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Sample records for f-18 labelling synthesis

  1. Synthesis of F-18 labeled raloxifene derivative

    Energy Technology Data Exchange (ETDEWEB)

    Lee, K. C.; Moon, B. S.; Jun, K. S. [KIRAMS, Seoul (Korea, Republic of); Lee, J. H.; Ji, D. Y. [Inha University, Incheon (Korea, Republic of)

    2005-07-01

    Raloxifene, [6-hydroxy-2-(4-hydroxy-phenyl) benzo [b] thiophen-3-yl]-[4-(2-piperidin-1-yl-ethoxy)phenyl] methanone, a tissue-selective estrogen mixed agonist/antagonist, classified as a selective estrogen receptor modulator (SERM), is currently under clinical evaluation for the prevention and treatment of postmenopausal osteoporosis, breast cancer, uterine dysfunction, and other disorders of the female reproductive system. Based on SAR studies of substituted raloxifenes, we synthesized 3 kinds of fluoroalkylated raloxifene derivatives. These compounds show high relative binding affinities (RBA) to the estrogen receptor in vitro (RBA of estradiol = 100%). The RBA values for compounds 1, 2 and 3 are 89, 60, and 45%, respectively, which are all higher than that of raloxifene itself (34%). Among these compounds, we selected to take the best RBA value one and F-18 labeled. Using 2 kinds of labeling method ; 1) Radiolabeling using [{sup 18}F]KF was carried out in anhydrous acetonitrile for 10 min at 120 .deg. C. 2) Radiolabeling using [{sup 18}F]KF was carried out in anhydrous acetonitrile for 15 min at 120 .deg. C in ionic liquid, [bmim][OTf]. Deprotection step added 1N HCl and reacted for 3 min at 120 .deg. C. [{sup 18}F]Fluoroethyl raloxifene derivative obtained 5-23% decay corrected labeling yield by HPLC system (C18 xterra, 10 i, 34% Acetonitrile/0.1 M formate buffer, flow rate: 4 mL/1 min, collection time : 28-29 min) and total time was around 70 min. Fluoroethyl raloxifene derivative has the best RBA value among the other synthesized derivatives and chose it for radiolabeling. [{sup 18}F]Fluoroethyl raloxifene derivative prepared 5-23% decay corrected labeling yield. This preparation is on going for labeling optimizing and preparing of in vitro and in vivo test.

  2. A comparison of conventional and click labeling approaches to the synthesis of F-18 labeled glucopyranosyl triazole

    Energy Technology Data Exchange (ETDEWEB)

    Kim, D. H.; Choi, Y. S.; Lee, K. H.; Choi, J. Y.; Choi, Y.; Kim, B. T. [Samsung Medical Center, Seoul (Korea, Republic of)

    2007-07-01

    Radiolabeled glucose analogs are attractive targets for in vivo imaging of glucose metabolism. In the present study, F-18 labeled glucopyranosyl triazole was synthesized using conventional and click labeling approaches, and their results were compared in terms of radiochemical yield, specific activity, and synthesis time. 4-[(2-Fluoroethyl)-1-(-D-glucopyranosyl)]-1H-1, 2, 3-triazole (1) was synthesized by the Cu(I)-catalyzed 1, 3-cycloaddition of tetraacetyl glucopyranosyl azide and 3-butyn-1-ol, hydroxy group fluorination, tetraacetyl group deprotection, and subsequent neutralization. [F-18]1 was synthesized using two conventional radiofluorination of tetraacetyl triazole tosylate precursor, followed by tetraacetyl group deprotection and Cu(I)-catalyzed 1, 3-cycloaddition of F-18 labeled butyne and glucopyranosyl azide. The radiotracer was purified by reverse phase HPLC and co-injected with 1 into a HPLC system to confirm its identity. Non-radiolabeled standard 1 was synthesized in overall 33% yield. In the synthesis of [F-18]1, the click labeling approach was superior to the conventional approach, due to a higher decay-corrected radiochemical yield (30% vs. 21%), higher specific activity (59.9 GBq/mol vs. 23.5 GBq/mol), and shorter synthesis time (75-80 min vs. 95-100 min). In addition, protection of the hydroxy groups of glucopyranosyl azide was not required in the former method. The radiotracer was identified by co-elution with 1 on HPLC. These results demonstrate that click labeling approach is a rapid and efficient method which does not require the protection of functional groups, and that it can readily be applied to the preparation of other radiotracers.

  3. F-18 labeled 3-fluorodiazepam

    Energy Technology Data Exchange (ETDEWEB)

    Luxen, A.; Barrio, J.R.; Bida, G.T.; Satyamurthy, N.; Phelps, M.E.

    1985-05-01

    3-Fluorodiazepam is a new and potent antianxiety agent with prolonged action. The authors found that molecular fluorine (0.5% in Ne) reacts cleanly with diazepam in freon or chloroform at room temperature to produce 3-fluorodiazepam in good yields. Successful syntheses have employed 2:1 to 5:1 molar ratios diazepam: fluorine to minimize the formation of byproducts. (/sup 18/F) 3-Fluorodiazepam, a potential candidate for PET studies, (specific activity 3-5 Ci/mmol) has been synthesized from /sup 18/F-F/sub 2/ using the same procedure, followed by column chromatographic purification (Silicagel, dichloromethane: ethyl acetate, 5:1) with a radiochemical yield of 12-20% (50% maximum) and a chemical and radiochemical purity >99% as judged by reversed-phase high pressure liquid chromatography analysis (Ultrasyl octyl column, 10 ..mu.. m, 4.6 x 250 mm i.d., 60% MeOH 40% water; flow rate, 1.0 ml/min; retention time for (/sup 18/F) fluorodiazepam, 11.4 min; for diazepam, 13.5 min; radioactivity and ultraviolet detectors). Lower radiochemical yields (5-7%), and significant formation of by-products were observed when (/sup 18/F)acetylhypofluorite, prepared in the gasphase, was used as the reagent. Readily accessible routes to /sup 18/F-labeled benzodiazepines of higher specific activity were also investigated. Approaches to the synthesis of high specific activity (>200 Ci/mmol) (/sup 18/F)3-fluorodiazepam involve nucleophilic displacement at carbon-3 (e.g. from 3-chlorodiazepam) with (/sup 18/F)fluoride ion. The results presented here demonstrate the synthetic accessibility of /sup 18/F-labeled benzodiazepines for application in neurotransmitter ligand studies with PET.

  4. Synthesis and evaluation of novel F-18 labeled quinazoline derivatives with low lipophilicity for tumor PET imaging.

    Science.gov (United States)

    Chong, Yan; Chang, Jin; Zhao, Wenwen; He, Yong; Li, Yuqiao; Zhang, Huabei; Qi, Chuanmin

    2017-08-18

    Four novel F-18 labeled quinazoline derivatives with low lipophilicity, [(18) F]4-(2-fluoroethoxy)-6,7-dimethoxyquinazoline ([(18) F]I), [(18) F]4-(3-((4-(2-fluoroethoxy)-7-methoxyquinazolin-6-yl)oxy)propyl)morpholine ([(18) F]II), [(18) F]4-(2-fluoroethoxy)-7-methoxy-6-(2-methoxyethoxy)quinazoline ([(18) F]III) and [(18) F]4-(2-fluoroethoxy)-6,7-bis(2-methoxyethoxy)quinazoline ([(18) F]IV), were synthesized via a two-step radiosynthesis procedure with an overall radiochemical yield of 10-38% (without decay correction) and radiochemical purities of > 98%. The lipophilicity and stability of labeled compounds were tested in vitro. The log P values of the four radiotracers ranged from 0.52 to 1.07. We then performed ELISA to measure their affinities to EGFR-TK. ELISA assay results indicated that each inhibitor was specifically bound to EGFR-TK in a dose-dependent manner. The EGFR-TK autophosphorylation IC50 values of [(18) F]I, [(18) F]II, [(18) F]III, and [(18) F]IV were 7.732 μM, 0.4698 μM, 0.1174 μM, and 0.1176 μM, respectively. All labeled compounds were evaluated via cellular uptake and blocking studies in HepG2 cell lines in vitro. Cellular uptake and blocking experiment results indicated that [(18) F]I and [(18) F]III had excellent cellular uptake at 120 min post-injection in HepG2 carcinoma cells (51.80±3.42 %ID/mg protein and 27.31±1.94 %ID/mg protein, respectively). Additionally, biodistribution experiments in S180 tumor-bearing mice in vivo indicated that [(18) F]I had a very fast clearance in blood and a relatively high uptake ratio of tumor to blood (4.76) and tumor to muscle (1.82) at 60 min post-injection. [(18) F]III had a quick clearance in plasma, and its highest uptake ratio of tumor to muscle was 2.55 at 15 min post-injection. These experimental results and experiences were valuable for the further exploration of novel radiotracers of quinazoline derivatives. This article is protected by copyright. All rights reserved.

  5. Synthesis of [F-18]fluoroatipamezole. Biodistribution in rats

    Energy Technology Data Exchange (ETDEWEB)

    Solin, O.; Enas, J.D.; Bergman, J. [Lawrence Berkeley Lab., CA (United States)] [and others

    1996-05-01

    Fluoroatipamezole, an analogue of the {alpha}2 adrenoreceptor antagonist atipamezole, is a potential candidate for mapping adrenergic innervation in the human brain with PET. As a nucleophilic route failed, F-18-labelling was achieved by electrophillic fluorination of a stannylated precursor. The fluorinated compound was injected into rats, and the uptake in various organs was studied as a function of time (30, 60, 120 min). Also autoradiographic images of microtome slices of rat brain were recorded and analysed. The synthesis yield was {approximately} 3% (decay-corrected) as calculated from the F-18-fluoride produced. The specific radioactivity was {approximately} 350 mCi/{mu}mole at EOS.

  6. Development of [F-18]-Labeled Amyloid Imaging Agents for PET

    Energy Technology Data Exchange (ETDEWEB)

    Mathis, CA

    2007-05-09

    The applicant proposes to design and synthesize a series of fluorine-18-labeled radiopharmaceuticals to be used as amyloid imaging agents for positron emission tomography (PET). The investigators will conduct comprehensive iterative in vitro and in vivo studies based upon well defined acceptance criteria in order to identify lead agents suitable for human studies. The long term goals are to apply the selected radiotracers as potential diagnostic agents of Alzheimer's disease (AD), as surrogate markers of amyloid in the brain to determine the efficacy of anti-amyloid therapeutic drugs, and as tools to help address basic scientific questions regarding the progression of the neuropathology of AD, such as testing the "amyloid cascade hypothesis" which holds that amyloid accumulation is the primary cause of AD.

  7. A New F-18 Labeled PET Agent For Imaging Alzheimer's Plaques

    Science.gov (United States)

    Kulkarni, Padmakar V.; Vasdev, Neil; Hao, Guiyang; Arora, Veera; Long, Michael; Slavine, Nikolai; Chiguru, Srinivas; Qu, Bao Xi; Sun, Xiankai; Bennett, Michael; Antich, Peter P.; Bonte, Frederick J.

    2011-06-01

    Amyloid plaques and neurofibrillary tangles are hallmarks of Alzheimer's disease (AD). Advances in development of imaging agents have focused on targeting amyloid plaques. Notable success has been the development of C-11 labeled PIB (Pittsburgh Compound) and a number of studies have demonstrated the utility of this agent. However, the short half life of C-11 (t1/2: 20 min), is a limitation, thus has prompted the development of F-18 labeled agents. Most of these agents are derivatives of amyloid binding dyes; Congo red and Thioflavin. Some of these agents are in clinical trials with encouraging results. We have been exploring new class of agents based on 8-hydroxy quinoline, a weak metal chelator, targeting elevated levels of metals in plaques. Iodine-123 labeled clioquinol showed affinity for amyloid plaques however, it had limited brain uptake and was not successful in imaging in intact animals and humans. We have been successful in synthesizing F-18 labeled 8-hydroxy quinoline. Small animal PET/CT imaging studies with this agent showed high (7-10% ID/g), rapid brain uptake and fast washout of the agent from normal mice brains and delayed washout from transgenic Alzheimer's mice. These promising results encouraged us in further evaluation of this class of compounds for imaging AD plaques.

  8. Synthesis and evaluation of 4-[F-18]fluoro thalidomide for the in vivo studies of angiogenesis

    Energy Technology Data Exchange (ETDEWEB)

    Kim, D. H.; Choi, Y. S.; Jeong, K. H.; Lee, K. H.; Choi, Y.; Kim, B. T. [Samsung Medical Center, Seoul (Korea, Republic of)

    2005-07-01

    Thalidomide has been recently rediscovered for its possible utility as an antitumor agent, although it was marketed as a sedative in the 1950s and later found to be a potent teratogen. In this study, therefore, F-18 labeled thalidomide was synthesized and evaluated for the in vivo studies of angiogenesis. 4-[F-18]Fluoro thalidomide ([F-18]1) was prepared by labeling of 4-trimethylammonium thalidomide triflate with TBA[F-18]F in DMSO (90 .deg. C, 10 min) and purified by HPLC. The triflate salt was prepared from 3-fluoro phthalic anhydride in 3 steps. [F-18]1 was incubated with HUVEC cells at 37 .deg. C for 15, 30, 60, and 120 min, respectively. Dynamic PET images of [F-18]1 was obtained in mice implanted with LLC cells. In vitro metabolism study of [F-18]1 was carried out using mouse, rabbit, or human liver microsomes in the presence of NADPH, and the metabolites obtained from the mouse liver microsomal incubation of 1 were analyzed using LC-MS. Radiochemical yield of [F-18]1 was 50-60%, and the specific activity was 42-120 GBq/imol. The HUVEC cell uptake of [F-18]1 increased with time (100% at 15 min and 241% at 120 min). PET images showed that the radioactivity was accumulated in the liver, the kidneys and the bladder of the mice, and brain uptake was shown from 40 min postinjection. However, there was low level of radioactivity uptake in tumor. [F-18]1 was not metabolized by mouse, rabbit, or human liver microsomes but was hydrolyzed significantly at physiological pH. The hydrolyzed product was further analyzed by LC-MS, showing a mass peak corresponding to that of 4-fluoro-N-(o-carboxybenzoyl)glutamic acid imide. This result suggests that [F-18]1 is easily hydrolyzed at physiological pH and thus may not be suitable for the in vivo studies of tumor angiogenesis at least in rodents, although it was reported that the hydrolysis product of thalidomide may be responsible for its angiogenesis activity in humans.

  9. Stimulation of Escherichia coli F-18Col- Type-1 fimbriae synthesis by leuX

    DEFF Research Database (Denmark)

    Newman, Joseph V.; Burghoff, Robert L.; Pallesen, Lars

    1994-01-01

    Escherichia coli F-18, a normal human fecal isolate, is an excellent colonizer of the streptomycin-treated mouse large intestine. E. coli F-18Col-, a derivative of E. coli F-18 which no longer makes the E. coli F-18 colicin, colonizes the large intestine as well as E. coli F-18 when fed to mice a...

  10. Fully automated synthesis module for the high yield one-pot preparation of 6-[F-18]fluoro-L-DOPA

    NARCIS (Netherlands)

    de Vries, EFJ; Luurtsema, G; Brussermann, M; Elsinga, PH; Vaalburg, W

    1999-01-01

    A fully automated one-pot synthesis of 6-[F-18]fluoro-L-DOPA, an important radiopharmaceutical for studies on the presynaptic dopamine metabolism with positron emission tomography,is described. 6-[F-18]Fluoro-L-DOPA was prepared in high radiochemical yield (33 +/- 4%, c.f.d.) and radiochemical

  11. F-18 Labeled Vasoactive Intestinal Peptide Analogue in the PET Imaging of Colon Carcinoma in Nude Mice

    Directory of Open Access Journals (Sweden)

    Dengfeng Cheng

    2013-01-01

    Full Text Available As large amount of vasoactive intestinal peptide (VIP receptors are expressed in various tumors and VIP-related diseases, radiolabeled VIP provides a potential PET imaging agent for VIP receptor. However, structural modification of VIP is required before being radiolabeled and used for VIP receptor imaging due to its poor in vivo stability. As a VIP analogue, [R8, 15, 21, L17]-VIP exhibited improved stability and receptor specificity in preliminary studies. In this study, F-18 labeled [R8,15,21, L17]-VIP was produced with the radiochemical yield being as high as 33.6%±3% (decay-for-corrected, n=5 achieved within 100 min, a specific activity of 255 GBq/μmol, and a radiochemical purity as high as 99% as characterized by radioactive HPLC, TLC, and SDS-Page radioautography. A biodistribution study in normal mice also demonstrated fast elimination of F-18 labeled [R8,15,21, L17]-VIP in the blood, liver, and gastrointestinal tracts. A further micro-PET imaging study in C26 colon carcinoma bearing mice confirmed the high tumor specificity, with the tumor/muscle radioactivity uptake ratio being as high as 3.03 at 60 min following injection, and no apparent radioactivity concentration in the intestinal tracts. In addition, blocking experiment and Western Blot test further confirmed its potential in PET imaging of VIP receptor-positive tumor.

  12. F-18 Labeled Diabody-Luciferase Fusion Proteins for Optical-ImmunoPET

    Energy Technology Data Exchange (ETDEWEB)

    Wu, Anna M

    2013-01-18

    The goal of the proposed work is to develop novel dual-labeled molecular imaging probes for multimodality imaging. Based on small, engineered antibodies called diabodies, these probes will be radioactively tagged with Fluorine-18 for PET imaging, and fused to luciferases for optical (bioluminescence) detection. Performance will be evaluated and validated using a prototype integrated optical-PET imaging system, OPET. Multimodality probes for optical-PET imaging will be based on diabodies that are dually labeled with 18F for PET detection and fused to luciferases for optical imaging. 1) Two sets of fusion proteins will be built, targeting the cell surface markers CEA or HER2. Coelenterazine-based luciferases and variant forms will be evaluated in combination with native substrate and analogs, in order to obtain two distinct probes recognizing different targets with different spectral signatures. 2) Diabody-luciferase fusion proteins will be labeled with 18F using amine reactive [18F]-SFB produced using a novel microwave-assisted, one-pot method. 3) Sitespecific, chemoselective radiolabeling methods will be devised, to reduce the chance that radiolabeling will inactivate either the target-binding properties or the bioluminescence properties of the diabody-luciferase fusion proteins. 4) Combined optical and PET imaging of these dual modality probes will be evaluated and validated in vitro and in vivo using a prototype integrated optical-PET imaging system, OPET. Each imaging modality has its strengths and weaknesses. Development and use of dual modality probes allows optical imaging to benefit from the localization and quantitation offered by the PET mode, and enhances the PET imaging by enabling simultaneous detection of more than one probe.

  13. SYNTHESIS AND EVALUATION OF 1'-[F-18]FLUOROMETOPROLOL AS A POTENTIAL TRACER FOR THE VISUALIZATION OF BETA-ADRENOCEPTORS WITH PET

    NARCIS (Netherlands)

    DEGROOT, TJ; VANWAARDE, A; ELSINGA, PH; VISSER, GM; BRODDE, OE; VAALBURG, W

    (+/-)-1'-[F-18]Fluorometoprol 4 was prepared from desisopropylmetoprolol and [F-18]fluoroisopropyl tosylate 2 with a radiochemical yield of 2% [corrected for decay to end of bombardment (EOB), synthesis time 90 min]. Synthon 2 was prepared from (S)-1,2-propanediol di(p-toluenesulfonate) in 45%

  14. An efficient in vitro method for metabolism studies of F-18 labeled radiotracers using mouse liver S9 fraction

    Energy Technology Data Exchange (ETDEWEB)

    Ryu, E. K.; Choi, Y. S.; Kim, D. H.; Ko, B. H.; Lee, K. H.; Choi, Y.; Kim, B. T. [Samsung Medical Center, Seoul (Korea, Republic of)

    2005-07-01

    Metabolism studies are prerequisite for characterization of novel radiotracers. In this study, in vitro metabolism method using mouse liver S9 fraction was established and evaluated using model radiotracers, and the results were compared with those of in vivo method and in vitro method using liver microsomes. 1-(4-[F-18] fluoro methylbenzyl)- ([F-18]1) and 1-(4-[F-18]fluorobenzyl)-4-phen ylpiperazine ([F-18]2) were synthesized and purified by HPLC. Liver S9 fraction and microsomes were prepared from mice. In the in vivo method, mice were injected with the radiotracer, and the bone and blood were collected at 1, 5, 15, 30 and 60 min postinjection. In the in vitro method, the radiotracer was incubated with either S9 fraction or microsomes in the presence of NADPH. The metabolites were analyzed by radio-TLC. Metabolic defluorination was also measured from the incubation of the metabolites with calcium phosphate. [F-18]1 and [F-18]2 were synthesized in 25-35% yield. In the in vivo method, [F-18]1 underwent severe metabolic defluorination based on the increase of bone uptake with time and appearance of [F-18]fluoride ion on radio-TLC in the blood samples. This result was consistent with the in vitro metabolism using either S9 fraction or microsomes, which showed a significant uptake by calcium phosphate. [F-18]2 was converted into unidentified polar metabolites both in vivo and in vitro. There was no increasing uptake by either bone or calcium phosphate with time. The in vitro metabolism of these radiotracers using S9 fraction gave the similar patterns to those using the blood as well as microsomes. This result demonstrated that liver S9 fraction can be used in place of microsomes as well as the blood for the metabolism studies of radiotracers. Moreover, the use of liver S9 fraction has advantages in that it is easily obtained during the early stage of liver microsomal preparation and contains both microsomal and cytosolic fractions.

  15. Targeting Prostate-Specific Membrane Antigen (PSMA) with F-18-Labeled Compounds: the Influence of Prosthetic Groups on Tumor Uptake and Clearance Profile.

    Science.gov (United States)

    Bouvet, Vincent; Wuest, Melinda; Bailey, Justin J; Bergman, Cody; Janzen, Nancy; Valliant, John F; Wuest, Frank

    2017-06-21

    Prostate-specific membrane antigen (PSMA) is an important biomarker expressed in the majority of prostate cancers. The favorable positron emission tomography (PET) imaging profile of the PSMA imaging agent 2-(3-(1-carboxy-5-[(6-[(18)F]fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-pentane-dioic acid [(18)F]DCFPyL in preclinical prostate cancer models and in prostate cancer patients stimulated the development and validation of other fluorine-containing PSMA inhibitors to further enhance pharmacokinetics and simplify production methods. Here, we describe the synthesis and radiopharmacological evaluation of various F-18-labeled PSMA inhibitors which were prepared through different prosthetic group chemistry strategies. Prosthetic groups N-succinimidyl-4-[(18)F]fluorobenzoate ([(18)F]SFB), 4-[(18)F]fluorobenzaldehyde, and 2-deoxy-2-[(18)F]fluoro-D-glucose ([(18)F]FDG) were used for bioconjugation reactions to PSMA-binding lysine-urea-glutamate scaffold via acylation and oxime formation. All fluorine-containing PSMA inhibitors were tested for their PSMA inhibitory potency in an in vitro competitive binding assay in comparison to an established reference compound [(125)I]TAAG-PSMA. Tumor uptake and clearance profiles of three F-18-labeled PSMA inhibitors ([(18)F]4, [(18)F]7, and [(18)F]8) were studied with dynamic PET imaging using LNCaP tumor-bearing mice. F-18-labeled PSMA inhibitors were synthesized in 32-69 % radiochemical yields using (1) acylation reaction at the primary amino group of the lysine residue with [(18)F]SFB and (2) oxime formation with 4-[(18)F]fluorobenzaldehyde and [(18)F]FDG using the respective aminooxy-functionalized lysine residue. Compound 7 displayed an IC50 value of 6 nM reflecting very high affinity for PSMA. Compounds 4 and 8 showed IC50 values of 13 and 62 nM, respectively. The IC50 value of reference compound DCFPyL was 13 nM. Dynamic PET imaging revealed the following SUV60min for radiotracer uptake in PSMA(+) LNCaP tumors: 0

  16. Synthesis and evaluation of (S)-[F-18]-fluoroethylcarazolol for in vivo beta-adrenoceptor imaging in the brain

    NARCIS (Netherlands)

    Doze, P; van Waarde, A; Tewson, TJ; Vaalburg, W; Elsinga, PH

    The beta-adrenergic receptor ligand (S)-4-(3-(2'-[F-18]-fluoroethylamino)-2-hydroxypropoxy)-carbazol ((S)-[F-18]-fluoroethylcarazolol) was prepared by reaction of [F-18]-fluoroethylamine with the corresponding (S)-epoxide and was evaluated in rats by studying its pharmacokinetics and its binding

  17. Syntheses and biological evaluation of F-18 and I-123 labeled porphyrins as potential tumor imaging agents

    Energy Technology Data Exchange (ETDEWEB)

    Lee, J. H.; Ji, D. Y. [Inha University, Incheon (Korea, Republic of); Moon, B. S.; Lee, T. S.; Lee, D. H.; Lee, K. C.; Ahn, G. I.; Yang, S. D.; Choi, C. W.; Jun, K. S. [KIRAMS, Seoul (Korea, Republic of)

    2005-07-01

    Photofrin has currently been approved for general use by licensing authorities to treatment for solid tumor and cancer using photodynamic therapy (PDT) that treat to photochemical effect induced by light. Recently, meso-tetra(3-hydroxyphenyl)porphyrin has been developed as one of best tumor localizer and also shown a favorable tissue distribution. We have studied to develop I-123 labeled meso-tetra(3-methoxyphenyl)porphyrins for tumor imaging. We have studied to develop iodine-123 labeled meso-tetra(3-carboxymethoxy phenyl)porphyrin for tumor imaging agent. The radioiodinated porphyrin compound was obtained by the iodination reaction of tin precursor (50 ig) of porphyrin with Na-123I (200 {mu}L, 100-200 mCi), in the presence of peracetic acid (40 {mu}L) in ethanol. Iodine-123 labeled porphyrin derivative was obtained in 20-30% radiochemical yield and purified by HPLC at 2 mL/min using EtOH/water gradient condition and the fraction at 24-26 min was collected and characterized to desired compound by co injection with cold porphyrin analogue. Total time was around 120 min. The in vitro and in vivo of I-123 labeled porphyrin derivative is under studying.

  18. F-18 labelled PSMA-1007: biodistribution, radiation dosimetry and histopathological validation of tumor lesions in prostate cancer patients.

    Science.gov (United States)

    Giesel, Frederik L; Hadaschik, B; Cardinale, J; Radtke, J; Vinsensia, M; Lehnert, W; Kesch, C; Tolstov, Y; Singer, S; Grabe, N; Duensing, S; Schäfer, M; Neels, O C; Mier, W; Haberkorn, U; Kopka, K; Kratochwil, C

    2017-04-01

    The prostate-specific membrane antigen (PSMA) targeted positron-emitting-tomography (PET) tracer (68)Ga-PSMA-11 shows great promise in the detection of prostate cancer. However, (68)Ga has several shortcomings as a radiolabel including short half-life and non-ideal energies, and this has motivated consideration of (18)F-labelled analogs. (18)F-PSMA-1007 was selected among several (18)F-PSMA-ligand candidate compounds because it demonstrated high labelling yields, outstanding tumor uptake and fast, non-urinary background clearance. Here, we describe the properties of (18)F-PSMA-1007 in human volunteers and patients. Radiation dosimetry of (18)F-PSMA-1007 was determined in three healthy volunteers who underwent whole-body PET-scans and concomitant blood and urine sampling. Following this, ten patients with high-risk prostate cancer underwent (18)F-PSMA-1007 PET/CT (1 h and 3 h p.i.) and normal organ biodistribution and tumor uptakes were examined. Eight patients underwent prostatectomy with extended pelvic lymphadenectomy. Uptake in intra-prostatic lesions and lymph node metastases were correlated with final histopathology, including PSMA immunostaining. With an effective dose of approximately 4.4-5.5 mSv per 200-250 MBq examination, (18)F-PSMA-1007 behaves similar to other PSMA-PET agents as well as to other (18)F-labelled PET-tracers. In comparison to other PSMA-targeting PET-tracers, (18)F-PSMA-1007 has reduced urinary clearance enabling excellent assessment of the prostate. Similar to (18)F-DCFPyL and with slightly slower clearance kinetics than PSMA-11, favorable tumor-to-background ratios are observed 2-3 h after injection. In eight patients, diagnostic findings were successfully validated by histopathology. (18)F-PSMA-1007 PET/CT detected 18 of 19 lymph node metastases in the pelvis, including nodes as small as 1 mm in diameter. (18)F-PSMA-1007 performs at least comparably to (68)Ga-PSMA-11, but its longer half-life combined with its superior energy

  19. F-18 labelled PSMA-1007: biodistribution, radiation dosimetry and histopathological validation of tumor lesions in prostate cancer patients

    Energy Technology Data Exchange (ETDEWEB)

    Giesel, Frederik L.; Vinsensia, M.; Mier, W.; Haberkorn, U.; Kratochwil, C. [University Hospital Heidelberg, Department of Nuclear Medicine, Heidelberg (Germany); Hadaschik, B.; Radtke, J.; Kesch, C. [University Hospital Heidelberg, Department of Urology, Heidelberg (Germany); Cardinale, J.; Schaefer, M.; Neels, O.C.; Kopka, K. [German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry, Heidelberg (Germany); Lehnert, W. [ABX-CRO, Dresden (Germany); Tolstov, Y.; Singer, S. [University Hospital Heidelberg, Section of Molecular Urooncology, Department of Urology, Medical Faculty Heidelberg, Heidelberg (Germany); Grabe, N. [University Hospital Heidelberg, Institute of Pathology, Heidelberg (Germany); University Hospital Heidelberg, Department of Medical Oncology, National Center for Tumor Diseases (NCT), Heidelberg (Germany); University of Heidelberg, Hamamatsu Tissue Imaging and Analysis Center, Heidelberg (Germany); Duensing, S. [University Hospital Heidelberg, Department of Urology, Heidelberg (Germany); University Hospital Heidelberg, Section of Molecular Urooncology, Department of Urology, Medical Faculty Heidelberg, Heidelberg (Germany)

    2017-04-15

    The prostate-specific membrane antigen (PSMA) targeted positron-emitting-tomography (PET) tracer {sup 68}Ga-PSMA-11 shows great promise in the detection of prostate cancer. However, {sup 68}Ga has several shortcomings as a radiolabel including short half-life and non-ideal energies, and this has motivated consideration of {sup 18}F-labelled analogs. {sup 18}F-PSMA-1007 was selected among several {sup 18}F-PSMA-ligand candidate compounds because it demonstrated high labelling yields, outstanding tumor uptake and fast, non-urinary background clearance. Here, we describe the properties of {sup 18}F-PSMA-1007 in human volunteers and patients. Radiation dosimetry of {sup 18}F-PSMA-1007 was determined in three healthy volunteers who underwent whole-body PET-scans and concomitant blood and urine sampling. Following this, ten patients with high-risk prostate cancer underwent {sup 18}F-PSMA-1007 PET/CT (1 h and 3 h p.i.) and normal organ biodistribution and tumor uptakes were examined. Eight patients underwent prostatectomy with extended pelvic lymphadenectomy. Uptake in intra-prostatic lesions and lymph node metastases were correlated with final histopathology, including PSMA immunostaining. With an effective dose of approximately 4.4-5.5 mSv per 200-250 MBq examination, {sup 18}F-PSMA-1007 behaves similar to other PSMA-PET agents as well as to other {sup 18}F-labelled PET-tracers. In comparison to other PSMA-targeting PET-tracers, {sup 18}F-PSMA-1007 has reduced urinary clearance enabling excellent assessment of the prostate. Similar to {sup 18}F-DCFPyL and with slightly slower clearance kinetics than PSMA-11, favorable tumor-to-background ratios are observed 2-3 h after injection. In eight patients, diagnostic findings were successfully validated by histopathology. {sup 18}F-PSMA-1007 PET/CT detected 18 of 19 lymph node metastases in the pelvis, including nodes as small as 1 mm in diameter. {sup 18}F-PSMA-1007 performs at least comparably to {sup 68}Ga-PSMA-11, but its

  20. [F-18]Fluorodihydrorotenone: Synthesis and evaluation of a mitochondrial electron transport chain (ETC) complex I probe for PET

    Energy Technology Data Exchange (ETDEWEB)

    VanBrocklin, H.F.; Enas, J.D.; Hanrahan, S.M. [Lawrence Berkeley Lab., CA (United States)] [and others

    1994-05-01

    The mitochondrial electron transport chain (ETC) consists of five enzyme complexes (I-V) which participate in the transfer of electrons to oxygen and phosphorylation of ADP (oxidative phosphorylation). ETC dysfunction has been linked to several genetic neurological diseases as well as implicated in Parkinson`s (complex I) and Huntington`s (complex I) disease and normal aging processes. Dihydrorotenone (DHR) is a specific high affinity inhibitor of complex I. In order to develop a PET tracer for complex I, we have labeled DHR with fluorine-18. The tosylate precursor was produced in three steps from commercially available rotenone. Fluorine-18 was introduced by nucleophilic displacement of the tosylate using tetrabutyl-ammonium fluoride. Subsequent oxidation with MnO{sub 2} and HPLC purification gave the desired [{sup 18}F]fluoro-DHR. Initial biodistribution studies were carried out in {approximately}200 g male Sprague-Dawley rats. The tracer was taken up rapidly in the heart, an organ highly enriched with mitochondria, (5.5-6% injected dose (ID)/g at 30 minutes) and in the brain ({approximately}1.5% ID/g at 1 hour).

  1. Synthesis Of Labeled Metabolites

    Science.gov (United States)

    Martinez, Rodolfo A.; Silks, III, Louis A.; Unkefer, Clifford J.; Atcher, Robert

    2004-03-23

    The present invention is directed to labeled compounds, for example, isotopically enriched mustard gas metabolites including: [1,1',2,2'-.sup.13 C.sub.4 ]ethane, 1,1'-sulfonylbis[2-(methylthio); [1,1',2,2'-.sup.13 C.sub.4 ]ethane, 1-[[2-(methylsulfinyl)ethyl]sulfonyl]-2-(methylthio); [1,1',2,2'-.sup.13 C.sub.4 ]ethane, 1,1'-sulfonylbis[2-(methylsulfinyl)]; and, 2,2'-sulfinylbis([1,2-.sup.13 C.sub.2 ]ethanol of the general formula ##STR1## where Q.sup.1 is selected from the group consisting of sulfide (--S--), sulfone (--S(O)--), sulfoxide (--S(O.sub.2)--) and oxide (--O--), at least one C* is .sup.13 C, X is selected from the group consisting of hydrogen and deuterium, and Z is selected from the group consisting of hydroxide (--OH), and --Q.sup.2 --R where Q.sup.2 is selected from the group consisting of sulfide (--S--), sulfone(--S(O)--), sulfoxide (--S(O.sub.2)--) and oxide (--O--), and R is selected from the group consisting of hydrogen, a C.sub.1 to C.sub.4 lower alkyl, and amino acid moieties, with the proviso that when Z is a hydroxide and Q.sup.1 is a sulfide, then at least one X is deuterium.

  2. Synthesis of [F-18]RGD-K5 by catalyzed [3+2] cycloaddition for imaging integrin alpha(v)beta(3) expression in vivo

    NARCIS (Netherlands)

    Mirfeizi, Leila; Walsh, Joe; Kolb, Hartmuth; Campbell-Verduyn, Lachlan; Dierckx, Rudi A.; Feringa, Ben L.; Elsinga, Philip H.; de Groot, Tjibbe; Sannen, Ivan; Bormans, Guy; Celen, Sofie

    2013-01-01

    In the last few years click chemistry reactions, and in particular copper-catalyzed cycloadditions have been used extensively for the preparation of new bioconjugated molecules such as F-18-radiolabeled radiopharmaceuticals for positron emission tomography (PET). This study is focused on the synthes

  3. GMP-compliant automated synthesis of [{sup 18}F]AV-45 (Florbetapir F 18) for imaging {beta}-amyloid plaques in human brain

    Energy Technology Data Exchange (ETDEWEB)

    Yao, C.-H. [Department of Nuclear Medicine and Molecular Imaging Center, Chang Gung Memorial Hospital, Taiwan (China); Lin, K.-J. [Department of Nuclear Medicine and Molecular Imaging Center, Chang Gung Memorial Hospital, Taiwan (China); Department of Medical Imaging and Radiological Sciences, Chang Gung University, 259 Wen-Hua 1st Road, Kweishan, Taoyuan 333, Taiwan (China); Weng, C.-C. [Department of Medical Imaging and Radiological Sciences, Chang Gung University, 259 Wen-Hua 1st Road, Kweishan, Taoyuan 333, Taiwan (China); Hsiao, I.-T. [Department of Nuclear Medicine and Molecular Imaging Center, Chang Gung Memorial Hospital, Taiwan (China); Department of Medical Imaging and Radiological Sciences, Chang Gung University, 259 Wen-Hua 1st Road, Kweishan, Taoyuan 333, Taiwan (China); Ting, Y.-S. [Department of Nuclear Medicine and Molecular Imaging Center, Chang Gung Memorial Hospital, Taiwan (China); Yen, T.-C. [Department of Nuclear Medicine and Molecular Imaging Center, Chang Gung Memorial Hospital, Taiwan (China); Department of Medical Imaging and Radiological Sciences, Chang Gung University, 259 Wen-Hua 1st Road, Kweishan, Taoyuan 333, Taiwan (China); Jan, T.-R. [Department and Graduate Institute of Veterinary Medicine, National Taiwan University, Taipei, Taiwan (China); Skovronsky, Daniel [Avid Radiopharmaceuticals, Inc., Philadelphia, PA 19104 (United States); Kung, M.-P. [Department of Nuclear Medicine and Molecular Imaging Center, Chang Gung Memorial Hospital, Taiwan (China); Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104 (United States); Wey, S.-P., E-mail: spwey@mail.cgu.edu.t [Department of Nuclear Medicine and Molecular Imaging Center, Chang Gung Memorial Hospital, Taiwan (China); Department of Medical Imaging and Radiological Sciences, Chang Gung University, 259 Wen-Hua 1st Road, Kweishan, Taoyuan 333, Taiwan (China)

    2010-12-15

    We report herein the Good Manufacturing Practice (GMP)-compliant automated synthesis of {sup 18}F-labeled styrylpyridine, AV-45 (Florbetapir), a novel tracer for positron emission tomography (PET) imaging of {beta}-amyloid (A{beta}) plaques in the brain of Alzheimer's disease patients. [{sup 18}F]AV-45 was prepared in 105 min using a tosylate precursor with Sumitomo modules for radiosynthesis under GMP-compliant conditions. The overall yield was 25.4{+-}7.7% with a final radiochemical purity of 95.3{+-}2.2% (n=19). The specific activity of [{sup 18}F]AV-45 reached as high as 470{+-}135 TBq/mmol (n=19). The present studies show that [{sup 18}F]AV-45 can be manufactured under GMP-compliant conditions and could be widely available for routine clinical use.

  4. SYNTHESIS AND INVIVO DISTRIBUTION IN THE RAT OF SEVERAL F-18 LABELED 5-HYDROXY-2-AMINOTETRALIN DERIVATIVES

    NARCIS (Netherlands)

    ZIJLSTRA, S; ELSINGA, PH; OOSTERHUIS, EZ; VISSER, GM; KORF, J; VAALBURG, W

    A method is described for the rapid production and purification of new potential dopamine agonists. Via thermal heating (refluxing in an oil bath) and microwave exposure 2-[N-n-3-fluoropropyl-N-(4-methylphenyl)ethylamino]-5-hydroxytetralin (12),

  5. Synthesis of exemestane labelled with (13)C.

    Science.gov (United States)

    Fontana, Erminia; Pignatti, Alberto; Giribone, Danilo; Di Salle, Enrico

    2008-08-01

    The synthesis of exemestane Aromasin, an irreversible steroidal aromatase inhibitor, specifically labelled with (13)C is reported. The preparation of [(13)C(3)]exemestane was achieved according to an eight-step procedure starting from the commercially available testosterone.

  6. Enzymic synthesis of labelled chiral substances.

    Science.gov (United States)

    Battersby, A R

    1985-01-01

    The enzymic synthesis of chiral substances in which one hydrogen atom of a methylene group has been replaced by deuterium or tritium is illustrated. Such labelled products can be used to determine the stereochemistry of other enzyme-catalysed reactions.

  7. Synthesis and in vitro affinities of various MDL 100907 derivatives as potential F-18-radioligands for 5-HT2A receptor imaging with PET

    DEFF Research Database (Denmark)

    Herth, Matthias Manfred; Kramer, Vasko; Piel, Markus

    2009-01-01

    Radiolabelled piperidine derivatives such as [(11)C]MDL 100907 and [(18)F]altanserin have played an important role in diagnosing malfunction in the serotonergic neurotransmission. A variety of novel piperidine MDL 100907 derivatives, possible to label with (18)F-fluorine, were synthesized to impr...

  8. PET imaging of liposomes labeled with an [18F]-fluorocholesteryl ether probe prepared by automated radiosynthesis

    DEFF Research Database (Denmark)

    Jensen, Andreas Tue Ingemann; Binderup, Tina; Andresen, Thomas Lars;

    2012-01-01

    A novel [F-18]-labeled cholesteryl ether lipid probe was prepared by synthesis of the corresponding mesylate, which was [F-18]-fluorinated by a [F-18]KF, Kryptofix-222, K2CO3 procedure. Fluorination was done for 10 minutes at 165 degrees C and took place with conversion between 3 and 17%, dependi...

  9. Synthesis of tritium labelled sparsomycin

    Energy Technology Data Exchange (ETDEWEB)

    Broek, L.A.G.M. van den (Katholieke Univ. Nijmegen (Netherlands)); Willemsen, K.C.M.W.; Schlachter, I.H.G.; Ottenheijm, H.C.J.; Kaspersen, F.M. (Organon International B.V., Oss (Netherlands). Scientific Development Group)

    1989-05-01

    The synthesis is described of tritiated sparsomycin (5), a broad-spectrum antitumor antibiotic, with high specific activity (31.4 Ci/mmol, 1/16 TBq/mmol). The radiolabel was introduced by reduction of the cysteine methyl ester 1 with lithium borotritide, [sup 3]H NMR analysis of the final product showed the concomitant formation of the mono-and ditritiated compound in a ratio of 2:1. (Author).

  10. Synthesis of deuterium labelled lorazepam

    Energy Technology Data Exchange (ETDEWEB)

    Koeves, G.J. (Centre of Forensic Sciences, Toronto, ON (Canada))

    1991-01-01

    Synthesis of {sup 2}H{sub 3}-lorazepam was achieved by modification of literature procedures for the unlabelled drug. The key step in the seven step procedure was the initial one where upon selective exchange of 2-amino-5,2'-dichloro-benzophenone was obtained in deuterated acids. Purifications were carried out by preparative HPLC. The {sup 2}H{sub 3}-lorazepam is suitable for use as an internal standard in GC-MS-NICI-SIM quantitative analysis in forensic case work. (author).

