1998-06-01

    Full text: The recommended method for the preparation of 99mTc-MIBI and 99mTc-MAG3 requires that they be heated in a boiling water bath for 10 minutes, after reconstitution with sodium pertechnetate. This method is both inconvenient and time consuming. A more rapid and convenient method for the preparation of these radiopharmaceuticals employs a conventional microwave oven. However, a serious limitation of this method is the hazard associated with an explosion of a vessel containing a radioactive substance. Traditionally, mixtures that can potentially explode are contained in a device called a `bomb`. We have developed a method, utilising such a device, that allows us to rapidly and safely prepare 99mTc-MIBI and 99mTc-MAG3 using a microwave oven. This device is used in our department on a daily basis. Since using the teflon bomb, there has been one incidence of an explosion, which was successfully contained within the bomb. There was no statistically significant difference between the radiochemical purity (RCP) of the microwave prepared samples and those obtained using the recommended method. In conclusion, 99mTc-MIBI and 99mTc-MAG3 can be safely prepared and quality controlled in under ten minutes using a microwave oven and our teflon bomb. The average RCP for 99mTc-MIBI and 99mTc-MAG3 prepared using a microwave oven were 97.0+2.0% (n=19) and 99.8+0.2 (n=7) respectively

  16. 99mTc-EDDA/HYNIC-TOC: a new 99mTc-labelled radiopharmaceutical for imaging somatostatin receptor-positive tumours; first clinical results and intra-patient comparison with 111In-labelled octreotide derivatives.

    Science.gov (United States)

    Decristoforo, C; Mather, S J; Cholewinski, W; Donnemiller, E; Riccabona, G; Moncayo, R

    2000-09-01

    [111In-diethylene triamine penta-acetic acid-D-Phe1]-octreotide (DTPA-octreotide) scintigraphy has gained widespread acceptance as a diagnostic clinical procedure in oncology for imaging somatostatin receptor-positive tumours. However, indium-111 as a radiolabel has several drawbacks, including limited availability, suboptimal gamma energy and high radiation burden to the patient. We have recently reported on the preclinical development of 99mTc-EDDA/HYNIC-TOC, a new octreotide derivative which showed promising results both in vitro and in vivo. We now report our initial clinical experiences with this new radiopharmaceutical in ten oncological patients. The clinical diagnoses were: carcinoid syndrome (n=5), thyroid cancer (n=3), pancreatic cancer (n=1) and pituitary tumour (n=1). The biodistribution and kinetics of 99mTc-EDDA/HYNIC-TOC were compared with those of 111In-DTPA-octreotide in six cases, and with those of 111In-DOTA-TOC in five cases. With the new tracer tumours were imaged within 15 min after injection and showed the highest target/non-target ratios 4 h after injection. Tumour uptake persisted up to 20 h p.i. The rate of blood clearance was similar to that of 111In-DTPA-octreotide but faster than that of 111In-DOTA-TOC, while urinary excretion was lower compared with the 111In derivatives. Semi-quantitative region of interest analysis showed that 99mTc-EDDA/HYNIC-TOC produced higher tumour/organ (target/non-target) ratios than the 111In derivatives, especially in relation to heart and muscle. Significantly more lesions could be detected in 99mTc images. We conclude that 99mTcEDDA/HYNIC-TOC shows better imaging properties for the identification of somatostatin receptor-positive tumour sites than currently available 111In-labelled octreotide derivatives.

  17. 99mTc-EDDA/HYNIC-TOC: a new 99mTc-labelled radiopharmaceutical for imaging somatostatin receptor-positive tumours: first clinical results and intra-patient comparison with 111In-labelled octreotide derivatives

    International Nuclear Information System (INIS)

    Decristoforo, C.; Cholewinski, W.; Donnemiller, E.; Riccabona, G.; Moncayo, R.

    2000-01-01

    [ 111 In-diethylene triamine penta-acetic acid-d-Phe 1 ]-octreotide (DTPA-octreotide) scintigraphy has gained widespread acceptance as a diagnostic clinical procedure in oncology for imaging somatostatin receptor-positive tumours. However, indium-111 as a radiolabel has several drawbacks, including limited availability, suboptimal gamma energy and high radiation burden to the patient. We have recently reported on the preclinical development of 99m Tc-EDDA/HYNIC-TOC, a new octreotide derivative which showed promising results both in vitro and in vivo. We now report our initial clinical experiences with this new radiopharmaceutical in ten oncological patients. The clinical diagnoses were: carcinoid syndrome (n=5), thyroid cancer (n=3), pancreatic cancer (n=1) and pituitary tumour (n=1). The biodistribution and kinetics of 99m Tc-EDDA/HYNIC-TOC were compared with those of 111 In-DTPA-octreotide in six cases, and with those of 111 In-DOTA-TOC in five cases. With the new tracer tumours were imaged within 15 min after injection and showed the highest target/non-target ratios 4 h after injection. Tumour uptake persisted up to 20 h p.i. The rate of blood clearance was similar to that of 111 In-DTPA-octreotide but faster than that of 111 In-DOTA-TOC, while urinary excretion was lower compared with the 111 In derivatives. Semi-quantitative region of interest analysis showed that 99m Tc-EDDA/HYNIC-TOC produced higher tumour/organ (target/non-target) ratios than the 111 In derivatives, especially in relation to heart and muscle. Significantly more lesions could be detected in 99m Tc images. We conclude that 99m Tc-EDDA/HYNIC-TOC shows better imaging properties for the identification of somatostatin receptor-positive tumour sites than currently available 111 In-labelled octreotide derivatives. (orig.)

  18. Comparison of biological properties of 99mTc-labeled cyclic RGD Peptide trimer and dimer useful as SPECT radiotracers for tumor imaging

    International Nuclear Information System (INIS)

    Zhao, Zuo-Quan; Yang, Yong; Fang, Wei; Liu, Shuang

    2016-01-01

    Introduction: This study sought to evaluate a 99m Tc-labeled trimeric cyclic RGD peptide ( 99m Tc-4P-RGD 3 ) as the new radiotracer for tumor imaging. The objective was to compare its biological properties with those of 99m Tc-3P-RGD 2 in the same animal model. Methods: HYNIC-4P-RGD 3 was prepared by reacting 4P-RGD 3 with excess HYNIC-OSu in the presence of diisopropylethylamine. 99m Tc-4P-RGD 3 was prepared using a kit formulation, and evaluated for its tumor-targeting capability and biodistribution properties in the BALB/c nude mice with U87MG human glioma xenografts. Planar and SPECT imaging studies were performed in athymic nude mice with U87MG glioma xenografts. For comparison purpose, 99m Tc-3P-RGD 2 (a α v β 3 -targeted radiotracer currently under clinical evaluation for tumor imaging in cancer patients) was also evaluated in the same animal models. Blocking experiments were used to demonstrate the α v β 3 specificity of 99m Tc-4P-RGD 3 . Results: 99m Tc-4P-RGD 3 was prepared with > 95% RCP and high specific activity (~ 200 GBq/μmol). 99m Tc-4P-RGD 3 and 99m Tc-3P-RGD 2 shared almost identical tumor uptake and similar biodistribution properties. 99m Tc-4P-RGD 3 had higher uptake than 99m Tc-3P-RGD 2 in the intestines and kidneys; but it showed better metabolic stability. The U87MG tumors were clearly visualized by SPECT with excellent contrast with 99m Tc-4P-RGD 3 and 99m Tc-3P-RGD 2 . Conclusion: Increasing peptide multiplicity from 3P-RGD 2 to 4P-RGD 3 offers no advantages with respect to the tumor-targeting capability. 99m Tc-4P-RGD 3 is as good a SPECT radiotracer as 99m Tc-3P-RGD 2 for imaging α v β 3 -positive tumors. -- Graphical abstract: This report presents evaluations of a 99m Tc-labeled cyclic RGD peptide trimer ( 99m Tc-4P-RGD 3 ) as the new SPECT radiotracer for tumor imaging. It was found that 99m Tc-4P-RGD 3 was able to accumulate in the xenografted U87MG tumors with high specificity. Display Omitted

  19. Evaluation of aptamers labelled with 99mTc for identification of Staphylococcus aureus bacteria

    International Nuclear Information System (INIS)

    dos Santos, Sara Roberta

    2014-01-01

    Staphylococcus aureus is specie of great medical importance because it is often associated with many infections in humans. This bacterium can cause diseases ranging from simple infections to life-threatening infections such as endocarditis, pneumonia, meningitis, toxic shock syndrome, septicemia, osteomyelitis, among others. S. aureus is the most commonly agent found in infections of the skin and soft tissues, bone infections and bone prostheses. The difficulty in early detection of specific foci caused by bacteria has raised the need to search for new techniques for this purpose. Diagnosis by scintigraphy has advantages over other methods because it is able to identify damage tissues without the need of invasive procedures and is able to perform an early diagnosis even before anatomic changes. Thus, nuclear medicine could contribute to an accurate diagnosis of bacterial infections, since specific radiopharmaceuticals were developed. Aptamers are oligonucleotides that have high affinity and specificity for their molecular targets and are emerging as a new class of molecules for radiopharmaceuticals development. Radiolabeled aptamers specific to the infectious agents, could give a significant contribution to the infection diagnosis by scintigraphy. In this study, aptamers selected to S. aureus were labeled with 99m Tc and used for the bacteria identification in vitro and in vivo. The aptamers labeled with 32 P and incubated in vitro with S. aureus cells showed high affinity for the bacterial cells when compared with the library of oligonucleotides with random sequences used as control. The aptamers labeled with 99m Tc also showed affinity for S. aureus cells when compared with the library, but unspecific binding was also verified. The 99m Tc labelled aptamers were stable in 0.9% saline, plasma of Swiss mice and in excess of cysteine. The in vivo biodistribution studies using Swiss mice with intramuscular infection in the right thigh showed that the aptamers labeled

  20. [{sup 99m}Tc]TRODAT-1: a novel technetium-99m complex as a dopamine transporter imaging agent

    Energy Technology Data Exchange (ETDEWEB)

    Meiping, Kung [Department of Radiology, University of Pennsylvania, Philadelphia (United States); Stevenson, D A [Department of Radiology, University of Pennsylvania, Philadelphia (United States); Ploessl, K [Department of Radiology, University of Pennsylvania, Philadelphia (United States); Meegalla, S K [Department of Radiology, University of Pennsylvania, Philadelphia (United States); Beckwith, A [Department of Radiology, University of Pennsylvania, Philadelphia (United States); Essman, W D [Department of Psychiatry, University of Pennsylvania, Philadelphia (United States); Mu, M [Department of Radiology, University of Pennsylvania, Philadelphia (United States); Lucki, I [Department of Psychiatry, University of Pennsylvania, Philadelphia (United States); [Department of Pharmacology, University of Pennsylvania, Philadelphia (United States); Kung, H F [Department of Radiology, University of Pennsylvania, Philadelphia (United States); [Department of Pharmacology, University of Pennsylvania, Philadelphia (United States)

    1997-04-01

    Technetium-99m is the most commonly used radionuclide in routine nuclear medicine imaging procedures. Development of {sup 99m}Tc-labeled receptor-specific imaging agents for studying the central nervous system is potentially useful for evaluation of brain function in normal and disease states. A novel {sup 99m}Tc-labeled tropane derivative, [{sup 99m}Tc]TRODAT-1, which is useful as a potential CNS dopamine transporter imaging agent, was evaluated and characterized. After i.v. injection into rats, [{sup 99m}Tc]TRODAT-1 displayed specific brain uptake in the rat striatal region (striatum-cerebellum/cerebellum ratio 1.8 at 60 min), where dopamine neurons are concentrated. The specific striatal uptake could be blocked by pretreating rats with a dose of competing dopamine transporter ligand, {beta}-CIT (or RTI-55, i.v., 1 mg/kg). However, the specific striatal uptake of [{sup 99m}Tc]TRODAT-1 was not affected by co-injection of excess free ligand (TRODAT-1, up to 200 {mu}g per rat) or by pretreating the rats with haloperidol (i.v., 1 mg/kg). The specific uptake in striatal regions of rats that had prior 6-hydroxydopamine lesion in the substantia nigra area showed a dramatic reduction. The radioactive material recovered from the rat striatal homogenates at 60 min after i.v. injection of [{sup 99m}Tc]TRODAT-1 showed primarily the original compound (>95%), a good indication of in vivo stability in brain tissue. Similar and comparable organ distribution patterns and brain regional uptakes of [{sup 99m}Tc]TRODAT-1 were obtained for male and female rats. (orig./AJ). With 4 figs., 6 tabs.