  11. Synthesis and labelling of epidepride

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    S-(-)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-iodo-2,3-dimethoxybenzamide (proposed generic name, epidepride) is a very potent dopamine D2 antagonist. It was synthesized by five steps from 3-methoxysalicylic acid. [131I]epidepride was obtained in 97.3% radiochemical yields from the corresponding 5-(tributyltin) derivative using hydrogen peroxide as the oxidant. The aryltin precursor was prepared from non-labelled epidepride by palladium-catalyzed stannylation using bis(tri-n-butyltin) in triethylamine. [131I]epidepride was stable under 4℃, and partition coefficient was 72.3 at pH 7.40. The biodistribution study in rats exihibited high localization in the striatum of the brain with the striatum/cerebellum ratio reaching 237/1 at 320 min postinjection.All these results suggest that[131I]epidepride may be usedd widely as a useful dopamineD2 receptor imaging agent for SPECT.

  12. Comparison of F-18-FLT PET and F-18-FDG PET in esophageal cancer

    NARCIS (Netherlands)

    van Westreenen, HL; Cobben, DCP; Jager, PL; van Dullemen, HM; Wesseling, J; Elsinga, PH; Plukker, JT

    F-18-FDG PET has gained acceptance for staging of esophageal cancer. However, FDG is not tumor specific and false-positive results may occur by accumulation of FDG in benign tissue. The tracer F-18-fluoro-3'-deoxy-3'-L-fluorothymidine (F-18-FLT) might not have these drawbacks. The aim of this study

  13. A simple method for the quality control of [F-18]FDG

    DEFF Research Database (Denmark)

    Koziorowski, J.

    2010-01-01

    Most automated synthesis modules produce [F-18]FDG within half an hour, but the quality control involving up to three separate methods and three different analytical systems is time consuming. The use of HPLC, TLC, and GC for the quality control of [F-18]FDG is both time consuming and expensive...

  14. F-18-FLT PET for visualization of laryngeal cancer : Comparison with F-18-FDG PET

    NARCIS (Netherlands)

    Cobben, DCP; van der Laan, BFAM; Maas, B; Vaalburg, W; Suurmeijer, AJH; Hoekstra, HJ; Jager, PL; Elsinga, PH

    The feasibility of F-18-3'-fluoro-3'-deoxy-L-thymidine PET (FLT PET) for detecting laryngeal cancer was investigated and compared with F-18-FDG PET. Methods: Eleven patients diagnosed with or strongly suspected of having recurrent laryngeal cancer and 10 patients with histologically proven primary

  15. Synthesis of some useful tritium labelled auxins

    Energy Technology Data Exchange (ETDEWEB)

    Buchman, O.; Pri-Bar, I.; Shimoni, M.; Azran, J. (Israel Atomic Energy Commission, Beersheba (Israel). Nuclear Research Center-Negev)

    1992-06-01

    The synthesis of six useful auxins labelled with tritium is described. The following compounds were prepared: 3-indoleacetic acid-5-[sup 3]H (28.9 Ci-1.07 TBq/mmol), 3-indolebutyric acid-5-[sup 3]H (7.3 Ci-270 GBq/mmol), 1-naphthylacetic acid-4-[sup 3]H (27.6 Ci-1.02 TBq/mmol), 2,4-dichloropheno-xyacetic acid-5-[sup 3]H (18.5 Ci-685 GBq/mmol), 2(2,4-dichlorophenoxy-5-[sup 3]H) -propionic acid (20.7 Ci-766 GBq/mmol), 2(2,4-dichlorophenoxy)-propionic acid-3-[sup 3]H (0.39 Ci-14.4 GMq/mmol), and 4-chlorophenoxyacetic acid-2-[sup 3]H (13.3 Ci-492 GBq/mmol). (author).

  16. 76 FR 37129 - Determination That SODIUM FLUORIDE F 18 (Sodium Fluoride F-18) Injection, 10 to 200 Millicuries...

    Science.gov (United States)

    2011-06-24

    ... HUMAN SERVICES Food and Drug Administration Determination That SODIUM FLUORIDE F 18 (Sodium Fluoride F... Drug Administration (FDA) has determined that SODIUM FLUORIDE F 18 (sodium fluoride F-18) injection, 10... FLUORIDE F 18 injection, 10 to 200 mCi/mL, if all other legal and regulatory requirements are met. FOR...

  17. Synthesis of tritium labelled 24-epibrassinolide

    Energy Technology Data Exchange (ETDEWEB)

    Kolbe, A.; Marquardt, V.; Adam, G. (Inst. of Plant Biochemistry Halle, Halle/Saale (Germany))

    1992-10-01

    Deuterium and tritium 5,7,7-tris-labelled 24-epibrassinolide were prepared by base catalyzed exchange reaction using 24-epicastasterone tetraacetate 1 or bis-isopropylidenedioxy-24-epicastasterone 8 and labelled water. Baeyer-Villiger oxidation of the obtained labelled 6-ketones 2 and 3 with CF[sub 3]CO[sub 3]H gave after alkaline deacetylation of the resulting 4 and 5 the desired tris-labelled 24-epibrassinolides 6 and 7, respectively, or starting from 9 under simultaneous oxidation and deprotection in one step the same final products. (author).

  18. Synthesis of deuterium labeled plant ethylene precursor

    Energy Technology Data Exchange (ETDEWEB)

    Nam, K.C. [Chonnam National Univ., Kwangju (Korea, Republic of). Dept. of Chemistry; Rapoport, H. [California Univ., Berkeley, CA (United States). Dept. of Chemistry

    1995-12-31

    Synthetic methods for the preparation of {beta}-deuterium labeled 2-keto-4-methylbutyric acid were investigated. Vinyl chloride was first reacted with the ethyl oxalyl chloride moiety using aluminum chloride as condensing agent and the addition of methyl mercaptan followed. Deuterium labeling was achieved by using NaBD{sub 4} reduction in pyridine. (author).

  19. Asymmetric Synthesis of Carbon-11 Labelled alpha-Amino Acids for PET

    NARCIS (Netherlands)

    Popkov, Alexander; Elsinga, Philip H.

    2013-01-01

    For PET applications in oncological and neurological diagnostics, amino acids have been studied both clinically and pre-clinically during the last 35 years. Nowadays two applications of labelled amino acids for visualisation of tumours attract the main attention: [C-11] or [F-18]amino acids as

  20. Asymmetric Synthesis of Carbon-11 Labelled alpha-Amino Acids for PET

    NARCIS (Netherlands)

    Popkov, Alexander; Elsinga, Philip H.

    2013-01-01

    For PET applications in oncological and neurological diagnostics, amino acids have been studied both clinically and pre-clinically during the last 35 years. Nowadays two applications of labelled amino acids for visualisation of tumours attract the main attention: [C-11] or [F-18]amino acids as subst

  1. Direct Synthesis of ESBO Derivatives-18O Labelled with Dioxirane

    Directory of Open Access Journals (Sweden)

    Stefano La Tegola

    2013-01-01

    Full Text Available This work addresses a new approach developed in our laboratory, consisting in the application of isolated dimethyldioxirane (DDO, 1a labelled with 18O for synthesis of epoxidized glyceryl linoleate (Gly-LLL, 2. We expect that this work could contribute in improving analytical methods for the determination of epoxidized soybean oil (ESBO in complex food matrices by adopting an 18O-labelled-epoxidized triacylglycerol as an internal standard.

  2. Synthesis of C13- and N15-Labeled DNAN

    Science.gov (United States)

    2014-07-24

    labeled methanol as a reagent readily allowed the synthesis of 13C-labeled DNAN, and any possible scrambling of the 13C-labeled carbon with the...with a 20-mm egg -shaped stir bar for 30 min. Chlorobenzene (99.8%, 2.55 mL, 25.0 mmol, 1 equiv) was added dropwise over 2 min and a condenser was...methanol (99.8%, 4.06 mL, 100 mmol, 8 equiv) was stirred in a 25-mL round bottom flask in a room temperature water bath at 600 rpm with a 20-mm egg

  3. Review of Domestic F-18 Multifunctional Module and Synthesis Positron Radiopharmaceuticals%国产氟-18多功能模块及合成正电子放射性药物概述

    Institute of Scientific and Technical Information of China (English)

    张帆; 于璟

    2016-01-01

    The ifeld of radiochemistry is moving towards exclusive use of automated synthesis modules for production of most clinical radiopharmaceutical doses. Such a move comes with many advantages, but also presents radiochemists with many chalenges. This review introduces the characteristic of the PET-MF-2V-IT-I synthesis module, and use it to automate synthetize a series of radiopharmaceutical with the method of single tube synthesis, double tube synthesis, click chemistry synthesis and combined with 1C-CH3I synthesis module, in order to meet the requirements of clinical and scientiifc research .%正电子放射性药品大多采用自动化模块合成以适应临床需要,这种全自动化模块的生产模式有其自身优势,但同时也带来了很大的挑战。本文介绍了国产PET-MF-2V-IT-I型氟-18多功能模块的特点,并运用该模块进行单反应管合成、双反应管合成、点击化学合成、联合11C碘代甲烷模块合成多种放射性药物,以满足临床及科研的需求。

  4. Stereoselective synthesis of stable-isotope-labeled amino acids

    Energy Technology Data Exchange (ETDEWEB)

    Unkefer, C.J.; Martinez, R.A.; Silks, L.A. III [Los Alamos National Laboratory, NM (United States); Lodwig, S.N. [Centralia College, WA (United States)

    1994-12-01

    For magnetic resonance and vibrational spectroscopies to reach their full potential, they must be used in combination with sophisticated site-specific stable isotope labeling of biological macromolecules. Labeled amino acids are required for the study of the structure and function of enzymes and proteins. Because there are 20 common amino acids, each with its own distinguishing chemistry, they remain a synthetic challenge. The Oppolzer chiral auxiliary provides a general tool with which to approach the synthesis of labeled amino acids. By using the Oppolzer auxiliary, amino acids can be constructed from several small molecules, which is ideal for stable isotope labeling. In addition to directing the stereochemistry at the {alpha}-carbon, the camphorsultam can be used for stereo-specific isotope labeling at prochiral centers in amino acids. By using the camphorsultam auxiliary we have the potential to synthesize virtually any isotopomer of all of the common amino acids.

  5. Synthesis of carbon-14 labeled vigabatrin. [Antieplileptic

    Energy Technology Data Exchange (ETDEWEB)

    Schuster, A.J.; Wagner, E.R. (Marion Merrell Dow Inc, Indianapolis, IN (United States))

    1993-01-01

    Carbon-14 labeled vigabatrin was synthesized in 5 steps from 5-hydroxymethyl-2-pyrrolidone tosylate and NaCN-[[sup 14]C]. A key step involved reduction of the resulting nitrile in the presence of excess dimethylamine to give the dimethylamino-ethyl 2-pyrrolidone derivative in one step. This afforded an overall radiochemical yield of 22% and radiochemical purity greater than 98%. (Author).

  6. Synthesis of carbon-14 labeled doxylamine succinate

    Energy Technology Data Exchange (ETDEWEB)

    Rao, P.N.; Damodaran, K.M.

    1986-05-01

    Doxylamine succinate, N,N-dimethyl-2-(1-phenyl-1-(2-pyridinyl)-ethoxy)ethanamine succinate is an antihistamine used primarily as a sedative. Carbon-14 labeled doxylamine succinate, required for toxicological studies, was synthesized in two steps starting from 2-benzoyl pyridine.

  7. Expedited Synthesis of Fluorine-18 Labeled Phenols. A Missing Link in PET Radiochemistry

    Energy Technology Data Exchange (ETDEWEB)

    Katzenellenbogen, John A. [Univ. of Illinois, Champaign, IL (United States); Zhou, Dong [Washington Univ., St. Louis, MO (United States)

    2015-03-26

    Fluorine-18 (F-18) is arguably the most valuable radionuclide for positron emission tomographic (PET) imaging. However, while there are many methods for labeling small molecules with F-18 at aliphatic positions and on electron-deficient aromatic rings, there are essentially no reliable and practical methods to label electron-rich aromatic rings such as phenols, with F-18 at high specific activity. This is disappointing because fluorine-labeled phenols are found in many drugs; there are also many interesting plant metabolites and hormones that contain either phenols or other electron-rich aromatic systems such as indoles whose metabolism, transport, and distribution would be interesting to study if they could readily be labeled with F-18. Most approaches to label phenols with F-18 involve the labeling of electron-poor precursor arenes by nucleophilic aromatic substitution, followed by subsequent conversion to phenols by oxidation or other multi-step sequences that are often inefficient and time consuming. Thus, the lack of good methods for labeling phenols and other electron-rich aromatics with F-18 at high specific activity represents a significant methodological gap in F-18 radiochemistry that can be considered a “Missing Link in PET Radiochemistry”. The objective of this research project was to develop and optimize a series of unusual synthetic transformations that will enable phenols (and other electron-rich aromatic systems) to be labeled with F-18 at high specific activity, rapidly, reliably, and conveniently, thereby bridging this gap. Through the studies conducted with support of this project, we have substantially advanced synthetic methodology for the preparation of fluorophenols. Our progress is presented in detail in the sections below, and much has been published or presented publication; other components are being prepared for publication. In essence, we have developed a completely new method to prepare o-fluorophenols from non-aromatic precursors

  8. First Clinical Results of (D)-F-18-Fluoromethyltyrosine (BAY 86-9596) PET/CT in Patients with Non Small Cell Lung Cancer and Head and Neck Squamous Cell Carcinoma

    NARCIS (Netherlands)

    Burger, Irene A.; Zitzmann-Kolbe, Sabine; Pruim, Jan; Friebe, Matthias; Graham, Keith; Stephens, Andrew; Dinkelborg, Ludger; Kowal, Kristin; Schibli, Roger; Luurtsema, Gert; Maas, Bram; Horn-Tutic, Michaela; Haerle, Stephan K.; Wiegers, Johan; Schaefer, Niklaus G.; Hany, Thomas F.; von Schulthess, Gustav K.

    2014-01-01

    (D)-F-18-fluoromethyltyrosine (D-F-18-FMT), or BAY 86-9596, is a novel F-18-labeled tyrosine derivative rapidly transported by the L-amino acid transporter (LAT-1), with a faster blood pool clearance than the corresponding L-isomer. The aim of this study was to demonstrate the feasibility of tumor d

  9. Synthesis and evaluation of fluorine-18 labeled glyburide analogs as {beta}-cell imaging agents

    Energy Technology Data Exchange (ETDEWEB)

    Schmitz, A.; Shiue, C.-Y. E-mail: Shiue@rad.upenn.edu; Feng, Q.; Shiue, G.G.; Deng, S.; Pourdehnad, M.T.; Schirrmacher, R.; Vatamaniuk, M.; Doliba, N.; Matschinsky, F.; Wolf, B.; Roesch, F.; Naji, A.; Alavi, A.A

    2004-05-01

    Glyburide is a prescribed hypoglycemic drug for the treatment of type 2 diabetic patients. We have synthesized two of its analogs, namely N-{l_brace}4-[{beta}-(2-(2'-fluoroethoxy)-5-chlorobenzenecarboxamido)ethyl] benzenesulfonyl{r_brace}-N'-cyclohexylurea (2-fluoroethoxyglyburide, 8b) and N-{l_brace}4-[{beta}-(2-(2'-fluoroethoxy)-5-iodobenzenecarboxamido)ethyl]benzenesulfonyl {r_brace}-N'-cyclohexylurea (2-fluoroethoxy-5-deschloro-5-iodoglyburide, 8a), and their fluorine-18 labeled analogs as {beta}-cell imaging agents. Both F-18 labeled compound 8a and compound 8b were synthesized by alkylation of the corresponding multistep synthesized hydroxy precursor 4a and 4b with 2-[{sup 18}F]fluoroethyl tosylate in DMSO at 120 degree sign C for 20 minutes followed by HPLC purification in an overall radiochemical yield of 5-10% with a synthesis time of 100 minutes from EOB. The octanol/water partition coefficients of compounds 8a and 8b were 141.21 {+-} 27.77 (n = 8) and 124.33 {+-} 21.61 (n = 8), respectively. Insulin secretion experiments of compounds 8a and 8b on rat islets showed that both compounds have a similar stimulating effect on insulin secretion as that of glyburide. In vitro binding studies showed that {approx}2% of compounds 8a and 8b bound to {beta}TC3 and Min6 cells and that the binding was saturable. Preliminary biodistribution studies in mice showed that the uptake of both compounds 8a and 8b in liver and small intestine were high, whereas the uptake in other organs studied including pancreas were low. Additionally, the uptake of compound 8b in vivo was nonsaturable. These results tend to suggest that compounds 8a and 8b may not be the ideal {beta}-cell imaging agents.

  10. Synthesis of deuterium labelled metabolites of warfarin and phenprocoumon

    Energy Technology Data Exchange (ETDEWEB)

    Heimark, L.D.; Toon, S.; Low, L.K.; Swinney, D.C.; Trager, W.F.

    1986-02-01

    The synthesis of deuterium labelled 4'-,6-,7- and 8-hydroxy metabolites of warfarin and phenprocoumon is described. The pentadeuterio labelled 6-,7- and 8-hydroxyphenprocoumons were prepared via alkylation of the respective 6-, 7- and 8-methoxy-4-hydroxycoumarins with 1-(phenyl-d/sub 5/)-1-bromopropane and subsequent cleavage of the methyl protecting group with boron tribromide. The synthesis of 1-(pentadeuteriophenyl)-1-bromopropane and the 6-, 7-and 8-methoxy-4-hydroxycoumarins are also presented. The pentadeuterio labelled 6-, 7- and 8-hydroxywarfarins were obtained by reaction of 4-(phenyl-d/sub 5/)-3-buten-2-one with the respective 6-, 7- and 8-hydroxy-4-hydroxycoumarins in methanol followed by hydrolysis of the intermediate cyclic methyl ketals in aqueous acid. 4-Hydroxycoumarin-5,6,7,8-d/sub 4/, prepared from phenyl-d/sub 6/ and tetradeuteriomalonic acid, was reacted with 1-(p-hydroxyphenyl)-1-propanol and 4-(p-hydroxyphenyl)-3-buten-2-one to yield labelled 4'-hydroxyphenprocoumon and 4'-hydroxywarfarin respectively.

  11. Synthesis and properties of differently charged chemiluminescent acridinium ester labels.

    Science.gov (United States)

    Natrajan, Anand; Sharpe, David

    2013-02-14

    Chemiluminescent acridinium dimethylphenyl esters containing N-sulfopropyl groups in the acridinium ring are highly sensitive, hydrophilic labels that are used in automated immunoassays for clinical diagnostics. Light emission from these labels is triggered with alkaline peroxide in the presence of a cationic surfactant. At physiological pH, N-sulfopropyl acridinium esters exist as water adducts that are commonly referred to as pseudobases. Pseudobase formation, which results from addition of water to the zwitterionic N-sulfopropyl acridinium ring, neutralizes the positive charge on the acridinium nitrogen and imparts a net negative charge to the label due to the sulfonate moiety. As a consequence, N-sulfopropyl acridinium ester conjugates of small molecule haptens as well as large molecules such as proteins gain negative charges at neutral pH. In the current study, we describe the synthesis and properties of two new hydrophilic acridinium dimethylphenyl ester labels where the net charge in the labels was altered. In one label, the structure of the hydrophilic N-alkyl group attached to the acridinium ring was changed so that the pseudobase of the label contains no net charge. In the second acridinium ester, two additional negative charges in the form of sulfopropyl groups were added to the acridinium ring to make this label's pseudobase strongly anionic. Chemiluminescence measurements of these labels, as well as their conjugates of an antibody with a neutral pI, indicate that acridinium ester charge while having a modest effect on emission kinetics has little influence on light output. However, our results demonstrate that acridinium ester charge can affect protein pI, apparent chemiluminescence stability and non-specific binding of protein conjugates to microparticles. These results emphasize the need for careful consideration of acridinium ester charge in order to optimize reagent stability and performance in immunoassays. In the current study, we observed that

  12. CYP4F18-Deficient Neutrophils Exhibit Increased Chemotaxis to Complement Component C5a

    Directory of Open Access Journals (Sweden)

    Rachel Vaivoda

    2015-01-01

    Full Text Available CYP4Fs were first identified as enzymes that catalyze hydroxylation of leukotriene B4 (LTB4. CYP4F18 has an unusual expression in neutrophils and was predicted to play a role in regulating LTB4-dependent inflammation. We compared chemotaxis of wild-type and Cyp4f18 knockout neutrophils using an in vitro assay. There was no significant difference in the chemotactic response to LTB4, but the response to complement component C5a increased 1.9–2.25-fold in knockout cells compared to wild-type (P < 0.01. This increase was still observed when neutrophils were treated with inhibitors of eicosanoid synthesis. There were no changes in expression of other CYP4 enzymes in knockout neutrophils that might compensate for loss of CYP4F18 or lead to differences in activity. A mouse model of dextran sodium sulfate colitis was used to investigate the consequences of increased C5a-dependent chemotaxis in vivo, but there was no significant difference in weight loss, disease activity, or colonic tissue myeloperoxidase between wild-type and Cyp4f18 knockout mice. This study demonstrates the limitations of inferring CYP4F function based on an ability to use LTB4 as a substrate, points to expanding roles for CYP4F enzymes in immune regulation, and underscores the in vivo challenges of CYP knockout studies.

  13. Synthesis of /sup 14/C-labelled crotamiton

    Energy Technology Data Exchange (ETDEWEB)

    Chaudhuri, N.K.; Potdar, S.V.; Ball, T.J. (CIBA-GEIGY Corp., Ardsley, NY (USA). Pharmaceuticals Div.)

    1982-01-01

    The synthesis of /sup 14/C-labelled crotamiton, which is a fungicide, an insecticide as well as a scabicide is described. Starting from 2-bromonitrobenzene and Cu/sup 14/CN, o-toluidine, labelled with /sup 14/C at the methyl group was prepared by the following sequence of reactions: NO/sub 2/-C/sub 6/H/sub 4/-Br ..-->.. NO/sub 2/-C/sub 6/H/sub 4/-/sup 14/CN ..-->.. NO/sub 2/-C/sub 6/H/sub 4/-/sup 14/COOH ..-->.. NO/sub 2/-C/sub 6/H/sub 4/-/sup 14/CH/sub 2/OH ..-->.. NO/sub 2/-C/sub 6/H/sub 4/-/sup 14/CH/sub 2/Br ..-->.. NH/sub 2/-C/sub 6/H/sub 4/-/sup 14/CH/sub 3/. Labelled o-toluidine was then heated with crotonic anhydride to give crotonic acid o-toluidide which was then ethylated by treatment with sodium hydride and ethyl iodide to obtain labelled crotamiton.

  14. Semi-Synthesis of Labeled Proteins for Spectroscopic Applications

    Directory of Open Access Journals (Sweden)

    Luca Domenico D'Andrea

    2013-01-01

    Full Text Available Since the introduction of SPPS by Merrifield in the 60s, peptide chemists have considered the possibility of preparing large proteins. The introduction of native chemical ligation in the 90s and then of expressed protein ligation have opened the way to the preparation of synthetic proteins without size limitations. This review focuses on semi-synthetic strategies useful to prepare proteins decorated with spectroscopic probes, like fluorescent labels and stable isotopes, and their biophysical applications. We show that expressed protein ligation, combining the advantages of organic chemistry with the easy and size limitless recombinant protein expression, is an excellent strategy for the chemical synthesis of labeled proteins, enabling a single protein to be functionalized at one or even more distinct positions with different probes.

  15. Imaging the pharmacokinetics of [F-18]FAU in patients with tumors: PET studies.

    Science.gov (United States)

    Sun, Haihao; Collins, Jerry M; Mangner, Thomas J; Muzik, Otto; Shields, Anthony F

    2006-02-01

    FAU (1-(2'-deoxy-2'-fluoro-beta-D: -arabinofuranosyl) uracil) can be phosphorylated by thymidine kinase, methylated by thymidylate synthase, followed by DNA incorporation and thus functions as a DNA synthesis inhibitor. This first-in-human study of [F-18]FAU was conducted in cancer patients to determine its suitability for imaging and also to understand its pharmacokinetics as a potential antineoplastic agent. Six patients with colorectal (n = 3) or breast cancer (n = 3) were imaged with [F-18]FAU. Serial blood and urine samples were analyzed using HPLC to determine the clearance and metabolites. Imaging showed that [F-18]FAU was concentrated in breast tumors and a lymph node metastasis (tumor-to-normal-breast-tissue-ratio 3.7-4.7). FAU retention in breast tumors was significantly higher than in normal breast tissues at 60 min and retained in tumor over 2.5 h post-injection. FAU was not retained above background in colorectal tumors. Increased activity was seen in the kidney and urinary bladder due to excretion. Decreased activity was seen in the bone marrow with a mean SUV 0.6. Over 95% of activity in the blood and urine was present as intact [F-18]FAU at the end of the study. Increased [F-18]FAU retention was shown in the breast tumors but not in colorectal tumors. The increased retention of FAU in the breast compared to bone marrow indicates that FAU may be useful as an unlabeled antineoplastic agent. The low retention in the marrow indicates that unlabeled FAU might lead to little marrow toxicity; however, the images were not of high contrast to consider FAU for diagnostic clinical imaging.

  16. Comparison of C-11-choline and F-18-FDG PET in primary diagnosis and staging of patients with thoracic cancer

    NARCIS (Netherlands)

    Pieterman, RM; Que, TH; Elsinga, PH; Pruim, J; van Putten, JWG; Willemsen, ATM; Vaalburg, W; Groen, HJM

    PET with F-18-FDG is used for detection and staging of thoracic cancer; however, more specific PET radiopharmaceuticals would be welcome. C-11-labeled choline (CHOL) is a new radiopharmaceutical potentially useful for tumor imaging, since it is incorporated into cell membranes as

  17. Improved methods to determine radionuclidic purity of F-18 compounds

    DEFF Research Database (Denmark)

    Jørgensen, Thomas; Micheelsen, Mille Ankerstjerne; Jensen, Mikael

    2012-01-01

    Current revisions of monographs for F-18 pharmaceuticals in the European Pharmacopoeia (Ph. Eur.) (Ph. Eur., 2011) call for a radionuclidic purity (RNP) of or better than 99.9%. However, the current method is not sufficient nor effective for testing this required RNP level. We present a theoretical...... model leading to a practical procedure for a simple test of RNP for F-18 compounds that tells whether or not the sample is pure with a statistical confidence of 97.5% (P=0.975). (C) 2011 Elsevier Ltd. All rights reserved....

  18. Quantifying [F-18]fluorodeoxyglucose uptake in the arterial wall

    DEFF Research Database (Denmark)

    Blomberg, Björn Alexander; Bashyam, A.; Ramachandran, A.

    2015-01-01

    Purpose The human arterial wall is smaller than the spatial resolution of current positron emission tomographs. Therefore, partial volume effects should be considered when quantifying arterial wall F-18-FDG uptake. We evaluated the impact of a novel method for partial volume effect (PVE) correcti...

  19. Activity-based costing evaluation of [F-18]-fludeoxyglucose production

    NARCIS (Netherlands)

    Krug, Bruno; Van Zanten, Annie; Pirson, Anne-Sophie; Crott, Ralph; Borght, Thierry Vander

    2008-01-01

    Introduction As healthcare expenses are escalating in many countries, the sector faces a new challenge of becoming more cost efficient. There is an urgent need for more accurate data on the costs of healthcare procedures. The cost of Positron Emission Tomography (PET) with [F-18]-fludeoxyglucose (F-

  20. Activity-based costing evaluation of [F-18]-fludeoxyglucose production

    NARCIS (Netherlands)

    Krug, Bruno; Van Zanten, Annie; Pirson, Anne-Sophie; Crott, Ralph; Borght, Thierry Vander

    2008-01-01

    Introduction As healthcare expenses are escalating in many countries, the sector faces a new challenge of becoming more cost efficient. There is an urgent need for more accurate data on the costs of healthcare procedures. The cost of Positron Emission Tomography (PET) with [F-18]-fludeoxyglucose (F-

  1. F-18 FDG PET in Detecting Renal Cell Carcinoma

    Energy Technology Data Exchange (ETDEWEB)

    Ak, I.; Can, C. [Osmangazi Univ. Medical Faculty, Eskisehir (Turkey). Depts. of Nuclear Medicine and Urology

    2005-12-01

    Purpose: To assess the role of F-18 FDG imaging with a dual head coincidence mode gamma camera (Co-PET) in the detection of renal cell carcinoma (RCC) in patients with renal masses. Material and Methods: An F-18 FDG Co-PET study was performed in 19 patients (7 F, 12 M; mean age 58.15{+-}2.5 years, age range 45-79 years) with suspected primary renal tumors based on conventional imaging techniques, including computed tomography (CT) and ultrasonography (US) before nephrectomy or surgical resection of the mass. Results: Histologically documented RCC was present in 15 patients. Of the 19 patients with suspected primary renal tumors, F-18 FDG Co-PET was true-positive in 13, false-negative in 2, true-negative in 3, and false-positive in 1 patient. Twangiomyolipomas and one renal mass due to infarction and hemorrhage showed a true-negative Co-PET result. The patient with false-positive FDG Co-PET study was diagnosed as xantogranulomatous pyelonephritis. Overall sensitivity, specificity, and accuracy of FDG Co-PET for RCC were 86% (13/15), 75% (3/4), and 84% (16/19), respectively. Positive predictive value for RCC was 92% and negative predictive value 60%. Conclusion: These findings suggest that F-18 FDG Co-PET may have a role in the diagnostic evaluation of patients with RCC and primary staging of disease. Positive F-18 FDG study may be predictive of the presence of RCC. However, a negative study does not exclude the RCC.

  2. Synthesis and detection of oxygen-18 labeled phosphate.

    Science.gov (United States)

    Melby, Eric S; Soldat, Douglas J; Barak, Phillip

    2011-04-04

    Phosphorus (P) has only one stable isotope and therefore tracking P dynamics in ecosystems and inferring sources of P loading to water bodies have been difficult. Researchers have recently employed the natural abundance of the ratio of (18)O/(16)O of phosphate to elucidate P dynamics. In addition, phosphate highly enriched in oxygen-18 also has potential to be an effective tool for tracking specific sources of P in the environment, but has so far been used sparingly, possibly due to unavailability of oxygen-18 labeled phosphate (OLP) and uncertainty in synthesis and detection. One objective of this research was to develop a simple procedure to synthesize highly enriched OLP. Synthesized OLP is made up of a collection of species that contain between zero and four oxygen-18 atoms and, as a result, the second objective of this research was to develop a method to detect and quantify each OLP species. OLP was synthesized by reacting either PCl(5) or POCl(3) with water enriched with 97 atom % oxygen-18 in ambient atmosphere under a fume hood. Unlike previous reports, we observed no loss of oxygen-18 enrichment during synthesis. Electrospray ionization mass spectrometry (ESI-MS) was used to detect and quantify each species present in OLP. OLP synthesized from POCl(3) contained 1.2% P(18)O(16)O(3), 18.2% P(18)O(2) (16)O(2), 67.7% P(18)O(3) (16)O, and 12.9% P(18)O(4), and OLP synthesized from PCl(5) contained 0.7% P(16)O(4), 9.3% P(18)O(3) (16)O, and 90.0% P(18)O(4). We found that OLP can be synthesized using a simple procedure in ambient atmosphere without the loss of oxygen-18 enrichment and ESI-MS is an effective tool to detect and quantify OLP that sheds light on the dynamics of synthesis in ways that standard detection methods cannot.

  3. Synthesis and detection of oxygen-18 labeled phosphate.

    Directory of Open Access Journals (Sweden)

    Eric S Melby

    Full Text Available Phosphorus (P has only one stable isotope and therefore tracking P dynamics in ecosystems and inferring sources of P loading to water bodies have been difficult. Researchers have recently employed the natural abundance of the ratio of (18O/(16O of phosphate to elucidate P dynamics. In addition, phosphate highly enriched in oxygen-18 also has potential to be an effective tool for tracking specific sources of P in the environment, but has so far been used sparingly, possibly due to unavailability of oxygen-18 labeled phosphate (OLP and uncertainty in synthesis and detection. One objective of this research was to develop a simple procedure to synthesize highly enriched OLP. Synthesized OLP is made up of a collection of species that contain between zero and four oxygen-18 atoms and, as a result, the second objective of this research was to develop a method to detect and quantify each OLP species. OLP was synthesized by reacting either PCl(5 or POCl(3 with water enriched with 97 atom % oxygen-18 in ambient atmosphere under a fume hood. Unlike previous reports, we observed no loss of oxygen-18 enrichment during synthesis. Electrospray ionization mass spectrometry (ESI-MS was used to detect and quantify each species present in OLP. OLP synthesized from POCl(3 contained 1.2% P(18O(16O(3, 18.2% P(18O(2 (16O(2, 67.7% P(18O(3 (16O, and 12.9% P(18O(4, and OLP synthesized from PCl(5 contained 0.7% P(16O(4, 9.3% P(18O(3 (16O, and 90.0% P(18O(4. We found that OLP can be synthesized using a simple procedure in ambient atmosphere without the loss of oxygen-18 enrichment and ESI-MS is an effective tool to detect and quantify OLP that sheds light on the dynamics of synthesis in ways that standard detection methods cannot.

  4. Synthesis of carbon-14 and tritium labeled methylprednisolone suleptanate

    Energy Technology Data Exchange (ETDEWEB)

    Stolle, W.T.; Runge, T.A.; Hsi, R.S.P. (Upjohn Co., Kalamazoo, MI (United States))

    1990-05-01

    Methylprednisolone suleptanate was initially labeled with tritium in the A-ring of the steroid portion of the molecule, and with carbon-14 at both carboxylic carbons of the suberic acid portion of the side chain. However these labels proved to lack total metabolic stability after administration to rats. Subsequently a second pair of labeled methylprednisolone suleptanates was synthesized, with tritium at C-7 in the B-ring of the steroid and carbon-14 exclusively at the carboxamide carbon in the side chain. These labeled compounds showed excellent metabolic stability of both the tritium and carbon-14 labels, and should be well suited for conducting drug disposition studies. (author).

  5. Synthesis of isotopically labeled versions of L-MTP-PE (mifamurtide) and MDP.

    Science.gov (United States)

    Li, Yuexian; Plesescu, Mihaela; Prakash, Shimoga R

    2013-01-01

    L-MTP-PE (1), an immunomodulator and its metabolite MDP (4) were synthesized from labeled l-alanine and its protected derivative, respectively. The key intermediate product for the labeled L-MTP-PE synthesis, [(13) C3 ,D4 ]-alanyl-cephalin (2A), was synthesized from [(13) C3 ,D4 ]-l-alanine (3A) in three steps. The key intermediate product for labeled MDP synthesis, amine 11, was prepared from [(13) C3 ,(15) N]-Boc-l-alanine (5A) in two steps.

  6. Unusual Soft Tissue Uptake of F-18 Sodium Fluoride in Three Patients Undergoing F-18 NaF PET/CT Bone Scans for Prostate Cancer.

    Science.gov (United States)

    Hawkins, Andrew S; Howard, Brandon A

    2017-09-01

    Three males aged 71 to 80 years with known stage IV metastatic prostate cancer underwent F-18 sodium fluoride (NaF) PET/CT to assess osseous metastatic disease burden and stability. In addition to F-18 NaF avid known osseous metastases, each patient also exhibited increased F-18 NaF activity in soft tissues. The first patient exhibited multiple F-18 NaF avid enlarged retroperitoneal and pelvic lymph nodes on consecutive PET/CT scans. The second patient demonstrated an F-18 NaF avid thyroid nodule on consecutive PET/CT scans. The third patient exhibited increased F-18 NaF activity in a hepatic metastasis.

  7. Experiments With Recirculating Target for F-18 Production

    Science.gov (United States)

    Kiselev, M. Y.

    2003-08-01

    Approximately 10 ml of O-18 water was loaded in an apparatus containing a 5 ml storage vessel, pump, silver target attached to a cyclotron, filter, backpressure regulator, conductivity meter, several valves and ion exchange cartridges. The water was continuously pumped through the target during proton bombardment at a rate 5 ml/min. Continuous irradiation with beam current ranging from 10 to 50 uA was conducted while pressure, temperature and conductivity were continuously monitored. The results indicate that recirculating of the target water can increase production of F-18 in relation to consumed O-18 water material. It can also increase productivity by eliminating idle periods for re-filling the target. A backpressure regulator can precisely control target pressure. This method also allows for continuous monitoring of the target material temperature, pressure, conductivity and accumulated radioactivity. Results of these observations provide important information about target performance and physical processes taking place inside the target.

  8. Synthesis and NMR of {sup 15}N-labeled DNA fragments

    Energy Technology Data Exchange (ETDEWEB)

    Jones, R.A. [Rutgers, The State Univ. of New Jersey, Piscataway, NJ (United States)

    1994-12-01

    DNA fragments labeled with {sup 15}N at the ring nitrogens and at the exocyclic amino groups can be used to obtain novel insight into interactions such as base pairing, hydration, drug binding, and protein binding. A number of synthetic routes to {sup 15}N-labeled pyrimidine nucleosides, purines, and purine nucleosides have been reported. Moreover, many of these labeled bases or monomers have been incorporated into nucleic acids, either by chemical synthesis or by biosynthetic procedures. The focus of this chapter will be on the preparation of {sup 15}N-labeled purine 2{prime}-deoxynucleosides, their incorporation into DNA fragments by chemical synthesis, and the results of NMR studies using these labeled DNA fragments.

  9. Synthesis of pentamidine labelled with tritium and carbon-14

    Energy Technology Data Exchange (ETDEWEB)

    Hesk, D.; Jones, J.R. (Surrey Univ., Guildford (UK). Dept. of Chemistry); Lockley, W.J.S.; Wilkinson, D.J. (Fisons plc, Loughborough (UK). Pharmaceutical Div.)

    1990-11-01

    Tritium labelled pentamidine has been prepared with a specific activity of 90 mCi mmol{sup -1} using a one-step exchange reaction between the unlabelled drug and tritiated water. The labelling utilised a homogeneous rhodium trichloride catalyst and yielded pentamidine regiospecifically labelled in the positions ortho to the amidine groups. Carbon-14 labelled pentamidine was prepared via a seven-step procedure in which the isotope was introduced via a nucleophilic substitution of 4-bromo-phenol with copper(I) ({sup 14}C)cyanide. (author).

  10. F-18 production with the TOP linac injector

    Energy Technology Data Exchange (ETDEWEB)

    Cianfarani, Cesidio [ENEA, Via E. Fermi 45, Frascati (Rome) (Italy); Cisbani, Evaristo [ISS, Viale Regina Elena 299, Rome (Italy); Orlandi, Gianluca [ENEA, Via E. Fermi 45, Frascati (Rome) (Italy); Frullani, Salvatore [ISS, Viale Regina Elena 299, Rome (Italy)]. E-mail: salvatore.frullani@iss.infn.it; Picardi, Luigi [ENEA, Via E. Fermi 45, Frascati (Rome) (Italy); Ronsivalle, Concetta [ENEA, Via E. Fermi 45, Frascati (Rome) (Italy)

    2006-06-23

    ENEA and ISS (Italian National Institute of Health), are collaborating to develop a dedicated proton medical accelerator, TOP (Oncological Therapy with Protons) linac, consisting of a sequence of three pulsed linear accelerators. The 7 MeV injector can be used in three operating modes: Protontherapy and Radiobiology Mode-injecting low current proton beam into the TOP linac accelerating sections; Radioisotope Mode-generating an intense proton beam (8-10 mA, 50-100 {mu}s, 30-100 Hz) to produce the positron-emitting radionuclide F18 for PET analyses. In the high current mode, at the exit of the injector the beam is guided through a magnetic quadrupoles channel to a target composed by a thin chamber (0.5 mm thick and 1 in. diameter) containing water enriched with O18. Production yield as well as total activity similar to these achieved with higher energy cyclotrons have been obtained. Environmental doses measured give indications on the shielding required for operation under current radioprotection regulations. Improvements are foreseen to optimize the production yield, the useful beam current and to better characterize gamma and neutron dose rates in the different operational modes.

  11. F-18 FDG uptake in respiratory muscle mimicking metastasis in patients with gastric cancer

    Energy Technology Data Exchange (ETDEWEB)

    Choi, Seung Jin; Hyun, In Young [Inha University College of Medicine, Incheon (Korea, Republic of); Kim, Jeong Ho [Gachon Medical School Gil Medical Center, Incheon (Korea, Republic of)

    2006-08-15

    A 67-year-old man with a history of chronic obstructive pulmonary disease (COPD) underwent F-18 fluorodeoxyglucose (FDG) positron emission tomography/computed tomography (PET/CT) for staging of gastric cancer. The projection images of F-18 FDG PET/CT showed intensely increased F-18 FDG uptake in the anterior neck, chest wall, and upper abdomen. We suspected distant metastases of cervical lymph nodes, ribs, and peritoneum in gastric cancer. However, the transaxial images of F-18 FDG PET/CT showed abnormal F-18 FDG uptake in scalene muscles of anterior neck, intercostal muscles of chest wall, and diaphragm of upper abdomen. Patients with COPD use respiratory muscles extensively on the resting condition. These excessive physiologic use of respiratory muscles causes increased F-18 FDG uptake as a result of increased glucose metabolism. The F-18 FDG uptake in respiratory muscles of gastric cancer patient with COPD mimicked distant metastases in cervical lymph nodes, ribs, and peritoneum.

  12. Synthesis of spin-labeled riboswitch RNAs using convertible nucleosides and DNA-catalyzed RNA ligation.

    Science.gov (United States)

    Büttner, Lea; Seikowski, Jan; Wawrzyniak, Katarzyna; Ochmann, Anne; Höbartner, Claudia

    2013-10-15

    Chemically stable nitroxide radicals that can be monitored by electron paramagnetic resonance (EPR) spectroscopy can provide information on structural and dynamic properties of functional RNA such as riboswitches. The convertible nucleoside approach is used to install 2,2,6,6-tetramethylpiperidin-1-oxyl (TEMPO) and 2,2,5,5-tetramethylpyrrolidin-1-oxyl (proxyl) labels at the exocyclic N(4)-amino group of cytidine and 2'-O-methylcytidine nucleotides in RNA. To obtain site-specifically labeled long riboswitch RNAs beyond the limit of solid-phase synthesis, we report the ligation of spin-labeled RNA using an in vitro selected deoxyribozyme as catalyst, and demonstrate the synthesis of TEMPO-labeled 53 nt SAM-III and 118 nt SAM-I riboswitch domains (SAM=S-adenosylmethionine).

  13. Synthesis and evaluation of a fluorine-18 labeled antisense oligonucleotide as a potential PET tracer for NOS mRNA expression

    NARCIS (Netherlands)

    de Vries, EFJ; Vroegh, J; Dijkstra, G; Moshage, H; Elsinga, PH; Jansen, PLM; Vaalburg, W

    2004-01-01

    Inducible NO synthase (iNOS) is overexpressed in inflammatory bowel diseases. An antisense oligonucleotide with good hybridization properties for iNOS mRNA was selected using RT-PCR. The oligonucleotide was reliably labeled with fluorine-18 using N-(4-[F-18]fluorobenzyl)-2-bromoacetamide. Cellular u

  14. Synthesis and evaluation of a fluorine-18 labeled antisense oligonucleotide as a potential PET tracer for NOS mRNA expression

    NARCIS (Netherlands)

    de Vries, EFJ; Vroegh, J; Dijkstra, G; Moshage, H; Elsinga, PH; Jansen, PLM; Vaalburg, W

    2004-01-01

    Inducible NO synthase (iNOS) is overexpressed in inflammatory bowel diseases. An antisense oligonucleotide with good hybridization properties for iNOS mRNA was selected using RT-PCR. The oligonucleotide was reliably labeled with fluorine-18 using N-(4-[F-18]fluorobenzyl)-2-bromoacetamide. Cellular u

  15. Fluorine-18 labeled tracers for PET studies in the neurosciences

    Energy Technology Data Exchange (ETDEWEB)

    Ding, Yu-Shin; Fowler, J.S.

    1995-12-31

    This chapter focuses on fluorine-18, the positron emitter with the longest half-life, the lowest positron energy and probably, the most challenging chemistry. The incorporation of F-18 into organic compounds presents many challenges, including: the need to synthesize and purify the compound within a 2--3 hour time frame; the limited number of labeled precursor molecules; the need to work on a microscale; and the need to produce radiotracers which are chemically and radiochemically pure, sterile and pyrogen-free, and suitable for intravenous injection. The PET method and F-18 labeling of organic molecules are described followed by highlights of the applications of F-18 labeled compounds in the neurosciences and neuropharmacology. It is important to emphasize the essential and pivotal role that organic synthesis has played in the progression of the PET field over the past twenty years from one in which only a handful of institutions possessed the instrumentation and staff to carry out research to the present-day situation where there are more than 200 PET centers worldwide. During this period PET has become an important scientific tool in the neurosciences, cardiology and oncology. It is important to point out that PET is by no means a mature field. The fact that a hundreds of different F-18 labeled compounds have been developed but only a few possess the necessary selectivity and sensitivity in vivo to track a specific biochemical process illustrates this and underscores a major difficulty in radiotracer development, namely the selection of priority structures for synthesis and the complexities of the interactions between chemical compounds and living systems. New developments in rapid organic synthesis are needed in order to investigate new molecular targets and to improve the quantitative nature of PET experiments.

  16. Synthesis of coumarin or ferrocene labeled nucleosides via Staudinger ligation

    Directory of Open Access Journals (Sweden)

    Kois Pavol

    2006-11-01

    Full Text Available Abstract Background Reaction of azides with triaryl phosphines under mild conditions gives iminophosphoranes which can react with almost any kind of electrophilic reagent, e.g. aldehydes/ketones to form imines or esters to form amides. This so-called Staudinger ligation has been employed in a wide range of applications as a general tool for bioconjugation including specific labeling of nucleic acids. Results A new approach for the preparation of labeled nucleosides via intermolecular Staudinger ligation is described. Reaction of azidonucleosides with triphenylphosphine lead to iminophosphorane intermediates, which react subsequently with derivatives of coumarin or ferrocene to form coumarin or ferrocene labeled nucleosides. Fluorescent properties of coumarin labeled nucleosides are determined. Conclusion New coumarin and ferrocene labeled nucleosides were prepared via intermolecular Staudinger ligation. This reaction joins the fluorescent coumarin and biospecific nucleoside to the new molecule with promising fluorescent and electrochemical properties. The isolated yields of products depend on the structure of azidonucleoside and carboxylic acids. A detailed study of the kinetics of the Staudinger ligation with nucleoside substrates is in progress.

  17. Synthesis of {sup 14}C-labeled levamisole and {sup 13}C-labeled tetramisole

    Energy Technology Data Exchange (ETDEWEB)

    Feil, V.J. [US Department of Agriculture, Agricultural Research Service, Biosciences Research Lab., Fargo, ND (United States)

    1996-12-01

    The syntheses of {sup 14}C-ring labeled levamisole ([-]-2,3,5,6-tetrahydro-6-phenyl [{sup 14}C]-UL imidazo[2,1-b]thiazole) from acetophenone-ring-UL-{sup 14}C in 5 steps plus resolution with a 7.5% overall yield, and {sup 13}C{sub 6}-ring labeled tetramisole ([{+-}]-2,3,5,6-tetrahydro-6-phenyl [{sup 13}C{sub 6}]imidazo[2,1-b]thiazole) from benzene-{sup 13}C{sub 6} in 6 steps with a 9.0% overall yield are described. (author).

  18. Synthesis and Preliminary Biological Evaluations of Fluorescent or 149Promethium Labeled Trastuzumab-Polyethylenimine

    Directory of Open Access Journals (Sweden)

    Jonathan Fitzsimmons

    2015-12-01

    Full Text Available Background: Radioimmunotherapy utilize a targeting antibody coupled to a therapeutic isotope to target and treat a tumor or disease. In this study we examine the synthesis and cell binding of a polymer scaffold containing a radiotherapeutic isotope and a targeting antibody. Methods: The multistep synthesis of a fluorescent or 149Promethium-labeled Trastuzumab-polyethyleneimine (PEI, Trastuzumab, or PEI is described. In vitro uptake, internalization and/or the binding affinity to the Her2/neu expressing human breast adenocarcinoma SKBr3 cells was investigated with the labeled compounds. Results: Fluorescent-labeled Trastuzumab-PEI was internalized more into cells at 2 and 18 h than fluorescent-labeled Trastuzumab or PEI. The fluorescent-labeled Trastuzumab was concentrated on the cell surface at 2 and 18 h and the labeled PEI had minimal uptake. DOTA-PEI was prepared and contained an average of 16 chelates per PEI; the compound was radio-labeled with 149Promethium and conjugated to Trastuzumab. The purified 149Pm-DOTA-PEI-Trastuzumab had a radiochemical purity of 96.7% and a specific activity of 0.118 TBq/g. The compound demonstrated a dissociation constant for the Her2/neu receptor of 20.30 ± 6.91 nM. Conclusion: The results indicate the DOTA-PEI-Trastuzumab compound has potential as a targeted therapeutic carrier, and future in vivo studies should be performed.

  19. Synthesis of deuterium-labelled isotopomer of deferasirox.

    Science.gov (United States)

    Havaldar, Freddy H; Dabholkar, Bhushan Vasant; Mule, Ganesh Baban; Kulkarni, Suhas

    2015-04-01

    A d4 -labeled isotopomer of deferasirox was synthesized as internal standard for use in a LC/mass spectroscopy (MS)/MS method developed for the simultaneous quantitative determination of deferasirox in human serum. d4 -deferasirox was synthesized from d8 -toluene.

  20. Association between the porcine Escherichia coli F18 receptor genotype and phenotype and susceptibility to colonisation and postweaning diarrhoea caused by E-coli O138 : F18

    DEFF Research Database (Denmark)

    Frydendahl, K.; Jensen, Tim Kåre; Andersen, Jens Strodl

    2003-01-01

    Porcine postweaning Escherichia coli enteritis is a cause of significant morbidity and mortality in pigs worldwide, and effective prevention remains an unsolved problem. This study examined the correlation between susceptibility of pigs to experimental infection with an E. coli F18 strain...... and the porcine intestinal F18 receptor genotypes. Thirty-one pigs classified as either belonging to the susceptible or the resistant genotype were inoculated with cultures of an E. coli 0138:F18 isolated from a pig with postweaning diarrhoea. Susceptibility to colonisation and diarrhoea was assessed by clinical...... and heterozygotic susceptible pigs. Faecal shedding of the challenge strain correlated with the genetic receptor profile. Twenty pigs examined immunohistochemically revealed focal to extensive small intestinal mucosal colonisation by E. coli O138:F18 in nine of 10 susceptible and three of 10 resistant pigs. Results...

  1. Flow cytometric measurement of RNA synthesis using bromouridine labelling and bromodeoxyuridine antibodies

    DEFF Research Database (Denmark)

    Jensen, P O; Larsen, J; Christiansen, J

    1993-01-01

    Nuclear RNA synthesis can be analysed by flow cytometry of cells labelled with 5-bromouridine (BrUrd) and stained with anti-bromodeoxyuridine (BrdUrd) antibody and FITC-conjugated secondary antibody. A panel of 5 different commercially available anti-BrdUrd antibodies was tested on cells of a HL-...

  2. Synthesis and properties of fluorescent cotton cellulose labeled with norfloxacin

    Institute of Scientific and Technical Information of China (English)

    2009-01-01

    To expand the application of cellulose in the field of fluorescence techniques, the cotton cellulose was labeled with norfloxacin (Cell-NF) via a three-step reaction, involving alkali treatment, epoxy activation, and opening of the epoxy rings with norfloxacin molecules. And the coordination complexes of Cell-NF with rare earth ions terbium (Cell-NF-Tb) and europium (Cell-NF-Eu) were obtained. The products were detected by IR, TG, XPS, UV and fluorescence spectra. Results showed that the norfloxacin content of the labeled cellulose was about 6.73 w‰ and the start temperature of decomposition of the Cell-NF was raised by 40°C compared with the stock cotton cellulose. When excited at 340 nm, the Cell-NF, Cell-NF-Tb, and Cell-NF-Eu in the solid state could emit violet (430 nm), green (549 nm) and red (620 nm) light, respectively.

  3. Synthesis, Characterisation and Application of 68Ga-labelled Macromolecules

    OpenAIRE

    Velikyan, Irina

    2005-01-01

    The positron emitting radionuclide 68Ga (T1/2 = 68 min) might become of practical interest for clinical positron emission tomography (PET). The metallic cation, 68Ga(III), is suitable for complexation with chelators, either naked or conjugated with biological macromolecules. Such labelling procedures require pure and concentrated preparations of 68Ga(III), which cannot be sufficiently fulfilled by the presently available 68Ge/68Ga generator eluate. This thesis presents methods to increase the...

  4. Synthesis of Constructs for Modeling Consumers’ Understanding and Perception of Eco-Labels

    Directory of Open Access Journals (Sweden)

    Khan Md Raziuddin Taufique

    2014-04-01

    Full Text Available The term “eco-labeling” has become a buzzword in today’s sustainable business world. The use of eco-labeling in various forms has been increasing notably for past many years, sometimes as an environmental “requirement” and sometimes merely as a marketing tool. Questions arise about how well these eco-labels are attended and understood by consumers. However, though mentionable studies are found on various aspects of eco-labels, gaps exist in exploring an inclusive set of parameters for investigating consumer perceptions of eco-labels. This paper aims at preparing a synthesis of all the possible factors to be incorporated for measuring consumer perceptions of eco-labeling of products. For making such synthesis, all major works in the field have been thoroughly reviewed. The paper comes up with a total of 10 parameters that include consumer awareness, consumer knowledge, consumer involvement, consumer trust, design and visibility, credibility of the source, type and level of information, clarity of meaning, persuasiveness, and private benefits. This tentative, yet inclusive, set of parameters is thought to be useful for designing large scale future empirical researches for developing a dependable inclusive set of parameters to test consumer understanding and perceptions of eco-label. A framework is proposed for further empirical research.

  5. Synthesis and application of PLGA labeled with 125I

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    The weight loss in vivo degradation of poly (lactide-co-glycolide) (PLGA) radiolabeled with 125I was investigated. PLGA with molecular weight (Mw) of 84000(LA/GA=85/15) were labeled with 125I in the chloroform media by circularly heating and round films of about 15 mm in diameter were formed. The composition and Mw of the 125I-PLGA were characterized by 1H-NMR and viscosimeter. The weight loss of this copolymer in vitro and in vivo degradation was quantified by determining radioactivity of materials. The results indicated that PLGA exhibited significantly faster degradation in vivo than that of in vitro conditions.

  6. [F-18]FLT-PET in oncology : current status and opportunities

    NARCIS (Netherlands)

    Suurmeijer, AJH; Cobben, DCP; Jager, PL; Hoekstra, HJ; Elsinga, PH

    2004-01-01

    In recent years, [F-18]-fluoro-3'-deoxy-3'-L-fluorothymidine ([F-18]FLT) has been developed as a proliferation tracer. Imaging and measurement of proliferation with PET could provide us with a non-invasive staging tool and a tool to monitor the response to anticancer treatment. In this review, the b

  7. Synthesis of 14C-labeled perfluorooctanoic and perfluorodecanoic acids; Purification of perfluorodecanoic acid

    Energy Technology Data Exchange (ETDEWEB)

    Reich, I.L.; Reich, H.J.; Menahan, L.A.; Peterson, R.E.

    1987-01-01

    Perfluorooctanoic and -decanoic acids are representative of a series of perfluorinated acids that have been used for a variety of industrial purposes primarily due to their surfactant properties. The toxicity of these compounds is being investigated in a number of laboratories. 14C-labeled materials would be useful in these studies but are not commercially available. Johncock prepared unlabeled PFOA in low yield by carbonation of the unstable perfluoroheptyllithium at -90 degrees Centigrade. We anticipated several problems in applying this procedure to the synthesis of the 14C-labeled material. Johncock's procedure was run on a fairly large scale (10 mmol) with excess CO2.

  8. Synthesis of Melamine-d6 and the Feasibility of Deuterium Labeled Compounds as Internal Standard

    Directory of Open Access Journals (Sweden)

    GUO Yang-zhen

    2015-11-01

    Full Text Available S-triazine is an important chemical intermediate. Melamine belongs to s-triazine, which has been widely used as an additive in the food industry. To study the stable isotope labeling method of heterocyclic triazine compounds and its application, one step synthesis of melamine-d6 was achieved with a yield of 30% (calculate in ND4OD, which started from ND4OD by the reaction with cyanuric chloride. According to the exchange mechanism of H/D, the feasibility and the necessary conditions were discussed for applying deuterium labeled compounds in isotope dilution mass spectrometry method.

  9. Synthesis of carbon-13 and carbon-14 labelled triazolo-1,4-benzodiazepines

    Energy Technology Data Exchange (ETDEWEB)

    Banks, W.R.; Hawi, A.A.; Digenis, G.A. (Kentucky Univ., Lexington, KY (USA). College of Pharmacy)

    1989-04-01

    An efficient two-step synthesis of 8-chloro-1-methyl-6-phenyl-(3H)-S-triazolo-(4,3-a)(1,4)-benzodiazepine (alprazolam) and 8-chloro-6-(2-chlorophenyl)-1-methyl-(3H)-S-triazolo-(4,3-a)(1,4)-benzodiazepine (triazolam) labelled with carbon-13 or carbon-14 from their corresponding hydrazines is reported. The method involved acylation of the appropriate hydrazine using the mixed carbonic anhydride of sodium ({sup 13}C) or ({sup 14}C) acetate and isobutylchloroformate under mild conditions. Thermolysis of the resulting acetylhydrazides gave the target carbon-14 and carbon-13 labelled compounds in good yields. (author).

  10. Sources of carrier F-19 in F-18 fluoride

    Energy Technology Data Exchange (ETDEWEB)

    Link, J. M.; Shoner, S. C.; Krohn, K. A. [University of Washington, Department of Radiology, Molecular Imaging Center, 1959 NE Pacific St., Box 356004, Seattle, WA 98195-6004 (United States)

    2012-12-19

    Fluorine-18 is used for many PET radiopharmaceuticals. Theoretically {sup 18}F should be carrier free and a good candidate for nanochemistry. However, {sup 18}F has 10 to 1000 times more stable fluorine atoms than radioactive atoms. In order to understand the source of carrier fluoride and other ions associated with {sup 18}F radiosynthesis, anion concentrations of different components of {sup 18}F target systems as well as solvents and chemicals used in radiosynthesis were measured. Results: The enriched water used for production of {sup 18}F had low levels of anions. In general, the sources of anions, particularly of fluoride, were the chemical reagents used for synthesis and trace contaminants in tubing, valves and fittings. A major component of contamination was nitrate from irradiation of dissolved nitrogen gas in the target water.

  11. Sources of carrier F-19 in F-18 fluoride

    Science.gov (United States)

    Link, J. M.; Shoner, S. C.; Krohn, K. A.

    2012-12-01

    Fluorine-18 is used for many PET radiopharmaceuticals. Theoretically 18F should be carrier free and a good candidate for nanochemistry. However, 18F has 10 to 1000 times more stable fluorine atoms than radioactive atoms. In order to understand the source of carrier fluoride and other ions associated with 18F radiosynthesis, anion concentrations of different components of 18F target systems as well as solvents and chemicals used in radiosynthesis were measured. Results: The enriched water used for production of 18F had low levels of anions. In general, the sources of anions, particularly of fluoride, were the chemical reagents used for synthesis and trace contaminants in tubing, valves and fittings. A major component of contamination was nitrate from irradiation of dissolved nitrogen gas in the target water.

  12. Isolated thymic Langerhans cell histiocytosis discovered on F-18 fluorodeoxyglucose positron emission tomography/computed tomography (F-18 FDG PET/CT)

    Energy Technology Data Exchange (ETDEWEB)

    Turpin, Sophie [CHU Sainte-Justine, Nuclear Medicine, Montreal (Canada); Carret, Anne-Sophie [CHU Sainte-Justine, Hemato-Oncology, Montreal (Canada); Dubois, Josee [CHU Sainte-Justine, Radiology, Montreal (Canada); Buteau, Chantal [CHU Sainte-Justine, Infectious Diseases, Montreal (Canada); Patey, Natalie [CHU Sainte-Justine, Pathology, Montreal (Canada)

    2015-11-15

    The thymic infiltration in young patients with multisystemic Langerhans cell histiocytosis and its radiologic features are well known. However, isolated thymic disease has seldom been reported in the literature. We report the case of a 10-month-old child admitted for fever of unknown origin. Whole-body F-18 fluorodeoxyglucose positron emission tomography/computed tomography (F-18 FDG PET/CT) was performed to identify a focus of infection. It demonstrated an unusual aspect of the thymus, which led to further investigation and revealed isolated infiltration of the thymus by Langerhans cell histiocytosis. The patient was treated accordingly and is now disease free. As evaluation of Langerhans cell histiocytosis patients with F-18 FDG PET/CT is becoming more frequent, it is important to be aware of the scintigraphical characteristics of thymic Langerhans cell histiocytosis. (orig.)

  13. Escherichia coli cell-free protein synthesis and isotope labeling of mammalian proteins.

    Science.gov (United States)

    Terada, Takaho; Yokoyama, Shigeyuki

    2015-01-01

    This chapter describes the cell-free protein synthesis method, using an Escherichia coli cell extract. This is a cost-effective method for milligram-scale protein production and is particularly useful for the production of mammalian proteins, protein complexes, and membrane proteins that are difficult to synthesize by recombinant expression methods, using E. coli and eukaryotic cells. By adjusting the conditions of the cell-free method, zinc-binding proteins, disulfide-bonded proteins, ligand-bound proteins, etc., may also be produced. Stable isotope labeling of proteins can be accomplished by the cell-free method, simply by using stable isotope-labeled amino acid(s) in the cell-free reaction. Moreover, the cell-free protein synthesis method facilitates the avoidance of stable isotope scrambling and dilution over the recombinant expression methods and is therefore advantageous for amino acid-selective stable isotope labeling. Site-specific stable isotope labeling is also possible with a tRNA molecule specific to the UAG codon. By the cell-free protein synthesis method, coupled transcription-translation is performed from a plasmid vector or a PCR-amplified DNA fragment encoding the protein. A milligram quantity of protein can be produced with a milliliter-scale reaction solution in the dialysis mode. More than a thousand solution structures have been determined by NMR spectroscopy for uniformly labeled samples of human and mouse functional domain proteins, produced by the cell-free method. Here, we describe the practical aspects of mammalian protein production by the cell-free method for NMR spectroscopy.

  14. Synthesis of carbon-11, fluorine-18, and nitrogen-13 labeled radiotracers for biomedical applications

    Energy Technology Data Exchange (ETDEWEB)

    Fowler, J.S.; Wolf, A.P.

    1981-01-01

    A number of reviews, many of them recent, have appeared on various aspects of /sup 11/C, /sup 18/F and /sup 13/N-labeled radiotracers. This monograph treats the topic principally from the standpoint of synthetic organic chemistry while keeping in perspective the necessity of integrating the organic chemistry with the design and ultimate application of the radiotracer. Where possible, recent examples from the literature of organic synthesis are introduced to suggest potentially new routes which may be applied to problems in labeling organic molecules with the short-lived positron emitters, carbon-11, fluorine-18, and nitrogen-13. The literature survey of carbon-11, fluorine-18 and nitrogen-13 labeled compounds presented are of particular value to scientists working in this field. Two appendices are also included to provide supplementary general references. A subject index concludes this volume.

  15. Metabolism of F18, a Derivative of Calanolide A, in Human Liver Microsomes and Cytosol

    Directory of Open Access Journals (Sweden)

    Xiangmeng Wu

    2017-07-01

    Full Text Available 10-Chloromethyl-11-demethyl-12-oxo-calanolide (F18, an analog of calanolide A, is a novel potent nonnucleoside reverse transcriptase inhibitor against HIV-1. Here, we report the metabolic profile and the results of associated biochemical studies of F18 in vitro and in vivo. The metabolites of F18 were identified based on liquid chromatography-electrospray ionization mass spectrometry and/or nuclear magnetic resonance. Twenty-three metabolites of F18 were observed in liver microsomes in vitro. The metabolism of F18 involved 4-propyl chain oxidation, 10-chloromethyl oxidative dechlorination and 12-carbonyl reduction. Three metabolites (M1, M3-1, and M3-2 were also found in rat blood after oral administration of F18 and the reduction metabolites M3-1 and M3-2 were found to exhibit high potency for the inhibition of HIV-1 in vitro. The oxidative metabolism of F18 was mainly catalyzed by cytochrome P450 3A4 in human microsomes, whereas flavin-containing monooxygenases and 11β-hydroxysteroid dehydrogenase were found to be involved in its carbonyl reduction. In human cytosol, multiple carbonyl reductases, including aldo-keto reductase 1C, short-chain dehydrogenases/reductases and quinone oxidoreductase 1, were demonstrated to be responsible for F18 carbonyl reduction. In conclusion, the in vitro metabolism of F18 involves multiple drug metabolizing enzymes, and several metabolites exhibited anti-HIV-1 activities. Notably, the described results provide the first demonstration of the capability of FMOs for carbonyl reduction.

  16. Stable-isotope-labeled carbohydrates and nucleosides: Synthesis and applications in chemistry and biology

    Energy Technology Data Exchange (ETDEWEB)

    Serianni, A.S. [Univ. of Notre Dame, IN (United States)

    1994-12-01

    Carbohydrates play important roles in many key biochemical processes in living cells. For example, they are metabolized to produce energy, mediate cell-cell recognition, and play an indirect role (as constituents of DNA and RNA) in DNA replication, RNA transcription, and protein synthesis. These roles, and others of comparable biochemical significance, have been studied to varying extends with the use of stable isotopically labeled molecules, usually in conjunction with NMR spectroscopy and/or mass spectrometry. For example, carbohydrate metabolism has been monitored in vitro and in vivo with the use of isotopically labeled compounds. Molecular aspects of cell-cell recognition, mediated by cell-surface glycoproteins and glycolipids, have been probed through NMR studies of isotopically labeled oligosaccharides. More recently, the solution behavior of DNA and RNA has been examined through the use of labeled oligonucleotides. In all of these pursuits, the effort and expense to prepare labeled molecules, both of which can be substantial, are more than offset by the wealth of information derived from these studies. This information often cannot be accessed, or can be accessed only with great difficulty, using natural (unlabeled) compounds.

  17. A Case of Acute Q Fever Hepatitis Diagnosed by F-18 FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Beak, Sora [Hallym Univ. College of Medicine, Seoul (Korea, Republic of); Oh, Minyoung; Lee, Sand-Oh; Yu, Eunsil; Ryu Jin-Sook [Univ. of Ulsan College of Medicine, Seoul (Korea, Republic of)

    2012-06-15

    A 53-year-old man with fever of unknown origin underwent F-18 fluorodeoxyglucose positron emission tomography/computed tomography (F-18 FDG PET/CT) as a workup for a fever of unknown origin. On presentation, he complained of fever, chills, and myalgia. The F-18 FDG PET/CT scan showed diffusely increased uptake of the liver with mild hepatomegaly. A liver biopsy then revealed fibrin-ring granulomas typically seen in Q fever. The patient was later serologically diagnosed as having acute Q fever as the titers for C. IgM and IgG were 64:1 and -16:1, respectively. He recovered completely following administration of doxycycline. This indicates that F-18 FDG PET/CT may be helpful for identifying hepatic involvement in Q fever as a cause of fever of unknown origin.

  18. [F-18]-AV-1451 binding correlates with postmortem neurofibrillary tangle Braak staging.

    Science.gov (United States)

    Marquié, Marta; Siao Tick Chong, Michael; Antón-Fernández, Alejandro; Verwer, Eline E; Sáez-Calveras, Nil; Meltzer, Avery C; Ramanan, Prianca; Amaral, Ana C; Gonzalez, Jose; Normandin, Marc D; Frosch, Matthew P; Gómez-Isla, Teresa

    2017-06-13

    [F-18]-AV-1451, a PET tracer specifically developed to detect brain neurofibrillary tau pathology, has the potential to facilitate accurate diagnosis of Alzheimer's disease (AD), staging of brain tau burden and monitoring disease progression. Recent PET studies show that patients with mild cognitive impairment and AD dementia exhibit significantly higher in vivo [F-18]-AV-1451 retention than cognitively normal controls. Importantly, PET patterns of [F-18]-AV-1451 correlate well with disease severity and seem to match the predicted topographic Braak staging of neurofibrillary tangles (NFTs) in AD, although this awaits confirmation. We studied the correlation of autoradiographic binding patterns of [F-18]-AV-1451 and the stereotypical spatiotemporal pattern of progression of NFTs using legacy postmortem brain samples representing different Braak NFT stages (I-VI). We performed [F-18]-AV-1451 phosphor-screen autoradiography and quantitative tau measurements (stereologically based NFT counts and biochemical analysis of tau pathology) in three brain regions (entorhinal cortex, superior temporal sulcus and visual cortex) in a total of 22 cases: low Braak (I-II, n = 6), intermediate Braak (III-IV, n = 7) and high Braak (V-VI, n = 9). Strong and selective [F-18]-AV-1451 binding was detected in all tangle-containing regions matching precisely the observed pattern of PHF-tau immunostaining across the different Braak stages. As expected, no signal was detected in the white matter or other non-tangle containing regions. Quantification of [F-18]-AV-1451 binding was very significantly correlated with the number of NFTs present in each brain region and with the total tau and phospho-tau content as reported by Western blot and ELISA. [F-18]-AV-1451 is a promising biomarker for in vivo quantification of brain tau burden in AD. Neuroimaging-pathologic studies conducted on postmortem material from individuals imaged while alive are now needed to confirm these observations.

  19. The findings of F-18 FDG camera-based coincidence PET in acute leukemia

    Energy Technology Data Exchange (ETDEWEB)

    Yoon, S. N.; Joh, C. W.; Lee, M. H. [Ajou University School of Medicine, Suwon (Korea, Republic of)

    2002-07-01

    We evaluated the usefulness of F-18 FDG coincidence PET (CoDe-PET) using a dual-head gamma camera in the assessment of patients with acute leukemia. F-18 FDG CoDE-PET studies were performed in 5 patients with acute leukemia (6 ALL and 2 AML) before or after treatment. CoDe-PET was performed utilizing a dual-head gamma camera equipped with 5/8 inch NaI(Tl) crystal. Image acquisition began 60 minutes after the injection of F-18 FDG in the fasting state. A whole trunk from cervical to inguinal regions or selected region were scanned. No attenuation correction was made and image reconstruction was done using filtered back-projection. CoDe-PET studies were evaluated visually. F-18 FDG image performed in 5 patients with ALL before therapy depicted multiple lymph node involvement and diffuse increased uptake involving axial skeleton, pelvis and femurs. F-18 FDG image done in 2 AML after chemotherapy showed only diffuse increased uptake in sternum, ribs, spine, pelvis and proximal femur and these may be due to G-CSF stimulation effect in view of drug history. But bone marrow histology showed scattered blast cell suggesting incomplete remission in one and completer remission in another. F-18 image done in 1 ALL after therapy showed no abnormal uptake. CoDe-PET with F-18 FDG in acute lymphoblastic lymphoma showed multiple lymphnode and bone marrow involvement in whole body. Therefore we conclude that CoDe-PET with F-18 FDG usefulness for evaluation of extent in acute lymphoblastic leukemia. But there was a limitation to assess therapy effectiveness during therapy due to reactive bone marrow.

  20. Design and synthesis of labeled analogs of PhTX-56, a potent and selective AMPA receptor antagonist

    DEFF Research Database (Denmark)

    Andersen, Trine F; Vogensen, Stine B; Jensen, Lars S

    2005-01-01

    antagonist of Ca2+-permeable AMPA receptors. PhTX-56 and its labeled derivatives are promising tools for structure-function studies of the ion channel of the AMPA receptor. We now describe the design and synthesis of 3H-, 13C-, and 15N-labeled derivatives of PhTX-56 for molecular level studies of AMPA....... These analogs can provide detailed information on the ligand-receptor interaction. In conclusion, synthesis of labeled derivatives of PhTX-56 provides important tools for future studies of the pore-forming region of AMPA receptors....

  1. High-throughput synthesis of stable isotope-labeled transmembrane proteins for targeted transmembrane proteomics using a wheat germ cell-free protein synthesis system.

    Science.gov (United States)

    Takemori, Nobuaki; Takemori, Ayako; Matsuoka, Kazuhiro; Morishita, Ryo; Matsushita, Natsuki; Aoshima, Masato; Takeda, Hiroyuki; Sawasaki, Tatsuya; Endo, Yaeta; Higashiyama, Shigeki

    2015-02-01

    Using a wheat germ cell-free protein synthesis system, we developed a high-throughput method for the synthesis of stable isotope-labeled full-length transmembrane proteins as proteoliposomes to mimic the in vivo environment, and we successfully constructed an internal standard library for targeted transmembrane proteomics by using mass spectrometry.

  2. Synthesis of ¹⁸F-labelled β-lactams by using the Kinugasa reaction.

    Science.gov (United States)

    Zlatopolskiy, Boris D; Krapf, Philipp; Richarz, Raphael; Frauendorf, Holm; Mottaghy, Felix M; Neumaier, Bernd

    2014-04-14

    Owing to their broad spectrum of biological activities and low toxicity, β-lactams are attractive lead structures for the design of novel molecular probes. However, the synthesis of positron emission tomography (PET)-isotope-labelled β-lactams has not yet been reported. Herein, we describe the simple preparation of radiofluorinated β-lactams by using the fast Kinugasa reaction between (18)F-labelled nitrone [(18)F]-1 and alkynes of different reactivity. Additionally, (18)F-labelled fused β-lactams were obtained through the reaction of a cyclic nitrone 7 with radiofluorinated alkynes [(18)F]-6 a,b. Radiochemical yields of the Kinugasa reaction products could be significantly increased by the use of different Cu(I) ligands, which additionally allowed a reduction in the amount of precursor and/or reaction time. Model radiofluorinated β-lactam-peptide and protein conjugates ([(18)F]-10 and (18)F-labelled BSA conjugate) were efficiently obtained in high yield under mild conditions (aq. MeCN, ambient temperature) within a short reaction time, demonstrating the suitability of the developed method for radiolabelling of sensitive molecules such as biopolymers.

  3. Synthesis and properties of chemiluminescent acridinium ester labels with fluorous tags.

    Science.gov (United States)

    Natrajan, Anand; Wen, David; Sharpe, David

    2014-06-21

    Acridinium dimethylphenyl esters are highly sensitive chemiluminescent labels that are used in clinical diagnostics. Light emission from these labels is triggered with alkaline peroxide in the presence of the cationic surfactant cetyltrimethylammonium chloride (CTAC). CTAC compresses emission times of these labels to ester chemiluminescence (light yield) is quite sensitive to the polarity of the micellar interface. In the current study, we report the synthesis of new acridinium ester labels with fluorous tags of varying fluorine content and their chemiluminescence in the presence of cationic micelles of CTAC, anionic micelles of sodium perfluorooctanoate (SPFO) as well as mixed micelles of CTAC and SPFO. These studies indicate that in the presence of the mixed micelle system of CTAC and SPFO and at low mole fractions of SPFO, polarity of the mixed micelle interface is lower than that of CTAC leading to a greater enhancement of chemiluminescence for both fluorinated acridinium esters as well as a structurally analogous but non-fluorinated acridinium ester. Chemiluminescence stability of the fluorinated acridinium esters was either comparable to or better than the stability of the non-fluorinated acridinium ester. Non-specific binding to paramagnetic microparticles was higher for fluorinated acridinium esters requiring a surfactant wash to reduce their non-specific binding to the same extent as that observed for the non-fluorinated acridinium ester.

  4. Synthesis of the sup 11 C-labelled. beta. -adrenergic receptor ligands atenolol, metoprolol and propanolol

    Energy Technology Data Exchange (ETDEWEB)

    Antoni, G.; Ulin, J.; Laangstroem, B. (Uppsala Univ. (Sweden). Dept. of Organic Chemistry)

    1989-01-01

    The {sup 11}C-labelled {beta}-adrenergic receptor ligands atenolol 1, metoprolol 2 and propranolol 3 have been synthesized by an N-alkylation reaction using (2-{sup 11}C)isopropyl iodide. The labelled isopropyl iodide was prepared in a one-pot reactor system from ({sup 11}C)carbon dioxide and obtained in 40% radiochemical yield within 14 min reaction time. The total reaction times for compounds 1-3, counted from the start of the isopropyl iodide synthesis and including purification were 45-55 min. The products were obtained in 5-15% radiochemical yields and with radiochemical purities higher than 98%. The specific activity ranged from 0.4 to 4 GBq/{mu}mol. In a typical experiment starting with 4 GBq around 75 MBq of product was obtained. (author).

  5. Expression of key glycosphingolipid biosynthesis-globo series pathway genes in Escherichia coli F18-resistant and Escherichia coli F18-sensitive piglets.

    Science.gov (United States)

    Dong, W H; Dai, C H; Sun, L; Wang, J; Sun, S Y; Zhu, G Q; Wu, S L; Bao, W B

    2016-08-01

    A pioneering study showed that the glycosphingolipid biosynthesis-globo series pathway genes (FUT1, FUT2, ST3GAL1, HEXA, HEXB, B3GALNT1 and NAGA) may play an important regulatory role in resistance to Escherichia coli F18 in piglets. Therefore, we analysed differential gene expression in 11 tissues of two populations of piglets sensitive and resistant respectively to E. coli F18 and the correlation of differential gene expression in duodenal and jejunal tissues. We found that the mRNA expression of the seven genes was relatively high in spleen, liver, lung, kidney, stomach and intestinal tract; the levels in thymus and lymph nodes were lower, with the lowest levels in heart and muscle. FUT2 gene expression in the duodenum and jejunum of the resistant population was significantly lower than that in the sensitive group (P gene expression was also significantly lower in the duodenum of the resistant population than in the sensitive group (P genes. The expression level of FUT1 was extremely significantly positively correlated with FUT2 and B3GALNT1 expression (P < 0.01) and also had a significant positive correlation with NAGA expression (P < 0.05). The expression level of FUT2 had extremely significant positive correlations with FUT1, ST3GAL1 and B3GALNT1 (P < 0.01). These results suggest that FUT2 plays an important role in E. coli F18 resistance in piglets. FUT1, ST3GAL1, B3GALNT1 and NAGA may also participate in the mechanism of resistance to E. coli F18.

  6. Radiosynthesis of F-18 DPA-714, a selective radioligand for imaging the translocator protein (18 kDa) with PET

    Energy Technology Data Exchange (ETDEWEB)

    Damont, A.; Hinnen, F.; Kuhnast, B.; Schollhorn-Peyronneau, M.A.; Tavitian, B.; Dolle, F. [CEA, I2BM, Service Hospitalier Frederic Joliot, Laboratoired' Imagerie Moleculaire Experimentale, F-91401 Orsay (France); James, M.; Luus, C. [University of Sydney, Department of Pharmacology, NSW 2006 (Australia); James, M.; Luus, C.; Kassiou, M. [University of Sydney, Brain and Mind Research Institute, NSW 2050 (Australia); Tavitian, B. [INSERM, U803, Service Hospitalier Frederic Joliot, F-91401 Orsay (France); Kassiou, M. [University of Sydney, Discipline of Medical Radiation Sciences, NSW 2006 (Australia); Kassiou, M. [University of Sydney, School of Chemistry, NSW 2006 (Australia)

    2008-07-01

    Recently, a novel series of 2-phenyl-pyrazolo[1,5-a]pyrimidine-acetamides has been reported as selective ligands of the translocator protein (18 kDa). Within this series, DPA-714 (NN-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a] pyrimidin-3-yl)acetamide, K-i=7.0 nM) is a compound, which had been designed with a fluorine atom in its structure, allowing labelling with fluorine-18 (half-life: 109.8 min) and in vivo imaging using positron emission tomography. DPA-714 and its tosyl-oxy derivative (NN-diethyl-2- (2- (4- (2-toluene-sulfonyl-oxy-ethoxy)phenyl) -5,7-dimethyl-pyrazolo [1,5-a]pyrimidin-3-yl) acetamide) as precursor for the labelling with fluorine-18 were synthesized in two steps from DPA-713 (N,N-diethyl-2-(2-(4-methoxy-phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin -3-yl)acetamide) and obtained in 32 and 42% yields, respectively. [(18)FIDPA-714 was synthesized using a simple one-step process (a tosyl-oxy-for-fluorine nucleophilic aliphatic substitution), which has been fully automated on our Zymate-XP robotic system. It involves: (A) reaction of K[F-18]F-Kryptofix 222 with the tosyl-oxy precursor (4.5-5.0 mg, 8.2-9.1 {mu}mol) at 165 degrees C for 5 min in dimethyl sulfoxide (0.6 ml) followed by (B) C18 PrepSep cartridge pre-purification and finally (C) semi-preparative high-performance liquid chromatography (HPLC) purification on a Waters X-Terra(TM) RP18. Typically, 5.6-7.4 GBq of [F-18]DPA-714 ({>=} 95% chemically and radiochemically pure) could be obtained with specific radioactivities ranging from 37 to 111 GBq/{mu}mol within 85-90 min (HPLC purification and SepPak (R)-based formulation included), starting from a 37 GBq[F-18]fluoride batch (overall non-decay-corrected and isolated radiochemical yield: 15-20%). (authors)

  7. Synthesis of {sup 15}N isotope labeled alanine; Sintese da alanina enriquecida com {sup 15}N

    Energy Technology Data Exchange (ETDEWEB)

    Oliveira, Claudineia R. de; Bendassolli, Jose Albertino; Sant' Ana, Carlos Roberto; Tagliassachi, Romulo Barbieri; Maximo, Everaldo; Prestes, Clelber Vieira [Centro de Energia Nuclear na Agricultura (CENA), Piracicaba, SP (Brazil). Dept. de Isotopos Estaveis]. E-mail: crolivei@cena.usp.br

    2005-07-01

    The application of light chemical elements and their stable isotopes in biological studies have been increased over the last years. The use of {sup 15}N labeled amino acids is an important tool for elucidation of peptides structures. This paper describe a method for the synthesis of {sup 15}N isotope labeled alanine at lower costs than international ones, as well as the details of the recovery system of the nitrogen residues. In the present work an amination of {alpha}-haloacids, with the bromopropionic carboxylic acid and labeled aqua ammonia ({sup 15}NH{sub 3} aq) was carried out. In order to avoid eventually losses of {sup 15}NH{sub 3}, special cares were adopted, since the production cost is high. Although the acquisition cost of the {sup 13}N (radioactive) labeled compounds is lower, the obtained stable tracer will allow the accomplishment of important studies of the nitrogen cycling in living things, less occupational and environment hazards, and the time limitation problems in field studies. The tests took place in triplicates with NH{sub 3} (aq) being employed. With the establishment of the system for {sup 15}NH{sub 3} recovery, an average of 94 % of the ammonia employed in the synthesis process was recovered. The purity of the amino acid was state determined by TLC (Thin Layer Chromatography) and HPLC (High-Performance Liquid Chromatography) with a fluorescence detector. The Rf and the retention time of the synthesized sample were similar the sigma standard. Finally, regarding the established conditions, it was possible to obtain the alanine with a production cost about 40 % lower than the international price. (author)

  8. Energy dependence of the total reaction cross section of isomeric F-18(m) on silicon below 400 MeV

    NARCIS (Netherlands)

    Roberts, DA; Becchetti, FD; Janecke, J; Lee, MY; O'Donnell, TW; Pham, K; Warner, RE; Ronningen, RM; Wilschut, HW

    2002-01-01

    A 25 MeV/nucleon primary O-17 beam was used to produce an isomeric state F-18(m) beam via the single-nucleon transfer reaction O-17 (C-12, B-11)F-18(m). The total nuclear reaction cross section, sigma(R), of F-18(m) (metastable) on silicon was measured using a stack of silicon surface barrier detect

  9. Development of a modular system for the synthesis of PET [{sup 11}C]labelled radiopharmaceuticals

    Energy Technology Data Exchange (ETDEWEB)

    Boschi, Stefano [PET Radiopharmacy, Nuclear Medicine, Azienda Ospedaliero Universitaria di Bologna, Policlinico S.Orsola-Malpighi, Via Massarenti 9, 40138 Bologna (Italy)], E-mail: stefano.boschi@aosp.bo.it; Lodi, Filippo [PET Radiopharmacy, Nuclear Medicine, Azienda Ospedaliero Universitaria di Bologna, Policlinico S.Orsola-Malpighi, Via Massarenti 9, 40138 Bologna (Italy); Cicoria, Gianfranco [Medical Physics, Azienda Ospedaliero Universitaria di Bologna, Policlinico S.Orsola-Malpighi (Italy); Raul Ledesma, Jorge [Fundacion Escuela de Medicina Nuclear, Mendoza (Argentina); Knopp, Roger [Eckert Ziegler-Eurotope, Berlin (Germany); Rizzello, Anna; Di Pierro, Donato; Trespidi, Silvia [PET Radiopharmacy, Nuclear Medicine, Azienda Ospedaliero Universitaria di Bologna, Policlinico S.Orsola-Malpighi, Via Massarenti 9, 40138 Bologna (Italy); Marengo, Mario [Medical Physics, Azienda Ospedaliero Universitaria di Bologna, Policlinico S.Orsola-Malpighi (Italy)

    2009-10-15

    [{sup 11}C]labelled radiopharmaceuticals as N-[{sup 11}C]methyl-choline ([{sup 11}C]choline), L-(S-methyl-[{sup 11}C])methionine ([{sup 11}C]methionine) and [{sup 11}C]acetate have gained increasing importance in clinical PET and for the routine production of these radiopharmaceuticals, simple and reliable modules are needed to produce clinically relevant radioactivity. On the other hand, flexible devices are needed not only for the routine synthesis but also for more complex applications as the development of new tracers. The aim of this work was the adaptation of an Eckert Ziegler modular system for easy routine synthesis of [{sup 11}C]choline, [{sup 11}C]methionine and [{sup 11}C]acetate using components that account for straightforward scaling up and upgrades.