  1. A fundamental study on brain scanning with sup(99m)Tc-citrate

    International Nuclear Information System (INIS)

    Ishii, Katsumi; Kobayashi, Takeshi; Yamada, Nobuaki; Horiike, Shigeharu; Nakazawa, Keiji

    1978-01-01

    We examined the sup(99m)Tc-citrate obtained by labelling citrate with sup(99m)Tc-pertechnetate using Solcocitran Kit. For our fundamental study--we measured the ratio of labelling by means of paper chromatography. By picking out each organs of each rats we also measured the velocity at which radiopharmaceuticals disappeared in each of their organs, and the distribution of radio-pharmaceuticals in their organs. For our clinical study--we performed brain scanning on 47 patients. The following are the results; Citrate was labelled as much as 99 - 95% into sup(99m)Tc-pertechnetate. The velocity of disappearance in each organ of the rats was quicker than in the case of sup(99m)TcO 4 - . Accumulation in the choroid plexus and salivary gland was not obserbed despite the fact that we did not use KClo 4 , and images of brain tumor were obtainable to a high degree. (author)

  2. Preparation and biological profile of 99mTc-lidocaine as a cardioselective imaging agent using 99mTc eluted from 99Mo/99mTc generator based on Al-Mo gel

    International Nuclear Information System (INIS)

    Sakr, T.M.; October University of Modern Sciences and Arts; Ibrahim, A.B.; Rashed, H.M.; Fasih, T.W.

    2017-01-01

    The current study is aimed to prepare 99m Tc-lidocaine as a new myocardial perfusion-imaging agent. The used 99m Tc was obtained from Al- 99 Mo-molybdate(VI) gel matrix. 99m Tc-lidocaine showed higher (15.4 ± 0.11% ID/g) and faster (15 min post injection) cardiac uptake than the recently studied 99m Tc-valsartan and 99m Tc-procainamide. Consequently, 99m Tc-lidocaine will be a valuable myocardial SPECT agent for diagnosis of emergency patients. Besides, the receptor affinity study confirmed the selectivity of 99m Tc-lidocaine for sodium channels in the heart. (author)

  3. Synthesis and biodistribution of 99mTc-Vancomycin in a model of bacterial infection

    International Nuclear Information System (INIS)

    Roohi, S.; Mushtaq, A.; Malik, S.A.

    2005-01-01

    Vancomycin Hydrochloride is an antibiotic produced by the growth of certain strains of Streptomyces orientalis. As vancomycin hydrochloride is poorly absorbed after oral administration; it is given intravenously for therapy of systemic infections. Vancomycin was labeled with technetium-99m pertechnetate using SnCl 2 . 2H 2 O as reducing agent. The labeling efficiency depends on ligand/reductant ratio, pH, and volume of reaction mixture. Radiochemical purity and stability of 99m Tc-Vancomycin was determined by thin layer chromatography. Biodistribution studies of 99m Tc-Vancomycin were performed in a model of bacterial infection in Sprague-Dawley rats. A significantly higher accumulation of 99m Tc-Vancomycin was seen at sites of S. aureus infected animals. Whereas uptake of 99m Tc-Vancomycin in turpentine inflamed rats were quite low. (orig.)

  4. Preparation of glucoheptonate - sup(99m) Tc using stannous ascorbate as reducing agent for TcO-4 ion

    International Nuclear Information System (INIS)

    Barboza, M.R.F.F. de; Silva, C.P.G. da.

    1983-12-01

    A preparation procedure of stannous ascorbate in lyophilized form is presented. This reducing agent was employed for the preparation of kits of calcium glucoheptonate (GHA) to be labelled with sup(99m) Tc for use in kidney scintigraphy. Comparative studies between kits prepared with stannous ascorbate and those prepared with stannous chloride as reducing agent were made. The labelling yield during 18 hours after the addition of sup(99m) TcO - 4 was higher when stannous ascorbate was used. The stability of kits of calcium glucoheptonate - sup(99m) Tc containing stannous ascorbate was studied during five months after its preparation in the lyophilized form. On the fifth month the labelling yield of GHA - sup(99m) Tc was 89-95%, being therefore suitable for kidney scintigraphy. (Author) [pt

  5. Comparative evaluation of 131I-hippuran and sup(99m)Tc-DTPA for renal function test

    International Nuclear Information System (INIS)

    Kempi, V.; Persson, R.B.R.; Svensson, L.

    1975-07-01

    131 I-labelled Hippuran and sup(99m)Tc-labelled DTPA have been compared as substances used for renal function tests. The radiation absorbed dose for 131 I-Hippuran and sup(99m)Tc-DTPA to different organs of an adult standard man is given i a table, showing considerably lower doses for sup(99m)Tc-DTPA. Good agreement was found between the renographic curves obtained with 131 I-Hippuran and sup(99m)Tc-DTPA compared to 131 I-Hippuran excellent scintiphotos of the kidney and also of the upper urinary ways were obtained with sup(99m)Tc-DTPA. With sup(99m)Tc-DTPA, repeated examinations make it possible to follow the development of a disease without great radiation risk to the patient (K.K.)

  6. {sup 201}Tl, {sup 99m}Tc-MIBI, {sup 99m}Tc-tetrofosmin and {sup 99m}Tc-furifosmin: relative retention and clearance kinetics in retrogradely perfused guinea pig hearts

    Energy Technology Data Exchange (ETDEWEB)

    Schaefer, Wolfgang M.; Moka, Detlef E-mail: detlef.moka@uni-koeln.de; Brockmann, Holger A.; Schomaecker, Klaus; Schicha, Harald

    2002-02-01

    Myocellular kinetics of {sup 201}Tl, {sup 99m}Tc-MIBI, {sup 99m}Tc-tetrofosmin and {sup 99m}Tc-furifosmin were investigated using retrogradely-perfused guinea-pig hearts. Relative retention decreased in the order {sup 99m}Tc-MIBI {yields}{yields} implies {sup 99m}Tc-tetrofosmin {yields}{yields} implies {sup 99m}Tc-furifosmin. {sup 201}Tl and {sup 99m}Tc-MIBI exhibited bi- (t1,t2), {sup 99m}Tc-tetrofosmin and {sup 99m}Tc-furifosmin triexponential (t1,t2,t3) time-activity-curves. Latest-phase elimination-half-life increased from {sup 201}Tl (t2) {yields}{yields} implies {sup 99m}Tc-MIBI (t2) {yields}{yields} implies {sup 99m}Tc-tetrofosmin (t3) {yields}{yields} implies {sup 99m}Tc-furifosmin (t3), showing a significant increase in deteriorating myocardium for all tracers but {sup 99m}Tc-furifosmin. Delayed elimination in deteriorating myocardium explains at least partly the redistribution phenomenon of {sup 201}Tl, and suggests a similar phenomenon for {sup 99m}Tc-MIBI and {sup 99m}Tc-tetrofosmin.

  7. Preclinical evaluation of 99mTc(CO)3-aspartic-N-monoacetic acid, 99mTc(CO)3(ASMA), a new renal radiotracer with pharmacokinetic properties comparable to 131I-OIH

    Science.gov (United States)

    Lipowska, Malgorzata; Klenc, Jeffrey; Marzilli, Luigi G.; Taylor, Andrew T.

    2014-01-01

    In an ongoing effort to develop a renal tracer with pharmacokinetic properties comparable to PAH and superior to those of both 99mTc-MAG3 and 131I-OIH, we evaluated a new renal tricarbonyl radiotracer based on the aspartic-N-monoacetic acid ligand, 99mTc(CO)3(ASMA). The ASMA ligand features two carboxyl groups and an amine function for the coordination of the {99mTc(CO)3}+ core as well as a dangling carboxylate to facilitate rapid renal clearance. Methods rac-ASMA and L-ASMA were labeled with a 99mTc-tricarbonyl precursor and radiochemical purity of the labeled products was determined by HPLC. Using 131I-OIH as an internal control, we evaluated biodistribution in normal rats with 99mTc(CO)3(ASMA) isomers and in rats with renal pedicle ligation with 99mTc(CO)3(rac-ASMA). Clearance studies were conducted in 4 additional rats. In vitro radiotracer stability was determined in PBS buffer pH 7.4 and in challenge studies with cysteine and histidine. 99mTc(CO)3(ASMA) metabolites in urine were analyzed by HPLC. Results Both 99mTc(CO)3(ASMA) preparations had > 99% radiochemical purity and were stable in PBS buffer pH 7.4 for 24 h. Challenge studies on both revealed no significant displacement of the ligand. In normal rats, % injected dose in urine at 10 and 60 min for both preparations averaged 103% and 106% that of 131I-OIH, respectively. The renal clearances of 99mTc(CO)3(rac-ASMA) and 131I-OIH were comparable (P = 0.48). The tracer was excreted unchanged in the urine, proving its in vivo stability. In pedicle-ligated rats, 99mTc(CO)3(rac-ASMA) had less excretion into the bowel (P ASMA) complexes have pharmacokinetic properties in rats comparable to or superior to those of 131I-OIH, and human studies are warranted for their further evaluation. PMID:22717977

  8. Experimental study of radiopharmaceuticals based on technetium-99m labeled derivative of glucose for tumor diagnosis

    Science.gov (United States)

    Zeltchan, R.; Medvedeva, A.; Sinilkin, I.; Bragina, O.; Chernov, V.; Stasyuk, E.; Rogov, A.; Il'ina, E.; Larionova, L.; Skuridin, V.; Dergilev, A.

    2016-06-01

    Purpose: to study the potential utility of 1-thio-D-glucose labeled with 99mTc for cancer imaging in laboratory animals. Materials and method: the study was carried out in cell cultures of normal CHO (Chinese hamster ovary cells CHO) and malignant tissues MCF-7 (human breast adenocarcinoma MCF-7). To evaluate the uptake of 99mTc-1-thio-D-glucose in normal and tumor tissue cells, 25 MBq of 1-thio-D-glucose labeled with 99mTc was added to the vials with 3 million cells and incubated for 30 minutes at room temperature. After centrifugation of the vials with cells, the supernatant was removed. Radioactivity in vials with normal and tumor cells was then measured. In addition, the study included 40 mice of C57B 1/6j lines with tumor lesion of the right femur. For neoplastic lesions, Lewis lung carcinoma model was used. Following anesthesia, mice were injected intravenously with 25MBq of 99mTc-1-thio-D-glucose. Planar scintigraphy was performed 15 minutes later in a matrix of 512x512 pixels for 5 minutes. Results: when measuring the radioactivity of normal and malignant cells after incubation with 99mTc-1-thio-D- glucose, it was found that the radioactivity of malignant cells was higher than that of normal cells. The mean values of radioactivity levels in normal and malignant cells were 0.3±0.15MBq and 1.07±0.6MBq, respectively. All examined animals had increased accumulation of 99mTc-1-thio- D-glucose at the tumor site. The accumulation of 99mTc-1-thio-D-glucose in the tumor was on average twice as high as compared to the symmetric region. Conclusion: The present study demonstrated that 99mTc-1-thio-D-glucose is a prospective radiopharmaceutical for cancer visualization. In addition, high accumulation of 99mTc-1-thio-D-glucose in the culture of cancer cells and in tumor tissue of animals demonstrates tumor tropism of the radiopharmaceutical.

  9. Experimental study of {sup 99m}Tc-aluminum oxide use for sentinel lymph nodes detection

    Energy Technology Data Exchange (ETDEWEB)

    Chernov, V. I., E-mail: Chernov@oncology.tomsk.ru; Sinilkin, I. G.; Zelchan, R. V.; Medvedeva, A. A. [Tomsk Cancer Research Institute, Kooperativny Street 5, Tomsk, 634050 (Russian Federation); Tomsk Polytechnic University, Lenin Avenue 30, Tomsk, 634050 (Russian Federation); Lyapunov, A. Yu., E-mail: Lyapunov1720.90@mail.ru [Tomsk Cancer Research Institute, Kooperativny Street 5, Tomsk, 634050 (Russian Federation); Bragina, O. D.; Varlamova, N. V.; Skuridin, V. S. [Tomsk Polytechnic University, Lenin Avenue 30, Tomsk, 634050 (Russian Federation)

    2016-08-02

    . Plateau of {sup 99m}Tc-Nanocis accumulation in the lymph node (average 2.05%) occurred after 2 hours of the study and remained almost on the same level (in average 2.3%) for 24 hours. Thus, the experimental study of a new domestic radiopharmaceutical showed that the {sup 99m}Tc-Al{sub 2}O{sub 3} accumulates actively in the lymph nodes several times as compared to the imported analogue and its practical application will facilitate intraoperative identification of sentinel lymph nodes.