  10. F-18 fluoride positron emission tomography-computed tomography for detecting atherosclerotic plaques

    Energy Technology Data Exchange (ETDEWEB)

    Kang, Won Jun [Dept. of Nuclear Medicine, Severance Hospital, Yonsei University College of Medicine, Seoul (Korea, Republic of)

    2015-12-15

    A large number of major cardiovascular events occur in patients due to minimal or some lumen narrowing of the coronary artery. Recent biological studies have shown that the biological composition or vulnerability of the plaque is more critical for plaque rupture compared to the degree of stenosis. To overcome the limitations of anatomical images, molecular imaging techniques have been suggested as promising imaging tools in various fields. F-18 fluorodeoxyglucose (FDG), which is widely used in the field of oncology, is an example of molecular probes used in atherosclerotic plaque evaluation. FDG is a marker of plaque macrophage glucose utilization and inflammation, which is a prominent characteristic of vulnerable plaque. Recently, F-18 fluoride has been used to visualize vulnerable plaque in clinical studies. F-18 fluoride accumulates in regions of active microcalcification, which is normally observed during the early stages of plaque formation. More studies are warranted on the accumulation of F-18 fluoride and plaque formation/vulnerability; however, due to high specific accumulation, low background activity, and easy accessibility, F-18 fluoride is emerging as a promising non-invasive imaging probe to detect vulnerable plaque.

  11. The Clinical Utility of Rectal Gas Distension F-18 FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Jin Suk; Lim, Seok Tae; Jeong, Young Jin; Kim, Dong Wook; Jeong, Hwan Jeong; Sohn, Myung Hee [Chonbuk National University Medical School and Hospital, Jeonju (Korea, Republic of)

    2009-12-15

    The aim of this study was to evaluate the clinical value of rectal gas distension F-18 FDG PET/CT imaging for the differentiation of the rectal focal uptake lesions. Twenty four patients (M:F=11:13, Age 62.8{+-}12.4 years) underwent rectal gas distension F-18 FDG PET/CT, prospectively: initial image at 50-60 min after the intravenous injection of F-18 FDG and rectal distension image after the infusion of air through the anus. Focally increased uptake lesions on initial images but disappeared on rectal distension images defined a physiological uptake. For the differential evaluation of persistent focal uptake lesions on rectal distension images, colonoscopy and histopathologic examination were performed. Among the 24 patients, 27 lesions of focal rectal uptake were detected on initial images of F-18 FDG PET/CT. Of these, 7 lesions were able to judge with physiological uptake because the focal increased uptake disappeared from rectal distension image. Remaining 3 lesions were non-rectal lesions (2 lesions: rectovesical space, 1 lesion: uterine myoma). Among 17 lesions which was showed persistent increased uptake in rectal distension image, 15 lesions were confirmed as the malignant tumor (SUVmax=15.9{+-}6.8) and 2 lesions were confirmed as the benign lesions including adenoma and inflammatory disease. The rectal distension F-18 FDG PET/CT imaging could be an important noninvasive method for the differentiation of malignant and benign focal rectal uptake lesions including physiologic uptake.

  12. Design, construction and testing of a low-cost automated (68)Gallium-labeling synthesis unit for clinical use.

    Science.gov (United States)

    Heidari, Pedram; Szretter, Alicia; Rushford, Laura E; Stevens, Maria; Collier, Lee; Sore, Judit; Hooker, Jacob; Mahmood, Umar

    2016-01-01

    The interest in (68)Gallium labeled PET probes continues to increase around the world. Widespread use in Europe and Asia has led to great interest for use at numerous sites in the US. One barrier to entry is the cost of the automated synthesis units for relatively simple labeling procedures. We describe the construction and testing of a relatively low-cost automated (68)Ga-labeling unit for human-use. We provide a guide for construction, including part lists and synthesis timelists to facilitate local implementation. Such inexpensive systems could help increase use around the globe and in the US in particular by removing one of the barriers to greater widespread availability. The developed automated synthesis unit reproducibly synthesized (68)Ga-DOTATOC with average yield of 71 ± 8% and a radiochemical purity ≥ 95% in a synthesis time of 25 ± 1 minutes. Automated product yields are comparable to that of manual synthesis. We demonstrate in-house construction and use of a low-cost automated synthesis unit for labeling of DOTATOC and similar peptides with (68)Gallium.

  13. Primary Malignant Peritoneal Mesothelioma Mimicking Peritoneal Carcinomatosis on F-18 FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Jin Suk; Lim, Seok Tae; Jeong, Young Jin; Kim, Dong Wook; Jeong, Hwan Jeong; Sohn, Myung Hee [Chonbuk National University Medical School and Hospital, Jeonju (Korea, Republic of)

    2009-08-15

    Malignant mesothelioma of the peritoneum is a rare neoplasm with a rapidly fatal course. The tumour arises from the mesothelial cells lining the pleura and peritoneum or, rarely, in the pericardium or tunica vaginalis. This neoplasm is characterized by being difficult to diagnose, having a rapid evolution and a poor response to therapy. Mesothelioma is very glucose avid, and malignant pleural mesothelioma has been reported concerning the utility of F-18 FDG PET or PET/CT. But little has been known about the imaging finding of malignant peritoneal mesothelioma on F-18 FDG PET/CT. We report a case of malignant peritoneal mesothelioma mimicking peritoneal carcinomatosis of F-18 FDG PET/CT.

  14. Retroperitoneal Pleomorphic Lipo sarcoma Mimicking Adrenal Cancer in F-18 FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Yoon, Minki; Kim, Seogjoon [Good Samaritan Hospital, Pohang (Korea, Republic of)

    2010-09-15

    Lipo sarcoma is the second most common type of soft tissue sarcoma, but pleomorphic lipo sarcoma is the least common subtype. We present the case of a 42-year-old man who had experienced intermittent left flank pain for a month. A large soft-tissue mass was detected by ultrasonography in a local clinic, and he was referred for further evaluation. Positron emission tomography/computed tomography (PET/CT) with F-18 fluoro-2-deoxy-D-glucose (F-18 FDG) showed intense uptake in the retroperitoneal mass, which mimicked an adrenal cancer. The patient underwent left radical nephroadrenalectomy, and the tumor was revealed to be a pleomorphic lipo sarcoma upon pathological examination. When there is a large retroperitoneal mass with intense F-18 FDG activity, the possibility of a pleomorphic lipo sarcoma should be considered.

  15. Growing cardiac hemangioma on serial F18 FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Jeong, Young Jin; Yoon, Hyun Jin; Kang, Do Young [Dong A Univ. Medical Center, Busan (Korea, Republic of)

    2012-09-15

    Cardiac hemangiomas are extremely rare, benign tumors, which can occur anywhere in the heart. Symptoms are variable according to the size, extension and tumor location, but most cases are asymptomatic and are detected incidentally. They may grow, remain stable and regress; therefore, the natural course of the tumors is unpredictable. Diagnosis mainly depends upon echocardiography, CT, MRI and angiography. Reports of detection by F18 FDG PET/CT are very limited. We report a case of cardiac hemangioma attached to the right ventricle, compressing the ventricle. It was revealed incidentally on F18 FDG PET/CT for routine evaluation of thyroid cancer. During two serial F18 FDG PET/CTs, it grew from 2.8cm to 4.0cm with mild FDG uptake. After surgery, the patient remained stable without any complications.

  16. The synthesis of 5-(1- sup 11 C)ethyl barbiturates from labelled malonic esters

    Energy Technology Data Exchange (ETDEWEB)

    Gee, A.; Laangstroem, B. (Uppsala Univ. (Sweden). Dept. of Organic Chemistry)

    1991-01-01

    The synthesis of ({sup 11}C)phenobarbital, ({sup 11}C)pentobarbital and({sup 11}C)amobarbital labelled in the 5-(1-{sup 11}C)ethyl position is reported. The malonic esters R- CH(CO{sub 2}Et){sub 2} R phenyl-, 1-methylbutyl-, and 3- methylbutyl- were alkylated with (1-{sup 11}C)ethyl iodide prepared from ({sup 11}C)carbon dioxide. Ring closure of the 2-(1-{sup 11}C)ethyl-labelled malonic esters with urea afforded 5-(1-{sup 11}C)ethyl-phenobarbital,-phenobarbital, -pentobarbital and -amobarbital synthesis times of 42-47 min, counted from ({sup 11}C) carbon dioxide. In typical syntheses starting with 3 GBq pentobarbitol and (81 mCi) ({sup 11}C)carbon dioxide, 150-215 MBq (4-6 mCi) were produced in 25-30% decay corrected -amobarbital radiochemical yields with radiochemical purities greater than 98%. (author).

  17. Synthesis of 1-/sup 11/C-labelled ethyl, propyl, butyl and isobutyl iodides and examples of alkylation reactions

    Energy Technology Data Exchange (ETDEWEB)

    Laangstroem, B.; Antoni, G.; Gullberg, P.; Halldin, C.; Naagren, K.; Rimland, A.; Svaerd, H.

    1986-01-01

    New /sup 11/C-labelled precursors (1-/sup 11/C)ethyl,(1-/sup 11/C)propyl, (1-/sup 11/C)butyl, and (1-/sup 11/C)isobutyl iodides have been prepared by a 3-step reaction route using a one-pot system. The labelled iodides were obtained in 20-55% radiochemical yields and 65-95% radiochemical purities, with a total time for synthesis of the order of 10-14 min. The labelled iodides have been used in alkylation reactions with nitrogen, oxygen and carbon nucleophiles. The nitrogen alkylation reactions are exemplified by the synthesis of the analgetics N-(1-/sup 11/C-ethyl)iodocaine and N-(1-/sup 11/C-butyl) bupivacaine. The synthesis of 3-nitrophenyl(1-/sup 11/C)propyl ether is also presented in this paper as an example of an oxygen alkylation.

  18. 1,2-Fucosyllactose Does Not Improve Intestinal Function or Prevent Escherichia coli F18 Diarrhea in Newborn Pigs

    DEFF Research Database (Denmark)

    Cilieborg, Malene Skovsted; Sangild, Per Torp; Jensen, Michael Ladegaard

    2017-01-01

     = 24) without (control) or with inoculation of enterotoxigenic Escherichia coli F18 (7.5 × 1010/day for 8 days) fed either no (F18) or 10 g/L 2′-FL (2FL-F18). Results: In vitro studies revealed decreased pathogen adhesion to intestinal epithelial cells with 2′-FL (5 g/L; P ... of mucosa and activities of some brush border enzymes in the proximal small intestine. In situ abundance of α-1,2-fucose and E coli was similar between groups, whereas sequencing showed higher abundance of Enterobacteriaceae in F18, Enterococcus in control and Lachnospiraceae in 2FL-F18 pigs. Conclusions: 2......′-FL inhibited in vitro adhesion of E coli F18 to epithelial cells, but had limited effects on diarrhea and mucosal health in newborn pigs challenged with E coli F18...

  19. The synthesis of Org 3770 labelled with sup 3 H, sup 13 C and sup 14 C. [Antidepressant

    Energy Technology Data Exchange (ETDEWEB)

    Kaspersen, F.M.; Rooij, F.A.M. van; Sperling, E.G.M.; Wieringa, J.H. (Organon International BV, Oss (Netherlands))

    1989-09-01

    The syntheses of 1,2,3,4,10,14b-hexahydro-2-methylpyrazino(2,1-a)pyrido(2,3-c)(2)benazepine (Org 3770) labelled with {sup 3}H (and {sup 2}H), {sup 13}C and {sup 14}C are described. Tritiated Org 3770 was prepared either by exchange under alkaline conditions with tritiated water or catalytic reductive dehalogenation of a chloro analogue with {sup 3}H{sub 2}. {sup 13}C-labelled material was obtained in a seven-step synthesis starting from {sup 13}C-labelled benzene whereas {sup 14}C-Org 3770 was prepared in a three-step synthesis starting with {sup 14}CO{sub 2}. All labelled compounds were analyzed by TLC, HPLC, MS and NMR. (author).

  20. NaF18-PET/CT imaging of second hyperparathyroidism

    Energy Technology Data Exchange (ETDEWEB)

    Win, Aung Zaw; Aparici, Carina Mari [San Francisco VA Medical Center, San Franciso (United States)

    2015-12-15

    The patient was a 59-year-old man with a history of hypertension and end-stage renal disease for 14 years. An NaF-18 positron emission tomography/CT bone scan was ordered to rule out osteosarcoma or other possible bone malignancies. A lesion representing a brown tumor was observed on the left femoral shaft. The incidence of ESRD is about 400 cases per million in the United States and it has risen fastest in older individuals. This is the second paper to report the use of NaF18-PET/CT to image secondary hyperparathyroidism, osteomalacia, mixed renal ostedystrophy and adyanmic bone disease.

  1. Factors Associated with Diffusely Increased Splenic F-18 FDG Uptake in Patients with Cholangiocarcinoma

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Keunyoung; Kim, Seongjang; Kim, Injoo; Kim, Dong Uk; Kim, Heeyoung; Kim, Sojung; Ahn, Sang Hyun [Pusan National Univ. Hospital, Busan (Korea, Republic of)

    2014-06-15

    Although diffuse splenic {sup 18}F-fluorodeoxyglucose (F-18 FDG) uptake exceeding hepatic activity, is considered abnormal, its clinical significance is rarely discussed in the literature. The aim of this study was to determine the contributing factors causing diffusely increased splenic FDG uptake in patients with cholangiocarcinoma. From January 2010 to March 2013, 140 patients (84 men, 56 women) were enrolled in this study. All patients had been diagnosed with cholangiocarcinoma and underwent F-18 FDG positron emission tomography/computed tomography (PET/CT) for the pretreatment staging work up. Clinical records were reviewed retrospectively. Various hematological parameters, C-reactive protein (CRP) level, CEA, CA19-9, pancreatic enzymes and liver function tests were conducted within 2 days after the F-18 FDG PET/CT study. Diffuse splenic uptake was observed in 23 patients (16.4%). Of those, 19 patients (82.6%) underwent endoscopic retrograde cholangiopancreastography (ERCP) 7 days before F-18 FDG PET/CT. The CRP level (p <0.001) and white blood cell count (p =0.023) were significantly higher in the group of patients with diffuse splenic FDG uptake. The hemoglobin (p <0.001) and the hematocrit (p <0.001) were significantly lower in patients with diffuse splenic FDG uptake. Pancreatic enzymes, liver function test results, and tumor markers were not significantly different between the patients who did or did not have diffusely increased splenic FDG uptake. The significant factors for diffuse splenic F-18 FDG uptake exceeding hepatic F-18 FDG uptake on multivariate analysis included: performing ERCP before F-18 FDG PET-CT (odds ratio [OR], 77.510; 95% CI, 7.624-132.105), and the presence of leukocytosis (OR, 12.436; 95% CI, 2.438-63.445) or anemia (OR, 1.211; 95% CI, 1.051-1.871). In conclusion, our study demonstrated that concurrent inflammation could be associated with diffusely increased splenic FDG uptake. We suggest that performing ERCP before F-18 FDG PET

  2. Chorea in systemic lupus erythematosus: evidence for bilateral putaminal hypermetabolism on F-18 FDG PET

    Energy Technology Data Exchange (ETDEWEB)

    Seo, Wook Jang; Chung, Son Mi; Koh, Su Jin; Lee, Chang Keun; Yoo, Bin; Moon, Hee Bom [College of Medicine, Ulsan Univ., Seoul (Korea, Republic of); Kim, Jae Seung; Im, Joo Hyuk [Asan Medical Center, Seoul (Korea, Republic of)

    2003-10-01

    We describe a 54-year-old woman with systemic lupus erythematosus (SLE) who suddenly presented with chorea and had positive antiphospholipid antibodies. F-18 FDG PET showed abnormally increased glucose metabolism in bilateral putamen and primary motor cotex. Tc-99m ECD SPECT also showed abnormally increased regional cerebral blood flow in bilateral putamen. She was treated with corticosteroid and aspirin after which the symptoms improved. Four months later, follow up F-18 FDG PET showed improvement with resolution of hypermetabolism in bilateral putamen. This case suggests that striatal hypermetabolism is associated with chorea in SLE.

  3. Synthesis of deuterium-labeled imipramine using acid-catalyzed exchange reaction

    Energy Technology Data Exchange (ETDEWEB)

    Baba, S.; Furuta, T.; Sasaki, Y.; Kasuya, Y. (Tokyo Coll. of Pharmacy (Japan))

    1985-02-01

    Synthesis of three forms of selectively deuterated imipramine with high isotopic purity using acid catalyzed hydrogen-deuterium exchange reaction is described. Deuterated imipramine labeled at the positions of 2,4,6 and 8 (IP-d/sub 4/(I)) was prepared directly by heating imipramine in 10% DC1-D/sub 2/O at 80/sup 0/ for 8hr. Imipramine labeled at all of the eight aromatic positions (IP-d/sub 8/) was synthesized from iminodibenzyl-1,2,3,4,6,7,8,9-d/sub 8/ which was prepared by treating iminodibenzyl (IDB) in 37% DC1-D/sub 2/O at 160/sup 0/ for 24hr. An imipramine labeled at the positions of 1,3,7 and 9 (IP-d/sub 4/(II)) was obtained by ''back-exchange'' of IP-d/sub 8/ under the protio condition according to the exchange procedure of IP-d/sub 4/(I).

  4. Considerations and protocols for the synthesis of custom protein labeling probes.

    Science.gov (United States)

    Corrêa, Ivan R

    2015-01-01

    Chemists and biologists have long recognized small molecule probes as powerful tools for functional genomics and proteomics studies. The possibility of specifically attaching chemical probes to individual proteins with spatial and temporal resolution has greatly improved our ability to visualize and characterize proteins in their native environment. The continued development of novel molecular probes for protein labeling is, therefore, of fundamental importance to gain new insights into biological processes in living cells and organisms. Several excellent approaches for the site-specific labeling of fusion proteins with chemical probes exist. Herein I discuss the design and generation of chemical probes for the SNAP-tag and CLIP-tag systems. The first part of this chapter is dedicated to reviewing the principles of the SNAP-tag technology, followed by a section dedicated to the development of chemical probes for unique applications, such as super-resolution imaging, protein trafficking and recycling, protein-protein interactions, and biomolecular sensing. The last part of the chapter contains experimental protocols and technical notes for the synthesis of selected SNAP-tag substrates and labeling of SNAP-tag fusion proteins in vitro and in living cells.

  5. CONVERGENT SYNTHESIS AND EVALUATION OF 18F-LABELED AZULENIC COX2 PROBES FOR CANCER IMAGING

    Directory of Open Access Journals (Sweden)

    Donald D. Nolting

    2013-01-01

    Full Text Available The overall objectives of this research are to (i develop azulene-based PET probes and (ii image COX2 as a potential biomarker of breast cancer. Several lines of research have demonstrated that COX2 is overexpressed in breast cancer and that its presence correlates with poor prognoses. While other studies have reported that COX2 inhibition can be modulated and used beneficially as a chemopreventive strategy in cancer, no viable mechanism for achieving that approach has yet been developed. This shortfall could be circumvented through in vivo imaging of COX2 activity, particularly using sensitive imaging techniques such as PET. Toward that goal, our laboratory focuses on the development of novel 18F-labled COX2 probes. We began the synthesis of the probes by transforming tropolone into a lactone, which was subjected to an [8+2] cycloaddition reaction to yield 2-methylazulene as the core ring of the probe. After exploring numerous synthetic routes, the final target molecule and precursor PET compounds were prepared successfully using convergent synthesis. Conventional 18F labeling methods caused precursor decomposition, which prompted us to hypothesize that the acidic protons of the methylene moiety between the azulene and thiazole rings were readily abstracted by a strong base such as potassium carbonate. Ultimately, this caused the precursors to disintegrate. This observation was supported after successfully using an 18F labeling strategy that employed a much milder phosphate buffer. The 18F-labeled COX2 probe was tested in a breast cancer xenograft mouse model. The data obtained via successive whole-body PET/CT scans indicated probe accumulation and retention in the tumor. Overall, the probe was stable in vivo and no defluorination was observed. A biodistribution study and Western blot analysis corroborate with the imaging data. In conclusion, this novel COX2 PET probe was shown to be a promising agent for cancer imaging and deserves further

  6. Fluorescent-labeled ligands for the benzodiazepine receptor - Part 1 : Synthesis and characterization of fluorescent-labeled benzodiazepines

    NARCIS (Netherlands)

    Janssen, MJ; Hulst, R; Kellogg, RM; Hendriks, MMWB; Ensing, K; De Zeeuw, RA

    2000-01-01

    Because radioactive labeled ligands in receptor assays have several disadvantages, we synthesized a number of fluorescent-labeled benzodiazepines. Several fluorophores were attached at different positions of 1,4-benzodiazepine molecules in order to assess the impact of the fluorophores and their cou

  7. Hepatosplenic Cat-Scratch Disease in Children and the Positive Contribution of F-18-FDG Imaging

    NARCIS (Netherlands)

    Kraft, Karianne E.; Doedens, Rienus A.; Slart, Riemer H. J. A.

    2015-01-01

    Two patients were referred to our hospital because of suspected malignancy. In patient 1, a 4-year-old boy, a F-18-FDG PET scan showed an enlarged liver with multiple FDG-positive nodular lesions. In patient 2, a 16-year-old boy, a FDG PET-(low-dose) CT showed an enlarged liver and spleen with multi

  8. [F-18] FDG-PET/CT parameters as predictors of outcome in inoperable NSCLC patients

    Directory of Open Access Journals (Sweden)

    Nappi Antonio

    2015-12-01

    Full Text Available Background. We evaluated the prognostic significance of standardized uptake value (SUVmax, metabolic tumour volume (MTV, and total lesion glycolysis (TLG in [F-18] FDG PET/CT findings in patients with inoperable non-small-cell lung cancer (NSCLC.

  9. Nanobody mediated inhibition of attachment of F18 Fimbriae expressing Escherichia coli.

    Directory of Open Access Journals (Sweden)

    Kristof Moonens

    Full Text Available Post-weaning diarrhea and edema disease caused by F18 fimbriated E. coli are important diseases in newly weaned piglets and lead to severe production losses in farming industry. Protective treatments against these infections have thus far limited efficacy. In this study we generated nanobodies directed against the lectin domain of the F18 fimbrial adhesin FedF and showed in an in vitro adherence assay that four unique nanobodies inhibit the attachment of F18 fimbriated E. coli bacteria to piglet enterocytes. Crystallization of the FedF lectin domain with the most potent inhibitory nanobodies revealed their mechanism of action. These either competed with the binding of the blood group antigen receptor on the FedF surface or induced a conformational change in which the CDR3 region of the nanobody displaces the D″-E loop adjacent to the binding site. This D″-E loop was previously shown to be required for the interaction between F18 fimbriated bacteria and blood group antigen receptors in a membrane context. This work demonstrates the feasibility of inhibiting the attachment of fimbriated pathogens by employing nanobodies directed against the adhesin domain.

  10. N-[F-18]-FLUOROALKYLATION OF NORAPORPHINES - MICROWAVE VERSUS THERMAL-TREATMENT

    NARCIS (Netherlands)

    ZIJLSTRA, S; DEGROOT, TJ; KOK, LP; VISSER, GM; VAALBURG, W

    1995-01-01

    A comparable study of microwave versus thermal heating is described for the N-[F-18]-fluoroalkylation of noraporphines. As compared to thermal treatment, different products were obtained during microwave treatment. Thermal treatment resulted in the loss of the protection of the catechol functionalit

  11. Comparison of C-11-methionine PET and F-18-fluorodeoxyglucose PET in differentiated thyroid cancer

    NARCIS (Netherlands)

    Phan, Ha T. T.; Jager, Pieter L.; Plukker, John T. M.; Wolffenbuttel, Bruce H. R.; Dierckx, Rudi A.; Links, Thera P.

    2008-01-01

    Background The purpose of this prospective study is to evaluate the possibility of C-11-methionine (Met) PET compared with F-18-fluorodeoxyglucose (FDG) PET for the detection of recurrent or metastatic disease in patients with differentiated thyroid cancer (DTC). Materials and methods Twenty patient

  12. Impact of [F-18]fluorodeoxyglucose positron emission tomography on surgical management of melanoma patients

    NARCIS (Netherlands)

    Bastiaannet, E; Oyen, WJG; Meijer, S; Hoekstra, OS; Wobbes, T; Jager, PL; Hoekstra, HJ

    Background: Several studies have shown adequate sensitivity and specificity of [F-18]fluorodeoxyglucose positron emission tomography (FDG-PET) for the detection of metastases from melanoma, but few have addressed its impact on treatment. The aim of this retrospective study was to assess the impact

  13. Predictive value of early F-18-fluoro-deoxyglucose positron emission tomography in chemosensitive relapsed lymphoma

    NARCIS (Netherlands)

    Schot, B; van Imhoff, G; Pruim, J; Sluiter, W; Vaalburg, W; Vellenga, E

    2003-01-01

    F-18-fluoro-deoxyglucose (FDG) positron emission tomography (PET) might be a better tool than computerized tomography (CT) in predicting long-term treatment outcome in patients with relapsed chemosensitive lymphoma who are candidates for autologous stem cell transplantation (ASCT). We studied patien

  14. Specificity of synthesis and analysis of molecules labelled with stable isotopes; Specificite des syntheses et analyses des molecules marquees avec les isotopes stables

    Energy Technology Data Exchange (ETDEWEB)

    Noel, J.P. [CEA Centre d`Etudes de Saclay, 91 - Gif-sur-Yvette (France). Dept. de Biologie Cellulaire et Moleculaire

    1994-12-31

    The various specificities of synthesis with stable isotopes are: unusual raw materials and use of precursors, possibility of producing several isotopomers corresponding to the same chemical compound, involvement of a reaction mechanism in labelling. As a matter of fact, isotopic synthesis are generally more complex than synthesis of non-labelled products. When preparing labelled molecules, it is of importance to avoid any isotopic dilution. Chemical purity for labelled molecules is controlled by various chromatographic techniques and isotopic analysis are carried out by nuclear magnetic resonance and mass spectrometry. 9 figs., 2 tabs.

  15. Imaging of accidental contamination with F-18-solution; a quick trouble-shooting procedure

    Directory of Open Access Journals (Sweden)

    Kalevi Kairemo

    2016-01-01

    Full Text Available To the best of our knowledge, imaging of accidental exposure to radioactive fluorine-18 (F-18 due to liquid spill has not been described earlier in the scientific literature. The short half-life of F-18 (t½=110 min, current radiation safety requirements, and Good Manufacturing Practice (GMP regulations on radiopharmaceuticals have restrained the occurrence of these incidents. The possibility of investigating this type of incidents by gamma and positron imaging is also quite limited. Additionally, a quick and precise analysis of radiochemical contamination is cumbersome and sometimes challenging if the spills of radioactive materials are low in activity. Herein, we report a case of accidental F-18 contamination in a service person during a routine cyclotron maintenance procedure. During target replacement, liquid F-18 was spilled on the person responsible for the maintenance. The activities of spills were immediately measured using contamination detectors, and the photon spectrum of contaminated clothes was assessed through gamma spectroscopy. Despite protective clothing, some skin areas were contaminated, which were then thoroughly washed. Later on, these areas were imaged, using positron emission tomography (PET, and a gamma camera (including spectroscopy. Two contaminated skin areas were located on the hand (9.7 and 14.7 cm2, respectively, which showed very low activities (19.0 and 22.8 kBq respectively at the time of incident. Based on the photon spectra, F-18 was confirmed as the main present radionuclide. PET imaging demonstrated the shape of these contaminated hot spots. However, the measured activities were very low due to the use of protective clothing. With prompt action and use of proper equipments at the time of incident, minimal radionuclide activities and their locations could be thoroughly analyzed. The cumulative skin doses of the contaminated regions were calculated at 1.52 and 2.00 mSv, respectively. In the follow-up, no skin

  16. Pathological correlations of [F-18]-AV-1451 imaging in non-alzheimer tauopathies.

    Science.gov (United States)

    Marquié, Marta; Normandin, Marc D; Meltzer, Avery C; Siao Tick Chong, Michael; Andrea, Nicolas V; Antón-Fernández, Alejandro; Klunk, William E; Mathis, Chester A; Ikonomovic, Milos D; Debnath, Manik; Bien, Elizabeth A; Vanderburg, Charles R; Costantino, Isabel; Makaretz, Sara; DeVos, Sarah L; Oakley, Derek H; Gomperts, Stephen N; Growdon, John H; Domoto-Reilly, Kimiko; Lucente, Diane; Dickerson, Bradford C; Frosch, Matthew P; Hyman, Bradley T; Johnson, Keith A; Gómez-Isla, Teresa

    2017-01-01

    Recent studies have shown that positron emission tomography (PET) tracer AV-1451 exhibits high binding affinity for paired helical filament (PHF)-tau pathology in Alzheimer's brains. However, the ability of this ligand to bind to tau lesions in other tauopathies remains controversial. Our goal was to examine the correlation of in vivo and postmortem AV-1451 binding patterns in three autopsy-confirmed non-Alzheimer tauopathy cases. We quantified in vivo retention of [F-18]-AV-1451 and performed autoradiography, [H-3]-AV-1451 binding assays, and quantitative tau measurements in postmortem brain samples from two progressive supranuclear palsy (PSP) cases and a MAPT P301L mutation carrier. They all underwent [F-18]-AV-1451 PET imaging before death. The three subjects exhibited [F-18]-AV-1451 in vivo retention predominantly in basal ganglia and midbrain. Neuropathological examination confirmed the PSP diagnosis in the first two subjects; the MAPT P301L mutation carrier had an atypical tauopathy characterized by grain-like tau-containing neurites in gray and white matter with heaviest burden in basal ganglia. In all three cases, autoradiography failed to show detectable [F-18]-AV-1451 binding in multiple brain regions examined, with the exception of entorhinal cortex (reflecting incidental age-related neurofibrillary tangles) and neuromelanin-containing neurons in the substantia nigra (off-target binding). The lack of a consistent significant correlation between in vivo [F-18]-AV-1541 retention and postmortem in vitro binding and tau measures in these cases suggests that this ligand has low affinity for tau lesions primarily made of straight tau filaments. AV-1451 may have limited utility for in vivo selective and reliable detection of tau aggregates in these non-Alzheimer tauopathies. ANN NEUROL 2017;81:117-128. © 2016 American Neurological Association.

  17. F-18 FDG PET scan findings in patients with pulmonary involvement in the hypereosinophilic syndrome

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Jae Hoon; Kim, Tae Hoon; Yun, Mi Jin [College of Medicine, Yonsei University, Seoul (Korea, Republic of)] (and others)

    2005-08-15

    Hypereosinophilic syndrome (HES) is an infiltrative disease of eosinophils affecting multiple organs including the lung. F-18 2-fluoro-2-deoxyglucose (F-18 FDG) may accumulate at sites of inflammation or infection, making interpretation of whole body PET scan difficult in patients with cancer. This study was to evaluate the PET findings of HES with lung involvement and to find out differential PET features between lung malignancy and HES with lung involvement. F-18 FDG PET and low dose chest CT scan was performed for screening of lung cancer. Eight patients who showed ground-glass attenuation (GGA) and consolidation on chest CT scan with peripheral blood eosinophilia were included in this study. The patients with history of parasite infection, allergy and collagen vascular disease were excluded. CT features and FDG PET findings were meticulously evaluated for the distribution of GGA and consolidation and nodules on CT scan and mean and maximal SUV of abnormalities depicted on F-18 FDG PET scan. In eight patients, follow-up chest CT scan and FDG PET scan were done one or two weeks after initial study. F-18 FDG PET scan identified metabolically active lesions in seven out of eight patients. Maximal SUV was ranged from 2.8 to 10.6 and mean SUV was ranged from 2.2 to 7.2. Remaining one patient had maximal SUV of 1.3. On follow-up FDG PET scan taken on from one to four weeks later showed decreased degree of initially noted FDG uptakes or migration of previously noted abnormal FDG uptakes. Lung involvement in the HES might be identified as abnormal uptake foci on FDG PET scan mimicking lung cancer. Follow-up FDG PET and CT scan for the identification of migration or resolution of abnormalities and decrement of SUV would be of help for the differentiation between lung cancer and HES with lung involvement.

  18. Synthesis of Isotope labeled Trichlorfon-methoxyl-D6 and Dichlorophos-methoxyl-D6

    Directory of Open Access Journals (Sweden)

    YANG Wei-cheng1;LV Jing1;QI Qing-rui2;SHENG Li-yan1;LI Mei-hua1;YANG Chao1;LUO Yong1

    2014-02-01

    Full Text Available The efficient synthesis of two labeled standards trichlorfon-methoxyl-D6 and dichlorophos- methoxyl-D6 with CD3OD as the precursor were presented. Esterification of phosphorus trichloride with CD3OD provided dimethyl phosphate-methoxyl-D6, which was used to condense with trichloroaldehyde to give trichlorfon-methoxyl-D6. Ttrichlorfon-methoxyl-D6 was further converted to dichlorophos-methoxyl-D6 by alkaline hydrolysis and rearrangement. The yields of trichlorfon-methoxyl-D6 and Dichlorophos-methoxyl-D6 were 57.7 % and 47.3% respectively based on CD3OD consumed. Both products were characterized by HPLC, MS, and NMR to be target compounds. Their chemical purities and isotopic enrichment were higher than 98.0%. The above compounds could be used as internal standards in the food safety field.

  19. Synthesis and preliminary biological evaluation of a technetium-99m labeled thymidine analog

    Institute of Scientific and Technical Information of China (English)

    Chun Xiong Lu; Zheng Wu Wang; Quan Fu Jiang; Jie Tang; Cheng Tan; Jian Kang Zhang

    2011-01-01

    The synthesis and labeling of 99mTc-N3-{N'-[2-sulfanyl-ethylamino)acetyl]-2-aminoethyl-sulfanyl-l-hexanamide}thymidine (99mTc-NHT) were studied. In the presence of sodium glucoheptonate (GH) and ethylene diamine tetraacetic acid (EDTA), 99mTc-NHT was obtained by using bisaminoethanethiol (N2S2) as a bifunctional coupling agent. The radiochemical purity of the 99mTc-NHT was over 95%. Biodistribution of 99mTc-NHT was performed in hepatoma HepA tumor-bearing mice. At 2 h p.i., the ratios of tumor-to-muscle, tumor-to-bone and tumor-to-blood were 4.41 ± 0.32, 2.45 ± 0.24 and 1.51 ±0.18, respectively.

  20. Synthesis and applications of selectively {sup 13}C-labeled RNA

    Energy Technology Data Exchange (ETDEWEB)

    SantaLucia, J. Jr.; Shen, L.X.; Lewis, H.; Cai, Z.; Tinoci, I. Jr. [Univ. of California, Berkeley, CA (United States)

    1994-12-01

    Spectral overlap is a substantial problem in NMR studies of RNA molecules >30 nucleotides. To overcome this difficulty, we synthesized selectively {sup 13}C-labeled RNAs and adapted several isotope-edited two- and three-dimensional NMR experiments originally developed for protein studies. We optimized protocols for synthesis of multi-gram quantities of CTP, UTp, ATP, and GTP using a combination of synthetic organic and enzymatic methods. Uracil is prepared in 40 to 50% yield from {sup 13}C-cyanide in two steps. Using acetyl- tribenzoyl-ribose and standard chemistry uracil is then attached to the sugar (90% yield). The tribenzoyl-uridine intermediate is converted into uridine or cytidine quantitatively, depending on the deblocking protocol. Labeled purines are synthesized using simple pyrimidine precursors and reacting with {sup 13}C-formic acid (80% yield). Purine nucleosides are then synthesized using uridine phosphorylase and purine nucleoside phosphorylase. The nucleosides were converted to NMPs by treatment with POC1{sub 3} in triethylphosphate. We converted NMPs to NTPs by standard enzymatic methods. Selectively labeled RNAs were synthesized by run-off transcription using {sup 13}C-labeled NTPs. Several different strategies help solve over-lap problems in larger RNAs. Isotope-edited two-dimensional NMR experiments such as {omega}1-1/2 X-filtered NOESY simplify NMR spectra by dividing the normal NOESY spectrum into two subspectra-one involving NOEs from protons bound to {sup 12}C and one from protons bound to {sup 13}C. For example, we labeled A and U residues of a 34-nucleotide pseudoknot, and the {sup 12}C subspectrum of the 1/2 X-filtered NOESY contained NOEs only from G and C residues (along with adenine 2H); the {sup 13}C subspectrum contained NOEs only from A and U residues. Each subspectrum has less overlap than the NOESY of an unlabeled sample; the editing strategy allows each resonance to be identified by residue type (A, C, G, or U).

  1. Synthesis and application of water-soluble, photoswitchable cyanine dyes for bioorthogonal labeling of cell-surface carbohydrates.

    Science.gov (United States)

    Mertsch, Alexander; Letschert, Sebastian; Memmel, Elisabeth; Sauer, Markus; Seibel, Jürgen

    2016-09-01

    The synthesis of cyanine dyes addressing absorption wavelengths at 550 and 648 nm is reported. Alkyne functionalized dyes were used for bioorthogonal click reactions by labeling of metabolically incorporated sugar-azides on the surface of living neuroblastoma cells, which were applied to direct stochastic optical reconstruction microscopy (dSTORM) for the visualization of cell-surface glycans in the nm-range.

  2. F-18-FDG-PET for differential diagnosis of pleural processes; F-18-FDG-PET zur Primaerdiagnostik und Dignitaetsbeurteilung pleuraler Prozesse

    Energy Technology Data Exchange (ETDEWEB)

    Buchmann, I.; Guhlmann, C.A.; Schirrmeister, H.; Kotzerke, J.; Buck, A.; Reske, S.N. [Ulm Univ. (Germany). Abt. Nuklearmedizin; Elsner, K. [Ulm Univ. (DE). Abt. Radiologie 2 (Strahlentherapie); Gfroerer, W. [Universitaetsklinik Ulm (Germany). Abt. fuer Allgemeinchirurgie

    1999-07-01

    Purpose: Positron emission tomography (PET) with 18-fluorodeoxyglucose (FDG) has been shown to be accurate for differentiating benign from malignant pulmonary lesions. Therefore, we evaluated the capability of FDG-PET in the characterisation of pleural lesions. Patients and methods: PET was performed in thirteen patients with pleural or intrapulmonal tumors (three with additional pleural effusion) and in three patients with aetiologically unclear pleural effusion demonstrated by CT. In all cases the diagnosis was confirmed histologically. The PET-imaging was carried out in fasted patients 50 minutes after injection of 400-670 MBq F-18-FDG without attenuation correction. Results: Twelve patients were found to have pleural or pulmonal malignomas (9 pleural mesotheliomas, 3 bronchogenic adenocarcinoma with carcinomatous pleurisy). Four patients had benign pleural changes (1 fibroma, 1 tuberculous pleurisy, 1 pleural fibrosis, 1 empyema). With FDG-PET, all 12 pleural or intrapulmonal malignomas had high FDG-uptake and were classified correctly. Due to very low or virtually deficient FDG-uptake, four histologically benign lesions were correctly interpreted as nonmalignant. Conclusion: These preliminary results suggest that FDG-PET is accurate in detecting malignant pleural tumors. (orig.) [German] Ziel: Zahlreiche Studien belegen die hohe Treffsicherheit der Positronen-Emissions-Tomographie (PET) mit 2-[F-18]-Fluoro-2-desoxy-D-Glukose (FDG) bei der Dignitaetsbeurteilung nicht-verkalkter Lungenrundherde. Ziel dieser Untersuchung war die Evaluation der Wertigkeit der FDG-PET in der Primaerdiagnostik und Dignitaetsbeurteilung pleuraler Veraenderungen. Patienten/Methode: Dreizehn Patienten mit computertomographisch bekannten pleuralen Raumforderungen, von denen drei zusaetzlich einen Pleuraerguss aufwiesen, sowie drei Patienten mit aetiologisch unklarem Pleuraerguss wurden einer FDG-PET unterzogen. Die PET wurde 50 min nach i.v. Injektion von 400-670 MBq F-18-FDG in

  3. Synthesis of deuterium and tritium labelled m-aminolevamisole and levamisole. [Antiparasitic agents

    Energy Technology Data Exchange (ETDEWEB)

    Sangster, N.C. (Sydney Univ. (Australia). Dept. of Veterinary Pathology); Lacey, E. (Commonwealth Scientific and Industrial Research Organization, Glebe (Australia). McMaster Lab.); Than, C.; Long, M.A. (New South Wales Univ., Kensington (Australia). School of Chemistry)

    1989-09-01

    Levamisole (LEV) is a widely used anti-parasitic agent. In order to characterise the biochemical pharmacology of LEF in parasitic nematodes, ({sup 3}H)LEV and a more active analogue ({sup 3}H)m-aminolevamisole (MAL) have been prepared. Labelling was accomplished by tritiated water exchange of MAL under acid conditions. Multiple site labelling was achieved in the positions ortho and para to the amino group of MAL. Tritiation of MAL HCl in ({sup 3}H){sub 2}O was achieved at 103{sup o}C for 23 h. Crude ({sup 3}H)MAL was diazotised and deaminated to effect the synthesis of ({sup 3}H)LEV. Products of both reactions were purified by preparative h.p.l.c. and characterised by h.p.l.c., t.l.c. and mass spectrometry. (Radiochemical yield was about 15% and purity >90%.) Specific activities of 39 Ci/mmol for ({sup 3}H)MAL and 37 Ci/mmol for ({sup 3}H)LEV were obtained. (author).

  4. Native SILAC: metabolic labeling of proteins in prototroph microorganisms based on lysine synthesis regulation.

    Science.gov (United States)

    Fröhlich, Florian; Christiano, Romain; Walther, Tobias C

    2013-07-01

    Mass spectrometry (MS)-based quantitative proteomics has matured into a methodology able to detect and quantitate essentially all proteins of model microorganisms, allowing for unprecedented depth in systematic protein analyses. The most accurate quantitation approaches currently require lysine auxotrophic strains, which precludes analysis of most existing mutants, strain collections, or commercially important strains (e.g. those used for brewing or for the biotechnological production of metabolites). Here, we used MS-based proteomics to determine the global response of prototrophic yeast and bacteria to exogenous lysine. Unexpectedly, down-regulation of lysine synthesis in the presence of exogenous lysine is achieved via different mechanisms in different yeast strains. In each case, however, lysine in the medium down-regulates its biosynthesis, allowing for metabolic proteome labeling with heavy-isotope-containing lysine. This strategy of native stable isotope labeling by amino acids in cell culture (nSILAC) overcomes the limitations of previous approaches and can be used for the efficient production of protein standards for absolute SILAC quantitation in model microorganisms. As proof of principle, we have used nSILAC to globally analyze yeast proteome changes during salt stress.

  5. Cerebral Toxoplasmosis in a Patient with AIDS on F-18 FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Hae Won; Won, Kyung Sook; Choi, Byung Wook; Zeon, Seok Kil [Keimyung University School of Medicine, Daegu (Korea, Republic of)

    2010-04-15

    The distinction between primary central nervous system (CNS) lymphoma and nonmalignant lesions due to opportunistic infections, in particular cerebral toxoplasmosis, is important because of the different treatments involved. A 32-year-old patient with AIDS was hospitalized for intermittent headaches. Brain magnetic resonance imaging (MRI) showed a small well-enhanced nodular lesion in the right frontal lobe. A fluorine-18 fluorodeoxyglucose (F-18 FDG) position emission tomography (PET)/ computed tomography (CT) scan showed moderate FDG uptake in the nodular lesion of the right frontal lobe. We present a case of cerebral toxoplasmosis in a patient with acquired immunodeficiency syndrome (AIDS) and the usefulness of F-18 FDG PET/CT in the differential diagnosis of the cerebral toxoplasmosis will be discussed.

  6. Giant cell tumor of the rib: Two cases of F-18 FDG PET/CT findings

    Energy Technology Data Exchange (ETDEWEB)

    Park, Hye Lim; Yoo, Le Ryung; Lee, Yeong Joo; Jung, Chan Kwon [Seoul St. Mary' s Hospital, College of MedicineThe Catholic University of Korea, Seoul (Korea, Republic of); Park, Sonya Young Ju [Molecular Imaging Program, Dept. of Radiology, Stanford Hospital and Clinics, Stanford (Korea, Republic of)

    2017-06-15

    We report two cases of giant cell tumor arising from the rib and their F-18 FDG PET/CT findings. The two patients complained of chest wall pain, and large lobulated soft tissue masses with intense FDG uptake were seen on F-18 FDG PET/CT. A malignant tumor such as osteosarcoma or chondrosarcoma was suspected due to the large size of the mass, bony destruction, and intense FDG uptake. En bloc resection was performed and final pathologic results revealed giant cell tumor of the rib. Giant cell tumor of the rib is very rare, and larger lesions with high FDG uptake can be misdiagnosed as an intrathoracic malignancy arising from the rib, pleura, or chest wall.

  7. F18-FDG PET/CT Scanning in Angiosarcoma: Report of Two Cases

    Directory of Open Access Journals (Sweden)

    Emel TOKMAK

    2011-08-01

    Full Text Available Angiosarcomas are uncommon tumors and constitute less than 5% of all soft tissue sarcomas. They are aggressive tumors with poor prognosis, therefore, it is quite important to determine disease extension and detect local recurrence and/or distant metastases for appropriate therapy management. In this paper, we aimed to demonstrate the potential role of 1F18-FDG PET/CT imaging by reporting two cases with angiosarcoma (MIRT 2011;20:63-66

  8. Data Impact of the DMSP F18 SSULI UV Data on the Operational GAIM Model

    Science.gov (United States)

    Dandenault, P. B.; Metzler, C. A.; Nicholas, A. C.; Coker, C.; Budzien, S. A.; Chua, D. H.; Finne, T. T.; Dymond, K.; Walker, P. W.; Schunk, R. W.; Scherliess, L.; Gardner, L. C.

    2011-12-01

    The Naval Research Laboratory (NRL) has developed five ultraviolet remote sensing instruments for the United States Air Force (USAF) Defense Meteorological Satellite Program (DMSP). The DMSP satellites are launched in a near-polar, sun-synchronous orbit at an altitude of approximately 830 km. Each Special Sensor Ultraviolet Limb Imager (SSULI) instrument measures vertical profiles of the natural airglow radiation from atoms, molecules and ions in the upper atmosphere and ionosphere by viewing the earth's limb within a tangent altitude range of approximately 50 km to 750 km. Limb observations are made from the extreme ultraviolet (EUV) to the far ultraviolet (FUV) over the wavelength range of 80 nm to 170 nm, with 1.8 nm resolution. Data products from SSULI observations include nightglow and dayglow Sensor Data Records (SDRs), as well as Environmental Data Records (EDRs) which contain vertical profiles of electron (Ne) densities, N2, O2, O, O+, and Temperature, hmF2, NmF2 and vertical Total Electron Content (TEC). On October 18, 2009, the third SSULI sensor launched from Vandenberg Air Force Base aboard the DMSP F18 spacecraft. The Calibration and Validation of the F18 instrument has completed and the SSULI program is scheduled to go operational at the Air Force Weather Agency (AFWA) in Fall 2011. The SSULI F18 data are ingested by the Global Assimilation of Ionospheric Measurements (GAIM) space weather model, which was developed by Utah State University and has been used operationally at AFWA since February 2006. A brief overview of the SSULI F18 SDR data assimilation process with GAIM is provided and the impact of the SSULI 1356 Å emission on the GAIM model is examined for spring and summer 2011 nightside data in the low-latitude region.

  9. Differential diagnosis of Parkinsonism using dual phase F 18 FP CIT PET imaging

    Energy Technology Data Exchange (ETDEWEB)

    Jin, So Young; Oh, Min Young; Ok, Seung Jun; Oh, Jung Su; Lee, Sang Ju; Chung, Sun Ju; Lee, Chong Sik; Kim, Jae Seung [Univ. of Ulsan, Seoul (Korea, Republic of)

    2012-03-15

    Dopamine transporter (DAT) imaging can demonstrate presynaptic dopaminergic neuronal loss in Parkinson's disease (PD). However, differentiating atypical parkinsonism (APD) from PD is often difficult. We investigated the usefulness of dual phase F 18 FP CIT positron emission tomography (PET) imaging in the differential diagnosis of parkinsonism. Ninety eight subjects [five normal, seven drug induced parkinsonism (DIP), five essential tremor (ET), 24 PD, 20 multiple system atrophy parkinson type (MSA-P), 13 multiple system atrophy cerebellar type (MSA-C), 13 progressive supranuclear palsy (PSP), and 11 dementia with Lewy bodies(DLB)] underwent F 18 FP CIT PET. PET images were acquired at 5 min (early phase) and 3 h (late phase) after F 18 FP CIT administration (185MBq). Regional uptake pattern of cerebral and cerebellar hemispheres was assessed on early phase images, using visual, quantitative, and statistical parametric mapping (SPM) analyses. Striatal DAT binding was normal in normal, ET, DIP, and MSA C groups, but abnormal in PD, MSA P PSP, and DLB groups. No difference was found in regional uptake on early phase images among normal DAT binding groups, except in the MSA C group. Abnormal DAT binding groups showed different regional uptake pattern on early phase images compared with PD in SPM analysis (FDR<0.05). When discriminating APD from PD, visual interpretation of the early phase image showed high diagnostic sensitivity and specificity (75.4% and 100%, respectively). Regarding the ability to distinguish specific APD, sensitivities were 81% for MSA P, 77% for MSA C, 23% for PSP, and 54.5% for DLB. Dual phase F 18 FP CIT PET imaging is useful in demonstrating striatal DAT loss in neurodegenerative parkinsonism, and also in differentiating APD, particularly MSA, from PD.

  10. Normal SUV values measured from NaF18- PET/CT bone scan studies.

    Directory of Open Access Journals (Sweden)

    Aung Zaw Win

    Full Text Available Cancer and metabolic bone diseases can alter the SUV. SUV values have never been measured from healthy skeletons in NaF18-PET/CT bone scans. The primary aim of this study was to measure the SUV values from normal skeletons in NaF18-PET/CT bone scans.A retrospective study was carried out involving NaF18- PET/CT bone scans that were done at our institution between January 2010 to May 2012. Our excluding criteria was patients with abnormal real function and patients with past history of cancer and metabolic bone diseases including but not limited to osteoporosis, osteopenia and Paget's disease. Eleven studies met all the criteria.The average normal SUVmax values from 11 patients were: cervical vertebrae 6.84 (range 4.38-8.64, thoracic vertebrae 7.36 (range 6.99-7.66, lumbar vertebrae 7.27 (range 7.04-7.72, femoral head 2.22 (range 1.1-4.3, humeral head 1.82 (range 1.2-2.9, mid sternum 5.51 (range 2.6-8.1, parietal bone 1.71 (range 1.3-2.4.According to our study, various skeletal sites have different normal SUV values. SUV values can be different between the normal bones and bones with tumor or metabolic bone disease. SUV can be used to quantify NaF-18 PET/CT studies. If the SUV values of the normal skeleton are known, they can be used in the characterization of bone lesions and in the assessment of treatment response to bone diseases.

  11. In vivo characterization of chronic traumatic encephalopathy using [F-18]FDDNP PET brain imaging.

    Science.gov (United States)

    Barrio, Jorge R; Small, Gary W; Wong, Koon-Pong; Huang, Sung-Cheng; Liu, Jie; Merrill, David A; Giza, Christopher C; Fitzsimmons, Robert P; Omalu, Bennet; Bailes, Julian; Kepe, Vladimir

    2015-04-21

    Chronic traumatic encephalopathy (CTE) is an acquired primary tauopathy with a variety of cognitive, behavioral, and motor symptoms linked to cumulative brain damage sustained from single, episodic, or repetitive traumatic brain injury (TBI). No definitive clinical diagnosis for this condition exists. In this work, we used [F-18]FDDNP PET to detect brain patterns of neuropathology distribution in retired professional American football players with suspected CTE (n = 14) and compared results with those of cognitively intact controls (n = 28) and patients with Alzheimer's dementia (AD) (n = 24), a disease that has been cognitively associated with CTE. [F-18]FDDNP PET imaging results in the retired players suggested the presence of neuropathological patterns consistent with models of concussion wherein brainstem white matter tracts undergo early axonal damage and cumulative axonal injuries along subcortical, limbic, and cortical brain circuitries supporting mood, emotions, and behavior. This deposition pattern is distinctively different from the progressive pattern of neuropathology [paired helical filament (PHF)-tau and amyloid-β] in AD, which typically begins in the medial temporal lobe progressing along the cortical default mode network, with no or minimal involvement of subcortical structures. This particular [F-18]FDDNP PET imaging pattern in cases of suspected CTE also is primarily consistent with PHF-tau distribution observed at autopsy in subjects with a history of mild TBI and autopsy-confirmed diagnosis of CTE.

  12. Determining synthesis rates of individual proteins in zebrafish (Danio rerio) with low levels of a stable isotope labelled amino acid.

    Science.gov (United States)

    Geary, Bethany; Magee, Kieran; Cash, Phillip; Young, Iain S; Whitfield, Phillip D; Doherty, Mary K

    2016-05-01

    The zebrafish is a powerful model organism for the analysis of human cardiovascular development and disease. Understanding these processes at the protein level not only requires changes in protein concentration to be determined but also the rate at which these changes occur on a protein-by-protein basis. The ability to measure protein synthesis and degradation rates on a proteome-wide scale, using stable isotope labelling in conjunction with mass spectrometry is now a well-established experimental approach. With the advent of more selective and sensitive mass spectrometers, it is possible to accurately measure lower levels of stable isotope incorporation, even when sample is limited. In order to challenge the sensitivity of this approach, we successfully determined the synthesis rates of over 600 proteins from the cardiac muscle of the zebrafish using a diet where either 30% or 50% of the L-leucine was replaced with a stable isotope labelled analogue ([(2) H7 ]L-leucine]. It was possible to extract sufficient protein from individual zebrafish hearts to determine the incorporation rate of the label into hundreds of proteins simultaneously, with the two labelling regimens showing a good correlation of synthesis rates.

  13. α1,2-Fucosyllactose Does Not Improve Intestinal Function or Prevent Escherichia coli F18 Diarrhea in Newborn Pigs

    DEFF Research Database (Denmark)

    Cilieborg, Malene Skovsted; Sangild, Per Torp; Jensen, Michael Ladegaard

    2017-01-01

    of mucosa and activities of some brush border enzymes in the proximal small intestine. In situ abundance of α-1,2-fucose and E. coli was similar between groups, whereas sequencing showed higher abundance of Enterobacteriaceae in F18, Enterococcus in Control and Lachnospiraceae in 2FL-F18 pigs. CONCLUSIONS...

  14. Pharmacologic Activation of Tumor Hypoxia : A Means to Increase Tumor 2-Deoxy-2-[F-18]Fluoro-D-Glucose Uptake?

    NARCIS (Netherlands)

    Mees, Gilles; Dierckx, Rudi; Vangestel, Christel; Laukens, Debby; Van Damme, Nancy; Van de Wiele, Christophe

    2013-01-01

    Tumor hypoxia and tumor metabolism are linked through the activation of metabolic genes following hypoxia-inducible factor 1 (HIF-1) activation. This raises the question of whether this relationship can be exploited to improve 2-deoxy-2-[F-18]fluoro-D-glucose positron emission tomography ([F-18]FDG-

  15. F-18 FDG PET Images of the Cervix at Various Time Points after the Loop Electrosurgical Excision Procedure

    Energy Technology Data Exchange (ETDEWEB)

    Jeong, Shin Young [Kyungpook National University Medical School, Daegu (Korea, Republic of); Min, Jung Joon [Chonnam National University Medical School, Gwangju (Korea, Republic of)

    2010-04-15

    F-18 FDG PET is useful for monitoring residual or recurrent tumors after surgical resection. We describe five F-18 FDG PET images of three patients who had cervical carcinoma and then underwent a loop electro surgical excision procedure (LEEP). Two of the images were taken within 15 days and three at least 2 months after LEEP. The earlier F-18 FDG PET images revealed linear hypermetabolic lesions in the cervix that were produced by inflammation. This was confirmed by pathological analysis. The later F-18 FDG PET images did not reveal any remarkable hypermetabolism in the cervix without any treatment. These observations suggest that, to determine the response to LEEP therapy, F-18 FDG PET should not be performed within 15 days of the procedure.

  16. Discrepancy of bone metastases between F-18 FDG PET/CT and bone scan in a patient with prostate cancer

    Energy Technology Data Exchange (ETDEWEB)

    Choi, Seung Jin; Kim, Chul Soo; Byun, Sung Su; Hyun, In Young [Inha University College of Medicine, Incheon (Korea, Republic of)

    2006-10-15

    We report the case of a 73-year-old man who had prostate cancer with bone metastases. Tc-99m HDP Whole body bone scan revealed multiple areas of increased bony uptake consistent with widespread bone metastases. F-18 fluorodeoxyglucose (FDG) positron emission tomography/computed tomography (PET/CT) demonstrated mild F-18 FDG uptake in the lymph nodes of neck, abdomen, and pelvis. However, abnormal F-18 FDG uptake was not seen in the skeletal system. Biopsy and immunohistochemical stains of left supraclavicular mass showed metastatic prostate adenocarcinoma. Currently, there are a few reported cases of F-18 FDG PET/CT evaluation of bone metastases in prostate cancer. We discuss the discrepancy between F-18 FDG PET/CT and bone scan in the detection of osseous metastases of prostate cancer.

  17. F-18 FDG PET/CT Findings of Subcutaneous Panniculitis - Like T- Cell Lymphoma : A Case Report

    Energy Technology Data Exchange (ETDEWEB)

    Kong, Eun Jung; Cho, Ihn Ho; Chun, Kyung Ah; Bae, Yeung Kyung; Choi, Joon Hyuk; Hyun, Myung Soo [Yeungnam University College of Medicine, Daegu (Korea, Republic of)

    2009-06-15

    F-18 FDG PET is a metabolic imaging modality that is efficacious in staging and assessment of treatment response for variety of lymphomas. We report usefulness of F-18 FDG PET/CT in evaluating severity of the disease and response to therapy in a patient with subcutaneous panniculitis- like T-cell lymphoma (SPTCL). Here we describe a case of SPTCL in 24-year-old man who had wide spread firm and tender nodular lesions with increased F-18 FDG uptake. After chemotherapy follow up F-18 FDG PET/CT image shows disseminated malignancy and then the patient died with hemophagocytic syndrome. This report suggests that F-18 FDG PET/CT may be useful in determining disease activity at the time of initial diagnosis, after treatment, and evaluating a suspected outcome of SPTCL.

  18. Stable isotope-labeled vitamin D, metabolites and chemical analogs: Synthesis and use in mass spectrometric studies

    Energy Technology Data Exchange (ETDEWEB)

    Coldwell, R.D.; Trafford, D.J.; Varley, M.J.; Kirk, D.N.; Makin, H.L. (London Hospital Medical College (England))

    1990-10-01

    Methods for the measurement of vitamin D and its metabolites using stable isotope-labeled internal standards and mass spectrometry are reviewed. The synthesis of both labeled and unlabeled standards is illustrated, and details of the synthesis of (26,26,27,27,27(-2)H5)-25,26-dihydroxyvitamin D3 and (28,28,28(-2)H3)-24,25-dihydroxyvitamin D2 are given. The use of in vitro biologic systems for the production of further metabolites of deuterated 25-hydroxyvitamin D3 is discussed. Use of deuterated 25-hydroxydihydrotachysterol3 as a substrate in the isolated perfused rat kidney has provided valuable data for the assignment of structure to a number of metabolites of 25-hydroxydihydrotachysterol3 formed in this system. 51 refs.

  19. Myocardial glucose metabolism in patients with hypertrophic cardiomyopathy. Assessment by F-18-FDG PET study

    Energy Technology Data Exchange (ETDEWEB)

    Uehara, Toshiisa [Osaka Univ., Suita (Japan). Medical School; Ishida, Yoshio; Hayashida, Kohei [and others

    1998-04-01

    In an investigation of myocardial metabolic abnormalities in hypertrophic myocardium, the myocardial glucose metabolism was evaluated with F-18-fluorodeoxyglucose (FDG) positron emission tomography (PET) in 32 patients with hypertrophic cardiomyopathy, and the results were compared with those in 9 patients with hypertensive heart disease. F-18-FDG PET study was performed in the fasting and glucose-loading states. The myocardial regional %dose uptake was calculated quantitatively. The average regional %dose uptake in the fasting state in the patients with asymmetric septal hypertrophy and dilated-phase hypertrophic cardiomyopathy was significantly higher than that in the patients with hypertensive heart disease (0.75{+-}0.34%, 0.65{+-}0.25%, and 0.43{+-}0.22%/100 g myocardium, respectively). In contrast, the average %dose uptake in the glucose-loading state in the patients with asymmetric septal hypertrophy and dilated-phase hypertrophic cardiomyopathy was not significantly different from that in patients with hypertensive heart disease (1.17{+-}0.49%, 0.80{+-}0.44% and 0.99{+-}0.45%, respectively). The patients with apical hypertrophy had also low %dose uptake in the fasting state (0.38{+-}0.21%) as in the hypertensive heart disease patients, so that the characteristics of asymmetric septal hypertrophy and dilated-phase hypertrophic cardiomyopathy are considered to be high FDG uptake throughout the myocardium in the fasting state. Patients with apical hypertrophy are considered to belong to other disease categories metabolically. F-18-FDG PET study is useful in the evaluation of the pathophysiologic diagnosis of patients with hypertrophic cardiomyopathy. (author)

  20. F-18 FDG PET/CT in Bilateral Diffuse Pulmonary Lymphangitic Carcinomatosis

    Energy Technology Data Exchange (ETDEWEB)

    Senthil, Raja; Parghane, Rahul; Kashyap, Raghava; Bhattacharya, Anish; Mittal, Bhagwant Rai [Postgraduate Institute of Medical Education and Resaarch, Chandigarh (India)

    2012-06-15

    A 51-year-old female patient, who had undergone left-sided modified radical mastectomy for left breast carcinoma 4 years ago, presented with dyspnea of 4 months duration F-18 FDG PET/CT of this patient showed diffusely in-creased FDG uptake in the bilateral lung fields along the thickened bronchovascular bundles. SUVmax of lymphangitic lung was 5.2. The standardized uptake ratio (SUR) of mediastinal blood pool to lymphangitic lung was 0.44. High resolution computed tomography (HRCT) of the same patient showed thickening of interlobular septa and bronchovaseular bundles, with preservation of normal parenchymal architecture. Multiple intrapulmonary nodules and bilateral hilar lymphadenopathy with pulmonary lymphangitic carcinomatosis (PLC). The lungs are the second most common sites for metastases after lymph nodes. These metastases are usually nodular on radiologic images. PLC with interstitial involvement constitutes only 7% of pulmonary metastastases. The most common primary sites, in order of frequency, are adenocarcinoma of the lung, breast, stomach, colon, and prostrate. HRCT has been the modality of choice in the radiologic diagnosis of PLC. Only a few studies have de-scribed the F-18 FDG PET/CT findings in pulmonary lymphangitic carcinomatosis. These studies have shown diffusely increased FDG uptake corresponding to the typical changes in the CT as the most common finding. One study has reported that F-18 FDG PET/CT is 100% specific and 86% sensitive in diagnosing PLC by subjective analysis. The mean SUV in the region of pulmonary lymphangitic lung was 1.26{+-}0.45 and that of blood pool to normal lung was 3.78{+-}1.37.

  1. Pelvic congestion syndrome initially detected by contrast enhanced F 18 FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Dae Weung; Kim, Myoung Hyoung; Kim, Woo Hyoung; Kim, Chang Guhn [Wonkwang Univ. School of Medicine, Iksan (Korea, Republic of)

    2012-03-15

    Pelvic congestion syndrome (PCS) is said to occur as a result of retrograde flow in an incompetent ovarian vein. Ovarian vein incompetence is seen in approximately 10% of women, and up to 60% with this abnormality can develop PCS. The etiology of PCS is poorly understood and is likely to be multifactorial. Absence of ovarian vein valves is an important factor in its development. The causes of ovarian varicoceles are multifactorial, involving both mechanical and hormonal factors. Dilatation of the ovarian veins can result in vascular incompetence and retrograde blood flow. On either CT or magnetic resonance (MR) imaging studies, pelvic varices in PCS appear as dilated, tortuous, enhancing tubular structures near the ovaries and uterus. In addition, the extension of varices to the broad ligament and paravaginal venous plexus can be appreciated. With CT, the tubular nature of these structures and the pattern of enhancement after intravenous contrast medium administration distinguish them from lymphadenopathy or adnexal masses. Unlike such masses, pelvic varices appear isodense with other veins after contrast enhancement. Contrast enhanced CT data as part of the combined PET/CT examination provide additional information when compared with non enhanced PET/CT. Because CT data supply the anatomic background for PET, the most important benefit relates to more precise anatomic localization of pathology by differentiation of the lesion from its surrounding structures. By supporting lesion detection and characterization, CT contrast agents can be of additional value in F 18 FDG non avid disease. As in the presented case, careful review of CT images in contrast enhanced PET/CT enables the detection of F 18 FDG non avid disease such as PCS. As contrast enhanced F 18 FDG PET/CT had been performed frequently, being familiar with the findings of PCS on the contrast enhanced CT images would have been helpful for the nuclear medicine physicians.

  2. Synthesis of {sup 15}N labeled glyphosate; Sintese do glifosato enriquecido com {sup 15}N

    Energy Technology Data Exchange (ETDEWEB)

    Oliveira, Claudineia R. de; Bendassolli, Jose Albertino; Tavares, Glauco Arnold; Rossete, Alexssandra L.R.M.; Tagliassachi, Romulo Barbieri; Prestes, Cleuber Vieira [Centro de Energia Nuclear na Agricultura (CENA), Piracicaba, SP (Brazil). Dept. de Isotopos Estaveis]. E-mail: crolivei@cena.usp.br

    2005-07-01

    Amongst the actually commercialized herbicides the Glyphosate is the most used in Brazil. Its efficiency as well as the others herbicides against undesirable weeds is harmed by its final composts left at the environment. Although studies has being carried out to improve the knowledge about the herbicides behavior at the environment its complexity has led them towards innumerous to new significant research work where the use of radiolabeled composts (radiative tracers) are recommended to evaluate their bio-availability in the soil. However is the use, the manipulation and the storage of radiolabeled composts is requires an extra care under chemical safety point of view. The use of non radiolabeled composts is a world tendency especially for field researches. Under this context the presented work describes a method for the synthesis of {sup 15}N labeled glyphosate. The {sup 15}N-herbicide was undertaken by phosphometilation with the phosphit dialquil and {sup 15}N-glycine. The tests where carried out through a micro scale production plant and of equimolars amounts. At these conditions it's was possible to reach approximately a 20% of yield. At the conclusion of a best operational condition its expected to offer another important toll that shall be used in glyphosate behavior at the environment and undesirably weeds. (author)

  3. Carbon-11 labelled ketamine-synthesis, distribution in mice and PET studies in baboons

    Energy Technology Data Exchange (ETDEWEB)

    Shiue, C.-Y.; Vallabhahosula, Shankar; Wolf, Alfred P.; Dewey, Stephen L.; Fowler, Joanna S.; Schlyer, David J.; Arnett, Carroll D.; Zhou Yiguo

    1997-02-01

    No-carrier-added (NCA)[{sup 11}C]({+-})-ketamine (2a) and its enantiomers (+)-2b and (-)-2c were synthesized by methylation of the corresponding norketamine (1a-c) with [{sup 11}C]H{sub 3}I in an overall radiochemical yield of 20% (EOB) with specific activities of 0.35-0.45 Ci/{mu}mole at EOB in a synthesis time of 40 min from EOB. Compound 2a was metabolized rapidly in mouse brain and labeled metabolites appeared in baboon plasma. PET studies of compounds 2a-c in a baboon showed that influx of compounds 2a-c into the brain was high for the first few min but radioactivity then declined rapidly. Although the retention of radioactivity in the baboon striatum was not significantly different for 2a-c 20 min post-injection, graphical analysis of time-activity data for each enantiomer and for the racemate in baboon striatum suggested that (+)-ketamine may interact with receptors slightly more effectively than its (-)-enantiomer or racemate. However, due to its rapid metabolism in the brain and a similar uptake in the striatum and cerebellum, [{sup 11}C]ketamine may not be an ideal tracer for studying NMDA receptor with PET.

  4. Synthesis of Salt Soluble Proteins in Barley. Pulse-Labeling Study of Grain Filling in Liquid-Cultured Detached Spikes

    DEFF Research Database (Denmark)

    Giese, Nanna Henriette; Hejgaard, Jørn

    1984-01-01

    The accumulation of salt-soluble proteins in the endosperm of developing barley (Hordeum vulgare L.) grains was examined. Detached spikes of barley were cultured at different levels of nitrogen nutrition and pulse-labeled with [14C] sucrose at specific times after anthesis. Proteins were extracted...... to increased nitrogen nutrition. Two major components, β-amylase and protein Z in particular, had a synthesis profile almost identical to that of the endosperm storage protein, hordein....

  5. F-18 FDG PET findings for Vogt-Koyanagi-Harada disease

    Energy Technology Data Exchange (ETDEWEB)

    Park, Hye Lim; Yoo, Ie Ryung; Park Sonya Young Ju [Dept. of of Radiology, Seoul St. Mary' s Hospital, College of MedicineThe Catholic University of Korea, Seoul (Korea, Republic of)

    2017-06-15

    Vogt-Koyanagi-Harada disease is a rare multisystemic granulomatous autoimmune disorder affecting pigmented tissues such as the choroid, meninges, inner ear, and the skin. Neurologic symptoms are usually mild. Clinical manifestations include generalized muscle weakness, headache, meningismus, vertigo, decreased visual acuity, hearing loss and mental changes ranging from mild confusion to psychosis, hemiparesis, dysarthria, and aphasia. Seizures are very rare. We describe a case of 18F-fluorodeoxyglucose (F-18 FDG) positron emission tomography (PET) and software-fused PET-magnetic resonance imaging (MRI) in Vogt-Koyanagi-Harada disease with seizure.

  6. A Novel imaging agent for acetylcholinesterase: 2-[F-18]fluoro-CP-118,954

    Energy Technology Data Exchange (ETDEWEB)

    Ryu, Y. K.; Choi, Y. S; Baek, J. Y.; Lee, K. H.; Choi, Y.; Kim, B. T [Sungkyunkwan University School of Medicine, Suwon (Korea, Republic of); Park, E. Y.; Kim, Y. R.; Kim, S. E [Seoul National University College of Medicine, Seoul (Korea, Republic of)

    2004-07-01

    AcetyIcholinesterase (AChE) is an important cholinergic marker for the diagnosis of Alzheimer's disease. Although many AChE inhibitors were developed as radioligands for AChE imaging, most of them showed a uniform regional brain distribution. In this study, 2-fluoro-CP-118,954 with excellent anti-AChE activity (IC{sub 50} = 0.74 nM) was prepared as the radioligand, 2-[F-18]fluoro-CP-118,954 ([F-l8]) and evaluated for AChE imaging. [F-l8] was prepared by reductive alkylation of CP-144,885 (Pfizer Inc. U.S.A.) with 2-[F-l8]fIuorobenzaldehyde at 130 .deg. for 15 min, followed by HPLC purification. Mice were injected with the radioligand [F-18] via tail vein. At the indicated time points (5, 15, 30, 60, 90 and 120 min), samples of bone and brain tissues were removed, weighed, and counted. Blocking experiments were carried out in mice by coinjection of the radioligand with, a dopamine receptor antagonist, or a sigma receptor agonist, and samples of brain tissues were collected at 60 min postinjection, weighed and counted. The radioligand [F-l8] was synthesized in 20-35% radiochemical yield and with high specific activity (40-42 GBq/mol). Tissue distribution studies demonstrated that the regional brain distribution of [F-18] was welI correlated with the known density of AChE in mouse brain, with the highest striatum to cerebellum uptake ratio (4.5) at 60 min postinjection. The high level of uptake was also shown at all time points in the olfactory tubercle that is known to have the dopaminergic neurons and also have high AChE staining in rat brain. The uptake in both the striatum and olfactory tubercle was not blocked by either dopamine receptor antagonists or a sigma receptor agonist. On the other hand, significant blocking of the uptake by suggested high specific binding of [F-l8] to AChE. This study demonstrated that [F-18] is a suitable imaging agent for AChE.

  7. New Cyclotron Targetry to Enhance F-18 clinical Position Emission Tomography

    Energy Technology Data Exchange (ETDEWEB)

    J. Michael Doster

    2008-12-19

    This project proposes to develop cyclotron targets that produce F-18 for clinical Positron Emission Tomography (PET) at significantly higher rates than that available from current targetry. This production rate of 18F is directly proportional to the beam current. Higher beam currents would result in increased 18F production but would be accompanied by higher heat loads to the target. The beam power available in most commercial cyclotrons exceeds the heat removal capacity of current target technology by a factor of two to four, significantly limiting the production rate of Fluorine-18.

  8. Economical synthesis of 13C-labeled opiates, cocaine derivatives and selected urinary metabolites by derivatization of the natural products.

    Science.gov (United States)

    Karlsen, Morten; Liu, Huiling; Johansen, Jon Eigill; Hoff, Bård Helge

    2015-03-25

    The illegal use of opiates and cocaine is a challenge world-wide, but some derivatives are also valuable pharmaceuticals. Reference samples of the active ingredients and their metabolites are needed both for controlling administration in the clinic and to detect drugs of abuse. Especially, (13)C-labeled compounds are useful for identification and quantification purposes by mass spectroscopic techniques, potentially increasing accuracy by minimizing ion alteration/suppression effects. Thus, the synthesis of [acetyl-(13)C4]heroin, [acetyl-(13)C4-methyl-(13)C]heroin, [acetyl-(13)C2-methyl-(13)C]6-acetylmorphine, [N-methyl-(13)C-O-metyl-(13)C]codeine and phenyl-(13)C6-labeled derivatives of cocaine, benzoylecgonine, norcocaine and cocaethylene was undertaken to provide such reference materials. The synthetic work has focused on identifying (13)C atom-efficient routes towards these derivatives. Therefore, the (13)C-labeled opiates and cocaine derivatives were made from the corresponding natural products.

  9. Myocardial Fibrosis in Hypertrophic Cardiomyopathy Demonstrated by Integrated Cardiac F-18 FDG PET/MR

    Energy Technology Data Exchange (ETDEWEB)

    Kong, Eunjung; Lee, Sanghee; Cho, Ihnho [Yeungnam Univ., Daegu (Korea, Republic of)

    2013-09-15

    Hypertrophic cardiomyopathy (HCM) is a common condition defined as a diffuse or segmental left ventricular (LV) hypertrophy with a nondilated and hyperdynamic chamber as well as cardiac arrhythmias. Cardiac MR (CMR) imaging is a key modality for evaluation of HCM. In addition to the assessment of LV wall thickness, LV function and aortic flow, CMR is capable of estimation of late gadolinium enhancement (LGE) in affected myocardium which has been shown to have a direct correlation with incidence and severity of arrhythmias in HCM. In patients with HCM, LGE on CMR is presumed to represent intramyocardial fibrosis. Meanwhile, F-18 FDG myocardial PET has been sporadically studied in HCM, mostly for evaluation of the metabolic status of a hypertrophic myocardial segment, especially after interventions or to demonstrate partial myocardial fibrosis. We presented here the case of a 25-year-old male patient referred for simultaneous F-18 FDG cardiac PET/MR for the evaluation of septal hypertrophy. The PET/MR revealed myocardial fibrosis in the septum associated with FDG-defect and LGE.

  10. [Investigations of radiation exposure of the medical personnel during F-18-FDG PET studies].

    Science.gov (United States)

    Linemann, H; Will, E; Beuthien-Baumann, B

    2000-01-01

    The aim of the investigation was the identification of those working steps with the highest radiation exposure for the medical personnel during F-18-FDG-PET studies and to evaluate the effectiveness of radiation protection devices and instructions developed in our PET-center. The personal dose and hand dose were measured for each working procedure during F-18-FDG-PET studies using electronic personal dosimeters and thermoluminescent dosimeters respectively. Additionally, measurements of the radiation level near the patient were taken. The mean personal dose resulting from syringe preparation was 1 microSv/syringe, from injection 3 microSv/patient, from blood sampling during quantitative studies 6 microSv/study, and from positioning and handling of the patient 6 microSv/study. The mean hand dose per syringe preparation was 710 microSv for each hand. The mean hand dose during injection was 13 microSv for the right hand and 27 microSv for the left hand. All above mentioned values were measured applying the routine radiation shielding in use in our PET center. With the developed radiation shielding and means to reduce radiation exposure applied the allowed annual dose for medical personnel are not exceeded. One exception is the hand dose resulting from syringe preparation. An automatic or remote filling device should be used at this working step.

  11. Impact of F-18 FDG-PET for the Clinical Multidisciplinary Evaluation of Dementia

    DEFF Research Database (Denmark)

    Prakash, Vineet; Vestergård, Karsten; Frost, Majbritt;

    .                       CONCLUSION            F-18 FDG-PET changed management in 44 % of patients seen in a specialist mutlidisciplinary dementia clinic.PET has promising clinical value for management decisions in patients where clinical evaluations combined with lab CSF results and dedicated MR imaging are equivocal for Alzheimers......PURPOSE            Dementia is a challenging clinical diagnosis. Compared with conventional clinical evaluations, F-18 Fluorodeoxyglucose (FDG) PET has been reported to improve not only the diagnostic accuracy of dementia but also help better define the underlying  type. This is because FDG PET...... demonstrates metabolic patterns reflecting neuronal function specific to different dementias.To assess the impact of PET on a multidisciplinary  dementia clinic for patients with suspected dementia by comparing it with the initial clinical evaluation and paraclinical tests.                       METHOD...

  12. F-18 fluorodeoxyglucose PET/CT and post hoc PET/MRI in a case of primary meningeal melanomatosis

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Hong Je [Dept. of Nuclear Medicine, Dongnam Institute of Radiological and Medical Sciences (DIRAMS), Busan (Korea, Republic of); Ahn, Byeong Cheol; Hwang, Seong Wook; Kim, Hae Won; Lee, Sang Woo; Hwang, Jeong Hyun; Lee, Jae Tae [Kyungpook National University School of Medicine, Kyungpook National University Hospital, Daegu (Korea, Republic of); Cho, Suk Kyong [Dept. of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul (Korea, Republic of)

    2013-04-15

    Primary meningeal melanomatosis is a rare, aggressive variant of primary malignant melanoma of the central nervous system, which arises from melanocytes within the leptomeninges and carries a poor prognosis. We report a case of primary meningeal melanomatosis in a 17-year-old man, which was diagnosed with 1{sup 8F}-fluorodeoxyglucose (F-18 FDG) PET/CT, and post hoc F-18 FDG PET/MRI fusion images. Whole-body F-18 FDG PET/CT was helpful in ruling out the extracranial origin of melanoma lesions, and in assessing the therapeutic response. Post hoc PET/MRI fusion images facilitated the correlation between PET and MRI images and demonstrated the hypermetabolic lesions more accurately than the unenhanced PET/CT images. Whole body F-18 FDG PET/CT and post hoc PET/MRI images might help clinicians determine the best therapeutic strategy for patients with primary meningeal melanomatosis.

  13. A significant discrepancy of uptake between I-131 MIBG and F-18 FDG in a patient with malignant paraganglioma

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Jong Su; Kim, Hyun Keun; Choi, Kyu Young; Park, Hyung Ki; Kim, Eun Sil; Kim, Yun Kwon; Kim, So Yon [National Police Hospital, Seoul (Korea, Republic of)

    2007-06-15

    A 38-year-old man who was diagnosed with malignant paraganglioma underwent computed tomography (CT) and I-131 metaiodobenzylguanidine (MIBG) scan. CT showed extensive lymph node enlargement in right iliac area and retroperitoneum with severe hydronephrosis and mass on posterior bladder wall. However, I-131 MIBG scan didn't showed abnormal uptake. He also underwent F-18 fluorodeoxyglucose (FDG) positron emission tomography/CT for localizing accurate tumor site. F-18 FDG PET/CT showed multiple metastases of left supraclavicular, hilar, mediastinal para-aortic, inguinal, right iliac lymph nodes, lung, vertebrae, and pelvis. There are a few reports showing that the F-18 FDG PET/CT is helpful for staging and localizing tumor site of patients who are diagnosed with negative on the MIBG scans. Thus, we report a case with paraganglioma which showed negative I-131 MIBG scan, but revealed multiple intense hypermetabolic foci in F-18 FDG PET/CT.

  14. Synthesis of [sup 14]C-labeled copolymers for drug delivery studies

    Energy Technology Data Exchange (ETDEWEB)

    Rhee, S.W.; Reist, E.J. (SRI International, Menlo Park, CA (United States)); Rock, M.T.

    1994-02-01

    [sup 14]C-labeled polyanhydride copolymers [(20:80)/1,3-bis(p-carboxyphenoxy)-propane (CPP):sebacic acid (SA)] were synthesized according to schemes I and II: [sup 14]C-labeled sebacic acid (2,9-[sup 14]C[sub 2]) and [sup 14]C-labeled CPP 1,3-bis(p-carboxyphenoxy)-propane (labeled at C-1, C-3 of the propyl group) were transformed to the corresponding mixed anhydrides as prepolymers respectively by reaction with acetic anhydride. The labeled mixed anhydride prepolymers were condensed with unlabeled counter-prepolymers to give the labeled polyanhydride copolymers. The labeled copolymers were identified and characterized by gel permeation chromatography (GPC). (author).

  15. Preliminary study on the evaluation of Langerhans cell histiocytosis using F-18-fluoro-deoxy-glucose PET/CT

    Institute of Scientific and Technical Information of China (English)

    Zhou Wenlan; Wu Hubing; Han Yanjiang; Wang Shaobo; Dong Ye; Wang Quanshi

    2014-01-01

    Background Limited number of studies have been reported regarding the utilization of F-18-fluoro-deoxy-glucose (F-18-FDG) positron emission tomography/computed tomography (F-18-FDG PET/CT) in Langerhans cell histiocytosis (LCH).The aim of this study was to assess the role of F-18-FDG PET/CT in the diagnosis and treatment of LCH.Methods Eight newly diagnosed and seven recurrent patients with LCH received F-18-FDG PET/CT scans.The diagnosis of LCH was established by pathology,multi-modality imaging,and clinical follow-up.Results F-18-FDG PET/CT was positive in 14 patients with 13 true positives and one false positive.All 45 LCH lesions were F-18-FDG avid including six small bone lesions <1.0 cm in diameter.The mean maximal standardized uptake value (SUVmax) was 7.13±4.91.F-18-FDG uptake showed no significant difference between newly diagnosed lesions vs recurrent lesions (SUVmax:6.50±2.97 vs.7.93±6.60,t=-0.901,P=0.376).Among 45 LCH lesions,68.9% (31/45) were found in bones and 31.1% (14/45) in soft tissue.The most commonly involved bones were the pelvis and vertebrae.There was no significant difference in F-18-FDG uptake between bone lesions vs.non-bone lesions (SUVmax:6.30±2.87 vs.8.97±7.58,t=1.277,P=0.221).In two patients,changes in F-18-FDG uptake on serial PET/CT scans reflected response of lesions to treatment.Conclusions The present study suggests that F-18-FDG PET/CT may be useful for diagnosis and assessing the treatment response of LCH.Because of the small sample size,further research is warranted to confirm our findings.