  10. Imaging of rat cerebral ischemia-reperfusion injury using99mTc-labeled duramycin

    International Nuclear Information System (INIS)

    Zhang Yuqing; Stevenson, Gail D.; Barber, Christy; Furenlid, Lars R.; Barrett, Harrison H.; Woolfenden, James M.; Zhao Ming; Liu Zhonglin

    2013-01-01

    Objectives: Prompt identification of necrosis and apoptosis in the infarct core and penumbra region is critical in acute stroke for delineating the underlying ischemic/reperfusion molecular pathologic events and defining therapeutic alternatives. The objective of this study was to investigate the capability of 99m Tc-labeled duramycin in detecting ischemia-reperfusion injury in rat brain after middle cerebral artery (MCA) occlusion. Methods: Ischemic cerebral injury was induced in ten rats by vascular insertion of a nylon suture in the left MCA for 3 hr followed by 21–24 hr reperfusion. After i.v. injection of 99m Tc-duramycin (1.0-3.5 mCi), dynamic cerebral images were acquired for 1 hr in six rats using a small-animal SPECT imager. Four other rats were imaged at 2 hr post-injection. Ex vivo images were obtained by autoradiography after sacrifice. Histologic analyses were performed to assess cerebral infarction and apoptosis. Results: SPECT images showed that 99m Tc-duramycin uptake in the left cerebral hemisphere was significantly higher than that in the right at 1 and 2 hr post-injection. The level of radioactive uptake in the ischemic brain varied based on ischemic severity. The average ratio of left cerebral hot-spot uptake to right hemisphere radioactivity, as determined by computerized ROI analysis, was 4.92 ± 0.79. Fractional washout at 1 hr was 38.2 ± 4.5% of peak activity for left cerebral hot-spot areas and 80.9 ± 2.0% for remote control areas (P 99m Tc-duramycin SPECT imaging may be useful for detecting and quantifying ongoing apoptotic neuronal cell loss induced by ischemia-reperfusion injury.

  11. Labelling and Organ Distrbution Characterisics of 99mTc Galacturonate Complex Using Dithionite as Reducing Agent

    International Nuclear Information System (INIS)

    Al Hilli, A.M.; Mirza, K.S.; Al Noori, T.H.J.

    2000-01-01

    The labelling conditions of 99m T c-galacturonate complex using dithionite as reducing agent for periechnetate have been described. GCS-method has been applied for radiochemical determination of the labelled complex. At a constant amount of the ligand (50mg) in the preparation, high labelling of 99m Tc -galacturonate complex was obtained in the presence of the reducing agent. The effect of pH on the labelling yield have show that labelling occurs only at near neutral to slightly alkaline pH. The organ distribution results of 99m Tc -galacturonate complex as a function of the reducing agent concentration was achieved in rats. On using 8mg of dithionite as reducing agent,the activity uptake in the kindneys was significantly low, while in the bones was higher, but decreased after 1 hr. of injection. This,however is due to the instability of the labelled complex releasing pertechnetate which was evident by the increase of activity in the stomach. The organ distribution picture of the complex has been reversed by increasing the concentration of dithionite(16 mg) in the preparation,where the activity uptake in the kidnys was increased to higher level and in the bones was decreased.The activity in the stomach was rather low indicating a more stable complex towards oxidation or decomposition

  12. Use of 99mTc from a commercial 99Mo/9mTc generator as yield tracer for the determination of 99Tc at low levels

    DEFF Research Database (Denmark)

    Hou, Xiaolin; Jensen, Mikael; Nielsen, Sven Poul

    2007-01-01

    The concentrations of Tc-99 and impurity radionuclides in the Tc-99m tracer solution obtained from a commercial Mo-99/Tc-99m generator were measured by gamma spectrometry and liquid scintillation counting. Mo-99 and Ru-103 were found in the Tc-99m eluate. A simple separation using two extra alumina...... cartridges was investigated to purify the eluate to obtain a suitable Tc-99m tracer with low Tc-99 concentration. The activity ratio of Tc-99/Tc-99m in the prepared Tc-99m solution is lower than 15 x 10(-9), which is higher than the theoretical ratio of less than 10 x 10(-9). The possible reason is discussed....... The Tc-99 in the 20 kBq spiked Tc-99m tracer was found to be less than 0.3mBq, which is lower than the detection limit of the radiometric method used for environmental samples. The purified Tc-99m eluate is used as yield tracer for the determination of low levels of Tc-99 in environmental samples. (c...

  13. Spent 99Mo/99mTc generator as an economical source of 99Mo

    International Nuclear Information System (INIS)

    El-Kolaly, M.T.

    1990-01-01

    An improved method for utilization and purification of 99 Mo from spent 90 Mo/ 99m Tc generators has been described. After washing the generator with saline to remove the generated 99m Tc, followed by 2 mL 5 M NaOH containing a few drops of H 2 O 2 , the 99 Mo was quantitatively eluted from the generator with 5 mL 5 M NaOH. The alkaline eluate containing 99 Mo was contaminated with partially dissolved alumina. In the present method, an anion-exchange resin Dowex 1 x 8 column was used for purification of 99 Mo from the contaminating alumina. The resultant 99 Mo was of high purity and contained 3+ /mL 99 Mo solution, as estimated by atomic absorption. (author)

  14. Preparation and preclinical pharmacological study on a novel bone imaging agent 99mTc-EMIDP

    International Nuclear Information System (INIS)

    Lin Jianguo; Luo Shineng; Chen Chuanqing; Qiu Ling; Wang Yan; Cheng Wen; Ye Wanzhong; Xia Yongmei

    2010-01-01

    A novel zoledronic acid (ZL) derivative, 1-hydroxy-2-(2-ethyl-4-methyl-1H-imidazol-1-yl)ethane-1,1-diyldiphosphonic acid (EMIDP), was prepared and labeled with 99m Tc successfully in a high labeling yield and good stability in vitro. The preclinical pharmacological properties of 99m Tc-EMIDP were investigated and compared with 99m Tc-MDP and 99m Tc-ZL. The studies of biodistribution in mice and SPECT bone imaging of the rabbit suggest that 99m Tc-EMIDP has highly selective uptake in the skeletal system and rapid clearance in the soft tissues. The present findings indicate that 99m Tc-EMIDP holds great potential for bone scintigraphy.

  15. Spectrophotometric determination of Sn+2 in lyophilized kit for labeling with 99mTc

    International Nuclear Information System (INIS)

    Araujo, Elaine Bortoleti; Sampel, Carolina Judith; Melo, Ivani Bortoleti; Okamoto, Miriam R.Y; Silva, Constancia P.G

    2004-01-01

    The preparation of 99 mTc labeled radiopharmaceuticals depends on the reduction of the technetium pertechnetate, commonly by stannous chloride (SnCl 2 ). The determination of the Sn +2 contents in the lyophilized preparations represents an important quality control procedure that may be applied to the process and to the final product. The objective os this work is the optimization of an spectrophotometric assay to the determination os Sn +2 contents in a citrate-stannous lyophilized kit for 99 mTc labeling. The spectrophotometric methodology employed is based in the colour development when Sn +2 reacts with sodium molybdate in the presence of potasium thiocyanate in chloridric medium. The colourfull reaction studied showed high stability after 60 minutes of the mixtures preparation. The sequence of reagents introduction in the reaction mixture was determinant to the assay. The molibdenium-stannous-tiocianate sequence produces calibration curves with good correlations (R2 ≥ 0.99). The concentrations of the molibdenium solution was also studied, in order to determine a ideal concentration for the Sn +2 range. The spectrophotometric method studied was usefull to the determination of Sn +2 content in different batches of citrate-stannous preparations. The method was fast and easy and can be applied to different stages of the production process, in order to guarantee the content of Sn +2 in the preparations (Au)

  16. Preparation and biological characteristics of 99mTc-diol a renal agent

    International Nuclear Information System (INIS)

    Castanheira, I.; Paulo, A.; Neves, M.; Patricio, L.; Sawas-Dimopoulou, C.

    1993-01-01

    The present work concerns the production of 1,2-dihydroxypropyl-1-phosphonic acid (diol) by acid hydrolysis of (-cis) 1,2-epoxypropylphosphonic acid (phosphomycin), and its formation as a kit easily labeled with [ 99m Tc]pertechnetate. Biodistribution studies and whole-body autoradiographies in mice show that 99m Tc-diol has a specific affinity for the kidneys: it is rapidly cleared from the blood and excreted in urine. Part of the injected activity remains in the kidney cortex sufficiently long to permit kidney imaging. In comparison with other agents which also localize in the kidney cortex, such as 99m Tc-DMSA and 99m Tc-glucoheptonate ( 99m Tc-GHA), the main differences are the following: the peak of renal activity is reached early in the 5 min post-injection period for 99m Tc-diol, only at about 10 min post-injection for 99m Tc-GHA and after 3 h post-injection for 99m Tc-DMSA. The uptake of 99m Tc-diol by other organs, especially by bones, is much smaller than in the case of 99m Tc-DMSA. Unlike 99m Tc-DMSA, the biodistribution of 99m Tc-diol is not significantly influenced by acid-base imbalance. Moreover, the retention effect of hyperuricemia on 99m Tc-diol blood clearance and kidney excretion could be the result of a competition mechanism between this radiopharmaceutical and uric acid for a common transport system. The above biological characteristics suggest that 99m Tc-diol is a kidney radiopharmaceutical with an ability for functional and imaging studies. (author)

  17. Study of factors that interfere in the labelling process of erythrocytes and plasma proteins with Technetium-99m

    International Nuclear Information System (INIS)

    Gutfilen, Bianca

    1989-01-01

    The labelling of red blood cells (RBC) with technetium-99m (Tc-99m) depends on several factors, as the stannous ion (Sn++) concentration, time, temperature, the presence of plasma proteins (PP) and others. However the Sn++ concentration seems to be the most important factor; probably because the uptake of this reducing agent by RBC is limited. The excess of Sn++ in extracellular medium can determine the labelling of PP. the modifications of RBC at 50 deg C described in the literature, the possibility of labelling RBC with Tc-99m at this temperature and experimental results obtained made it possible to perform spleen selective scintigraphy through a simple technique with few manipulations. The effect of gentamicin, nifedipine and verapamil in the labelling of RBC and plasma proteins with Tc-99m was studied because of similarities between Ca++ and Sn++. The results show that, under some conditions, these drugs are capable to alter this Tc-99m incorporation. The modification of the ionic distribution determined by these drugs or the blockage of Sn++ and/or Tc-99m or the fact that they bind theirselves to plasma proteins, or the possibility of the labelling of these drugs, are factors that can interfere in the labelling process of red blood cells and plasma proteins with Tc-99m. (author)

  18. Radiochemical purity and in vitro stability of Tc-99m radiopharmaceuticals

    International Nuclear Information System (INIS)

    Vucina, J.

    2001-01-01

    The increased contents of long lived 99 Tc, oxygen and cupric ions could affect the labeling yield of eight radiopharmaceuticals. Oxygen and in leaser extend copper were found to affect the radiochemical purity of the preparations. In vitro stability of radiopharmaceuticals, examined on 99m Tc(Sn)-pyrosphoshate solutions, was extended when ascorbic acid was added as the chemical stabilizer. The quantity of 5x10 -7 mol/dm 3 of ascorbic acid was found to be sufficient to keep the content of 99m Tc-pertechnetate below 1 % six hours after labeling even in the cases when 99m Tc was present in high radioactive concentrations (740-814 GBq/dm 3 ). The results led to the development of the kits in which ascorbic or gentisic acid are the standards component in the kit composition (author)

  19. Comparison of sup(99m)Tc-MDP to sup(99m)Tc-pertechnetate by computerized quantitative joint scintigraphy

    International Nuclear Information System (INIS)

    Rekonen, A.; Moettoenen, T.; Oka, M.