  16. Supplementation with Lactobacillus paracasei or Pediococcus pentosaceus does not prevent diarrhoea in neonatal pigs infected with Escherichia coli F18

    DEFF Research Database (Denmark)

    Andersen, Anders Daniel; Cilieborg, Malene Skovsted; Lauridsen, Charlotte

    2017-01-01

    caesarean-delivered, colostrum-deprived term piglets on parenteral nutrition for the first 15 h, were used as models for sensitive newborn infants. A commercially available probiotic strain, Lactobacillus paracasei F19 (LAP, 2·6x108 colony-forming units (CFU)/kg per d) and a novel LAB isolate, Pediococcus...... increased diarrhoea and density of F18 in the intestinal mucosa (Prelative to F18 alone (P

  17. Synthesis of radioactively labelled CdSe/CdS/ZnS quantum dots for in vivo experiments

    Science.gov (United States)

    Stachowski, Gordon M; Bauer, Christoph; Waurisch, Christian; Bargheer, Denise; Nielsen, Peter; Heeren, Jörg; Hickey, Stephen G

    2014-01-01

    Summary During the last decades of nanoparticles research, many nanomaterials have been developed for applications in the field of bio-labelling. For the visualization of transport processes in the body, organs and cells, luminescent quantum dots (QDs) make for highly useful diagnostic tools. However, intercellular routes, bio-distribution, metabolism during degradation or quantification of the excretion of nanoparticles, and the study of the biological response to the QDs themselves are areas which to date have not been fully investigated. In order to aid in addressing those issues, CdSe/CdS/ZnS QDs were radioactively labelled, which allows quantification of the QD concentration in the whole body or in ex vivo samples by γ-counting. However, the synthesis of radioactively labelled QDs is not trivial since the coating process must be completely adapted, and material availability, security and avoidance of radioactive waste must be considered. In this contribution, the coating of CdSe/CdS QDs with a radioactive 65ZnS shell using a modified, operator-safe, SILAR procedure is presented. Under UV illumination, no difference in the photoluminescence of the radioactive and non-radioactive CdSe/CdS/ZnS colloidal solutions was observed. Furthermore, a down-scaled synthesis for the production of very small batches of 5 nmol QDs without loss in the fluorescence quality was developed. Subsequently, the radio-labelled QDs were phase transferred by encapsulation into an amphiphilic polymer. γ-counting of the radioactivity provided confirmation of the successful labelling and phase transfer of the QDs. PMID:25551066

  18. Synthesis of radioactively labelled CdSe/CdS/ZnS quantum dots for in vivo experiments

    Directory of Open Access Journals (Sweden)

    Gordon M. Stachowski

    2014-12-01

    Full Text Available During the last decades of nanoparticles research, many nanomaterials have been developed for applications in the field of bio-labelling. For the visualization of transport processes in the body, organs and cells, luminescent quantum dots (QDs make for highly useful diagnostic tools. However, intercellular routes, bio-distribution, metabolism during degradation or quantification of the excretion of nanoparticles, and the study of the biological response to the QDs themselves are areas which to date have not been fully investigated. In order to aid in addressing those issues, CdSe/CdS/ZnS QDs were radioactively labelled, which allows quantification of the QD concentration in the whole body or in ex vivo samples by γ-counting. However, the synthesis of radioactively labelled QDs is not trivial since the coating process must be completely adapted, and material availability, security and avoidance of radioactive waste must be considered. In this contribution, the coating of CdSe/CdS QDs with a radioactive 65ZnS shell using a modified, operator-safe, SILAR procedure is presented. Under UV illumination, no difference in the photoluminescence of the radioactive and non-radioactive CdSe/CdS/ZnS colloidal solutions was observed. Furthermore, a down-scaled synthesis for the production of very small batches of 5 nmol QDs without loss in the fluorescence quality was developed. Subsequently, the radio-labelled QDs were phase transferred by encapsulation into an amphiphilic polymer. γ-counting of the radioactivity provided confirmation of the successful labelling and phase transfer of the QDs.

  19. Synthesis of radioactively labelled CdSe/CdS/ZnS quantum dots for in vivo experiments.

    Science.gov (United States)

    Stachowski, Gordon M; Bauer, Christoph; Waurisch, Christian; Bargheer, Denise; Nielsen, Peter; Heeren, Jörg; Hickey, Stephen G; Eychmüller, Alexander

    2014-01-01

    During the last decades of nanoparticles research, many nanomaterials have been developed for applications in the field of bio-labelling. For the visualization of transport processes in the body, organs and cells, luminescent quantum dots (QDs) make for highly useful diagnostic tools. However, intercellular routes, bio-distribution, metabolism during degradation or quantification of the excretion of nanoparticles, and the study of the biological response to the QDs themselves are areas which to date have not been fully investigated. In order to aid in addressing those issues, CdSe/CdS/ZnS QDs were radioactively labelled, which allows quantification of the QD concentration in the whole body or in ex vivo samples by γ-counting. However, the synthesis of radioactively labelled QDs is not trivial since the coating process must be completely adapted, and material availability, security and avoidance of radioactive waste must be considered. In this contribution, the coating of CdSe/CdS QDs with a radioactive (65)ZnS shell using a modified, operator-safe, SILAR procedure is presented. Under UV illumination, no difference in the photoluminescence of the radioactive and non-radioactive CdSe/CdS/ZnS colloidal solutions was observed. Furthermore, a down-scaled synthesis for the production of very small batches of 5 nmol QDs without loss in the fluorescence quality was developed. Subsequently, the radio-labelled QDs were phase transferred by encapsulation into an amphiphilic polymer. γ-counting of the radioactivity provided confirmation of the successful labelling and phase transfer of the QDs.

  20. Apparent Catalase Synthesis in Sunflower Cotyledons during the Change in Microbody Function: A Mathematical Approach for the Quantitative Evaluation of Density-labeling Data.

    Science.gov (United States)

    Betsche, T; Gerhardt, B

    1978-10-01

    Density-labeling with 10 mm K(15)NO(3)/70% (2)H(2)O has been used to investigate catalase synthesis in different developmental stages of sunflower (Helianthus annuus L.) cotyledons. A mathematical approach is introduced for the quantitative evaluation of the density-labeling data. The method allows, in the presence of preexisting enzyme activity, calculation of this synthesized activity (apparent enzyme synthesis) which results from the balance between actual enzyme synthesis and the degradation of newly synthesized enzyme at a given time. During greening of the cotyledons, when the catalase activity declines and the population of leaf peroxisomes is formed, the apparent catalase synthesis is lower than, or at best equal to, that occurring during a developmental stage when the leaf peroxisome population is established and catalase synthesis and degradation of total catalase are in equilibrium. This result suggests a formation, in fatty cotyledons, of the leaf peroxisomes by transformation of the glyoxysomes rather than by de novo synthesis.

  1. Relationship between the expression level of SLA-DQA and Escherichia coli F18 infection in piglets.

    Science.gov (United States)

    Bao, Wen-bin; Ye, Lan; Zi, Chen; Liu, Lu; Zhu, Jing; Pan, Zhang-yuan; Zhu, Guo-qiang; Huang, Xue-gen; Wu, Sheng-long

    2012-02-15

    The expression of SLA-DQA was assayed by Real-time PCR to analyze the differential expression between ETEC F18-resistant and -sensitive post-weaning piglets, and then to compare the expression levels of SLA-DQA in 11 different tissues from 8-, 18-, 30- and 35-day-old ETEC F18-resistant piglets, which aimed at discussing the role of SLA-DQA in resistance to ETEC F18. The results showed that SLA-DQA is broadly expressed in 11 tissues with the highest expression level in lymph nodes, and a relatively higher expression level in lung, spleen, jejunum, and duodenum. In tissues of lymph node, lung, spleen, jejunum, and duodenum, the mRNA expression of SLA-DQA in resistant individuals was significantly higher than that in sensitive ones (PSLA-DQA increased from 8 to 18 and 30 days (weaning day), and increased persistently to 35 days of post-weaning. Expression levels of SLA-DQA on 35 days in most tissues were significant higher than that on 8, 18 and 30 days (PSLA-DQA to a certain extent. The analysis suggested that SLA-DQA may be not the direct immune factor that resisted the Escherichia coli F18, but perhaps enhanced humoral immunity and cell immunity to reduce the transmembrane signal transduction of ETEC F18 bacterial LPS and then led to the resistance to ETEC F18 in piglets. Copyright © 2011 Elsevier B.V. All rights reserved.

  2. Clinical utility of F-18 FDG PET-CT in the initial evaluation of lung cancer

    DEFF Research Database (Denmark)

    Madsen, Poul Henning; Holdgaard, Paw Christian; Buck Christensen, Janne

    2016-01-01

    PURPOSE: Positron emission tomography-computed tomography (PET-CT) is a resource-demanding imaging modality with increasing popularity in the workup of patients with suspected or proven lung cancer. METHODS: To review the clinical usefulness of this imaging modality in the diagnosis, staging...... the predefined criteria and were read in full to identify relevant original articles on F-18 FDG PET-CT (1) in the evaluation of solitary pulmonary nodules (n = 14), (2) in curative-intent treatment trials (n = 9), and (3) in planning of invasive procedures (n = 18). RESULTS: We found the following important...... results from the literature review: 1) PET-CT can rule out malignancy in most solitary pulmonary nodules due to high sensitivity (recommendation level A). 2) PET-CT reduces the number of futile treatment trials (recommendation level A). 3) The sensitivity of PET-CT in general is insufficient to rule out...

  3. Neural responses of rats in the forced swimming test: [F-18]FDG micro PET study.

    Science.gov (United States)

    Jang, Dong-Pyo; Lee, So-Hee; Lee, Sang-Yoon; Park, Chan-Woong; Cho, Zang-Hee; Kim, Young-Bo

    2009-10-12

    The forced swimming test (FST) is a widely used tool in the assessment of behavioral despair and prediction of response to antidepressants. However, the neural mechanisms underlying behavioral changes between pretest and test sessions of the FST remain unclear. In this study, we investigated changes in rat brain activity during the FST using [F-18]Fluorodeoxyglucose micro PET. In both pretest and test sessions, the activity of the cerebellum and striatum increased, whereas significant deactivation was observed in the hippocampus, inferior colliculus, orbital cortex, and insula. The periaqueductal gray (PAG) region activated markedly in the pretest session, but did not activate in the test session. There was a significant increase in immobility and a decrease in climbing during the behavioral analysis test session. These results suggest that the PAG region may play an important role in the modulation of FST coping strategies subsequent to failure of the escape response during the pretest session.

  4. Cranberry extract inhibits in vitro adhesion of F4 and F18(+)Escherichia coli to pig intestinal epithelium and reduces in vivo excretion of pigs orally challenged with F18(+) verotoxigenic E. coli.

    Science.gov (United States)

    Coddens, Annelies; Loos, Michaela; Vanrompay, Daisy; Remon, Jean Paul; Cox, Eric

    2017-04-01

    F4(+)E. coli and F18(+)E. coli infections are an important threat for pig industry worldwide. Antibiotics are commonly used to treat infected piglets, but the emerging development of resistance against antibiotics raises major concerns. Hence, alternative therapies to prevent pigs from F4(+)E. coli and F18(+)E. coli infections need to be developed. Since cranberry previously showed anti-adhesive activity against uropathogenic E. coli, we aimed to investigate whether cranberry extract could also inhibit binding of F4(+)E. coli and F18(+)E. coli to pig intestinal epithelium. Using the in vitro villus adhesion assay, we found that low concentrations of cranberry extract (20μg or 100μg/ml) have strong inhibitory activity on F4(+)E. coli (75.3%, S.D.=9.31 or 95.8%, S.D.=2.56, respectively) and F18(+)E. coli adherence (100% inhibition). This effect was not due to antimicrobial activity. Moreover, cranberry extract (10mg or 100mg) could also abolish in vivo binding of F4 and F18 fimbriae to the pig intestinal epithelium in ligated loop experiments. Finally, two challenge experiments with F18(+)E. coli were performed to address the efficacy of in-feed or water supplemented cranberry extract. No effect could be observed in piglets that received cranberry extract only in feed (1g/kg or 10g/kg). However, supplementation of feed (10g/kg) and drinking water (1g/L) significantly decreased excretion and diarrhea. The decreased infection resulted in a decreased serum antibody response indicating reduced exposure to F18(+)E. coli. Copyright © 2017 Elsevier B.V. All rights reserved.

  5. Fluorinase: a tool for the synthesis of ¹⁸F-labeled sugars and nucleosides for PET.

    Science.gov (United States)

    Onega, Mayca; Winkler, Margit; O'Hagan, David

    2009-08-01

    There is an increasing interest in the preparation of (18)F-labeled radiopharmaceuticals with potential applications in PET for medicinal imaging. Appropriate synthetic methods require a quick and efficient route in which to incorporate the (18)F into a ligand, due to the relatively short half-life of the (18)F isotope. Enzymatic methods are rare in this area; however, the discovery of a fluorinating enzyme from Streptomyces cattleya (EC 2.5.1.63) has opened up the possibility of the enzymatic synthesis and formation of C-(18)F bonds from the [(18)F]fluoride ion. In this article, the development of enzymatic preparations of (18)F-labeled sugars and nucleosides as potential radiotracers using the fluorinase from S. cattleya for PET applications is reviewed. Enzymatic reactions are not traditional in PET synthesis, but this enzyme has some attractive features. The enzyme is available in an overexpressed form from Escherichia coli and it is relatively stable and can be easily purified and manipulated. Most notably, it utilizes [(18)F] fluoride, the form of the isotope normally generated by the cyclotron and usually in very high specific radioactivity. The disadvantage with the enzyme is that it is substrate specific; however, when the fluorinase is used in combination biotransformations with a second or third enzyme, then a range of radiolabeled nucleosides and ribose sugars can be prepared. The fluorinase enzyme has emerged as a curiosity from biosynthesis studies, but it now has some potential as a new catalyst for (18)F incorporation for PET syntheses. The focus is now on delivering a user-friendly catalyst to the PET synthesis community and establishing a clinical role for some of the (18)F-labeled molecules available using this technology.

  6. Estimation of Whole Body Radiation Exposure to Nuclear Medicine Personnel During Synthesis of (177)Lutetium-labeled Radiopharmaceuticals.

    Science.gov (United States)

    Arora, Geetanjali; Mishra, Rajesh; Kumar, Praveen; Yadav, Madhav; Ballal, Sanjana; Bal, Chandrasekhar; Damle, Nishikant Avinash

    2017-01-01

    With rapid development in the field of nuclear medicine therapy, radiation safety of the personnel involved in synthesis of radiopharmaceuticals has become imperative. Few studies have been done on estimating the radiation exposure of personnel involved in the radio labeling of (177)Lu-compounds in western countries. However, data from the Indian subcontinent are limited. We have estimated whole body radiation exposure to the radiopharmacist involved in the labeling of: (177)Lu-DOTATATE, (177)Lu-PSMA-617, and (177)Lu-EDTMP. Background radiation was measured by keeping a pocket dosimeter around the workbench when no radioactive work was conducted. The same pocket dosimeter was given to the radiopharmacist performing the labeling of (177)Lu-compounds. All radiopharmaceuticals were synthesized by the same radiopharmacist with 3, 1 and 3 year experience, respectively, in radiolabeling the above compounds. One Curie (1 Ci) of (177)Lu was received fortnightly by our department. Data were collected for 12 syntheses of (177)Lu-DOTATATE, 8 syntheses of (177)Lu-PSMA-617, and 3 syntheses of (177)Lu-EDTMP. Mean time required to complete the synthesis was 0.81, 0.65, and 0.58 h, respectively. Mean whole body radiation exposure was 0.023 ± 0.01 mSv, 0.01 ± 0.002 mSv, and 0.002 ± 0.0006 mSv, respectively. Overall mean radiation dose for all the three (177)Lu-compounds was 0.014 mSv. Highest exposure was obtained during the synthesis of (177)Lu-DOTATATE. Our data suggest that the manual radiolabeling of (177)Lu compounds is safe, and the whole body radiation exposure to the involved personnel is well within prescribed limits.

  7. Simplified Synthesis of Isotopically Labeled 5,5-Dimethyl-pyrroline N-Oxide

    Directory of Open Access Journals (Sweden)

    Ronald P. Mason

    2011-10-01

    Full Text Available 5,5-Dimethylpyrroline N-oxide (15N and 5,5-di(trideuteromethylpyrroline N-oxide were synthesized from the respective isotopically labeled 2-nitropropane analogs obtained from the reaction of sodium nitrate with 2-halopropanes. This facile, straightforward process allows synthesizing isotopically labeled DMPO analogs in a 4-step reaction without special equipment.

  8. Synthesis of two sup 14 C-labeled catechol-o-methyltransferase inhibitors

    Energy Technology Data Exchange (ETDEWEB)

    Karlsson, Carita; Honkanen, Erkki (Orion Corporation Ltd., Espoo (Finland). Research Center)

    1991-02-01

    {sup 14}C-labelled 3-(3,4-dihydroxy-5-nitrophenylmethylidene)-2,4-pentanedione and {sup 14}C-labelled E-N,N-diethyl-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide have been synthesized from (carbonyl-{sup 14}C)vanillin. (author).

  9. Synthesis and properties of peptide nucleic acid labeled at the N-terminus with HiLyte Fluor 488 fluorescent dye.

    Science.gov (United States)

    Hnedzko, Dziyana; McGee, Dennis W; Rozners, Eriks

    2016-09-15

    Fluorescently labeled peptide nucleic acids (PNAs) are important tools in fundamental research and biomedical applications. However, synthesis of labeled PNAs, especially using modern and expensive dyes, is less explored than similar preparations of oligonucleotide dye conjugates. Herein, we present a simple procedure for labeling of the PNA N-terminus with HiLyte Fluor 488 as the last step of solid phase PNA synthesis. A minimum excess of 1.25equiv of activated carboxylic acid achieved labeling yields close to 90% providing a good compromise between the price of dye and the yield of product and significant improvement over previous literature procedures. The HiLyte Fluor 488-labeled PNAs retained the RNA binding ability and in live cell fluorescence microscopy experiments were brighter and significantly more photostable than PNA labeled with carboxyfluorescein. In contrast to fluorescein-labeled PNA, the fluorescence of PNAs labeled with HiLyte Fluor 488 was independent of pH in the biologically relevant range of 5-8. The potential of HiLyte Fluor 488-labeling for studies of PNA cellular uptake and distribution was demonstrated in several cell lines.

  10. A Rationale for the Use of F18-FDG PET/CT in Fever and Inflammation of Unknown Origin

    Science.gov (United States)

    Balink, H.; Verberne, H. J.; Bennink, R. J.; van Eck-Smit, B. L. F.

    2012-01-01

    This review focuses on the diagnostic value of hybrid F18-FDG Positron Emission Tomography/Computerized tomography (PET/CT) in fever of unknown origin (FUO) and inflammation of unknown origin (IUO). Due to the wide range of possible causes both FUO and IUO remain a clinical challenge for both patients and physicians. In addition, the aetiology of IUO shows the same variation in diseases as the FUO spectrum and probably requires the same diagnostic approach as FUO. There are numerous historically used diagnostic approaches incorporating invasive and non-invasive, and imaging techniques, all with relative high specificity but limited sensitivity. This hampers the generalization of these diagnostic approaches. However, recently published reports show that F18-FDG PET/CT in FUO and IUO has a high sensitivity and a relative non-specificity for malignancy, infection and inflammation. This makes F18-FDG PET/CT an ideal diagnostic tool to start the diagnostic process and to guide subsequent focused diagnostic approaches with higher specificity. In addition, F18-FDG PET/CT has a relative high negative predictive value. Therefore F18 FDG PET/CT should be incorporated in the routine diagnostic work-up of patients with FUO and IUO, preferably at an early stage in the diagnostic process. PMID:23316356

  11. A Rationale for the Use of F18-FDG PET/CT in Fever and Inflammation of Unknown Origin

    Directory of Open Access Journals (Sweden)

    H. Balink

    2012-01-01

    Full Text Available This review focuses on the diagnostic value of hybrid F18-FDG Positron Emission Tomography/Computerized tomography (PET/CT in fever of unknown origin (FUO and inflammation of unknown origin (IUO. Due to the wide range of possible causes both FUO and IUO remain a clinical challenge for both patients and physicians. In addition, the aetiology of IUO shows the same variation in diseases as the FUO spectrum and probably requires the same diagnostic approach as FUO. There are numerous historically used diagnostic approaches incorporating invasive and non-invasive, and imaging techniques, all with relative high specificity but limited sensitivity. This hampers the generalization of these diagnostic approaches. However, recently published reports show that F18-FDG PET/CT in FUO and IUO has a high sensitivity and a relative non-specificity for malignancy, infection and inflammation. This makes F18-FDG PET/CT an ideal diagnostic tool to start the diagnostic process and to guide subsequent focused diagnostic approaches with higher specificity. In addition, F18-FDG PET/CT has a relative high negative predictive value. Therefore F18 FDG PET/CT should be incorporated in the routine diagnostic work-up of patients with FUO and IUO, preferably at an early stage in the diagnostic process.

  12. Synthesis and optical properties of pyrrolidinyl peptide nucleic acid carrying a clicked Nile red label

    Directory of Open Access Journals (Sweden)

    Nattawut Yotapan

    2014-09-01

    Full Text Available DNA or its analogues with an environment-sensitive fluorescent label are potentially useful as a probe for studying the structure and dynamics of nucleic acids. In this work, pyrrolidinyl peptide nucleic acid (acpcPNA was labeled at its backbone with Nile red, a solvatochromic benzophenoxazine dye, by means of click chemistry. The optical properties of the Nile red-labeled acpcPNA were investigated by UV–vis and fluorescence spectroscopy in the absence and in the presence of DNA. In contrast to the usual quenching observed in Nile red-labeled DNA, the hybridization with DNA resulted in blue shifting and an enhanced fluorescence regardless of the neighboring bases. More pronounced blue shifts and fluorescence enhancements were observed when the DNA target carried a base insertion in close proximity to the Nile red label. The results indicate that the Nile red label is located in a more hydrophobic environment in acpcPNA–DNA duplexes than in the single-stranded acpcPNA. The different fluorescence properties of the acpcPNA hybrids of complementary DNA and DNA carrying a base insertion are suggestive of different interactions between the Nile red label and the duplexes.

  13. Synthesis and optical properties of pyrrolidinyl peptide nucleic acid carrying a clicked Nile red label.

    Science.gov (United States)

    Yotapan, Nattawut; Charoenpakdee, Chayan; Wathanathavorn, Pawinee; Ditmangklo, Boonsong; Wagenknecht, Hans-Achim; Vilaivan, Tirayut

    2014-01-01

    DNA or its analogues with an environment-sensitive fluorescent label are potentially useful as a probe for studying the structure and dynamics of nucleic acids. In this work, pyrrolidinyl peptide nucleic acid (acpcPNA) was labeled at its backbone with Nile red, a solvatochromic benzophenoxazine dye, by means of click chemistry. The optical properties of the Nile red-labeled acpcPNA were investigated by UV-vis and fluorescence spectroscopy in the absence and in the presence of DNA. In contrast to the usual quenching observed in Nile red-labeled DNA, the hybridization with DNA resulted in blue shifting and an enhanced fluorescence regardless of the neighboring bases. More pronounced blue shifts and fluorescence enhancements were observed when the DNA target carried a base insertion in close proximity to the Nile red label. The results indicate that the Nile red label is located in a more hydrophobic environment in acpcPNA-DNA duplexes than in the single-stranded acpcPNA. The different fluorescence properties of the acpcPNA hybrids of complementary DNA and DNA carrying a base insertion are suggestive of different interactions between the Nile red label and the duplexes.

  14. Isotopic labeling of mouse interferon by incorporation of radioactive amino acids during synthesis

    Energy Technology Data Exchange (ETDEWEB)

    DeMaeyer-Guignard, J.; Cachard, A.; DeMaeyer, E.

    1982-07-30

    Mouse interferon produced by C-243 cells induced with Newcastle disease virus was isotopically labeled by adding either (/sup 35/S)methionine or a /sup 14/C-labeled amino acid mixture to the culture medium. A method combining butyric acid and theophylline treatment and resulting in high interferon yields was used. Following purification by two-step affinity chromatography on poly(U) and antibody columns, the resulting material was analyzed on SDS-PAGE. The migration pattern of radioactivity and interferon coincided well and autoradiography revealed three major bands at migration distances corresponding, respectively, to 35, 28, and 22 K. Interferon represented 3.8% of all (/sup 35/S)methionine-labeled proteins and 2.6% of all /sup 14/C-amino acid-labeled proteins released into the medium.

  15. Current concepts in F18 FDG PET/CT-based Radiation Therapy planning for Lung Cancer

    Directory of Open Access Journals (Sweden)

    Percy eLee

    2012-07-01

    Full Text Available Radiation therapy is an important component of cancer therapy for early stage as well as locally advanced lung cancer. The use of F18 FDG PET/CT has come to the forefront of lung cancer staging and overall treatment decision-making. FDG PET/CT parameters such as standard uptake value and metabolic tumor volume provide important prognostic and predictive information in lung cancer. Importantly, FDG PET/CT for radiation planning has added biological information in defining the gross tumor volume as well as involved nodal disease. For example, accurate target delineation between tumor and atelectasis is facilitated by utilizing PET and CT imaging. Furthermore, there has been meaningful progress in incorporating metabolic information from FDG PET/CT imaging in radiation treatment planning strategies such as radiation dose escalation based on standard uptake value thresholds as well as using respiratory gated PET and CT planning for improved target delineation of moving targets. In addition, PET/CT based follow-up after radiation therapy has provided the possibility of early detection of local as well as distant recurrences after treatment. More research is needed to incorporate other biomarkers such as proliferative and hypoxia biomarkers in PET as well as integrating metabolic information in adaptive, patient-centered, tailored radiation therapy.

  16. Radiation assessment to paediatric with F-18-FDG undergo whole-body PET/CT examination

    Energy Technology Data Exchange (ETDEWEB)

    Dhalisa, H., E-mail: dhalisa82@gmail.com; Rafidah, Z. [Kluster Oncology Science and Radiology, Advanced Medical Dental Institute, Universiti Sains Malaysia (USM), Bertam, Penang (Malaysia); Mohamad, A. S. [Department of Nuclear Medicine, National Cancer Institute, No 4 Jalan P7, Presint 7, Putrajaya (Malaysia)

    2016-01-22

    This study was carried out on wholebody radiation dose assessment to paediatrics patient who undergo PET/CT scanner at Institut Kanser Negara. Consist of 68 patients with varies of malignancies and epilepsy disease case covering age between 2 years to 12 years old. This is a retrospective study from 2010-2014. The use of PET/CT scanner as an advanced tool has been proven to give an extra radiation dose to the patient. It is because of the radiation exposure from the combination of both CT and PET scans rather than a single CT or PET scan. Furthermore, a study on radiation dose to paediatric patient undergoing PET/CT is rare in Malaysia. So, the aim of this study is to estimate the wholebody effective dose to paediatric patient in Malaysia. Effective dose from PET scan was calculated based on the activity of F18 FDG and dose coefficient reported in International Commission on Radiological Protection (ICRP) Publication 106. Effective dose from CT was determined using k coefficient as reported in ICRP publication 102 and Dose Length Product (DLP) value. The average effective dose from PET and CT were found to be 7.05mSv and 5.77mSv respectively. The mean wholebody effective dose received by a patient with combined PETCT examination was 12.78mSv. These results could be used as reference for dosimetry of a patient undergoing PETCT examination in Malaysia.

  17. SPECT Imaging of Epilepsy: An Overview and Comparison with F-18 FDG PET

    Directory of Open Access Journals (Sweden)

    Sunhee Kim

    2011-01-01

    Full Text Available Epilepsy surgery is highly effective in treating refractory epilepsy, but requires accurate presurgical localization of the epileptogenic focus. Briefly, localization of the region of seizure onset traditionally dependents on seizure semiology, scalp EEG recordings and correlation with anatomical imaging modalities such as MRI. The introduction of noninvasive functional neuroimaging methods, including single-photon emission computed tomography (SPECT and positron emission tomography (PET has dramatically changed the method for presurgical epilepsy evaluation. These imaging modalities have become powerful tools for the investigation of brain function and are an essential part of the evaluation of epileptic patients. Of these methods, SPECT has the practical capacity to image blood flow functional changes that occur during seizures in the routine clinical setting. In this review we present the basic principles of epilepsy SPECT and PET imaging. We discuss the properties of the SPECT tracers to be used for this purpose and imaging acquisition protocols as well as the diagnostic performance of SPECT in addition to SPECT image analysis methods. This is followed by a discussion and comparison to F-18 FDG PET acquisition and imaging analysis methods.

  18. F-18 FDG PET/CT imaging of primary hepatic neuroendocrine tumor

    Directory of Open Access Journals (Sweden)

    Katsuya Mitamura

    2015-01-01

    Full Text Available Primary hepatic neuroendocrine tumors (PHNETs are extremely rare neoplasms. Herein, we report a case of a 70-year-old man with a hepatic mass. The non-contrast computed tomography (CT image showed a low-density mass, and dynamic CT images indicated the enhancement of the mass in the arterial phase and early washout in the late phase. F18- fluorodeoxyglucose (18F-FDG positron emission tomography (PET and fused PET/CT images showed increased uptake in the hepatic mass. Whole-body 18F-FDG PET images showed no abnormal activity except for the liver lesion. Presence of an extrahepatic tumor was also ruled out by performing upper gastrointestinal endoscopy, total colonoscopy, and chest and abdominal CT. A posterior segmentectomy was performed, and histologic examination confirmed a neuroendocrine tumor (grade 1. The patient was followed up for about 2 years after the resection, and no extrahepatic lesions were radiologically found. Therefore, the patient was diagnosed with PHNET. To the best of our knowledge, no previous case of PHNET have been detected by 18F-FDG PET imaging.

  19. Evaluation of acetazolamine response in patients with cerebellar ataxia using dynamic quantitative F-18-FDG PET

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Y. K.; Lee, D. S.; Lee, J. S.; Kim, M. H.; Lee, K. M.; Yeo, J. S.; Chung, J. K.; Lee, M. C. [College of Medicine, Seoul National Univ., Seoul (Korea, Republic of)

    2001-07-01

    Cerebellar Ataxia (CA) usually shows dramatic response to acetazolamide treatment. But few cases of acetazolamide unresponse CA were reported recently. Using dynamic FDG PET, we tried to evaluate the metabolic abnormality and its drug response in CA. Quantitative F-18-FDG PET was performed prior and after treatment of acetazolamide (250 mg qid for 10 days) in two patient suspected episodic cerebellar ataxia. Using Model-based clustering method, the regional cerebral glucose metabolic rate (rCMRglu) was calculated. Two patients showed different treatment response to acetazolamide. In one patient who showed markedly reduced frequency of the ataxic attack after treatment. FDG PET showed that mean cerebellar glucose metabolism was increased after treatment ({delta}rCMRglu:9%). However, in the other who showed poor response to acetazolamide, FDG PET showed the more decrease metabolism in cerebellar metabolism after treatment ({delta}rCMRglu:-17%). The change of the cerebellar glucose metabolism on FDG PET reflected the symptomatic improvement after acetazolamide in these two CA patients. We could expected that FDG PET might be a very useful tool to quantitatively predict the treatment response in CA and other neurologic disorder.

  20. F-18 FDG PET/CT Findings of a Patient with Takayasu Arteritis Before and After Therapy

    Directory of Open Access Journals (Sweden)

    Sait Sağer

    2012-04-01

    Full Text Available Vasculitis is defined as inflammation and necrosis with leukocytic infiltration of the blood vessel wall. Takayasu arteritis is a chronic inflammatory arteritis that primarily involves the aorta and its main branches. A 64-year-old female patient with a 2-month history of fever of unknown origin was presented to our clinic for F-18 FDG PET/CT imaging. Baseline PET/CT images demonstrated intense F-18 FDG uptake in the aorta, bilateral subclavian and brachiocephalic arteries consistent with Takayasu arteritis. After 2 months of immunosuppressive therapy, she was asymptomatic and follow-up FDG PET/CT scan showed almost complete disappearance of large vessels’ F-18 FDG uptake. FDG PET/CT is a sensitive technique for assessing presence of large-vessel vasculitis such as Takayasu arteritis, extent of large-vessel inflammation and disease activity after therapy. (MIRT 2012;21:32-34

  1. A Case of Urethral Metastasis from Sigmoid Colon Cancer Diagnostically and Prognostically Indicated by F 18 FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Seo, Han Seok; Kim, Eun Sil; Kim, Soyon; Im, Su Jin; Park, Yong Hyun; Lee, Ju Hyoung; Hur, So Chong [National Police Hospital, Seoul (Korea, Republic of)

    2011-12-15

    Urethral metastasis from colorectal cancer is rare and is known to have a poor prognosis. A 72 year old man with a history of colectomy and colostomy due to sigmoid colon cancer was admitted to the emergency room with bowel distension, rectal bleeding and urinary symptoms. Computed tomography of the abdominopelvis showed sigmoid colon cancer with multiple metastases involving the liver. Positron emission tomography with F 18 fluorodeoxyglucose (FDG) showed multiple hypermetabolic foci in the liver, penis and pubic bone, which otherwise could not be diagnosed. The lesions revealed no improvement with chemotherapy and urological surgery on follow up F 18 FDG PET/CT. We present a case of urethral metastasis of sigmoid colon cancer diagnostically and prognostically indicated by F 18 FDG PET/CT.

  2. Rapidly growing complex fibroadenoma with surrounding ductal hyperplasia mimics breast malignancy on serial F-18 FDG PET/CT imaging.

    Science.gov (United States)

    Makis, William; Ciarallo, Anthony; Hickeson, Marc; Derbekyan, Vilma

    2011-07-01

    A 30-year-old woman was referred for an F-18 fluorodeoxyglucose (FDG) PET/CT to rule out lymphoma, and was found to have an incidental FDG-avid right breast nodule that grew significantly in size and FDG uptake on a subsequent scan, raising suspicion of a growing breast malignancy. Histologic evaluation showed a complex fibroadenoma with adenosis and surrounding ductal hyperplasia. Although variable F-18 FDG uptake in fibroadenomas has been described, a distinction between simple and complex fibroadenomas has not been made in the PET literature, even though complex fibroadenomas have a higher propensity to develop into malignancies. This case shows that a rapidly growing complex fibroadenoma can mimic a breast malignancy on serial F-18 FDG PET/CT scans, showing significant increase in both size and FDG-avidity on follow-up studies.

  3. Synthesis of enantiomerically pure [(14) C]-labelled morpholine derivatives for a class of trace amine-associate receptor 1 agonists.

    Science.gov (United States)

    Edelmann, Martin R; Hartung, Thomas; Trussardi, René; Iding, Hans; Galley, Guido; Pflieger, Philippe; Norcross, Roger D

    2016-12-01

    Various agonists of the trace amine-associate receptor 1, under consideration as potential clinical development candidates, were labelled with carbon-14 for use in preclinical in vitro and in vivo drug metabolism studies. Herein, the [(14) C]-radiosynthesis of 2-phenyl-substituted morpholines 1 is described. After evaluating and optimizing different synthetic routes, 4-iodonitrobenzene 3 was selected as starting material for the 14-step synthesis. Incorporation of carbon-14 into the acetyl moiety allowed a safe and efficient synthesis of [(14) C]-labelled 4-nitroacetophenone 2 in five steps and 38% yield. Further transformation of 2 to the target compounds 1 was achieved in a 9-step synthesis. In a representative example, [(14) C]-labelled 1 was obtained in an overall yield of 11% and was isolated in >99% radiochemical purity and a specific activity of 47 mCi/mmol.

  4. Evaluation of fluorine-18-labeled alkylating agents as potential synthons for the labeling of oligonucleotides

    NARCIS (Netherlands)

    de Vries, EFJ; Vroegh, J; Elsinga, PH; Vaalburg, W

    2003-01-01

    Six fluorine-18-labeled alkylating agents were selected as potentially suitable synthons for the labeling of antisense oligonucleotides. The selected synthons were evaluated in a model reaction with the monomer adenosine 5'-O-thiomonophosphate. Of these synthons, alpha-bromo-alpha'-[F-18]fluoro-m-xy

  5. Synthesis and Evaluation of 125I Labeled Chalcone Derivatives Containing Bithiophene Moiety as Potential Aβ Probes

    Directory of Open Access Journals (Sweden)

    PENG Cheng

    2015-11-01

    Full Text Available In continuation of the investigation on the bithiophene structure as potential Aβ probes, two halogenated chalcone derivatives containing bithiophene moiety were designed and evaluated as imaging probes for Aβ plaques. In vitro fluorescence staining indicated that they could stain Aβ plaques in the brain sections of AD model mice specifically, in vitro binding assay further confirmed that they displayed high binding affinities to Aβ aggregates (Ki=2.33 nM and 0.88 nM. One radio-iodinated probe, 125I labeleled chalcone derivatives was obtained via iododestannylation reaction with high radiochemical yield and purity (>99%. Moreover, the 125I-labeling compound displayed specific labeling of Aβ plaques in the brain sections of AD model mice with low background, and the specific labeling could be confirmed by thioflavin-S staining. In vivo biodistribution in normal mice indicated that the 125I labeling compound exhibited low initial brain uptake (1.19%ID/g at 2 min and rapid clearance. These preliminary results suggest that 125I labeling compound may serve as novel Aβ imaging probe, although further modifications are needed to improve initial brain uptake.

  6. F18-FDG PET-CT analyses of small peripheral adenocarcinoma of the lung

    Energy Technology Data Exchange (ETDEWEB)

    Takahashi, Yoshiyuki; Takashima, Shodayu [Osaka Univ. Graduate School of Medicine, Div. of Allied Health Sciences, Dept. of Diagnostic Radiological Imaging, Osaka (Japan)], e-mail: yoshi_seat_128@yahoo.co.jp; Watanabe, Shinichiro [Osaka University Graduate School of Medicine, Department of Nuclear Medicine and Tracer Kinetics, Osaka (Japan)

    2013-03-15

    Background: Radiological discrimination of histologic subtypes of small peripheral adenocarcinoma of the lung is clinically important. Although there are many articles in which CT findings were used for this purpose, there are only a few reports on the capability of FDG PET-CT findings for histologic classification of this tumor. Purpose: To investigate the correlation between visual assessment or maximum standard uptake values (SUVmax) on F18-FDG PET-CT and histology grading of small peripheral adenocarcinoma of the lung. Material and Methods: Proportions of positive PET-CT diagnoses and SUVmax were retrospectively reviewed on 96 solitary pulmonary nodules of {<=}2 cm in 90 consecutive patients. Tumors were classified into four groups according to Noguchi's classification (group 1 [n = 10], atypical adenomatous hyperplasia and type A tumors; group 2 [n = 12], type B tumors; group 3 [n = 42], type C tumors; group 4 [n = 32], types D, E, and F tumors). Proportions of positive PET-CT diagnoses and mean SUVmax of lesions among four groups were compared using trend tests to examine if there is a significant linear correlation with the progression of the histology grading of tumors. Then, an optimal threshold of SUVmax was proposed to best discriminate tumors of poor (groups 3 and 4) from good (groups 1 and 2) prognosis. Results: There was a significant linear trend for both visual assessment (P < 0.01) and SUVmax (P < 0.01). A SUVmax of 0.42 showed the highest accuracy of 84% with 95% sensitivity and 50% specificity for predicting tumors of poor prognosis. A SUVmax of 2.05 showed 100% specificity with 49% sensitivity, and 60% accuracy. Positive visual diagnoses showed accuracy of 83% with 90% sensitivity and 59% specificity. Conclusion: Visual assessment and SUVmax on PET-CT correlated well with the histology grading of small peripheral adenocarcinoma of the lung.

  7. Clinical utility of F-18 FDG PET-CT in the initial evaluation of lung cancer

    Energy Technology Data Exchange (ETDEWEB)

    Madsen, Poul Henning [Vejle Hospital, Department of Medicine, Division of Respiratory Medicine, Vejle (Denmark); Holdgaard, Paw Christian [Vejle Hospital, Department of Nuclear Medicine, Vejle (Denmark); Christensen, Janne Buck [Odense University Hospital/University of Southern Denmark, Department of Quality and Research/HTA, Odense University Hospital and Medical Research Library, Odense (Denmark); Hoeilund-Carlsen, Poul Flemming [Odense University Hospital, Department of Nuclear Medicine, Odense (Denmark)

    2016-10-15

    Positron emission tomography-computed tomography (PET-CT) is a resource-demanding imaging modality with increasing popularity in the workup of patients with suspected or proven lung cancer. To review the clinical usefulness of this imaging modality in the diagnosis, staging, and pre-operative evaluation, we conducted a systematic literature search, review, and quality assessment using the rapid evidence assessment toolkit and the Oxford Centre for Evidence-Based Medicine methodology. The literature search resulted in 4,208 records including 918 reviews, of which 139 met the predefined criteria and were read in full to identify relevant original articles on F-18 FDG PET-CT (1) in the evaluation of solitary pulmonary nodules (n = 14), (2) in curative-intent treatment trials (n = 9), and (3) in planning of invasive procedures (n = 18). We found the following important results from the literature review: (1) PET-CT can rule out malignancy in most solitary pulmonary nodules due to high sensitivity (recommendation level A). (2) PET-CT reduces the number of futile treatment trials (recommendation level A). (3) The sensitivity of PET-CT in general is insufficient to rule out mediastinal lymph node metastasis (recommendation level A). (1) With few exceptions, solitary pulmonary nodules can safely be considered benign if the PET-CT scan is negative. Exceptions consist of small (<1 cm) and non-solid, solitary pulmonary nodules. These abnormalities should be followed up by CT in a structured programme. (2) No curative-intent treatment should be commenced until a PET-CT scan has excluded occult distant metastases. (3) In general, lymph node metastasis in the mediastinum cannot be ruled out on the basis of a negative PET-CT, and confirmative invasive staging should be performed in most patients before mediastinal metastasis is confirmed or ruled out. (orig.)

  8. Amyloid-β assessed by florbetapir F 18 PET and 18-month cognitive decline

    Science.gov (United States)

    Sperling, Reisa A.; Coleman, R. Edward; Johnson, Keith A.; Reiman, Eric M.; Davis, Mat D.; Grundman, Michael; Sabbagh, Marwan N.; Sadowsky, Carl H.; Fleisher, Adam S.; Carpenter, Alan; Clark, Christopher M.; Joshi, Abhinay D.; Mintun, Mark A.; Skovronsky, Daniel M.

    2012-01-01

    Objectives: Florbetapir F 18 PET can image amyloid-β (Aβ) aggregates in the brains of living subjects. We prospectively evaluated the prognostic utility of detecting Aβ pathology using florbetapir PET in subjects at risk for progressive cognitive decline. Methods: A total of 151 subjects who previously participated in a multicenter florbetapir PET imaging study were recruited for longitudinal assessment. Subjects included 51 with recently diagnosed mild cognitive impairment (MCI), 69 cognitively normal controls (CN), and 31 with clinically diagnosed Alzheimer disease dementia (AD). PET images were visually scored as positive (Aβ+) or negative (Aβ−) for pathologic levels of β-amyloid aggregation, blind to diagnostic classification. Cerebral to cerebellar standardized uptake value ratios (SUVr) were determined from the baseline PET images. Subjects were followed for 18 months to evaluate changes in cognition and diagnostic status. Analysis of covariance and correlation analyses were conducted to evaluate the association between baseline PET amyloid status and subsequent cognitive decline. Results: In both MCI and CN, baseline Aβ+ scans were associated with greater clinical worsening on the Alzheimer's Disease Assessment Scale–Cognitive subscale (ADAS-Cog (p < 0.01) and Clinical Dementia Rating–sum of boxes (CDR-SB) (p < 0.02). In MCI Aβ+ scans were also associated with greater decline in memory, Digit Symbol Substitution (DSS), and Mini-Mental State Examination (MMSE) (p < 0.05). In MCI, higher baseline SUVr similarly correlated with greater subsequent decline on the ADAS-Cog (p < 0.01), CDR-SB (p < 0.03), a memory measure, DSS, and MMSE (p < 0.05). Aβ+ MCI tended to convert to AD dementia at a higher rate than Aβ− subjects (p < 0.10). Conclusions: Florbetapir PET may help identify individuals at increased risk for progressive cognitive decline. PMID:22786606

  9. C11-Acetate and F-18 FDG PET for Men With Prostate Cancer Bone Metastases

    Science.gov (United States)

    Yu, Evan Y.; Muzi, Mark; Hackenbracht, Joy A.; Rezvani, Brian B.; Link, Jeanne M.; Montgomery, Robert Bruce; Higano, Celestia S.; Eary, Janet F.; Mankoff, David A.

    2011-01-01

    Purpose of the Report This study tested the feasibility of C11-acetate (acetate) positron emission tomography (PET) imaging to assess response to therapy in men with bone metastatic prostate cancer and compared results for disease detection and response evaluation with F-18 fluorodeoxyglucose (FDG) PET. Materials and Methods Men with ≥3 prostate cancer bone metastases identified by Tc-99m methylene diphosphonate (MDP) bone scintigraphy and/or computed tomography were enrolled in a prospective study of serial acetate and FDG PET imaging. Patients were imaged before and 6 to 12 weeks after initial androgen deprivation therapy for new metastatic prostate cancer or first-line chemotherapy with docetaxel for castration-resistant prostate cancer. Qualitative assessment and changes in the tumor:normal uptake ratio were used to assess response by both acetate and FDG PET. In addition, the detection of bone metastases pretherapy was compared for acetate and FDG PET. Results A total of 8 patients with documented bone metastases were imaged, of which 6 were imaged both pre- and post-therapy. Acetate PET detected bone metastases in all 8 patients, whereas FDG PET detected lesions in 6 of the 7 imaged patients. Acetate PET generally detected more metastases with a higher tumor:normal uptake ratio. Qualitative and quantitative assessments of post-treatment response correlated with composite clinical designations of response, stable disease, or progression in 6 of 6 and 5 of 6 by acetate and 4 of 5 and 3 of 5 by FDG PET, respectively. Conclusions In this pilot study, results indicate that acetate PET holds promise for response assessment of prostate cancer bone metastases and is complementary to FDG PET in bone metastasis detection. PMID:21285676

  10. F-18 fluoromisonidazole PET predicts early lesion progression in acute ischemic stroke patients

    Energy Technology Data Exchange (ETDEWEB)

    Lee, G. H.; Kim, J. S.; Oh, S. J.; Cho, A. H.; Cho, K. H.; Kang, D. H.; Kim, J. S.; Kwon, S. E. [Asan Medical Center, Seoul (Korea, Republic of)

    2007-07-01

    F-18 fluoromisonidazole (FMISO) PET has been known to image viable hypoxic area. We performed this study to define whether FMISO PET can reveal ischemic penumbra of acute ischemic stroke. We prospectively selected acute ischemic stroke patients with large diffusion-perfusion mismatch due to occlusion of MCA or ICA on MRI among patients who visited emergency room within 24 hours after stroke onset. FMISO PET and diffusion weighted MR image (DWI) performed within 48 hours after initial MRI. We excluded the patients who performed any reperfusion procedure. To define the final infarcted area, DWI was performed again 2 days after PET scan. Brain FMISO PET was performed 3 hour after the injection of FMISO (370 MBq). FMISO PET was assessed by visual and quantitative analysis. The extent of abnormally increased FMISO uptake was automatically calculated by the number and size of voxels having higher count than upper 3SD of the mean count of contralateral normal hemisphere. We compared the extent of abnormal FMISO uptake area with the change of the extent of ischemic lesions on DWI. Fifteen patients were enrolled in this study. Ten of these patients showed abnormally increased FMISO uptake in peri-infarct area. Ischemic lesion size on follow-up DWI significantly increased in all patients with abnormally increased FMISO uptake except one patient of whom the MCA spontaneously recanalized on follow up angiogram. Ischemic lesions on DWI increased in only one of five patients without abnormally increased FMISO uptake. The extent of abnormally increased FMISO uptake area was positively correlated with infarct size progression on DWI (Spearman correlation coefficient = 0.757, p<0.01). FMISO uptake specifically and sensitively predicted early lesion progression in acute ischemic stroke patients with large diffusion-perfusion mismatch. Therefore, FMISO PET will be a good indicator of the revascularization or reperfusion procedure for acute ischemic stroke by defining ischemic

  11. Pyelo-cystic Reflux in F-18 FDG PET Scan Due to Ureteral Obstruction

    Energy Technology Data Exchange (ETDEWEB)

    Reyhan, Mehmet [Baskent Univ., Adana (Turkmenistan)

    2013-09-15

    A 72-year-old woman with a history of cervical cancer was treated with brachytherapy and chemotherapy. Combined F-18 FDG PET/CT performed for restaging demonstrated increased FDG uptake in a hypodense cystic lesion at the posterior part of the right renal cortex and a hypermetabolic soft tissue mass at the right parailiac region suggestive of a metastatic lymph node causing ureteral obstruction. There had been no FDG uptake in the cystic lesion on the FDG PET/CT study performed 1 year before. These findings suggest that the increased FDG uptake in the cystic lesion was caused by pyelocystic reflux due to ureteral obstruction secondary to parailiac lymph node metastasis (Figs. 1 and 2). Several renal lesions may have increased metabolism, such as renal cell carcinoma, lymphoma, oncocytoma, adult Wilms' tumor, angiomyolipoma, metastatic lesions, xanthogranulo-matous pyelonephritis and infected cyst. Most of these lesions are solid. Some infected renal cysts may be FDG avid, but in this situation increased FDG uptake is observed on the wall of the cyst. In our case, FDG uptake was seen in the entire cystic lesion. The patient had no symptoms or laboratory findings related to infection. Cysts are the most common space-occupying lesions of the kidney. The vast majority of these are simple cysts that are usually unilateral and solitary. Simple cysts are asymptomatic, except when complications exist such as hemorrhage, infection or rupture. There have been a few reports on spontaneous communications between renal cysts and the pyelocaliceal system, in most cases involving ruptures of the cysts into the pyelocaliceal system due to increased intracystic pressure caused by bleeding or infection of the cyst. In the present case, the cause of the connection between the cystic cavity and the pyelocaliceal system is the increased pressure in the renal pelvic cavity due to the ureteral obstruction secondary to parailiac lymph node metastasis.

  12. 13C-labeled D-ribose: chemi-enzymic synthesis of various isotopomers.

    Science.gov (United States)

    Serianni, A S; Bondo, P B

    1994-04-01

    Current interest in the use of heteronuclear multidimensional NMR methods to assess the structures, conformations and/or dynamics of oligonucleotides in solution has created an immediate need for nucleosides and their derivatives labeled in various ways with stable isotopes (13C, 2H, 15N and/or 17,18O). This short review focuses exclusively on chemienzymic methods to introduce one or more 13C labels into D-ribose, a precursor to ribo- and 2'-deoxyribonucleosides. It will be demonstrated that five convenient reactions, applied in specific sequences, provide access to 26 of the 32 13C-labeled isotopomers of D-ribose in acceptable yields. While not explicitly discussed herein, these same reactions, appropriately modified, can also be used to insert one or more 2H and/or 17,18O isotopes into this aldopentose.

  13. Chemienzymatic synthesis of Uridine. Nucleotides labeled with [15N] and [13C

    DEFF Research Database (Denmark)

    Gilles, Anne-Marie; Cristea, Ioan; Palibroda, Nicolae

    1995-01-01

    +necessary for the oxidation of glucose 6-phosphate and 6-phosphogluconate was recycled by glutamate dehydrogenase and excess of ammonia and a-oxoglutarate. Despite the number and complexity of the enzymatic steps, the synthesis of [15N,13C]UTP is straightforward with an overall yield exceeding 60%. This method, extended...... and diversified to the synthesis of all natural ribonucleotides, is a more economical alternative for obtaining nucleic acids for structural analysis by heteronuclear NMR spectroscopy....

  14. Straightforward preparation of labeled potassium cyanate by ozonation and application to the synthesis of [13C] or [14C]ureidocarboxylic acids.

    Science.gov (United States)

    Loreau, Olivier; Marlière, Philippe

    2013-06-15

    The development of new efficient syntheses of labeled reagents is a great challenge. Avoidance of overcomplicated procedures, availability and cost of starting materials are important considerations in choosing the synthetic route. In this report, we describe a facile and rapid preparation of labeled cyanate by ozonation of cyanide, a basic precursor. The crude cyanate was used without purification for the synthesis of various [(13)C] or [(14)C]ureidocarboxylic acids (20-68% yield from potassium cyanide). According to these results, cyanide ozonation may prove to be a promising alternative to traditional preparations of labeled cyanate.

  15. Synthesis of /sup 14/C-labeled perfluorooctanoic and perfluorodecanoic acids: purification of perfluorodecanoic acid

    Energy Technology Data Exchange (ETDEWEB)

    Reich, I.L.; Reich, H.J.; Menahan, L.A.; Peterson, R.E.

    1987-10-01

    Perfluoro-n-octanoic acid (PFOA) and perfluoro-n-decanoic acid (PFDA), two widely used industrial products, have been synthesized with /sup 14/C-labeling in the C-1 position. The carboxyl labeled materials were prepared in 48% and 53% yield by carbonation of perfluoroheptyllithium and perfluorononyllithium at -100/sup 0/C. An efficient chemical method for purification of PFDA was also developed. Treatment of commercial PFDA with refluxing potassium hydroxide solution resulted in removal of the mono and diprotio impurities to give 99% pure PFDA.

  16. Synthesis of singly /sup 2/H-, /sup 3/H-, and /sup 14/C- and doubly labeled acetaminophen, phenacetin, and p-acetanisidine

    Energy Technology Data Exchange (ETDEWEB)

    Chan, K.K. (University of Southern California, Los Angeles (USA)); Pang, K.S. (Houston Univ., TX (USA))

    1982-03-01

    Several efficient procedures for the synthesis of deuterium, tritium, and /sup 14/C-labeled acetaminophen, phenacetin, and p-acetanisidine are described. p-Aminophenol was acylated by the appropriate acetic anhydride under mild conditions yielding labeled acetaminophen. With O-alkylation using NaCH/sub 2/SOCH/sub 3/ and appropriate labeled and unlabeled alkyl halides, labeled phenacetin and p-acetanisidine were also obtained. Phenacetin labeled both with /sup 14/C on the acyl group and deuterium on the ethoxy group was synthesized in high yield by acylation of p-phenetidine-d/sub 5/. The last compound was obtained by acid hydrolysis of phenacetin-d/sub 5/ synthesized previously.

  17. In Vivo Responses of Human A375M Melanoma to a sigma Ligand : F-18-FDG PET Imaging

    NARCIS (Netherlands)

    Rybczynska, Anna A.; de Bruyn, Marco; K. Ramakrishnan, Nisha; de Jong, Johan R.; Elsinga, Philip H.; Helfrich, Wijnand; Dierckx, Rudi A. J. O.; van Waarde, Aren

    2013-01-01

    sigma-ligands can kill tumor cells. Previously we have shown that a short in vitro incubation of C6 tumor cells with sigma-ligands (24 h) results in a dose-dependent increase of cellular F-18-FDG uptake and that the magnitude of this increase is predictive of subsequent cell death. Here, we aimed to

  18. F-18 Fluorodeoxy Glucose Positron Emission Tomography/Computed Tomography Findings in a Rare Case of Penile Leiomyosarcoma

    Directory of Open Access Journals (Sweden)

    Kuruva Manohar

    2011-01-01

    Full Text Available Penile cancer is a rare entity accounting for only 0.4% all male malignancies. Penile leiomyosarcomas are even rarer with only around 35 cases reported in literature. We report a rare case of penile leiomyosarcoma illustrating F-18 Fluorodeoxy glucose (FDG positron emission tomography/computed tomography (PET/CT features and histopathology correlation.

  19. Symmetric increased skeletal muscular uptake of F-18 fluoro-deoxyglucose: A clue for the diagnosis of Graves' disease.

    Science.gov (United States)

    Santhosh, Sampath; Mittal, Bhagwant Rai; Kashyap, Raghava; Bhattacharya, Anish; Singh, Baljinder

    2011-07-01

    F-18 fluoro-deoxyglucose (FDG) uptake in the thyroid and thymus is well reported in patients with Graves' disease. Incidental skeletal muscle uptake has also been reported in other non-musculoskeletal (benign and malignant) pathologies. We report a patient of Graves' disease showing symmetrical skeletal muscle uptake but no thyroidal or thymus uptake of FDG.

  20. Quantification of the beta-adrenoceptor ligand S-1'[F-18]fluorocarazolol in plasma of humans, rats and sheep

    NARCIS (Netherlands)

    vanWaarde, A; Posthumus, H; Elsinga, PH; Anthonio, RL; van Loenen - Weemaes, Anne-miek; Beaufort-Krol, Gertie C. M.; Paans, AMJ; Vaalburg, W; Visser, Thomas; Visser, Gerben

    1996-01-01

    Myocardial and pulmonary beta-adrenoceptors can be imaged with 2-(S)-(-)-(9H-carbazol-4-yl-oxy)-3-[1-(fluoromethyl)ethyl]amino-2-propanol (S-1'-[F-18]fluorocarazolol, I). Quantification of unmodified fluorocarazolol in plasma is necessary for analysis of PET images in terms of receptor densities. We

  1. F-18 Polyethyleneglycol stilbenes as PET imaging agents targeting A{beta} aggregates in the brain

    Energy Technology Data Exchange (ETDEWEB)

    Zhang Wei [Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104 (United States); Oya, Shunichi [Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104 (United States); Kung Meiping [Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104 (United States); Hou, Catherine [Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104 (United States); Maier, Donna L. [Department of Neuroscience, AstraZeneca, Wilmington, DE 19850 (United States); Kung, Hank F. [Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104 (United States) and Department of Pharmacology, University of Pennsylvania, Philadelphia, PA 19104 (United States)]. E-mail: kunghf@sunmac.spect.upenn.edu

    2005-11-01

    This paper describes a novel series of {sup 18}F-labeled polyethyleneglycol (PEG)-stilbene derivatives as potential {beta}-amyloid (A{beta}) plaque-specific imaging agents for positron emission tomography (PET). In these series of compounds, {sup 18}F is linked to the stilbene through a PEG chain, of which the number of ethoxy groups ranges from 2 to 5. The purpose of adding PEG groups is to lower the lipophilicity and improve bioavailability. The syntheses of the 'cold' compounds and the {sup 18}F-labeled PEG stilbene derivatives are successfully achieved. All of the fluorinated stilbenes displayed high binding affinities in an assay using postmortem AD brain homogenates (K {sub i}=2.9-6.7 nM). Labeling was successfully performed by a substitution of the mesylate group of 10a-d by [{sup 18}F]fluoride giving the target compounds [{sup 18}F]12a-d (EOS, specific activity, 900-1500 Ci/mmol; radiochemical purity >99%). In vivo biodistribution of these novel {sup 18}F ligands in normal mice exhibited excellent brain penetrations and rapid washouts after an intravenous injection (6.6-8.1 and 1.2-2.6% dose/g at 2 and 60 min, respectively). Autoradiography of postmortem AD brain sections of [{sup 18}F]12a-d confirmed the specific binding related to the presence of A{beta} plaques. In addition, in vivo plaque labeling can be clearly demonstrated with these {sup 18}F-labeled agents in transgenic mice (Tg2576), a useful animal model for Alzheimer's disease. In conclusion, the preliminary results strongly suggest these fluorinated PEG stilbene derivatives are suitable candidates as A{beta} plaque imaging agents for studying patients with Alzheimer's disease.

  2. Synthesis and Photochromic Properties of Azido Analogues of Spiropyran and Spirooxazine as Nucleic Acid Labeling Reagent

    Institute of Scientific and Technical Information of China (English)

    Hui GUO; Wu Xin ZOU; Qi JI; Ji Ben MENG

    2005-01-01

    A series of photo active azido analogues have been synthesized and their photochromic properties have also been investigated by UV-Vis spectrum. It will be used for the rapid and reliable preparation of large amounts of stable, non-radioactive labeled DNA and RNA hybridization probes. And it is supposed to be easily detected for its photochromic properties.

  3. Synthesis of isotopically labelled 2-isopropylthioxanthone from 2,2'-dithiosalicylic acid and deuterium cumene.

    Science.gov (United States)

    Fang, Chao; Yang, Weicheng; Yang, Chao; Wang, Haoran; Sun, Kai; Luo, Yong

    2016-06-30

    Two efficient synthetic routes of stable deuterium labelled 2-isopropylthioxanthone were presented with 98.1% and 98.8% isotopic abundance in acceptable yields and excellent chemical purities. Their structures and the isotope-abundance were confirmed according to proton nuclear magnetic resonance and liquid chromatography-mass spectrometry.

  4. Synthesis of amino-group functionalized superparamagnetic iron oxide nanoparticles and applications as biomedical labeling probes

    Science.gov (United States)

    Ma, Ming; Zhan, Yanqiang; Shen, Yaqi; Xia, Xing; Zhang, Suming; Liu, Zuli

    2011-08-01

    Superparamagnetic iron oxide (SPIO) nanoparticles were synthesized by coprecipitation technique and further functionalized with amino-group to obtain amino-group functionalized (amino-SPIO) nanoparticles. The X-ray diffraction results reveal the structure of amino-SPIO nanoparticles, from which the average iron core diameter is approximately 10 nm by calculation; while Zetasizer reveals their hydrodynamic diameter are mainly distributed in the range of 40-60 nm. These nanoparticles can be taken up by liver tissue, resulting in dramatically darkening of liver tissue under T2-magnetic resonance imaging (MRI). The spin-spin relaxivity coefficient of these nanoparticles is 179.20 mM-1 s-1 in a 1.5 T magnetic resonance system. In addition, amino-SPIO nanoparticles were conjugated to Tat (FITC) peptide and incubated with neural stem cells in vitro, the authors can detect the positive-labeling (labeled) neural stem cells showing green fluorescence, which indicates Tat (FITC) peptide-derivated amino-SPIO nanoparticles are able to enter cells. Furthermore, it was also find significant negative T2 contrast enhancement when compared with the non-nanoparticles-labeled neural stem cells in T2-weighted MRI. The amino-SPIO nanoparticles show promising potential as a new type of labeling probes, which can be used in magnetic resonance-enhanced imaging and fluorescence diagnosis.

  5. Synthesis of deuterium-labelled halogen derivatives of L-tryptophan catalysed by tryptophanase.

    Science.gov (United States)

    Winnicka, Elżbieta; Szymańska, Jolanta; Kańska, Marianna

    2016-06-01

    The isotopomers of halogen derivatives of l-tryptophan (l-Trp) (4'-F-, 7'-F-, 5'-Cl- and 7'-Br-l-Trp), specifically labelled with deuterium in α-position of the side chain, were obtained by enzymatic coupling of the corresponding halogenated derivatives of indole with S-methyl-l-cysteine in (2)H2O, catalysed by enzyme tryptophanase (EC 4.1.99.1). The positional deuterium enrichment of the resulting tryptophan derivatives was controlled using (1)H NMR. In accordance with the mechanism of the lyase reaction, a 100% deuterium labelling was observed in the α-position; the chemical yields were between 23 and 51%. Furthermore, β-F-l-alanine, synthesized from β-F-pyruvic acid by the l-alanine dehydrogenase reaction, has been tested as a coupling agent to obtain the halogenated deuterium-labelled derivatives of l-Trp. The chemical yield (∼30%) corresponded to that as observed with S-methyl-l-cysteine but the deuterium label was only 63%, probably due to the use of a not completely deuterated incubation medium.

  6. A Facile Synthesis of Spin Labeled 4'-Epi-N-Trifuoroactyldaunomycin Derivatives

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    The spin labeled 4'-Epi-N-trifuoroacetyldaunomycin derivatives 6-7 were conveniently synthesized from daunomycin in middle yield. The key steps were the protection of compd. 5 at 9-position and nucleophilic displacement of 5 with R.COOH and DBU at room temperature.

  7. False-positive F-18 FDG uptake in PET/CT studies in pediatric patients with abdominal Burkitt's lymphoma.

    Science.gov (United States)

    Riad, Raef; Omar, Walid; Sidhom, Iman; Zamzam, Manal; Zaky, Iman; Hafez, Magdy; Abdel-Dayem, Hussein M

    2010-03-01

    In pediatric patients with abdominal Burkitt's lymphoma, the involvement of the gastrointestinal tract and abdominal lymph nodes are the main presenting feature of the disease. Chemotherapy is the main treatment modality and could be preceded by surgical excision of the abdominal masses. To achieve cure or long-term disease-free survival a balance has to be struck between aggressive chemotherapy and the probability of tumor necrosis secondary to treatment complicated by acute infections, perforation or intestinal bleeding. F-18 fluorodeoxyglucose-positron emission tomography/computed tomography (F-18 FDG-PET/CT) has been recommended over conventional imaging modalities for the follow-up of these patients and for monitoring treatment response. As the incidences of postchemotherapy complications are high, the positive predictive value of PET/CT studies in these patients is very low and the false-positive rate is high from acute infections and tumor necrosis. Accordingly, histopathological confirmation of positive lesions on F-18 FDG-PET/CT studies is essential. This is especially important as post-therapy complications might present with nonspecific and nonurgent symptoms. At the same time initiating a second course of salvage chemotherapy is risky. Retrospectively reviewed F-18 FDG-PET/CT studies for 28 pediatric patients with abdominal Burkitt's lymphoma and diffuse large B-cell lymphoma after their treatment with chemotherapy or surgery. Four positive studies were found. All had pathological verification and were because of acute inflammation and tumor necrosis and there was no evidence of viable tumor cells. One patient had multiple recurrent lesions in the abdomen after the initial surgical excision and before starting chemotherapy. The incidence of acute complications in this series is 10.7%. This study confirms the high incidence of tumor necrosis and inflammation after chemotherapy for the abdominal Burkitt's lymphoma and consequently, the incidence of true

  8. Very low-dose adult whole-body tumor imaging with F-18 FDG PET/CT

    Science.gov (United States)

    Krol, Andrzej; Naveed, Muhammad; McGrath, Mary; Lisi, Michele; Lavalley, Cathy; Feiglin, David

    2015-03-01

    The aim of this study was to evaluate if effective radiation dose due to PET component in adult whole-body tumor imaging with time-of-flight F-18 FDG PET/CT could be significantly reduced. We retrospectively analyzed data for 10 patients with the body mass index ranging from 25 to 50. We simulated F-18 FDG dose reduction to 25% of the ACR recommended dose via reconstruction of simulated shorter acquisition time per bed position scans from the acquired list data. F-18 FDG whole-body scans were reconstructed using time-of-flight OSEM algorithm and advanced system modeling. Two groups of images were obtained: group A with a standard dose of F-18 FDG and standard reconstruction parameters and group B with simulated 25% dose and modified reconstruction parameters, respectively. Three nuclear medicine physicians blinded to the simulated activity independently reviewed the images and compared diagnostic quality of images. Based on the input from the physicians, we selected optimal modified reconstruction parameters for group B. In so obtained images, all the lesions observed in the group A were visible in the group B. The tumor SUV values were different in the group A, as compared to group B, respectively. However, no significant differences were reported in the final interpretation of the images from A and B groups. In conclusion, for a small number of patients, we have demonstrated that F-18 FDG dose reduction to 25% of the ACR recommended dose, accompanied by appropriate modification of the reconstruction parameters provided adequate diagnostic quality of PET images acquired on time-of-flight PET/CT.

  9. A study on the synthesis, labeling and its biodistribution of estradiol derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Sang Wook; Yang, Seung Dae; Suh, Yong Sup [College of Medicine, Dongguk Univ., Seoul (Korea, Republic of)] [and others

    2000-10-01

    Due to the heterogeneous receptor distribution and changes of receptor status over time, the biochemical measurement of estrogen receptor status of biopsy specimens is not sufficient to diagnose breast cancer. As a result, I-123 labeled estradiols have been applied for the diagnosis. The purpose of this study was to develop a suitable radioligand for imaging estrogen receptor-positive human breast tumors. Among the various estradiol derivatives, 17{alpha}-[{sup 123}I]iodovinyl estradiol ([{sup 123}]IVE) has been prepared from 17{alpha}-ethynyl estradiol. Labeling of E-17{alpha}-[{sup 123}I]iodovinyl estradiol ([{sup 123}]IVE] was carried out using peracetic acid with [{sup 123}I]Nal and Z-[{sup 123}I]IVE labelling was archived using chloamine T/HCL solution with [{sup 123}I]Nal. Labeling yield was determined by silica thin-layer chromatography (TLC) and radiochemical purity was measured by high performance liquid chromatography (HPLC). The biodistribution of E-[{sup 123}I]IVE was measured in immature female rats at 60 min, 120 min and 300 min after injection. The labeling yield of two isomers was 92% and 94% (E-[{sup 123}I]IVE and Z-[{sup 123}I]IVE, respectively). The radiochemical purity was more than 98% after purification. The highest uptake was observed at 120 min in uterus (3.11% ID/g for E-[{sup 123}I]IVE. These results suggest the possibility of using E-[{sup 123}I]IVE as an imaging agent for the evaluation of the presence of estrogen receptor in patients with breast cancer.

  10. The role of F18-FDG PET scans in predicting micropapillary thyroid cancer aggressiveness

    Energy Technology Data Exchange (ETDEWEB)

    Cho, E. H.; Cho, H. J.; Kim, T. S.; Kang, W. J.; Yun, M. J.; Lee, J. D. [Severance Hospital, Seoul (Korea, Republic of)

    2007-07-01

    The purpose is to evaluate F18-FDG PET in predicting micropapillary thyroid cancer aggressiveness. 41 patients (38 female, mean age 50y) who had PET before total thyroidectomy between 2002.1{approx}2007.8 were reviewed. Patients with thyroiditis and multiple nodules were excluded. Thyroid nodules were visually analyzed into groups with increased and no FDG uptake. Peak SUV ratio of liver-to-nodule (pSUV ratio) was taken. pSUV ratio was correlated with nodule size and micropapillary cancer aggressiveness. Perithyroid extension and/or LN metastasis was used as an indicator of micropapillary cancer aggressiveness 20 patients had 0.89 and nodules with increased FDG uptake, with an average pSUV ratio of 1.67 0.15. 21 patients had nodules that were not visible, average size of 0.66 cm 0.24. FDG uptake and nodule size correlation was with an average size of 0.52 cm significant (p=0.051). The nodules were divided into two groups using a cut-off value of pSUV ratio of 0.9. 19 patients had nodules with a pSUV ratio of 0.9 or higher, and 15 of the 19 patients had perithyroid extension and/or LN metastasis. 22 patients had nodules with pSUV ratio lower than 0.9 and 7 of these patients had perithyroid extension and/or LN metastasis. Patients with higher pSUV ratio showed more perithyroid extension or LN metastasis than those with lower pSUV ratio (p=0.01). A total of 8 patients had LN metastasis, but none were visualized on PET. Higher FDG uptake seems to be significantly correlated with tumor aggressiveness in micropapillary thyroid carcinomas. But FDG uptakes in primary tumors were also correlated with tumor size. In other words, larger nodules tend to show aggressive behavior in micropapillary thyroid carcinomas and FDG it self may not be an independent factor for tumor aggressiveness. Also, PET shows an extremely poor sensitivity for the detection of LN metastasis. Therefore, PET may not have any role in the evaluation of patients with micropapillary thyroid carcinomas.

  11. F-18 HARV yaw rate expansion flight #125 with Inverted Recovery

    Science.gov (United States)

    1991-01-01

    NASA's Dryden Flight Research Center, Edwards, CA, used an F-18 Hornet fighter aircraft as its High Angle-of-Attack (Alpha) Research Vehicle (HARV) in a three-phased flight research program lasting from April 1987 until September 1996. The aircraft completed 385 research flights and demonstrated stabilized flight at angles of attack between 65 and 70 degrees using thrust vectoring vanes, a research flight control system, and (eventually) forebody strakes (hinged structures on the forward side of the fuselage to provide control by interacting with vortices, generated at high angles of attack, to create side forces). This combination of technologies provided carefree handling of a fighter aircraft in a part of the flight regime that was otherwise very dangerous. Flight research with the HARV increased our understanding of flight at high angles of attack (angle of the wings with respect to the direction in which the aircraft was heading), enabling designers of U.S. fighter aircraft to design airplanes that will fly safely in portions of the flight envelope that pilots previously had to avoid. Flight 125 with the HARV involved yaw rate expansion up to 50 degrees per second (moving the nose to the left or right at that rate). NASA research pilot Ed Schneider was the pilot, and the purpose of the flight was to look at the spin characteristics of the HARV. The sequence in this particular video clip includes the first and second maneuvers in the flight. On the first maneuver, the pilot attempted to achieve a yaw rate of 40 degrees per second and actually went to 47 degrees. The spin was oscillatory in pitch (up and down) and roll (rotating around the longitudinal axis). Recovery was normal. On the second maneuver of the flight in which Schneider tried to achieve a yaw rate of 40 degrees per second, the aircraft overshot to 54 degrees per second during an oscillatory spin. In the course of the recovery, the aircraft rolled after a large sideslip buildup. Moderate aft stick

  12. Synthesis of ( sup 18 F)fluoro-labeled progestins for PET

    Energy Technology Data Exchange (ETDEWEB)

    Groot, T.J. de; Verhagen, Aalt; Elsinga, P.H.; Vaalburg, Willem (Groningen Univ. and Hospital (Netherlands). PET Center)

    1991-01-01

    The synthesis of 21-({sup 18}F)fluoro-16{alpha}-methyl-19-norprogesterone, 21-({sup 18}F)fluoro-16{alpha}-ethyl-19-norprogesterone, 21-({sup 18}F)fluoro-16{alpha}-methylprogesterone and 21-({sup 18}F)fluoro-16{alpha}-ethylprogesterone is described. These compounds are prepared with a specific activity greater than 200 TBq/mmol (5000 Ci/mmol) from the corresponding tosylates in 10% radiochemical yield (EOB). A remote controlled system has been developed for this synthesis. (author).

  13. Metabolism of Nonessential N15-Labeled Amino Acids and the Measurement of Human Whole-Body Protein Synthesis Rates

    Science.gov (United States)

    Stein, T. P.; Settle, R. G.; Albina, J. A.; Dempsey, D. T.; Melnick, G.

    1991-01-01

    Eight N-15 labeled nonessential amino acids plus (15)NH4Cl were administered over a 10 h period to four healthy adult males using a primed-constant dosage regimen. The amount of N-15 excreted in the urine and the urinary ammonia, hippuric acid, and plasma alanine N-15 enrichments were measured. There was a high degree of consistency across subjects in the ordering of the nine compounds based on the fraction of N-15 excreted (Kendall coefficient of concordance W = 0.83, P is less than 0.01). Protein synthesis rates were calculated from the urinary ammonia plateau enrichment and the cumulative excretion of N-15. Glycine was one of the few amino acids that gave similar values by both methods.

  14. Controlled synthesis of conjugated microporous polymer films: versatile platforms for highly sensitive and label-free chemo- and biosensing.

    Science.gov (United States)

    Gu, Cheng; Huang, Ning; Gao, Jia; Xu, Fei; Xu, Yanhong; Jiang, Donglin

    2014-05-05

    Conjugated microporous polymers (CMPs), in which rigid building blocks form robust networks, are usually synthesized as insoluble and unprocessable powders. We developed a methodology using electropolymerization for the synthesis of thin CMP films. The thickness of these films is synthetically controllable, ranging from nanometers to micrometers, and they are obtained on substrates or as freestanding films. The CMP films combine a number of striking physical properties, including high porosity, extended π conjugation, facilitated exciton delocalization, and high-rate electron transfer. We explored the CMP films as versatile platforms for highly sensitive and label-free chemo- and biosensing of electron-rich and electron-poor arenes, metal ions, dopamine, and hypochloroic acid, featuring rapid response, excellent selectivity, and robust reusability.

  15. Cancer Localization in the Prostate with F-18 Fluorocholine Position Emission Tomography

    Science.gov (United States)

    2008-01-01

    sterile in- ammatory lesion was much less than uptake in an im- lanted tumor, whereas the uptake of tritium-labeled deoxy- lucose was relatively increased...injection. Al- hough the renal excretion of FCH is not ideal for evaluations f the urinary tract, it has not proven intractable in actual ractice...emission tomography for prostate, bladder, and renal cancer. Semin Nucl Med 34:274-292, 2004 0. Shreve PD, Grossman HB, Gross MD, et al: Metastatic

  16. Response Assessment and Prediction in Esophageal Cancer Patients via F-18 FDG PET/CT Scans

    Science.gov (United States)

    Higgins, Kyle J.

    Purpose: The purpose of this study is to utilize F-18 FDG PET/CT scans to determine an indicator for the response of esophageal cancer patients during radiation therapy. There is a need for such an indicator since local failures are quite common in esophageal cancer patients despite modern treatment techniques. If an indicator is found, a patient's treatment strategy may be altered to possibly improve the outcome. This is investigated with various standard uptake volume (SUV) metrics along with image texture features. The metrics and features showing the most promise and indicating response are used in logistic regression analysis to find an equation for the prediction of response. Materials and Methods: 28 patients underwent F-18 FDG PET/CT scans prior to the start of radiation therapy (RT). A second PET/CT scan was administered following the delivery of ~32 Gray (Gy) of dose. A physician contoured gross tumor volume (GTV) was used to delineate a PET based GTV (GTV-pre-PET) based on a threshold of >40% and >20% of the maximum SUV value in the GTV. Deformable registration was used in VelocityAI software to register the pre-treatment and intra-treatment CT scans so that the GTV-pre-PET contours could be transferred from the pre to intra scans (GTV-intra-PET). The fractional decrease in the maximum, mean, volume to the highest intensity 10%-90%, and combination SUV metrics of the significant previous SUV metrics were compared to post-treatment pathologic response for an indication of response. Next for the >40% threshold, texture features based on a neighborhood gray-tone dimension matrix (NGTDM) were analyzed. The fractional decrease in coarseness, contrast, busyness, complexity, and texture strength were compared to the pathologic response of the patients. From these previous two types of analysis, SUV and texture features, the two most significant results were used in logistic regression analysis to find an equation to predict the probability of a non

  17. Bovine serum albumin-directed synthesis of biocompatible CdSe quantum dots and bacteria labeling.

    Science.gov (United States)

    Wang, Qisui; Ye, Fangyun; Fang, Tingting; Niu, Wenhan; Liu, Peng; Min, Xinmin; Li, Xi

    2011-03-01

    A simple method was developed for preparing CdSe quantum dots (QDs) using a common protein (bovine serum albumin (BSA)) to sequester QD precursors (Cd(2+)) in situ. Fluorescence (FL) and absorption spectra showed that the chelating time between BSA and Cd(2+), the molar ratio of BSA/Cd(2+), temperature, and pH are the crucial factors for the quality of QDs. The average QD particle size was estimated to be about 5 nm, determined by high-resolution transmission electron microscopy. With FL spectra, Fourier transform infrared spectra, and thermogravimetric analysis, an interesting mechanism was discussed for the formation of the BSA-CdSe QDs. The results indicate that there might be conjugated bonds between CdSe QDs and -OH, -NH, and -SH groups in BSA. In addition, fluorescence imaging suggests that the QDs we designed can successfully label Escherichia coli cells, which gives us a great opportunity to develop biocompatible tools to label bacteria cells.

  18. Synthesis of Se-75 labeled catecholamine derivatives: adrenal medulla tumor specific radiopharmaceuticals

    Energy Technology Data Exchange (ETDEWEB)

    Basmadjian, G.P.; Sadek, S.; Ice, R.D. (Oklahoma Univ., Oklahoma City (USA). Health Sciences Center)

    Three classes of /sup 75/Se-labelled catecholamines have been synthesised. In class I the /sup 75/Se replaces the amine function of dopamine, using Na/sup 75/SeH. In class II the selenomethyl group replaces the -OH function in epinephrine. In class III /sup 75/Se replaces the ..beta..-carbon in catecholamine. NMR and mass spectroscopy were used to characterise the compounds.

  19. Labelling of Cells Engaged in DNA Synthesis: Autoradiography and BrdU Staining

    DEFF Research Database (Denmark)

    Madsen, Peder Søndergaard

    2010-01-01

    The cell cycle is divided in four phases: G1 phase, S phase (DNA-synthesis), G2 phase (together termed interphase) and M phase (mitosis). Cells that have ceased proliferation enter a state of quiescence called G0. M phase is itself composed of two tightly coupled processes: mitosis, in which...

  20. One-Pot Synthesis of Biocompatible CdSe/CdS Quantum Dots and Their Applications as Fluorescent Biological Labels.

    Science.gov (United States)

    Zhai, Chuanxin; Zhang, Hui; Du, Ning; Chen, Bingdi; Huang, Hai; Wu, Yulian; Yang, Deren

    2011-12-01

    We developed a novel one-pot polyol approach for the synthesis of biocompatible CdSe quantum dots (QDs) using poly(acrylic acid) (PAA) as a capping ligand at 240°C. The morphological and structural characterization confirmed the formation of biocompatible and monodisperse CdSe QDs with several nanometers in size. The encapsulation of CdS thin layers on the surface of CdSe QDs (CdSe/CdS core-shell QDs) was used for passivating the defect emission (650 nm) and enhancing the fluorescent quantum yields up to 30% of band-to-band emission (530-600 nm). Moreover, the PL emission peak of CdSe/CdS core-shell QDs could be tuned from 530 to 600 nm by the size of CdSe core. The as-prepared CdSe/CdS core-shell QDs with small size, well water solubility, good monodispersity, and bright PL emission showed high performance as fluorescent cell labels in vitro. The viability of QDs-labeled 293T cells was evaluated using a 3-(4,5-dimethylthiazol)-2-diphenyltertrazolium bromide (MTT) assay. The results showed the satisfactory (>80%) biocompatibility of as-synthesized PAA-capped QDs at the Cd concentration of 15 μg/ml.

  1. One-Pot Synthesis of Biocompatible CdSe/CdS Quantum Dots and Their Applications as Fluorescent Biological Labels

    Directory of Open Access Journals (Sweden)

    Huang Hai

    2011-01-01

    Full Text Available Abstract We developed a novel one-pot polyol approach for the synthesis of biocompatible CdSe quantum dots (QDs using poly(acrylic acid (PAA as a capping ligand at 240°C. The morphological and structural characterization confirmed the formation of biocompatible and monodisperse CdSe QDs with several nanometers in size. The encapsulation of CdS thin layers on the surface of CdSe QDs (CdSe/CdS core–shell QDs was used for passivating the defect emission (650 nm and enhancing the fluorescent quantum yields up to 30% of band-to-band emission (530–600 nm. Moreover, the PL emission peak of CdSe/CdS core–shell QDs could be tuned from 530 to 600 nm by the size of CdSe core. The as-prepared CdSe/CdS core–shell QDs with small size, well water solubility, good monodispersity, and bright PL emission showed high performance as fluorescent cell labels in vitro. The viability of QDs-labeled 293T cells was evaluated using a 3-(4,5-dimethylthiazol-2-diphenyltertrazolium bromide (MTT assay. The results showed the satisfactory (>80% biocompatibility of as-synthesized PAA-capped QDs at the Cd concentration of 15 μg/ml.

  2. Synthesis of sup 11 C-labeled imipramine and its biodistribution in mice; A potential tracer for positron emission tomography

    Energy Technology Data Exchange (ETDEWEB)

    Nakamura, Hitoshi; Edo, Kiyoto; Hishinuma, Takanori; Mizugaki, Michinao (Tohoku University Hospital, Sendai (Japan). Department of Pharmaceutical Sciences); Takahashi, Toshihiro; Ido, Tatsuo

    1989-12-01

    A tricyclic antidepressant, {sup 11}C-labeled imipramine was synthesized by N-methylation of desipramine with {sup 11}CH{sub 3}I to assist in the imaging of the human imipramine receptor by positron emission tomography. The radiochemical yield after purification of {sup 11}C-imipramine by high performance liquid chromatography was 28-63% at a specific activity of 26-53 Ci/mmol. The time required for synthesis, including purification was 30 min from the end of {sup 11}CH{sub 3}I trapping. The organ distribution of {sup 11}C-imipramine was investigated in mice at various times after i.v. injection. The main accumulation of radioactivity was in the kidney, followed by the lung and the heart. In the brain, the radioactivity levels in the hypothalamus and striatum were the highest and remained constant, differentiating them from other portions of the brain. Furthermore, the result of a binding assay with {sup 3}H-labeled imipramine suggested that the regional distribution of {sup 11}C-imipramine in the same mouse brain correlated to that of the high affinity imipramine binding site. (author).

  3. Synthesis and tissue distribution of four Se-labeled tertiary amines, potential brain pH imaging agents.

    Science.gov (United States)

    Plenevaux, A; Cantineau, R; Brihaye, C; Lemaire, C; Christiaens, L; Guillaume, M

    1990-01-01

    Four new tertiary amines: bis(3-N,N-dimethyl aminopropyl)selenide (PROMOSE), bis(3-N-(morpholino)propyl)selenide, N-methyl-selenomorpholine and N-phenyl-selenomorpholine structurally related to MOSE proposed by Kung and Blau, have been labeled through a radiochemical procedure suitable for both 75Se and 73Se. The radiochemical yields of the carrier added synthesis ranged between 64 and 85% for the four 75Se labelings and was 64% EOB time corrected for [73Se]PROMOSE. The chemical and radiochemical purities were higher than 99% after chromatographic purifications. The n-octanol/phosphate buffer partition coefficients (P) were measured at various pH (6.5-8) for each compound and the tissue distributions of PROMOSE in rats were also carried out. The experimental results showed a good correlation between the P = f(pH) function and the in vivo behaviour of the considered compound. PROMOSE was selected for further investigations as a brain pH indicator.