    1982-01-01

    99mTc-pertechnetate was compared to 99mTc-MDP in joint pairs with asymmetric arthritis. Markedly elevated joint activity ratios (inflamed/uninflamed joint) were measured in all the joint pairs studied. In the joints affected by reactive arthritis and without roentgenologic changes the mean joint activity was the same with both tracers. A very high activity ratio with 99mTc-MDP was found in septic arthritis. In rheumatoid arthritis the sensitivity of 99mTc-MDP as an indicator of active arthritis seemed to be better than that of 99mTc-pertechnetate. Even in joints without erosions in roentgenograms the joint activity ratios were markedly elevated with 99mTc-MDP. This suggests, that high activity in 99mTc-MDP scanning might be prognostic of erosive joint changes. In this work a profile curve was used for quantitation differences between joints

  20. Evaluation of inflammatory processes in temporomandibular joint employing technetium-99m-labelled autologous leukocytes in an animal model; Avaliacao de processos inflamatorios na articulacao temporomandibular empregando leucocitos autologos marcados com tecnecio-99m em modelo animal

    Energy Technology Data Exchange (ETDEWEB)

    Brasileiro, Claudia Borges [Centro Universitario Newton Paiva, Belo Horizonte, MG (Brazil)]. E-mail: claudiabb.prof@newtonpaiva.br; cbbrasileiro@bol.com.br; Cardoso, Valbert Nascimento; Ruckert, Bianca [Minas Gerais Univ., Belo Horizonte, MG (Brazil). Faculdade de Farmacia; Campos, Tarcisio Passos Ribeiro de [Minas Gerais Univ., Belo Horizonte, MG (Brazil). Escola de Engenharia. Dept. de Engenharia Nuclear

    2006-07-15

    Objective: the present study was aimed at identifying temporomandibular joint inflammatory processes employing technetium-99m hexamethyl propylene amine oxime (99mTc-HMPAO)-labeled autonomous leukocytes. Materials and methods: we have utilized an experimental model of arthritis induction in ten adult male New Zealand rabbits by means of ovalbumin intra-articular injection into each left temporomandibular joint. For control purposes, saline solution was injected. After leukocytes radiolabeling with 99mTc-HMPAO and injection into rabbits, scintigraphic images were obtained. Results: a higher 99mTc-HMPAO-leukocytes uptake was observed in left temporomandibular joint in comparison with the contralateral joint. Wilcoxon non-parametric test was applied for statistical analysis. There was a statistically significant difference between counts of radioactivity per minute in the inflamed joint and the contralateral one (p = 0.0073). Conclusion: the method employing 99mTc-HMPAO-labelled autologous leukocytes allows an early and accurate detection of inflammatory processes, contributing to the adoption of a therapeutic conduct for patients before structural alterations have occurred. (author)

  1. Preparation of freeze dried kit of sodium citrate labeled with Tc-99m used as a new kidney functional agent

    International Nuclear Information System (INIS)

    Merzah, K. S.; Abdulkrim, H. M.; Resen, H. M.; Badi, J. M.

    2012-12-01

    A new freeze-dried kit of sodium citrate complex has been prepared, to be labeled with technetium-99m can be used for diagnosis of kidney function. The labeling conditions of Tc-99m citrate complex using stannous chloride as a reducing agent for pertechnetate have been described. The GCS method reveals that the labeling efficiency of Tc-99m citrate complex is promoted by raisinng the pH of the preparation to (pH=4) using 1 N NaOH. The optimal amounts of the reactants in the preparation to obtain labeled and stable complex with high kidney uptake were found to be not less than (1 mg) sodium citrate and not more than (100μg) SnCI 2 2HO. The results show that high labeling yield (≥95%) for the labeled complex (Tc-99 Sn- citrate) can be perform due to the suitable reactant materials. The data of biodistribution experiments in the laboratory animals (Mice), clear high radioactivity accumulation labeled complex in kidney at 5 minutes post injection. The results of the radiochemical purity and biodistribution studies of the lyophilized kit approved that it was stable for about more than seven moths under normal conditions (2-8 o C ). The results of biodistribution of labeled kit have shown a good biological behavior with low radioactivity accumulation in the non-target organs (blood, liver and other organs). the aim of this study was to evaluate the potential of Tc-99-citrate complex as a new kidney functional agents and the efficiency of the freeze dried kit in the diagnosis of kidney function. (Author)

  2. Development of kits for 99mTc radiopharmaceuticals for infection imaging. Report of a co-ordinated research project 2000-2003

    International Nuclear Information System (INIS)

    2004-09-01

    Infectious diseases remain a major health problem and cause of death worldwide, particularly in developing countries. Nuclear medicine imaging, because of its sensitivity, offers an attractive option for diagnosis of focal infections. This needs a reliable radiopharmaceutical that can selectively concentrate in sites of infection. Over the years 67 Ga and other radiopharmaceuticals that localize in inflammation associated with infection sites, also known as 'non-specific agents' have been used for infection imaging. However, experience has shown that an 'infection specific agent' that concentrates selectively at sites of infection and not inflammation would have several advantages. The first such agent developed more than two decades ago was 111 In-leucocytes which is still considered a 'gold standard'. Considerations of cost, availability, and superior properties for imaging make 99 mTc a better label than 111 In. 99 mTc white blood cell (WBC) was developed subsequently and used for infection imaging. However, both 111 In and 99 mTc WBCs have a number of drawbacks, in particular: each patient's blood sample has to be collected and individually radiolabelled; well-trained staff and suitable facilities for separating and labelling the patient's blood are needed; the risk of infection and cross-contamination associated with potential blood-borne microorganisms; and cost of materials. Because of these, considerable efforts have been continuously made towards developing convenient replacements for 99 mTc WBCs with limited success, 99 mTc antigranulocyte antibody being a good example. However, these radiopharmaceuticals still have many disadvantages, related to either their cost and availability or their performance. In view of the large potential for applications in patients, the development of new and improved 99 mTc labelled infection specific imaging agents was considered as a very worthwhile aim for scientific research in general and, in particular, for the

  3. Physicochemical and Biological Analysis of 99mTc-Glutathione Radiopharmaceuticals

    International Nuclear Information System (INIS)

    ME- Sriyani; N- Zainuddin

    2013-01-01

    99m Tc-glutathion ( 99m Tc-GSH) radiopharmaceutical is available in the GSH lyophilized-kit in which ready to use directly after adding 99m Tc radionuclide. In nuclear medicine, 99m Tc-GSH diagnostic kit is a radiopharmaceutical commonly utilized for cancer diagnoses using imaging method. This paper described the physicochemical and biological characteristics as well as the quality of 99m Tc-GSH diagnostic kit prepared from the GSH lyophilized-kit. The radiochemical purity was determined with thin layer chromatography (TLC) method, performed on a TLC-SG stationary phase with a mobile phase of a dried acetone and 0,9% of NaCl solution. Studies on the effect of volume and radioactivity of Na 99m TcO 4 solution to the radiochemical purity of 99m Tc-GSH were carried out. The sterility of GSH-lyophilized kit and toxicity of 99m Tc-GSH were also investigated. The stability test on GSH lyophilized kit and 99m Tc-GSH in several storage conditions, as well as the plasma stability of 99m Tc-GSH was performed. The analysis result showed that the GSH lyophilized-kit was sterile; the 99m Tc-GSH was non toxic with 99.54 ± 0.01% of radiochemical purity and remained stable 5 hours either at room temperature or 4℃. The volume more than 4 mL of Na 99m TcO 4 solution on the labeling of GSH could decreased the 99m Tc-GSH radiochemical purity, while the radioactivity more than 20 mCi in 7 mL of volume extended the incubation time. In-vitro stability test of 99m Tc-GSH in plasma showed that in the two hours of storage, the radiochemical purity decreased to 51.84 ± 2.52%, and until 5 hours of storage it did not change significantly. From the result, it can be concluded that the GSH lyophilized-kit was remained stable after 13 month of storage either at room temperature or 4℃ with 99% of 99m Tc-GSH radiochemical purity. (author)

  4. Effects of broccoli extract on biodistribution and labeling blood components with {sup 99m}Tc-GH

    Energy Technology Data Exchange (ETDEWEB)

    Cekic, Betul; Muftuler, Fazilet Zumrut Biber; Kilcar, Ayfer Yurt; Ichedef, Cigdem; Unak, Perihan [Ege University, Izmir (Turkey). Inst. of Nuclear Sciences. Dept. of Nuclear Applications

    2011-09-15

    Purpose: people consume vegetables without the knowledge of the side effects of the biological and chemical contents and interactions between radiopharmaceuticals and herbal extract. To this end, current study is focused on the effects of broccoli extract on biodistribution of radiolabeled glucoheptonate ({sup 99m}Tc-GH) and radiolabeling of blood components. Methods: GH was labeled with {sup 99m}Tc. Quality control studies were done utilizing TLC method. Biodistribution studies were performed on male rats which were treated via gavage with either broccoli extract or SF as control group for 15 days. Blood samples were withdrawn from rats' heart. Radiolabeling of blood constituents performed incubating with GH, SnCl{sub 2} and {sup 99m} Tc. Results: radiochemical yield of {sup 99m}Tc-GH is 98.46{+-}1.48 % (n=8). Biodistribution studies have shown that according to the control, the treated group with broccoli has approximately 10 times less uptake in kidney. The percentage of the radioactivity ratios of the blood components is found to be same in both groups. Conclusions: although there is no considerable effect on the radiolabeling of blood components, there is an outstanding change on the biodistribution studies especially on kidneys. The knowledge of this change on kidney uptake may contribute to reduce the risk of misdiagnosis and/or repetition of the examinations in Nuclear Medicine. (author)

  5. Method for in vitro labelling of erythrocytes with 99mTc-pertechnetate

    International Nuclear Information System (INIS)

    Kostadinova, I.D.; Hadzhikostova, H.K.; Shejretova, E.T.; Garcheva-Tsacheva, M.B.

    1987-01-01

    The method is easy to apply and gives a possibility to lead the radiopharmaceutical directly to erythrocytes. It includes: blocking of the structures accumulating 99m Tc-pertechnetate by potassium perchlorite; attenuation of the erythrocytes by an intervenous injection of tin pyrophosphate; preparation of the necessary blood quantity with acidum citricum dextrose mixing with 99m Tc-pertechnetate and reinjection. 1 cl

  6. Detection of low-grade prosthetic joint infections using 99mTc-antigranulocyte SPECT/CT: initial clinical results

    International Nuclear Information System (INIS)

    Graute, Vera; Lehner, Sebastian; Haug, Alexander; Bartenstein, Peter; Hacker, Marcus; Feist, Markus; Mueller, Peter Ernst

    2010-01-01

    Low-grade joint infections are characterized by infiltration of granulocytes, which mediate aspects of inflammatory changes. We evaluated retrospectively the contribution of SPECT/CT as an addition to planar scintigraphy with 99m Tc-labelled antigranulocyte antibodies for diagnosing and localizing low-grade joint infections. Planar scintigraphy using 99m Tc-labelled antigranulocyte BW 250/183 antibodies was performed in 31 patients with suspected joint infections at 5 min, 5 h and 24 h after injection, with additional SPECT/CT performed 6 h after injection. With reference to gold standard clinical data, we assessed the diagnostic sensitivity of scintigraphy alone and in conjunction with SPECT/CT. Joint infections were diagnosed clinically in 9 of the 31 patients (1 hip and 8 knee prostheses). Planar scintigraphy revealed 6 true-positives, 13 true-negatives, 9 false-positives and 3 false-negative results, indicating sensitivity, specificity, positive and negative predictive values of, respectively, 0.66, 0.60, 0.4 and 0.81. With the addition of SPECT images, corresponding sensitivity, specificity, positive and negative predictive values increased to 0.89, 0.45, 0.40 and 0.91. Implementation of fused SPECT/CT led to a further increase to 0.89, 0.73, 0.57 and 0.94. Relative to planar scintigraphy, SPECT with and without CT substantially improved the utility of imaging with 99m Tc-labelled antigranulocyte antibodies for diagnosis and localization of suspected joint infections. Optimal accuracy was obtained through image fusion, which permitted anatomical allocation of foci of pathological tracer accumulation as well as providing information on the extent of the infection. This imaging method seems suited for selection of patients requiring surgical therapy. (orig.)

  7. Breast tumor targeting with 99mTc-HYNIC-PR81 complex as a new biologic radiopharmaceutical

    International Nuclear Information System (INIS)

    Salouti, Mojtaba; Rajabi, Hossein; Babaei, Mohammad Hossein; Rasaee, Mohammad Javad

    2008-01-01

    Human epithelial mucin, MUC1, is commonly overexpressed in adenocarcinoma that includes more than 80% of breast cancers. The PR81 is a murine anti-MUC1 monoclonal antibody (MAb) that was prepared against the human breast cancer. We developed an indirect method for labeling of this antibody with 99m Tc in order to use the new preparation in immunoscintigraphy studies of BALB/c mice bearing breast tumors. The 99m Tc-PR81 complex was prepared using the HYNIC as a chelator and tricine as a coligand. The labeling efficiency determined by instant thin-layer chromatography (ITLC) was 89.2%±4.7%, and radiocolloides measured by cellulose nitrate electrophoresis were 3.4%±0.9%. The in vitro stability of labeled product was determined at room temperature by ITLC and in human serum by gel filtration chromatography - 88.3%±4.6% and 79.8%±5.7% over 24 h, respectively. The integrity of labeled MAb was checked by means of sodium dodecyl sulfate polyacrylamide gel electrophoresis, and no significant fragmentation was seen. The results of cell binding studies showed that both labeled and unlabeled PR81 were able to compete for binding to MCF 7 cells. Biodistribution studies performed in female BALB/c mice with breast tumor xenografts at 4, 16 and 24 h after the 99m Tc-HYNIC-PR81 injection demonstrated a specific localization of the compound at the site of tumors and minimum accumulation in non target organs. The tumor imaging was performed in BALB/c mice with breast xenograft tumors at 4, 8, 12, 16, 20, 24, 28, 32 and 36 h after the complex injection. The tumors were visualized with high sensitivity after 8 h. The findings showed that the new radiopharmaceutical is a promising candidate for radioimmunoscintigraphy of the human breast cancer

  8. Chemistry of /sup 99m/Tc labeling kits

    International Nuclear Information System (INIS)

    Srivastava, S.C.; Meinken, G.; Richards, P.

    1976-01-01

    Problems have been reported with the use of kit-produced /sup 99m/Tc radiopharmaceuticals. This study was undertaken to understand the chemistry involved in various stannous kit systems. The relation between Tc, tin, and the ligands used to complex the reduced Tc was investigated. It is concluded that for reliable performance, stannous kits should be prepared so that most of the tin is kept in the usable (reducing) form; a solution would be to use minimum tin and a large excess of complexing agent. Oxidation of the Tc complex to free pertechnetate is not a major problem in most kit systems. 5 figures

  9. Preparation and evaluation of 99mTc-cefuroxime, a potential infection specific imaging agent: A reliable thin layer chromatographic system to delineate impurities from the 99mTc-antibiotic

    International Nuclear Information System (INIS)

    Chattopadhyay, Sankha; Ghosh, Mayuri; Sett, Sucharita; Das, Malay Kanti; Chandra, Susmita; De, Kakali; Mishra, Mridula; Sinha, Samarendu; Ranjan Sarkar, Bharat; Ganguly, Shantanu

    2012-01-01

    Technetium-99m labelled cefuroxime, a second-generation cephalosporin antibiotic and potential bacteria specific infection imaging agent was evaluated. A good radiochemical purity (95%) of the labelled product was obtained after filtering the reaction mixture through a 0.22 μm filter. Scintigraphy study of the purified product showed uptake in infectious lesions 45 min after injection and abscess-to-muscle ratios were found to be 1.80, 1.85 and 1.88 at 45 min, 1.5 hr and 3 hr, respectively. A versatile and reliable chromatographic technique to assess the radiochemical purity of 99m Tc-cefuroxime has also been described. - Highlights: ► Preparation of 99m Tc-cefuroxime in presence of Sn-tartrate as reducing agent. ► Physiochemical and biological evaluation of 99m Tc-cefuroxime. ► A versatile and reliable chromatographic technique to assess the radiochemical purity of 99m Tc-cefuroxime.

  10. Experimental studies on the accumulation of 99mTc-MDP in the bupivacaine hydrochloride induced myopathy

    International Nuclear Information System (INIS)

    Sone, Shinsuke

    1989-01-01

    It has recently been demonstrated that several 99m Tc-labeled phosphate compounds accumulate in skeletal muscle in patients with myopathies including Duchenne muscular dystrophy (DMD). However, the mechanism by which these compounds accumulate in skeletal muscles is unknown. In order to analyze the mechanisms of tracer-localization in skeletal muscles of myopathies, the uptake of 99m Tc-methylendiphosphonate ( 99m Tc-MDP) by muscles examined in rats treated by intramuscular injection of a local anesthetic, bupivacaine. At the same time, the histological and biochemical changes of the injured muscles were studied, and findings obtained were correlated with the procedure of 99m Tc-MDP uptake. Intramuscular injection of bupivacaine resulted in markedly increased uptake of 99m Tc-MDP in the injected muscle at 12 and 24 hours after injection. The plasma creatine phosphokinase (CK) concentration increased 2-3 folds during the period from 3 to 24 hours after bupivacaine injection. Four days following injection, the CK isozyme MB activity in muscle increased. Twenty hours after injection of bupivacaine, changes such as hypercontraction and disruptin of myofibrils, Z-band lysis, and swelling of mitochondria occurred. Four days after the injection, myoblasts and myotubes were found in the damaged areas of the muscle. These results show that the increased muscle uptake of 99m Tc-MDP reflects the early degenerative changes of skeletal muscle. (author)

  11. BFCA for labeling with the M(CO)3 precursor (M = Re, 99mTc) : cysteine toward a tridentate complex

    International Nuclear Information System (INIS)

    Hong, Young Don; Choi, Ok Ja; Gwon, Hui Jeong; Choi, Sang Mu; Park, Sang Hyun; Park, Kyung Bae; Choi, Sun Ju

    2004-01-01

    Organometallic complexes of techneutium in its low oxidation states received little attention till the development of very stable water-soluble organometallic Tc(I) complexes using monodentate isonitrile ligands. The Tc(I) oxidation state is pratically advantegeous because of the kinetic inertness inherent in its low-spin d 6 configuration and good stability in aqueous media. That is, Tc(I) or Re(I) tricarbonyl complexes are ideal candidates for the radiolabeling of biomolecules which M(CO) 3 core allows the high efficient labelling with the retention of the biological affinity. To be used as a BFCA, it should possess not only both a strong metal-binding moiety and a group that binds to a biomolecules, but also the metal complex should maintain the high stability in vitro and in vivo. In this investigation, to estimate the usefulness of thiol modified L-cysteine as a new BFCA with M(CO)3 precursor for the conjugation to biomolecules while maintaining high stability, their non-carrier added and macroscopic level complexes of L-cycteine (L 1 ), S-methyl L-cysteine (L 2 ), L-methionine (L 3 ), and S-carboxymethyl-L-cysteine (L 4 ) were prepared for the evaluation of radiolabelling efficiency with 99m Tc(CO) 3 and macroscopic characteristics. Furthermore, in order to study in vivo pharmacokinetics, scintigraphic imaging scans using gamma camera were acquired after intravenous administration of each 99m Tc(CO) 3 complex and biodistribution study on 99m Tc(CO) 3 -L 4 was implemented using ICR mice

  12. Effect of iron deficiency anemia on the biodistribution of {sup 99m}Tc radiopharmaceuticals

    Energy Technology Data Exchange (ETDEWEB)

    Calmanovici, Gabriela P. [Radioisotopes Laboratory, Physics Department, School of Pharmacy and Biochemistry, University of Buenos Aires, Junin 956 - 1113, Buenos Aires (Argentina); Salgueiro, Maria J. [Radioisotopes Laboratory, Physics Department, School of Pharmacy and Biochemistry, University of Buenos Aires, Junin 956 - 1113, Buenos Aires (Argentina); Janjetic, Mariana A. [Physics Department, School of Pharmacy and Biochemistry, University of Buenos Aires, Junin 956 - 1113, Buenos Aires (Argentina); Leonardi, Natalia M. [Radioisotopes Laboratory, Physics Department, School of Pharmacy and Biochemistry, University of Buenos Aires, Junin 956 - 1113, Buenos Aires (Argentina); Boccio, Jose R. [Physics Department, School of Pharmacy and Biochemistry, University of Buenos Aires, Junin 956 - 1113, Buenos Aires (Argentina); Zubillaga, Marcela B. [Radioisotopes Laboratory, Physics Department, School of Pharmacy and Biochemistry, University of Buenos Aires, Junin 956 - 1113, Buenos Aires (Argentina)]. E-mail: mzubi@ffyb.uba.ar

    2006-05-15

    The distribution of colloids and labeled cells in organs is influenced by their intrinsic properties and by the state of the investigated subject. Iron deficiency remains an unsolved nutritional problem all over the world; one of its severe consequences is anemia. Because iron metabolism principally takes place in the liver, spleen, bone marrow, skeletal muscle and blood, we studied the effect of iron deficiency anemia on the biodistribution of {sup 99m}Tc phytate, {sup 99m}Tc gelatin colloid and {sup 99m}Tc RBC (red blood cells labeled with {sup 99m}Tc). Our results show that iron deficiency anemia modifies the pattern of biodistribution of the two colloids assayed. However, this behavior is different for both of them. This work contributes to studies that kinetically and statistically establish that iron deficiency anemia induces a significant inversion in the spleen-liver activity relationship when centellographic studies are performed with colloids such as {sup 99m}Tc phytate.

  13. Detection of Aspergillus fumigatus pulmonary fungal infections in mice with 99mTc-labeled MORF oligomers targeting ribosomal RNA

    International Nuclear Information System (INIS)

    Wang Yuzhen; Chen Ling; Liu Xinrong; Cheng Dengfeng; Liu Guozheng; Liu Yuxia; Dou Shuping; Hnatowich, Donald J.; Rusckowski, Mary

    2013-01-01

    Purpose: Invasive aspergillosis is a major cause of infectious morbidity and mortality in immunocompromised patients. The fungus Aspergillus fumigatus (A. fumigatus) is the primary causative agent of invasive aspergillosis. However, A. fumigatus infections remain difficult to diagnose particularly in the early stages due to the lack of a rapid, sensitive and specific diagnostic approach. In this study, we investigated 99m Tc labeled MORF oligomers targeting fungal ribosomal RNA (rRNA) for the imaging detection of fungal infections. Procedures: Three phosphorodiamidate morpholino (MORF) oligomer (a DNA analogue) probes were designed: AGEN, complementary to a sequence of the fungal 28S ribosomal RNA (rRNA) of Aspergillus, as a genus-specific probe; AFUM, complementary to the 28S rRNA sequence of A. fumigatus, as a fungus species-specific probe; and cMORF, irrelevant to all fungal species, as a control probe. The probes were conjugated with Alexa Fluor 633 carboxylic acid succinimidyl ester (AF633) for fluorescence imaging or with NHS-mercaptoacetyl triglycine (NHS-MAG3) for nuclear imaging with 99m Tc and then evaluated in vitro and in vivo. Results: The specific binding of AGEN and AFUM to fungal total RNA was confirmed by dot blot hybridization while specific binding of AGEN and AFUM in fixed and live A. fumigatus was demonstrated by both fluorescent in situ hybridization (FISH) analysis and accumulation in live cells. SPECT imaging of BALB/c mice with pulmonary A. fumigatus infections and administered 99m Tc labeled AGEN and AFUM showed immediate and obvious accumulation in the infected lungs, while no significant accumulation of the control 99m Tc-cMORF in the infected lung was observed. Compared to non-infected mice, with sacrifice at 1 h, the accumulation of 99m Tc-AGEN and 99m Tc-AFUM in the lungs of mice infected with A. fumigatus was 2 and 2.7 fold higher respectively. Conclusions: In vivo targeting fungal ribosomal RNA with 99m Tc labeled MORF probes AGEN

  14. Evaluation of sup(99m)Tc-Sn-colloid on liver scintigram

    Energy Technology Data Exchange (ETDEWEB)

    Matsuyuki, Y; Kanao, K; Honda, M; Ishihara, S [Sumitomo Hospital, Osaka (Japan)

    1975-04-01

    sup(99m)Tc-Sn-colloid injectable solution and Sn-colloid preparation set were used for nuclear medical examination of the liver and their efficiency was discussed. Both sup(99m)Tc-Sn-colloid injectable solution and Sn-colloid preparation set showed the same kinetics in vivo, and the sup(99m)Tc-Sn-colloid rapidly disappeared from the serum and concentrated to the liver and spleen. Comparing /sup 198/Au-colloid, sup(99m)Tc-Sn-colloid could be increased the administration dose, and provided easy examination within short time period, easy observation from multiple directions, and improvement of resolution by scinticamera. Imaging of the spleen with sup(99m)Tc-Sn-colloid was slightly superior to that with sup(99m)Tc-sulfur-colloid. sup(99m)Tc-Sn-colloid injectable solution which required no procedure of labeling was evaluated as the most safe and easy technique. Side effects were not recognized. As the results, already made preparation, such as sup(99m)Tc-Sn-colloid injectable solution, which provided easy preparation with less absorbed dose of the tissue and high resolution would be frequently required.

  15. Evaluation of sup(99m)Tc-Sn-colloid on liver scintigram

    International Nuclear Information System (INIS)

    Matsuyuki, Yoshihiko; Kanao, Keisuke; Honda, Minoru; Ishihara, Shizumori

    1975-01-01

    sup(99m)Tc-Sn-colloid injectable solution and Sn-colloid preparation set were used for nuclear medical examination of the liver and their efficiency was discussed. Both sup(99m)Tc-Sn-colloid injectable solution and Sn-colloid preparation set showed the same kinetics in vivo, and the sup(99m)Tc-Sn-colloid rapidly disappeared from the serum and concentrated to the liver and spleen. Comparing 198 Au-colloid, sup(99m)Tc-Sn-colloid could be increased the administration dose, and provided easy examination within short time period, easy observation from multiple directions, and improvement of resolution by scinticamera. Imaging of the spleen with sup(99m)Tc-Sn-colloid was slightly superior to that with sup(99m)Tc-sulfur-colloid. sup(99m)Tc-Sn-colloid injectable solution which required no procedure of labeling was evaluated as the most safe and easy technique. Side effects were not recognized. As the results, already made preparation, such as sup(99m)Tc-Sn-colloid injectable solution, which provided easy preparation with less absorbed dose of the tissue and high resolution would be frequently required. (Mukohata, S.)

  16. Clinical evaluation of {sup 99m}Tc-HMPAO labeled leukocyte imaging in ulcerative colitis

    Energy Technology Data Exchange (ETDEWEB)

    Saitoh, Yasuhiro; Aburano, Tamio; Takashio, Tetsuya; Shuke, Noriyuki; Ayabe, Tokiyoshi; Nomura, Masashi; Kohgo, Yutaka; Ishikawa, Yukio; Satoh, Junichi [Asahikawa Medical Coll., Hokkaido (Japan)

    1996-07-01

    Inflammatory imaging using {sup 99m}Tc-HMPAO-labeled mixed leukocytes was assessed for use in treating 11 cases diagnosed as ulcerative colitis: 10 cases with total colitis and 1 with left-sided colitis. They consisted of 8 patients with relapse-remitting type and 3 with chronic continuous type. Radionuclide abdominal images were obtained at 1 hr, 4 hr and 24 hr after intravenous injection of 200 MBq prepared {sup 99m}Tc leukocytes. Obvious colonic activity noted at 4 hr served as the basis for positive comparative criterion in the present study. The diagnostic efficacy of radionuclide imaging was compared with endoscopic findings (based on Matts` classification) and the clinical manifestations as reference. The sensitivity and specificity of this imaging were 83.3% and 85.7%, respectively, these values being consistent with endoscopic findings and clinical manifestations at sites of disease activity. All of positive images changed to negative after treatment by leukocyte apheresis or glucocorticoid. Based on these results, {sup 99m}Tc leukocyte imaging can be used to accurately evaluate severity and treatment response in ulcerative colitis. Leukocytes may be closely related to the pathogenesis of ulcerative colitis. (author)

  17. Application of photoactivation in the preparation of radiopharmaceuticals. Pt. 3. Human serum albumin labelled with technetium (99mTc)

    International Nuclear Information System (INIS)

    Komarek, P.; Kleisner, I.; Konopkova, M.; Komarkova, I.

    1997-01-01

    Human serum albumin was photoactivated with UV light at 254 nm and labelled with technetium ( 99m Tc) by reducing pertechnetate ( 99m Tc) with stannous chloride. Radiochemical purity was determined by using paper chromatography, columns and electrophoresis. The biodistribution of labelled albumin in rats was assessed by activity counting in isolated organs 15 and 60 minutes after administration. Photoactivation increases the number of free SH groups, which affect favourably the labelling efficiency. Irradiated albumin exhibits a higher labelling efficiency (99%) than non-irradiated albumin (96%). The structural changes depend on the UV radiation dose, concentration of irradiated substances, and metal ion content (Sn 2+ ). The results obtained suggest that the elimination from blood of albumin whose structure has been altered by photoactivation can be accelerated, thereby creating favourable conditions for its application in the diagnosis of inflammatory diseases. (author)

  18. Studies on sup(99m)Tc-pertechnetate from the MEK solvent extraction generator

    International Nuclear Information System (INIS)

    Mohammad, R.; Moore, D.E.; Maddalena, D.J.; Boyd, R.E.

    1984-12-01

    Analysis by gas chromatography-mass spectrometry and high performance liquid chromatography has revealed organic residues in sup(99m)Tc-pertechnetate obtained from 99 Mo-molybdate by extraction, using the organic solvent methylethylketone (MEK). The organic residues have been identified as either (i) low molecular weight carbonyl compounds such as formaldehyde, acetaldehyde and acetone, presumably caused by the effects of γ-radiation on MEK, or (ii) condensation products resulting from the action of strong alkali on MEK during the extraction process. The quantities of organic residues varied from batch to batch of extracted pertechnetate; up to 40 μ mL -1 was found. When these compounds were tested, in rats, by addition to a pyrophosphate bone-seeking radiopharmaceutical, the tissue distribution was not significantly different from that in the control, which contained no added compound. Assay for 99 Tc in MEK-derived pertechnetate indicated up to 10 μg mL -1 of 99 Tc carrier. An assessment of the biological effect of 99 Tc carrier was obtained by (i) red blood cell labelling, where 6 ng mL -1 of 99 Tc was sufficient to reduce labelling efficiency; and (ii) pyrophosphate tissue distribution, where a significant effect was obtained in the presence of 10 μ mL -1 of 99 Tc carrier

  19. Comparison of technetium-99m sulfur colloid and technetium-99m albumin colloid labeled solid meals for gastric emptying studies.

    Science.gov (United States)

    Taillefer, R; Douesnard, J M; Beauchamp, G; Guimond, J

    1987-08-01

    A Tc-99m albumin colloid (Tc-AC) kit has been introduced as an alternative to Tc-99m sulfur colloid (Tc-SC) for liver-spleen imaging. Since there is no need for boiling, the use of Tc-AC reduces preparation time and manipulation. Tc-SC is one of the most commonly used radiopharmaceuticals for the labeling of solid-phase markers in gastric emptying studies. In vitro studies were performed to evaluate the labeling efficiency and stability in hydrochloric acid and in human gastric juice of intracellularly labeled chicken liver and scrambled eggs labeled with Tc-SC and Tc-AC. Gastric emptying studies also were performed on 20 healthy volunteers with both Tc-SC and Tc-AC labeled scrambled egg sandwiches. There was no significant difference between Tc-SC and Tc-AC in the labeling efficiency of chicken liver (98% +/- 1% for Tc-SC, 96% +/- 2% for Tc-AC) and scrambled eggs (92% +/- 2% for Tc-SC, 91% +/- 3% for Tc-AC). However, both Tc-SC and Tc-AC labeled scrambled eggs showed a lower stability than chicken liver, particularly in human gastric juice. Gastric emptying curves from both meals in 20 normal subjects were also similar, with a mean half-emptying time of 85 +/- 13 minutes and 87 +/- 16 minutes for the meals containing Tc-SC and Tc-AC respectively. Tc-AC is a reliable alternative to Tc-SC as a radiotracer for solid-phase gastric emptying studies.

  20. Renal imaging with a new agent sup(99m)Tc-d1-DMS

    International Nuclear Information System (INIS)

    Tanaka, A.

    1980-01-01

    By using sup(99m)-Tc-d1 DMS labeled with 99 m-Tc using stannous chloride and prepared with freeze-dried d1-DMS containing a 3:1 molar ratio of DMS and Sn +2 the effect of stereochemical factor of DMS on kidney affinity, renal images, blood clearance, urinary excretion was studied in experimental animals and two normal volunteers and 75 patients. The comparation revealed a quite similar formation of complex II from d1-DMS to that from the meso-form, judge from its absorption spectra and absorption behavior into the gel. The stereochemical difference of DMS is not a critical factor for the formation of the sup(99m)-Tc-DMS complex with high affinity for the kidney, although it is believed that the renal accumulation of Tc-complex will depend greatly on chemical configuration of the complex. (APR)

  1. Oxygen bubbling can improve the labelling of pentavalent technetium-99m dimercaptosuccinic acid

    International Nuclear Information System (INIS)

    Kobayashi, Hisataka; Suzuki, K.H.; Sakahara, Harumi; Yao Zhengsheng; Yokoyama, Akira; Konishi, Junji

    1995-01-01

    We performed studies in animals (mice) and humans to investigate the effect of such oxygen bubbling on the labelling efficiency of and on the renal uptake of 99m Tc. The method of labelling of 99m Tc (V) DMSA was that of Hirano. It was found that oxygen bubbling oxidized the contaminated 99m Tc (III) DMSA into 99m Tc (V) DMSA in vitro and decreased the uptake of radioactivity in the kidney in both amimals and humans. (orig.)

  2. [Screening with angiographic images prior to (99m)Tc-HMPAO labelled leukocyte scintigraphy in the diagnosis of periprosthetic infection].

    Science.gov (United States)

    Granados, U; Fuster, D; Soriano, A; García, S; Bori, G; Martínez, J C; Mayoral, M; Perlaza, P; Tomás, X; Pons, F

    2015-01-01

    To evaluate the impact of the angioscintigrapy of the three phase bone scan as screening method to rule out infection of the hip and knee prosthesis prior to performing the (99m)Tc-HMPAO leukocyte scintigraphy. A total of 120 (70 women, 50 men; mean age 71±11years) with clinical suspicion of hip (n=63) or knee (n=57) infection of the prosthesis and clinical suspicion of infection were evaluated prospectively. All patients underwent three-phase bone scan (angioscintigraphy, vascular and bone phase) and (99m)Tc-HMPAO-labelled white blood cell scintigraphy. Final diagnosis of infection was made by microbiological documentation or clinical follow-up for at least 12months. Eighteen out of 120 patients were diagnosed of infection of hip prosthesis (n=10) or knee prosthesis (n=8). The angioscintigraphy was positive in 15/18 infected cases and in 21/102 of the non-infected cases with a sensitivity of 83%, specificity of 79% and negative predictive value of 97%. Sensitivity and specificity of (99m)Tc-HMPAO leukocyte scintigraphy were 72% and 95%, respectively. If the leukocyte labeled scintigraphies had been used exclusively for patients with positive angioscintigraphy, this would have saved up to 70% of the (99m)Tc-HMPAO leukocyte scintigraphies performed. There were no cases of infection with positive labeled leukocyte scintigraphy and negative angioscintigraphy. Angioscintigraphy (blood flow phase of bone scan) is a useful technique for screening for hip and knee joint prosthesis infection, significantly reducing the need for (99m)Tc-HMPAO leukocyte scintigraphy without affecting the sensitivity of the technique. Copyright © 2014 Elsevier España, S.L.U. and SEMNIM. All rights reserved.

  3. Evaluation of fibrinogen-DTPA-99mTc. Biodistribution and imaging studies

    International Nuclear Information System (INIS)

    Lungu, V.; Mihailescu, G.; Fugaru, V.; Preda, A.

    1998-01-01

    Labelling with 99m Tc of fibrinogen, using DTPA anhydride as the bifunctional chelating agent, was studied in animals with venous thrombi. The parameters studied were: i) coupled reaction of 99m Tc with the fibrinogen-DTPA-Sn(II) in lyophilised form; ii) biodistribution studies of fibrinogen- 99m Tc in animals with venous thrombi, and iii) imaging studies by scintigraphic methods. The present study showed that the radiochemical purity of fibrinogen-DTPA- 99m Tc is > 95% for a maximum of 5 mCi (185 MBq) radioactivity of 99m Tc in the 1.5-2 ml volume. Above this level of radioactivity we found a drastic decrease in the radiochemical purity. The radioactivity ratio of the venous thrombi to the blood was 2.32+-0.45. The scintigraphic images showed a significant accumulation of fibrinogen-DTPA- 99m Tc in 1-hour-old thrombi, 1 hour after injection. From this results the diagnostic potential of fibrinogen-DTPA-Sn(II) in kit form was evaluated. (author)

  4. Determination of 99Mo contamination in 99mTc elute obtained from 99Mo/99mTc- generator

    International Nuclear Information System (INIS)

    Momennezhad, M.; Zakavi, S. R.; Sadeghi, R.

    2010-01-01

    99m Tc is a widely used radioisotope in nuclear medicine centers which is obtained by elution from Mo-99/Tc-99m generators. Usually the generators are either supplied by the Iran Atomic Energy Agency or by private companies from foreign countries. In this study we have measured 99 Mo contamination in 99m Tc elute from different generators in a period of one year. Materials and Methods: The radionuclide impurity of the 99m Tc elute were studied in two types of radionuclide generators (A: produced in Iran and B: Imported from other country). In-vitro measurements were performed using dose calibrator. Direct measurements were made, using a standard canister at the time of milking of the generators and also in Subsequent hours after milking. Results: The results showed a mean of 99 Mo impurity in generators A and B to be 0.00932±0.0043 and 0.0170±0.0127 respectively. Although the results showed that the 99 Mo contamination in 99 mTc elute was lesser than the maximum accepted activity limit of 0.015%, the difference in these two types may reflect different methods of productions of generator, as well as the quality control procedures. Conclusion: The mean of 99 Mo contamination in generators produced in Iran Atomic Energy Organization was lesser than generators imported from foreign origin.

  5. Labeling of red blood cells with Tc-99m after oral administration of SnCl2. Concise communication

    International Nuclear Information System (INIS)

    Patel, M.C.; Parab, P.B.; Samuel, A.M.; Ganatra, R.D.

    1979-01-01

    In vivo labeling of red blood cells with Tc-99m was possible after prior oral administration of SnCl 2 , both in rats and human volunteers. Absorption of oral SnCl 2 was low but sufficient for more than 95% labeling efficiency. Prior i.v. administration of stannous chloride is known to induce in vivo labeling of red blood cells with pertechnetate. We have observed that such labeling is possible even after oral administration of stannous chloide. Nearly 95% of the circulating radioactivity and 93.7% of the administered radioactivity was in RBCs 30 min after i.v. injection of /sup 99m/TcO 4 - in rats that were fed 5 mg of stannous chloride (3.13 mg Sn 2+ ion) 2 hr before injection. Red blood cells from four human volunteers could bind pertechnetate, both in vitro and in vivo, after oral administration of 100 mg of SnCl 2 . We have obtained a blood-pool image of the human heart by labeling the RBCs in vivo by this method. We have also studied various parameters affecting the in vivo binding of RBCs with Tc-99m - such as the amount of orally administered SnCl 2 , the time of injection of radionuclide after oral SnCl 2 , and the optimum time for the imaging

  6. Technetium-99m labeling and fibronectin binding ability of Corynebacterium diphtheriae

    International Nuclear Information System (INIS)

    Souza, S.M.S.; Nagao, P.E.; Bernardo-Filho, M.; Pereira, G.A.; Napoleao, F.; Andrade, A.F.B.; Hirata Junior, R.; Mattos-Guaraldi, A.L.

    2004-01-01

    The use of radionuclides has permitted advances in areas of clinical and scientific knowledge. Several molecules and cells have been labelled with Technetium-99m ( 99m Tc). The stannous chloride (SnCl 2 ) has a significant influence on the labeling and stability of 99m Tc radiotracers. The frequent risk of diphtheria epidemics has intensified interest in the virulence factors of Corynebacterium diphtheriae. Although studies have looked at potential adhesins including haemagglutinins and exposed sugar residues, the molecular basis of mechanisms of adherence remains unclear. Adherence of pathogens to mammalian tissues may be mediated by fibronectin (FN) found in body fluids, matrix of connective tissues, and cell surfaces. In the present study we evaluated the binding ability to human plasma FN by 99m Tc labeled-C.diphtheriae. Due to adverse effects of stannous ions, microorganisms were submitted to survival and filamentation induction assays. Data showed a dose dependent susceptibility to SnCl 2 bactericidal effects. Cell filamentation was observed for concentrations of SnCl 2 > 110 μg/ml. Adherence levels of 99m Tc labelled 241strain to coverslips coated with 20 μg/ml FN were higher (P = 0.0037) than coated with bovine serum albumin. FN binding by the sucrose fermenting 241 C. diphtheriae strain (8.9% + 2.6) was significantly lower (P=0.0139) than Staphylococcus aureus Cowan I strain (34.1% ± 1.2). Therefore, bacterial 99m Tc labeling represents an additional tool that may contribute to the comprehension of C. diphtheriae interactions with host receptors such as FN that act as biological organizers by holding bacterial cells in position and guiding their migration. (author)

  7. Sequential hepatobiliary scintigraphy of the patients with constitutional jaundice, ICG excretory defect disease and hepatocellular carcinoma with 99mTc-PI, 99mTc-HIDA and 99mTc-EHIDA

    International Nuclear Information System (INIS)

    Mitani, Tsuyoshi

    1987-01-01

    Sequential 2 min scintiphotos were obtained with a scintilation camera after intravenous injection of 3 mCi of 99m Tc-HIDA or 99m Tc-PI. Digital matrix images were simultaneously recorded with computer. Sequential samples for the blood clearance of 99m Tc-HIDA or 99m Tc-PI were obtained for 120 min following injection to the patient of constitutional hyperbilirubinemia and ICG excretory defect disease. In Dubin-Johnson syndrome, the hepatic uptake of 99m Tc-HIDA was faster or normal but the excretion was extremely slower than in normal cases. Both hepatic uptake and excretion of 99m Tc-PI were almost normal. In Rotor's disease, hepatic uptake of 99m Tc-HIDA or 99m Tc-PI was very poor, showing almost no hepatic images in all time. In Gilbert's disease and ICG excretory defect disease, hepatic uptake and excretion of 99m Tc-HIDA or 99m Tc-PI were within normal limit. From these results, Dubin-Johnson syndrome, Rotor's disease and Gilbert's disease show the different patterns between hepatic uptake and excretion of 99m Tc-HIDA and 99m Tc-PI hepatobiliary scintigraphy and these patterns contribute to the differential diagnosis of constitutional jaundice. The usefulness of hepatobiliary imaging with 99m Tc-EHIDA in diagnosis of hepatocellular carcinoma was studied in 15 patients with histologically verified HCC. In 15 patients, 3 patients (20 %) showed increased radioactivity with 99m Tc-EHIDA image, where liver scan with 99m Tc-Sn colloid showed filling defect. These results indicate that use of 99m Tc-EHIDA scan and 67 Ga-citrate imaging is useful for positive visualization of HCC. (author)

  8. An experimental model for measuring gastrointestinal bleeding rate using Tc-99m DTPA in rabbits

    International Nuclear Information System (INIS)

    Owunwanne, A.; Abdel-Dayem, H.M.; Sadek, S.; Yakoub, T.; Mahajan, K.K.; Ericsson, S.B.

    1987-01-01

    An animal experimental model to measure the rate of gastrointestinal bleeding rate in a rabbit using Tc-99m DTPA is described. It was possible to detect a bleeding rate of 0.1 ml/min. However, the model could not be used to calculate the minimum amount of radioactivity needed to detect the bleeding site. (orig.) [de

  9. Radionuclide phlebography with sup(99m)Tc labelled autolog platelets

    International Nuclear Information System (INIS)

    Schroth, H.J.; Berberich, R.; Wilhelm, H.

    1982-01-01

    Platelets labelled with sup(99m)Tc-phytate are suitable for the detection of venous thrombosis. The accumulation of the platelets in the thrombotic area is dependent on the acuteness of the thrombotic process. In 30 patients we have combined with the injection a phlebography of the legs and the pelvis. The advantage of the method is mainly the better visuality of thrombotic areas in the veins of the pelvis. The exploration is without risque especially in patients which suffer from a hypersensibility of a contrast medium. The labelled platelets are injected in a superficial vein of the foot. Then a serial scintigraphy is performed with a #betta#-camera and a connected computer to judge the venous blood flow. With this method it is possible to visualize collateral systems and to dinstinguish between old and fresh thrombotic processes. (Author)

  10. Comparison of Tc-99m maraciclatide and Tc-99m sestamibi molecular breast imaging in patients with suspected breast cancer.

    Science.gov (United States)

    O'Connor, Michael K; Morrow, Melissa M B; Hunt, Katie N; Boughey, Judy C; Wahner-Roedler, Dietlind L; Conners, Amy Lynn; Rhodes, Deborah J; Hruska, Carrie B

    2017-12-01

    Molecular breast imaging (MBI) performed with 99m Tc sestamibi has been shown to be a valuable technique for the detection of breast cancer. Alternative radiotracers such as 99m Tc maraciclatide may offer improved uptake in breast lesions. The purpose of this study was to compare relative performance of 99m Tc sestamibi and 99m Tc maraciclatide in patients with suspected breast cancer, using a high-resolution dedicated gamma camera for MBI. Women with breast lesions suspicious for malignancy were recruited to undergo two MBI examinations-one with 99m Tc sestamibi and one with 99m Tc maraciclatide. A radiologist interpreted MBI studies in a randomized, blinded fashion to assign an assessment score (1-5) and measured lesion size. Lesion-to-background (L/B) ratio was measured with region-of-interest analysis. Among 39 analyzable patients, 21 malignant tumors were identified in 21 patients. Eighteen of 21 tumors (86%) were seen on 99m Tc sestamibi MBI and 19 of 21 (90%) were seen on 99m Tc maraciclatide MBI (p = 1). Tumor extent measured with both radiopharmaceuticals correlated strongly with pathologic size ( 99m Tc sestamibi, r = 0.84; 99m Tc maraciclatide, r = 0.81). The L/B ratio in detected breast cancers was similar for the two radiopharmaceuticals: 1.55 ± 0.36 (mean ± S.D.) for 99m Tc sestamibi and 1.62 ± 0.37 (mean ± S.D.) for 99m Tc maraciclatide (p = 0.53). No correlation was found between the L/B ratio and molecular subtype for 99m Tc sestamibi (r s  = 0.12, p = 0.63) or 99m Tc maraciclatide (r s  = -0.12, p = 0.64). Of 20 benign lesions, 10 (50%) were seen on 99m Tc sestamibi and 9 of 20 (45%) were seen on 99m Tc maraciclatide images (p = 0.1). The average L/B ratio for benign lesions was 1.34 ±0.40 (mean ±S.D.) for 99m Tc sestamibi and 1.41 ±0.52 (mean ±S.D.) for 99m Tc maraciclatide (p = 0.75). Overall diagnostic performance was similar for both radiopharmaceuticals. AUC from ROC

  11. On the separation of 99mTcO4-, 99mTc-DTPA and 99mTc-citrate as marker species for the determination of Tc chemical forms in plant material using capillary zone electrophoresis

    NARCIS (Netherlands)

    Krijger, G.C.; Claessens, H.A.; Wolterbeek, H.Th.

    1996-01-01

    The present paper addresses the potential use of capillary zone electrophoresis (CZE) as an anal. tool in 99Tc speciation studies. To optimize sampling, storage and anal. procedures, the three marker compds. 99mTcO4-, 99mTc-DTPA and 99mTc-citrate were synthesized and used in test-measurements with

  12. Intra-arterial and intraportal infusion liver scintigraphy using 99mTc-labeled colloid

    International Nuclear Information System (INIS)

    Inoue, Yusuke; Ohtake, Tohru; Momose, Toshimitsu; Watanabe, Toshiaki; Kosaka, Noboru; Nishikawa, Jun-ichi; Sasaki, Yasuhito; Sawada, Toshio; Muto, Tetsuichiro

    1991-01-01

    Intra-arterial infusion liver scintigraphy was performed in 11 patients with primary or metastatic liver tumor. and intraportal infusion liver scintigraphy was performed in 6 patients for prophylaxis of liver metastasis from colorectal cancer. 99m Tc-Sn colloid or 99m Tc-phytate was administered through the catheter of which tip was placed in the portal vein or the hepatic artery, and then liver image was obtained. When 99m Tc-phytate was infused intra-arterially, significant amount of the infused tracer passed through the liver and we could not get sufficient information to assess the distribution of drug administered through the catheter. On the other hand, intraportal infusion liver scintigraphy using 99m Tc-Sn colloid or 99m Tc-phytate and intra-arterial infusion liver scintigraphy using 99m Tc-Sn colloid revealed heterogenity of liver uptake, tracer uptake in spleen, low uptake area corresponding to the liver tumor and high uptake area around it. The findings will be clinically useful, and these methods are thought to be helpful to confirm the satisfactory drug distribution. (author)

  13. Exploring the Potential of (99m)Tc(CO)3-Labeled Triazolyl Peptides for Tumor Diagnosis.

    Science.gov (United States)

    Gaonkar, Raghuvir H; Ganguly, Soumya; Baishya, Rinku; Dewanjee, Saikat; Sinha, Samarendu; Gupta, Amit; Ganguly, Shantanu; Debnath, Mita C

    2016-04-01

    In recent years the authors have reported on (99m)Tc(CO)3-labeled peptides that serve as carriers for biomolecules or radiopharmaceuticals to the tumors. In continuation of that work they report the synthesis of a pentapeptide (Met-Phe-Phe-Gly-His; pep-1), a hexapeptide (Met-Phe-Phe-Asp-Gly-His; pep-2), and a tetrapeptide (Asp-Gly-Arg-His; pep-3) and the attachment of 3-amino-1,2,4-triazole to the β carboxylic function of the aspartic acid unit of pep-2 and pep-3. The pharmacophores were radiolabeled in high yields with [(99m)Tc(CO)3(H2O)3](+) metal aqua ion, characterized for their stability in serum and saline, as well as in His solution, and found to be substantially stable. B16F10 cell line binding studies showed favorable uptake and internalization. In vivo behavior of the radiolabeled triazolyl peptides was assessed in mice bearing induced tumor. The (99m)Tc(CO)3-triazolyl pep-3 demonstrated rapid urinary clearance and comparatively better tumor uptake. Imaging studies showed visualization of the tumor using (99m)Tc(CO)3-triazolyl pep-3, but due to high abdominal background, low delineation occurred. Based on the results further experiments will be carried out for targeting tumor with triazolyl peptides.

  14. Synthesis, Characterization, and In Vitro Evaluation of New (99m)Tc/Re(V)-Cyclized Octreotide Analogues: An Experimental and Computational Approach.

    Science.gov (United States)

    Li, Yawen; Ma, Lixin; Gaddam, Vikram; Gallazzi, Fabio; Hennkens, Heather M; Harmata, Michael; Lewis, Michael R; Deakyne, Carol A; Jurisson, Silvia S

    2016-02-01

    Radiolabeled proteolytic degradation-resistant somatostatin analogues have been of long-standing interest as cancer imaging and radiotherapy agents for targeting somatostatin receptor-positive tumors. Our interest in developing (186)Re- and (188)Re-based therapeutic radiopharmaceuticals led to investigation of a new Re(V)-cyclized octreotide analogue, Re(V)-cyclized, thiolated-DPhe(1)-Cys(2)-Tyr(3)-DTrp(4)-Lys(5)-Thr(6)-Cys(7)-Thr(OH)(8) (Re-SDPhe-TATE) using both experimental and quantum chemical methods. The metal is directly coordinated to SDPhe-TATE through cyclization of the peptide around the [ReO](3+) core. Upon complexation, four isomers were observed; the isolated/semi-isolated isomers exhibited different somatostatin receptor (sstr) binding affinities, 0.13 to 1.5 μM, in rat pancreatic tumor cells. Two-dimensional NMR experiments and electronic structure calculations were employed to elucidate the structural differences among the different isomers. According to NMR studies, the metal is coordinated to three thiolates and the backbone amide of Cys(2) in isomers 1 and 4, whereas the metal is coordinated to three thiolates and the backbone amide of Tyr(3) in isomer 2. Quantum chemical methods clarified the stereochemistry of Re-SDPhe-TATE and the possible peptide arrangements around the [ReO](3+) core. The re-cyclization reaction was translated to the (99m)Tc radiotracer level with four isomers observed on complexation with comparable HPLC retention times as the Re-SDPhe-TATE isomers. About 85% total (99m)Tc labeling yield was achieved by ligand exchange from (99m)Tc-glucoheptonate at 60 °C for an hour. About 100% and 51% of (99m)Tc(V)-cyclized SDPhe-TATE remained intact in phosphate buffered saline and 1 mM cysteine solution under physiological conditions at 6 h, respectively.

  15. Clinical utility of immunoscintigraphy with the Immu-4 99mTc-Fab' antibody

    International Nuclear Information System (INIS)

    Moffat, F.L.; Pinsky, C.M.; Hammershaimb, L.; Petrelli, N.J.; Patt, Y.Z.; Whaley, F.S.; Goldenberg, D.M.

    1996-01-01

    The purpose of these prospective, pivotal studies was to assess the performance and the potential clinical impact of a new antibody imaging agent, CEA-Scan TM , in 210 pre-surgical patients with advanced recurrent or metastatic colorectal carcinomas. CEA-Scan TM , an anti-carcinoembryonic antigen (CEA) Fab' antibody fragment labeled with 99m Tc, was injected IV and external scintigraphy performed 2-5 h and 18-24 h later. Imaging with conventional diagnostic modalities (CDM) was also performed, and findings were confirmed by surgery and histology. The sensitivity of CEA-Scan TM was superior to that of CDM in the extrahepatic abdomen (55 % vs 32 %, ρ 0,007) and pelvis (69 % vs 48 %, p = 0,005), and CEA-Scan TM findings complemented those of CDM in the liver. Among 122 patients with known disease, the positive predictive value was significantly higher when both modalities were positive (98 %) as compared to each alone (68 % - 70 %), potentially obviating the need for histological confirmation when both tests are positive. Imaging accuracy also was significantly improved y adding CEA-Scan TM to CDM. In 88 patients with occult cancer, imaging accuracy was enhanced significantly by CEA-Scan TM combined with CDM (61 % vs 33 %). Potential clinical benefit from CEA-Scan TM was demonstrated in 89 of 210 patients. Only two patients developed human anti-mouse antibodies (HAMA) to CEA-Scan TM after a single injection, and none of 19 assessable patients after two injections. (author)

  16. Investigations of (99m)Tc-labeled glucarate as a SPECT radiotracer for non-small cell lung cancer (NSCLC) and potential tumor uptake mechanism.

    Science.gov (United States)

    Meng, Lanfang; Xiu, Yan; Li, Yanli; Xu, Xiaobo; Li, Shanqun; Li, Xiao; Pak, Koon Y; Shi, Hongcheng; Cheng, Dengfeng

    2015-07-01

    This study attempted to evaluate the feasibility of (99m)Tc-labeled glucarate ((99m)Tc-GLA) imaging in non-small cell lung cancer (NSCLC) and the potential tumor uptake mechanism. Cell lysates from two NSCLC cell lines, H292 and H1975, were immunoblotted with anti-glucose transporter 5 (GLUT5) antibody for Western blotting. Thereafter, the two cell lines were used to examine cellular uptake of (99m)Tc-GLA with or without fructose. SPECT/CT imaging studies were performed on small animals bearing H292 and H1975 tumors. Biodistribution studies were also conducted to achieve accurate tissue uptake of this tracer in two tumor models. Hematoxylin & eosin (H&E) staining and GLUT5, Ki67 and cytokeratin-7 (CK-7) immunohistochemistry (IHC) analysis were further investigated on tumor tissues. In Western blotting, H292 cells showed higher levels of GLUT5 compared to the H1975 cells. Meanwhile, the in vitro cell assays indicated GLUT5-dependent uptake of (99m)Tc-GLA in H292 and H1975 cells. The fructose competition assays showed a significant decrease in (99m)Tc-GLA uptake by H292 and H1975 cells when fructose was added. The (99m)Tc-GLA accumulation was as much as two-fold higher in H292 implanted tumors than in H1975 implanted tumors. (99m)Tc-GLA exhibited rapid clearance pharmacokinetics and reasonable uptake in human NSCLC H292 (1.69±0.37 ID%/g) and H1975 (0.89±0.06 ID%/g) implanted tumors at 30min post injection. Finally, the expression of GLUT5, Ki67 and CK-7 on tumor tissues also exhibited positive correlation with the in vitro cell test results and in vivo SPECT/CT imaging results in xenograft tumors. Both in vitro and ex vivo studies demonstrated that the uptake of (99m)Tc-GLA in NSCLC is highly related to GLUT5 expression. Imaging and further IHC results support that (99m)Tc-GLA could be a promising SPECT imaging agent for NSCLC diagnosis and prognosis evaluation. Copyright © 2015 Elsevier Inc. All rights reserved.

  17. The role of Tc-99m IDA hepatobiliary and Tc-99m colloid hepatic imaging in primary biliary cirrhosis

    International Nuclear Information System (INIS)

    Aburano, T.; Yokoyama, K.; Shuke, N.; Kinuya, S.; Takayama, T.; Tonami, N.; Hisada, K.

    1991-01-01

    To assess the presence of primary biliary cirrhosis, 15 patients at various histopathologic stages were studied by Tc-99m IDA hepatobiliary and/or Tc-99m colloid hepatic imaging. In the earlier stages (I and II), seven of eight patients (88%) showed uniform hepatic retention of Tc-99m IDA. Of seven patients in the same stage, however, four (57%) showed no abnormality on Tc-99m colliod imaging. In three of these four negative patients (75%), uniform hepatic retention of Tc-99m IDA was noted. In the later stages (III and IV), all seven patients showed decreased clearance with or without delayed tracer appearance in the intestine and prominent hepatic retention on Tc-99m IDA imaging; with Tc-99m colloid imaging there was enlargement of the spleen and increased activity in the spleen and bone marrow. Thus, Tc-99m IDA imaging is considered to be more useful in revealing this functional disorder at the earlier stage of primary biliary cirrhosis and in evaluating progression from an earlier to a later stage of disease. Tc-99m colloid imaging also effectively evaluated progression

  18. Accumulation of Tc-99m-MIBI and Tc-99m-tetrofosmin in tumor cells. Uptake and washout studies

    International Nuclear Information System (INIS)

    Rodrigues, M.; Aghajanian, A.A.; Sinzinger, H.; Kalinowska, W.; Zielinski, C.

    2002-01-01

    Aim: To investigate in-vitro the uptake and washout of Tc-99m-MIBI and Tc-99m-tetrofosmin in human breast adenocarcinoma and soft tissue sarcoma cell lines. Methods: The uptake of Tc-99m-MIBI and Tc-99m-tetrofosmin (at 37 0 C, 10, 30 and 60 minutes after incubation with 7.4x10E5 Bq each tracer) was investigated in breast adenocarcinoma MCF-7 and SK-BR-3 cells, synovial sarcoma SW 982 cells and chondrosarcoma SW 1353 cells (concentration of 1x10E6 cells/ml incubation medium). Tracer uptake in cells incubated with ouabain (Na/K-ATPase pump inhibitor; 100 μM and 1mM; 15 and 30 minutes), nigericin (increases mitochondrial potential and disrupts cell membrane potential; 5 and 50 μg/ml; 15 minutes) and carbonyl cyanide m-chlorophenylhydrazone (CCCP) (depolarizes mitochondrial membrane; 10 and 100 μM; 30 minutes) was compared to that in cells without incubation with chemical agents (control cells). The washout (at 37 0 C, 10-60 minutes, 30 and 60 minutes after tracer incubation) of Tc-99m-MIBI and Tc-99m-tetrofosmin was studied in MCF-7 cells, SK-BR-3 cells , SW 1353 cells and fibrosarcoma SW 684 cells. Results: Cellular tracer uptake decreased with ouabain (decrease of Tc-99m-tetrofosmin > Tc-99m-MIBI in SK-BR-3 cells and SW 982 cells) and increased with nigericin (increase of Tc-99m-MIBI > Tc-99m-tetrofosmin in all cells) as compared to the uptake in control cells. With CCCP, decrease of Tc-99m-MIBI uptake in cells preincubated with nigericin was higher than that in cells under basal conditions, whereas a similar decrease of Tc-99m-tetrofosmin uptake in these two group of cells was found. Washout of Tc-99m-MIBI from all cells was lower than that of Tc-99m-tetrofosmin. No significant difference in cell-associated activity of both tracers was found between washout after 30 minutes and that after 60 minutes of incubation, in all cells. Washout of Tc-99m-MIBI from SK-BR-3 cells Tc-99m-tetrofosmin) and Na/K-ATPase pump (Tc-99m-tetrofosmin > Tc-99m-MIBI). Tc-99m-MIBI and

  19. Tc-99m-hexakis(t-butylisonitrile)-technetium(I) (Tc-99m-TBI)

    International Nuclear Information System (INIS)

    Angelberger, P.; Dudczak, R.; Jones, A.G.; Lister-James, J.; Wagner-Loffler, M.; Buchheit, O.; Fally, F.

    1986-01-01

    The potassium analog (Tl-201)/sup +/ is widely used in nuclear cardiology but has inferior scintigraphic (80 keV photons), dosimetric and economic properties as compared to Tc-99m. Therefore considerable efforts have been made to develop a Tc-compound that would accumulate in the myocardium in relation to regional blood flow. This study was aimed at optimizing the preparation of Tc-TBI with n.c.a. Tc-99m, analyze and purify the product with HPLC, verify biodistribution in mice and undertake a clinical evaluation

  20. A modified method for the in vivo labeling of red blood cells with /sup 99m/Tc: concise communication

    International Nuclear Information System (INIS)

    Callahan, R.J.; Froelich, J.W.; McKusick, K.A.; Leppo, J.; Strauss, H.W.

    1982-01-01

    The rate of incorporation of /sup 99m/Tc into red blood cells pretinned in vivo was measured by collecting blood samples in stannous DTPA solution, which served as a competing ligand for /sup 99m/Tc. This collection technique permitted a measurement of high-affinity red-cell labeling efficiency at the instant of sampling. At 0.5 min after injection only 62% of technetium is tightly bound to the red cell; this rises to 94.5% at 10 min. Based on the graded labeling of the red cells, the in vivo labeling procedure was modified by isolating pertechnetate and red blood cells tinned in vivo in a syringe during the first 10 min of labeling. The pertechnetate is thus prevented from distributing to extravascular compartments, and 90% of the injected /sup 99m/Tc is firmly bound to red blood cells at the time of injection. In a series of 23 patients, seven were tested with the in vivo method and seven with the modified in vivo method, and nine patients were tested with each method on separate occasions. A decrease in gastric activity and improved image quality were found with the modified method compared with the standard method of in vivo red-cell labeling