  4. Synthesis of carbon-11 labeled dexetimide and levetimide for studying muscarinic acetylcholine receptors

    Energy Technology Data Exchange (ETDEWEB)

    Dannals, R.F.; Langstrom, B.; Ravert, H.T.; Wilson, A.A.; Wagner, H.N. Jr.

    1985-05-01

    The localization and quantitation of the muscarinic acetylcholine receptor (m-AChR) in the living human brain using a non-invasive method, such as positron emission tomography (PET), may provide valuable information about receptor changes which have been observed post mortem in patients with Huntington's chorea and Alzheimer's dementia, as well as normal brain mechanisms mediated by the m-AChR. Although quinuclidinyl benzilate has been radioiodinated and radiomethylatd, the former is not useful with PET and the latter does not penetrate the blood-brain barrier; therefore, the authors chose to radiolabel dexetimide, a ligand which labels m-AChR in vitro and in vivo, and levetimide, its inactive enantiomer. Carbon-11 labeled carbon dioxide is bubbled through a tetrahydrofuran (THF) solution of phenylmagnesium chloride (1 M, l ml) after which 2 mg of lithium aluminium hydride is added in THF (500 ..mu..l). After evaporation of the solvent, 48% hydriodic acid (l ml) is added and the solution is heated for 1 minute. Carbon-11 labeled benzyl iodide is extracted into methylene chloride, added to a solution of nor-benzyl dexetimide or levetimide, and heated for several minutes. Purification is accomplished using semi-preparative reverse phase high performance liquid chromatography (HPLC). Analytical HPLC is used to determine the radiochemical purity and specific activity.

  5. The Diagnosis and Prevention of Florbetapir F18 in Alzheimer's Disease%略谈Florbetapir F18在阿尔茨海默病诊断和防治中的应用

    Institute of Scientific and Technical Information of China (English)

    蒋雨平; 林伟

    2013-01-01

    阿尔茨海默病(AD)的临床诊断尚存在一定问题,确诊必须要有生物学诊断标准的辅助.正电子发射断层(PET)显像是诊断AD的一项极具临床应用前景的生物学检测方法,本文介绍Florbetapir F18(18F-AV-45)PET显像的研究进展.%The definitive diagnosis of Alzheimer's disease(AD) are hampered by the lack of effective biomarkers of the underlying pathology. The positron emission tomographic (PET) is one of the most potential biomarker of clinical diagnosis of Alzheimer disease. The progress of florbetapir F18(18F-AV-45)PET imaging to identify β-amyloid pathology in the brains of individuals during life were introduced.

  6. F-18 fluorodeoxyglucose position emission tomography/computed tomography imaging for diagnosing ovarian small cell carcinoma of the hypercalcaemic type

    Energy Technology Data Exchange (ETDEWEB)

    Park, Soon Ah; Kim, Hun Soo [Wonkwang University School of Medicine and Institute of Wonkwang Medical Science, Iksan (Korea, Republic of); Oldan, Jorge Daniel [Radiology, Cardiovascular Imaging at the Cleveland Clinic, Cleveland (United States)

    2016-03-15

    A 19-year-old woman presented with lower abdominal pain. Laboratory results showed elevated levels of ionized calcium 1.85 mmol/1, and total calcium, 3.75 mmol/1, but a low level of parathyroid hormone, 1.2 ng/l. This F-18 FDG PET/CT study demonstrated a hypermetabolic unilateral complex mass, composed of solid and necrotic portions, with a concomitant increase in FDG uptake on osteolytic lesions throughout the axial breakdown of bone. In young women, pelvic neoplasms are often difficult to characterize with imaging, because it is often difficult to classify a tumor as benign or malignant based on its appearance on imaging studies. Therefore, features such as ovarian masses in girl and adolescents, a high calculcium level, and the diffuse FDG-avid asterolytic lesions on F-18 FDG PET/CT are probably suggestive of a malignant OSCCHT secreting the PTH-rP.

  7. F18-FDG-PET/CT for evaluation of intraductal papillary mucinous neoplasms (IPMN): a review of the literature.

    Science.gov (United States)

    Bertagna, Francesco; Treglia, Giorgio; Baiocchi, Gian Luca; Giubbini, Raffaele

    2013-04-01

    Intraductal papillary mucinous neoplasms (IPMN) are intraductal mucin-producing neoplasms with tall columnar, mucin-containing epithelium, with or without papillary projections, involving the main pancreatic duct and/or major side branches. They account for approximately 25 % of all cystic neoplasms and can be subdivided into benign lesions, borderline lesions, and carcinoma. In this clinical scenario accurate preoperative diagnosis can eliminate unnecessary surgery, which is risky and potentially harmful, yet enable effective selection of patients who are candidates for surgery. In this review we try to provide a complete evaluation of the use of F18-FDG-PET/CT for diagnosis of this neoplasm on the basis of published papers. F18-FDG-PET/CT seems to be an useful technique for preoperative work-up of patients with suspected IPMN and is an improvement over conventional imaging in distinguishing benign from malignant lesions, especially for selecting patients for surgical treatment or for long-term follow-up.

  8. Hot-atom synthesis of tritium-labeled mixed methyl-phenyl phosphonium derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Nefedov, V.D.; Toropova, M.A.; Shchepina, N.E.; Avrorin, V.V.; Shchepin, V.V.; Zhuravlev, V.E.

    1987-11-01

    The hot-atom method has been used with tritiated phenyl cations and organic phosphines to synthesize tritiated mixed methyl-phenyl onium derivatives of phosphorus. The replacement of phenyl groups by various numbers of methyl ones in the initial phosphines and correspondingly in the phosphonium compounds has provided a means of examining the effects of stearic and electronic factors on the formation of organic onium phosphorus derivatives. The yields are given for the phosphonium derivatives produced by heterolytic decomposition of labeled diphenyl; the relative reactivities of the phosphines have been determined together with the stabilities of the substituted phosphonium cations.

  9. A novel synthesis of carbon-labelled quinolone-3-carboxylic acid antibacterials

    Energy Technology Data Exchange (ETDEWEB)

    Carr, R.M.; Sutherland, D.R. (Glaxo Research and Development Ltd., Greenford (United Kingdom). Isotope Chemistry Group)

    1994-10-01

    3-Iodoquinolones were prepared from the corresponding quinolone-3-carboxylic acids by Hunsdiecker-type iododecarboxylation reactions with lead tetraacetate and iodine. Cyanation of the iodo compounds with mixtures of potassium [[sup 13]C]cyanide and copper (1) iodide, gave [3-[sup 13]C]cyanoquinolones which on acidic hydrolysis afforded quinolone-[3-[sup 13]C]carboxylic acids. In this way, nalidixic acid, an immediate precursor of norfloxacin, and quinolone WIN57273 were labelled with carbon-13 in the metabolically stable carboxylic acid fragment. (author).

  10. Correlation of Glut-1 and Glut-3 expression with F-18 FDG uptake in pulmonary inflammatory lesions

    OpenAIRE

    Wang, Zhen Guang; Yu, Ming Ming; Han, Yu; Wu, Feng Yu; Yang, Guang Jie; Li, Da Cheng; Liu, Si Min

    2016-01-01

    Abstract The aim of the study was to investigate the correlation of glucose transporter-1 (Glut-1) and glucose transporter-3 (Glut-3) expression with F-18 FDG uptake in pulmonary inflammatory lesions. Twenty-two patients with pulmonary inflammatory lesions underwent positron emission tomography/computed tomography (PET/CT) examination preoperatively, and Glut-1 and Glut-3 expression were detected by immunohistochemistry in these lesions. Correlations of Glut-1 and Glut-3 with 18F-FDG uptake w...

  11. Correlation of Glut-1 and Glut-3 expression with F-18 FDG uptake in pulmonary inflammatory lesions.

    Science.gov (United States)

    Wang, Zhen Guang; Yu, Ming Ming; Han, Yu; Wu, Feng Yu; Yang, Guang Jie; Li, Da Cheng; Liu, Si Min

    2016-11-01

    The aim of the study was to investigate the correlation of glucose transporter-1 (Glut-1) and glucose transporter-3 (Glut-3) expression with F-18 FDG uptake in pulmonary inflammatory lesions.Twenty-two patients with pulmonary inflammatory lesions underwent positron emission tomography/computed tomography (PET/CT) examination preoperatively, and Glut-1 and Glut-3 expression were detected by immunohistochemistry in these lesions. Correlations of Glut-1 and Glut-3 with F-FDG uptake were assessed using Spearman's rank correlation test.The maximum standardized uptake value (SUVmax) of pulmonary inflammatory lesions in 22 patients was 0.50 to 7.50, with a mean value of 3.66 ± 1.62. Immunohistochemical staining scores of Glut-1 and Glut-3 were 2.18 ± 0.96 and 2.82 ± 1.37, respectively. The expression of Glut-1 and Glut-3 was positively correlated with F-18 FDG uptake. Glut-3 expression was evidently higher than Glut-1 expression in 22 patients.Glut-1 and Glut-3 expressions are high in pulmonary inflammatory lesions, and Glut-3 plays a more important role in F-18 FDG uptake in pulmonary inflammatory lesions.

  12. Synthesis, characterization and theranostic evaluation of Indium-111 labeled multifunctional superparamagnetic iron oxide nanoparticles.

    Science.gov (United States)

    Zolata, Hamidreza; Abbasi Davani, Fereydoun; Afarideh, Hossein

    2015-02-01

    Indium-111 labeled, Trastuzumab-Doxorubicin Conjugated, and APTES-PEG coated magnetic nanoparticles were designed for tumor targeting, drug delivery, controlled drug release, and dual-modal tumor imaging. Superparamagnetic iron oxide nanoparticles (SPIONs) were synthesized by thermal decomposition method to obtain narrow size particles. To increase SPIONs circulation time in blood and decrease its cytotoxicity in healthy tissues, SPIONs surface was modified with 3-Aminopropyltriethoxy Silane (APTES) and then were functionalized with N-Hydroxysuccinimide (NHS) ester of Polyethylene Glycol Maleimide (NHS-PEG-Mal) to conjugate with thiolated 3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene-3,6,9,-triacetic acid (PCTA) bifunctional chelator (BFC) and Trastuzumab antibody. In order to tumor SPECT/MR imaging, SPIONs were labeled with Indium-111 (T1/2=2.80d). NHS ester of monoethyl malonate (MEM-NHS) was used for conjugation of Doxorubicin (DOX) chemotherapeutic agent onto SPIONs surface. Mono-Ethyl Malonate allows DOX molecules to be attached to SPIONs via pH-sensitive hydrazone bonds which lead to controlled drug release in tumor region. Active and passive tumor targeting were achieved through incorporated anti-HER2 (Trastuzumab) antibody and EPR effect of solid tumors for nanoparticles respectively. In addition to in vitro assessments of modified SPIONs in SKBR3 cell lines, their theranostic effects were evaluated in HER2 + breast tumor bearing BALB/c mice via biodistribution study, dual-modal molecular imaging and tumor diameter measurements.

  13. Synthesis,labelling and animal experiments of the derivative of phenylpentadecanoic acid(CACPPA)

    Institute of Scientific and Technical Information of China (English)

    WuChun-Ying; JiShu-Ren; 等

    1998-01-01

    The synthsis and biodistribution were discrideb for 99mTc labelled fatty acid,p[N,N'-di-carboxymethy]) aminomethyl carboxyamino]-phenylpentadecanoic acid(CACPPA).99mTc-CACPPA was prepared by the reduction of Na99mTcO4 with stannous chloride in aqueous solution at pH 8.5-9.5,the labelling yield and chemical purity were over 90% determined by TLC and HPLC.Biodistribution of 99mTc-CACPPA in mice demonstrated that the highest myocardial uptake of 99mTc-CACPPA was 18.17±2.67%ID/g,When blood disappearance of 99mTc-CACPPA was analysed with a biexponential model,an initial half time of 1.11min and a late half time of 20.08min were obtained.99mTc-CACPPA exhibited high binding to HSA in vitro,and partition coefficients were 10.98and 11.45 at pH7.00 and pH7.40,respectively.

  14. Chiral dimethylamine flutamide derivatives-modeling, synthesis, androgen receptor affinities and carbon-11 labeling

    Energy Technology Data Exchange (ETDEWEB)

    Jacobson, Orit [Department of Medical Biophysics and Nuclear Medicine, Hebrew University of Jerusalem, Hadassah Hospital, Jerusalem 91120 (Israel); Laky, Desideriu [Department of Medical Biophysics and Nuclear Medicine, Hebrew University of Jerusalem, Hadassah Hospital, Jerusalem 91120 (Israel); Carlson, Kathryn E. [Department of Chemistry, University of Illinois, Urbana, IL 61801 (United States); Elgavish, Sharona [Bioinformatics Unit, Hebrew University of Jerusalem, Jerusalem 91120 (Israel); Gozin, Michael [School of Chemistry, Raymond and Beverly Sackler Faculty of Exact Sciences, Tel Aviv University, Tel Aviv 69978 (Israel); Even-Sapir, Einat [Department of Nuclear Medicine, Tel Aviv Sourasky Medical Center, Sackler School of Medicine, Tel Aviv University, Tel Aviv 64239 (Israel); Leibovitc, Ilan [Department of Urology, Meir Medical Center, Sackler School of Medicine, Tel Aviv University, Kfar Sava 44281 (Israel); Gutman, Mordechai [Department of Surgery A, Sapir Medical Center, Sackler School of Medicine, Tel Aviv University, Kfar Sava 44281 (Israel); Chisin, Roland [Department of Medical Biophysics and Nuclear Medicine, Hebrew University of Jerusalem, Hadassah Hospital, Jerusalem 91120 (Israel); Katzenellenbogen, John A. [Department of Chemistry, University of Illinois, Urbana, IL 61801 (United States); Mishani, Eyal [Department of Medical Biophysics and Nuclear Medicine, Hebrew University of Jerusalem, Hadassah Hospital, Jerusalem 91120 (Israel)]. E-mail: mishani@md.huji.ac.il

    2006-08-15

    Most prostate cancers are androgen dependent upon initial diagnosis. On the other hand, some very aggressive forms of prostate cancer were shown to have lost the expression of the androgen receptor (AR). Although the AR is routinely targeted in endocrine treatment, the clinical outcome remains suboptimal. Therefore, it is crucial to demonstrate the presence and activity of the AR in each case of prostate cancer, before and after treatment. While noninvasive positron emission tomography (PET) has the potential to determine AR expression of tumor cells in vivo, fully optimized PET imaging agents are not yet available. Based on molecular modeling, three novel derivatives of hydroxyflutamide (Compounds 1-3) were designed and synthesized. They contain an electron-rich group (dimethylamine) located on the methyl moiety, which may confer a better stability to the molecule in vivo. Compounds 1-3 have AR binding that is similar or higher than that of the currently used commercial drugs. An automated carbon-11 radiolabeling route was developed, and the compounds were successfully labeled with a 10-15% decay-corrected radiochemical yield, 99% radiochemical purity and a specific activity of 4Ci/{mu}mol end of bombardment (n=15). These labeled biomarkers may facilitate the future quantitative molecular imaging of AR-positive prostate cancer using PET and may also allow for image-guided treatment of prostate cancer.

  15. Quantifying protein synthesis and degradation in Arabidopsis by dynamic 13CO2 labeling and analysis of enrichment in individual amino acids in their free pools and in protein.

    Science.gov (United States)

    Ishihara, Hirofumi; Obata, Toshihiro; Sulpice, Ronan; Fernie, Alisdair R; Stitt, Mark

    2015-05-01

    Protein synthesis and degradation represent substantial costs during plant growth. To obtain a quantitative measure of the rate of protein synthesis and degradation, we supplied (13)CO2 to intact Arabidopsis (Arabidopsis thaliana) Columbia-0 plants and analyzed enrichment in free amino acids and in amino acid residues in protein during a 24-h pulse and 4-d chase. While many free amino acids labeled slowly and incompletely, alanine showed a rapid rise in enrichment in the pulse and a decrease in the chase. Enrichment in free alanine was used to correct enrichment in alanine residues in protein and calculate the rate of protein synthesis. The latter was compared with the relative growth rate to estimate the rate of protein degradation. The relative growth rate was estimated from sequential determination of fresh weight, sequential images of rosette area, and labeling of glucose in the cell wall. In an 8-h photoperiod, protein synthesis and cell wall synthesis were 3-fold faster in the day than at night, protein degradation was slow (3%-4% d(-1)), and flux to growth and degradation resulted in a protein half-life of 3.5 d. In the starchless phosphoglucomutase mutant at night, protein synthesis was further decreased and protein degradation increased, while cell wall synthesis was totally inhibited, quantitatively accounting for the inhibition of growth in this mutant. We also investigated the rates of protein synthesis and degradation during leaf development, during growth at high temperature, and compared synthesis rates of Rubisco large and small subunits of in the light and dark.

  16. Construction and evaluation of F-18 FDG PET probabilistic MAP for voxel based analysis of the rat brain

    Energy Technology Data Exchange (ETDEWEB)

    Im, K. C.; Kim, J. S.; Na, Y. S.; Moon, D. H.; Ryu, J. S. [Asan Medical Center, Seoul (Korea, Republic of)

    2007-07-01

    The purpose of this study was to develop F-18 FDG PET and MRI template for normal rat brain. Also, feasibility of SPM in detailed regional analysis of molecular changes in the rat brain was explored for F-18 FDG PET imaging of a model of traumatic brain injury (TBI). Ten normal rats were scanned with PET and MRI. The PET images were acquired with 3D mode using microPET focus 120 scanner after injection of 37 MBq F-18 FDG. T2-weighted MR images were acquired using 4.7T MRI system. A MRI-based spatial normalization was used. The PET images were coregistered to T2-weighted MR images. Maximum mutual information (MMI) registrations and affine spatial normalizations were performed using SPM2. The spatial normalization of the MRI to the standard MRI was applied to the integral images. The normalized PET images were averaged voxel wise to create PET template. Eight TBI model rats were subjected to a moderate lateral fluid percussion injury. At 2 days, 1 week, 3 weeks and 5 weeks post FPI, PET images of 8 TBI rats were acquired 4 times. TBI PET images were realigned, spatially normalized to a created PET-template and smoothed (8 mm FWHM). To assess the extent and severity of significant hypo metabolic lesions in TBI compared to normal controls were obtained by a two-sided t-test of SPM (uncorrected p < 0.001, 50 voxels). Visually acceptable PET and MRI templates were created. Registration errors were negligible when MMI procedure was used to register a translated or rotated image volume. Thirty-two PET studies of 8 TBI model subjects were obtained. SPM analysis showed injured distribution of decrease F-18 FDG uptake in TBI rats compared with normal rats. In SPM analysis, the extent and severity of significant hypo metabolic lesions were decreased according to a significant effect of time. At 5 weeks injured animals showed F-18 FDG uptake recovery using SPM analysis. These results indicate that voxel-based method will be useful for future longitudinal studies of rat brain.

  17. A Randomised Controlled Trial Assessing the Effect of Oral Diazepam on F-18-FDG Uptake in the Neck and Upper Chest Region

    NARCIS (Netherlands)

    Sturkenboom, M.G.G.; Hoekstra, O.S.; Postema, E.J.; Zijlstra-Baalbergen, J.M.; Berkhof, J.; Franssen, E.J.F.

    2009-01-01

    A distinctive pattern of physiological symmetrical uptake of F-18-fluorodeoxyglucose (F-18-FDG) in the neck and upper chest region is a phenomenon that is sometimes observed on positron emission tomography (PET) scans of some oncologic patients. Initially, it was assumed to be muscle uptake secondar

  18. F-18 FLT PET : A Noninvasive Diagnostic Tool for Visualization of the Bone Marrow Compartment in Patients With Aplastic Anemia A Pilot Study

    NARCIS (Netherlands)

    Agool, Ali; Slart, Riemer H. J. A.; Kluin, Philip M.; de Wolf, Joost Th. M.; Dierckx, Rudi A. J. O.; Vellenga, Edo

    2011-01-01

    Rationale: A discordant relationship between bone marrow cellularity and peripheral blood findings is regularly noticed in patients with aplastic anemia (AA). Therefore, the feasibility of 3-F-18 fluoro-3-deoxy-L-thymidine (F-18 FLT PET was tested as a noninvasive tool to visualize the total distrib

  19. Manipulation of [C-11]-5-hydroxytryptophan and 6-[F-18]fluoro-3,4-dihydroxy-L-phenylalanine accumulation in neuroendocrine tumor cells

    NARCIS (Netherlands)

    Neels, Oliver C.; Koopmans, Klaas P.; Jager, Pieter L.; Vercauteren, Laya; van Waarde, Aren; Doorduin, Janine; Timmer-Bosscha, Hetty; Brouwers, Adrienne H.; de Vries, Elisabeth G. E.; Dierckx, Rudi A. J. O.; Kema, Ido P.; Elsinga, Philip H.

    2008-01-01

    [C-11]-5-Hydroxytryptophan ([C-11]HTP) and 6-[F-18]fluoro-3,4-dihydroxy-L-phenylalanine [F-18]FDOPA) are used to image neuroendocrine tumors with positron emission tomography. The precise mechanism by which these tracers accumulate in tumor cells is unknown. We aimed to study tracer uptake via large

  20. [C-11]FMAU and [F-18]FHPG as PET tracers for herpes simplex virus thymidine kinase enzyme activity and human cytomegalovirus infections

    NARCIS (Netherlands)

    de Vries, EFJ; van Waarde, A; Harmsen, MC; Mulder, NH; Vaalburg, W; Hospers, GAP

    [C-11]-2'-Fluoro-5-methyl-1-beta-D-arabinofuranosyluracil ([C-11]FMAU) and [F-18]-9-[(3-fluoro-1-hydroxy-2-propoxy)methyl]guanine ([F-18]FHPG), radiolabeled representatives of two classes of antiviral agents, were evaluated as tracers for measuring herpes simplex virus thymidine kinase (HSV-tk)

  1. Synthesis of carbon-14 labelled spiro-piperidyl-rifamycins (LM 118) and rifabutin (LM 427)

    Energy Technology Data Exchange (ETDEWEB)

    Fontana, E.; Giarda, S.; Vioglio, S.; Vicario, G.P.

    1987-11-01

    The syntheses of radiolabelled spiro-piperidyl-rifamycins are described. A five steps synthesis (Scheme 1) was performed to give 4-deoxo-3,4-(2-spiro-(N-(/sup 14/C)methyl-4-piperidyl))-(1H)-imidazo-(2,5-di-hydro)-rifamycin S ((/sup 14/C)LM 118), in an overall radiochemical yield of approx. 20%, 98% radiochemically pure and with a specific activity of 440 MBq/mmol (11.9 mCi/mmol) starting from (/sup 14/C)methyl iodide. A three steps synthesis (Scheme 2) was performed to give 4-deoxo-3,4-(2-spiro-(N-2-methyl(1-/sup 14/C)propane-4-piperidyl))-(1H)-imida-zo-(2,5-dihydro)-rifamycin S ((/sup 14/C) rifabutin) in an overall radiochemical yield of approx. 38%, 97% radiochemically pure with a specific activity of 1.27 GBq/mmol (34.32 m/Ci/mmol). 1-(2-Methyl (1-/sup 14/C)propanoyl)-piperazin-4-one ethylene ketal was employed as starting material.

  2. Usefulness of F-18 FDG PET/CT in subcutaneous panniculitis-like T cell lymphoma: disease extent and treatment response evaluation.

    Science.gov (United States)

    Kim, Jin-Suk; Jeong, Young Jin; Sohn, Myung-Hee; Jeong, Hwan-Jeong; Lim, Seok Tae; Kim, Dong Wook; Kwak, Jae-Yong; Yim, Chang-Yeol

    2012-12-01

    BACKGROUND.: Subcutaneous panniculitis-like T-cell lymphoma (SPTCL) is a rare form of cutaneous lymphomas, accounting for less than 1% of cases of non-Hodgkin's lymphoma. Fluorine-18 fluorodeoxyglucose (F-18 FDG) positron-emission tomography/computed tomography (PET/CT) findings of SPTCL before and after treatment were rarely reported. CASE REPORT.: We report a case of SPTCL in which F-18 FDG PET/CT showed increased FDG accumulations in numerous subcutaneous nodules without extracutaneous disease. Contrast-enhanced CT during F-18 FDG PET/CT showed multiple minimally enhancing nodules with an infiltrative pattern in the subcutaneous layer throughout the body. Follow-up F-18 FDG PET/CT after three cycles of CHOP chemotherapy showed a complete metabolic remission of the lesions. CONCLUSIONS.: F-18 FDG PET/CT is suggested to be useful in assessing the disease activity, extent and treatment response in SPTCL.

  3. Completion of proteomic data sets by Kd measurement using cell-free synthesis of site-specifically labeled proteins.

    Directory of Open Access Journals (Sweden)

    Paul Majkut

    Full Text Available The characterization of phosphotyrosine mediated protein-protein interactions is vital for the interpretation of downstream pathways of transmembrane signaling processes. Currently however, there is a gap between the initial identification and characterization of cellular binding events by proteomic methods and the in vitro generation of quantitative binding information in the form of equilibrium rate constants (Kd values. In this work we present a systematic, accelerated and simplified approach to fill this gap: using cell-free protein synthesis with site-specific labeling for pull-down and microscale thermophoresis (MST we were able to validate interactions and to establish a binding hierarchy based on Kd values as a completion of existing proteomic data sets. As a model system we analyzed SH2-mediated interactions of the human T-cell phosphoprotein ADAP. Putative SH2 domain-containing binding partners were synthesized from a cDNA library using Expression-PCR with site-specific biotinylation in order to analyze their interaction with fluorescently labeled and in vitro phosphorylated ADAP by pull-down. On the basis of the pull-down results, selected SH2's were subjected to MST to determine Kd values. In particular, we could identify an unexpectedly strong binding of ADAP to the previously found binding partner Rasa1 of about 100 nM, while no evidence of interaction was found for the also predicted SH2D1A. Moreover, Kd values between ADAP and its known binding partners SLP-76 and Fyn were determined. Next to expanding data on ADAP suggesting promising candidates for further analysis in vivo, this work marks the first Kd values for phosphotyrosine/SH2 interactions on a phosphoprotein level.

  4. Completion of proteomic data sets by Kd measurement using cell-free synthesis of site-specifically labeled proteins.

    Science.gov (United States)

    Majkut, Paul; Claußnitzer, Iris; Merk, Helmut; Freund, Christian; Hackenberger, Christian P R; Gerrits, Michael

    2013-01-01

    The characterization of phosphotyrosine mediated protein-protein interactions is vital for the interpretation of downstream pathways of transmembrane signaling processes. Currently however, there is a gap between the initial identification and characterization of cellular binding events by proteomic methods and the in vitro generation of quantitative binding information in the form of equilibrium rate constants (Kd values). In this work we present a systematic, accelerated and simplified approach to fill this gap: using cell-free protein synthesis with site-specific labeling for pull-down and microscale thermophoresis (MST) we were able to validate interactions and to establish a binding hierarchy based on Kd values as a completion of existing proteomic data sets. As a model system we analyzed SH2-mediated interactions of the human T-cell phosphoprotein ADAP. Putative SH2 domain-containing binding partners were synthesized from a cDNA library using Expression-PCR with site-specific biotinylation in order to analyze their interaction with fluorescently labeled and in vitro phosphorylated ADAP by pull-down. On the basis of the pull-down results, selected SH2's were subjected to MST to determine Kd values. In particular, we could identify an unexpectedly strong binding of ADAP to the previously found binding partner Rasa1 of about 100 nM, while no evidence of interaction was found for the also predicted SH2D1A. Moreover, Kd values between ADAP and its known binding partners SLP-76 and Fyn were determined. Next to expanding data on ADAP suggesting promising candidates for further analysis in vivo, this work marks the first Kd values for phosphotyrosine/SH2 interactions on a phosphoprotein level.

  5. Monitoring of Tumor Response to Neoadjuvant Radio-Chemotherapy of Esophageal Carcinoma by F-18-FDG-PET%F-18-FDG-PET监测新辅助疗法食管癌的反应

    Institute of Scientific and Technical Information of China (English)

    Peter Theissen; Paul M.Schneider; Stephan E.Baldus; Alexandra Jost; Markus Dietlein; Rolf P.Müller; Arnulf H.H(o)lscher; Harald Schicha

    2004-01-01

    Introduction: For clinical assessment of neoadjuvant radiochemotherapy of esophageal cancer reliable in-vivo methods are necessary. Therefore, the capabilities of F-18-Fluorodesoxyglucose-PET in comparison to histomorphological grading of tumor regression were studied. Methods: In 33 patients with locally advanced esophageal carcinoma (uT3, uN0-1, cM0) F-18-FDG-PET was performed before and 2weeks after radiochemotherapy. All tumors were resected by transthoracic en-bloc esophagectomy 3-4 weeks after induction therapy. A subgroup of 11 patients underwent weekly PET scan during neoadjuvant therapy.PET was performed in a dedicated scanner 1.3 h after administration of 370 MBq F-18-FDG. Data analysis based on maximum SUV data derived from individual regions of interest in pre- and posttherapeutic images. PET data were compared to histomorphological grading parameters for tumor regression whithin the resected tissues. Results: The comparison of histopathological tumor regression after neoadjuvant therapy and PET SUV differences showed a significant X2 P-value of 0.006. There was a significant decrease of the SUV data from 9.1±3.5 to 4.3±1.9 (P<0.0001). In therapy responders SUV was diminished by 59% and in non-responders by 34 %. Longitudinal SUV measurement during neoadjuvant therapy showed a strong SUV decrease already after one and two weeks (P=-0.021 and 0.003). Conclusion: The recent data of the FDG-PET follow-up after neoadjuvant therapy show that PET is able to predict therapy response.Longitudinal PET data advocate that it may be possible to recognize response also very early during radiochemotherapy.

  6. Elucidating the Stereochemistry of Enzymatic Benzylsuccinate Synthesis with Chirally Labeled Toluene.

    Science.gov (United States)

    Seyhan, Deniz; Friedrich, Peter; Szaleniec, Maciej; Hilberg, Markus; Buckel, Wolfgang; Golding, Bernard T; Heider, Johann

    2016-09-12

    Benzylsuccinate synthase is a glycyl radical enzyme that initiates anaerobic toluene metabolism by adding fumarate to the methyl group of toluene to yield (R)-benzylsuccinate. To investigate whether the reaction occurs with retention or inversion of configuration at the methyl group of toluene, we synthesized both enantiomers of chiral toluene with all three H isotopes in their methyl groups. The chiral toluenes were converted into benzylsuccinates preferentially containing (2) H and (3) H at their benzylic C atoms, owing to a kinetic isotope effect favoring hydrogen abstraction from the methyl groups. The configuration of the products was analyzed by enzymatic CoA-thioester synthesis and stereospecific oxidation using enzymes involved in benzylsuccinate degradation. Assessment of the configurations of the benzylsuccinate isomers based on loss or retention of tritium showed that inversion of configuration at the methyl group occurs when the chiral toluenes react with fumarate.

  7. Improved synthesis of anti-[18F]FACBC: improved preparation of labeling precursor and automated radiosynthesis.

    Science.gov (United States)

    McConathy, Jonathan; Voll, Ronald J; Yu, Weiping; Crowe, Ronald J; Goodman, Mark M

    2003-06-01

    The non-natural amino acid anti-1-amino-3-[18F]fluorocyclobutyl-1-carboxylic acid (FACBC) has shown promise for tumor imaging with positron emission tomography. An improved synthesis of the precursor of anti-[18F]FACBC has been devised which demonstrates high stereoselectivity and suitability for large-scale preparations. An automated radiosynthesis has been developed which provides anti-[18F]FACBC in 24% decay-corrected yield. Additionally, the major non-radioactive species present in doses of anti-[18F]FACBC has been identified as anti-1-amino-3-hydroxycyclobutane-1-carboxylic acid. Together, these results are important steps towards the routine production of anti-[18F]FACBC for human use.

  8. Synthesis of acetylene-substituted probes with benzene-phosphate backbones for RNA labeling.

    Science.gov (United States)

    Kitamura, Yoshiaki; Ueno, Yoshihito; Kitade, Yukio

    2014-06-24

    Conversion of dimethyl 5-aminoisophthalate into the iodoarene via the corresponding diazonium intermediate, followed by Sonogashira coupling with trimethylsilylacetylene afford the alkynylarene, which is reduced with LiAlH4 to give 5-ethynyl-1,3-benzenedimethanol (B(E)). One hydroxyl group is protected with a 4,4'-dimethoxytrityl (DMTr) group and subsequently another hydroxyl group is phosphitylated to produce the phosphoramidite. The mono-DMTr compound is also modified to afford the corresponding succinate, which is then reacted with controlled pore glass (CPG) to provide the solid support. Either the phosphoramidite or the solid support is employed in solid-phase synthesis of RNA containing B(E). RNA oligomers bearing B(E) rapidly react with 4-fluorobenzylazide to produce the cycloaddition products in good to excellent yield.

  9. Granulomatous prostatitis after intravesical bacillus Calmette-Guérin instillation therapy: A potential cause of incidental F-18 FDG uptke in the prostate gland on F-18 FDG PET/CT in patients with bladder cancer

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Choon Young; Lee, Sang Woo; Choi, Seock Hwan; Son, Seung Hyun; Jung, Ji Hoon; Lee, Chang Hee; Jeong, Shin Young; Ahn, Byeong Cheol; Lee, Jae Tae [Kyungpook National University Medical Center and School of Medicine, Daegu (Korea, Republic of)

    2016-03-15

    This study aimed to evaluate the possibility that Bacillus Calmette-Guérin (BCG)-induced granulomatous prostatitis can be a potential cause of benign F-18 FDG uptake. A total of 395 bladder cancer patients who underwent F-18 FDG PET/CT (PET/CT) were retrospectively evaluated. Patients were divided into two groups according to BCG therapy status. Elapsed time after BCG therapy, serum PSA level, results of prostate biopsy, and the SUV{sub max} and uptake pattern in the prostate gland were reviewed. For patients who underwent follow-up PET/CT, the changes in SUV{sub max} were calculated. While 35 % of patients showed prostate uptake in the BCG therapy group, only 1 % showed prostate uptake in the non-BCG therapy group (p < 0.001). Among 49 patients with FDG-avid prostate lesions, none had suspected malignancy during the follow-up period (median: 16 months). Five patients revealed granulomatous prostatitis on biopsy. The incidence of FDG-avid prostate lesions was significantly higher if the elapsed time after BCG therapy was less than 1 year compared to more than 1 year (p < 0.001). Serum PSA was normal in 88 % of patients. All patients with incidental F-18 FDG uptake in the prostate gland showed focal or multifocal prostate uptake, and median SUV{sub max} was 4.7. In 16 patients who underwent follow-up PET/CT, SUV{sub max} was decreased in 14 patients (88 %) without treatment, and no patients demonstrated further increased prostate uptake (p < 0.001). BCG-induced granulomatous prostatitis can be a potential cause of benign F-18 FDG uptake, especially in those with a history of bladder cancer treated with BCG. In BCG-induced granulomatous prostatitis, focal or multifocal prostate uptake is frequently seen within 1 year after BCG therapy, and the intensity of prostate uptake is decreased on the follow-up PET/CT without any treatment.

  10. Synthesis and biodistribution of [sup 18]F-labeled fleroxacin. [Fluoroquinolone antibiotic

    Energy Technology Data Exchange (ETDEWEB)

    Livni, E.; Babich, J.; Alpert, N.M. (Massachusetts General Hospital, Boston, MA (United States). Radiology Dept.) (and others)

    1993-01-01

    [[sup 18]F]Fleroxacin (6,8-difluoro-1,4-dihydro-1-(2-[[sup 18]F] fluoroethyl)-4-oxo-7-(4-methyl-1-piperazinyl)-3-quinolinecarboxylic acid) was synthesized from its methylsulfonyl ester precursor. 6,7,8-Trifluoro-4-hydroxy-quinoline-3-carboxylic acid ethyl ester (Ro 19-7423) was alkylated with 2-bromoethanol to produce 6,7,8-trifluoro-1,4-dihydro-1-(2-hydroxyethyl)-4-oxo-3-quinolinecarboxylic acid ethyl ester in 76% yield which was then condensed with 1-methyl-piperazine to produce 6,8-difluoro-1,4-dihydro-1-(2-hydroxyethyl)-7-(4-methyl-1-piperazi nyl)4-oxo-3-quinolinecarboxylic acid ethyl ester in 67% yield. This product was reacted with methanesulfonyl chloride to produce the mesylate precursor of fleroxacin in 66% yield. Nucleophilic substitution of the mesylate with [sup 18]F[sup -] in the presence of Kryptofix 2.2.2 followed by basic hydrolysis produced [[sup 18]F]fleroxacin with a radiochemical yield of 5-8% (EOS) within 90 min. The pattern of biodistribution of [[sup 18]F]fleroxacin was similar to the [sup 14]C-labeled drug. (Author).

  11. Diselenide-Labeled Cyclic Polystyrene with Multiple Responses: Facile Synthesis, Tunable Size, and Topology.

    Science.gov (United States)

    Cai, Zhaoxiong; Lu, Weihong; Gao, Feng; Pan, Xiangqiang; Zhu, Jian; Zhang, Zhengbiao; Zhu, Xiulin

    2016-05-01

    Diselenide-containing polymers have attracted more and more attention due to their redox sensitivity and bioapplication. In this work, a bifunctional diselenocarbonate is prepared and used to mediate the reversible addition-fragmentation chain transfer (RAFT) polymerization, producing α,ω-selenocarbonate-labeled telechelic polystyrene. Based on effective aminolysis of the terminal selenocarbonates and the followed spontaneous oxidation coupling reaction of diselenols, monoblock cyclic polystyrene linked by one diselenide bond and multiblock cyclic copolymer linked by several diselenide bonds are prepared by manipulating the concentration of α,ω-telechelic polystyrene in solution. The progress of aminolysis and the subsequent spontaneous oxidation of selenols to diselenides are monitored by UV-vis, gel permeation chromatography (GPC), and NMR characterizations, confirming the cyclic topologies of the resultant polymers (monocyclic or multiblock cyclic polymer). The monoblock cyclic or multiblock polymers show redox sensitivity, which can be converted to linear polymer by reducing or oxidizing agent. Moreover, the obtained monoblock cyclic polymer or multiblock cyclic copolymer can be transformed to each other under UV irradiation by adjusting the concentration of the cyclic polystyrene. For the first time, this work provides an alternative and promising approach to realize the topological transformation of polymers by installing multiresponsive diselenide moities into the backbone of cyclic polymer.

  12. Discovery of competing anaerobic and aerobic pathways in umpolung amide synthesis allows for site-selective amide 18O-labeling.

    Science.gov (United States)

    Shackleford, Jessica P; Shen, Bo; Johnston, Jeffrey N

    2012-01-03

    The mechanism of umpolung amide synthesis was probed by interrogating potential sources for the oxygen of the product amide carbonyl that emanates from the α-bromo nitroalkane substrate. Using a series of (18)O-labeled substrates and reagents, evidence is gathered to advance two pathways from the putative tetrahedral intermediate. Under anaerobic conditions, a nitro-nitrite isomerization delivers the amide oxygen from nitro oxygen. The same homolytic nitro-carbon fragmentation can be diverted by capture of the carbon radical intermediate with oxygen gas (O(2)) to deliver the amide oxygen from O(2). This understanding was used to develop a straightforward protocol for the preparation of (18)O-labeled amides in peptides by simply performing the umpolung amide synthesis reaction under an atmosphere of 18O2.

  13. Radiosynthesis of [F-18]fluoxetine as a potential radiotracer for serotonin reuptake sites

    Energy Technology Data Exchange (ETDEWEB)

    Das, M.K.; Mukherjee, Jogeshwar (Chicago Univ., IL (United States). Dept. of Radiology)

    1993-05-01

    Synthesis of 4-nitro-[alpha]-bromo-[alpha],[alpha]-difluorotoluene was accomplished in two steps starting from 4-nitrobenzaldehyde, with a 30% overall yield. Radiolabeling of 4-nitro-[alpha]-bromo-[alpha], [alpha]-difluorotoluene with no-carrier-added [[sup 18]F]fluoride provided 4-nitro-[alpha],[alpha]-difluoro-[alpha]-[[sup 18]F] fluorotoluene in 2-4% yields with a specific activity of 2590 GBq/mmol (70 Ci/mmol). The effect of the reaction temperature on the radiochemical yield and specific activity of the radiolabeling reaction was studied. Radiochemical yields increased, whereas specific activity decreased, with increasing temperature. Radiosynthesis of [[sup 18]F] fluoxetine involved coupling of 4-nitro-[alpha],[alpha]-difluoro-[alpha]-[[sup 18]F]fluorotoluene with the sodium alkoxide of (S)-3-(methylamino)-1-phenyl-1-propanol. The overall yield of HPLC purified [[sup 18]F]fluoxetine was 1-2% (decay-corrected; total radiosynthesis time, 150-180 min). The specific activity of the product was 1480 GBq/mmol (40 Ci/mmol). (Author).

  14. Strigolactone Analogs as Molecular Probes in Chasing the (SLs) Receptor/s: Design and Synthesis of Fluorescent Labeled Molecules

    Institute of Scientific and Technical Information of China (English)

    Cristina Prandi; Helèna Rosso; Beatrice Lace; Ernesto G. Occhiato; Alberto Oppedisano; Silvia Tabasso; Gabriele Alberto

    2013-01-01

    Originally identified as allelochemicals involved in plant-parasite interactions,more recently,Strigolactones (SLs) have been shown to play multiple key roles in the rhizosphere communication between plants and mycorrhizal fungi.Even more recent is the hormonal role ascribed to SLs which broadens the biological impact of these relatively simple molecules.In spite of the crucial and multifaceted biological role of SLs,there are no data on the receptor(s) which bind(s) such active molecules,neither in the producing plants nor in parasitic weeds or AM fungi.Information about the putative receptor of SLs can be gathered by means of structural,molecular,and genetic approaches.Our contribution on this topic is the design and synthesis of fluorescent labeled SL analogs to be used as probes for the detection in vivo of the receptor(s).Knowledge of the putative receptor structure will boost the research on analogs of the natural substrates as required for agricultural applications.

  15. Preclinical testing of F-18 and I-123 radioligands involving autoradiography and a phosphor-imaging device

    Energy Technology Data Exchange (ETDEWEB)

    Gatley, S.J.; Pyatt, B.; Gifford, A.N. [Brookhaven National Lab., Upton, NY (United States)] [and others

    1997-05-01

    During the development and validation of a receptor-binding radiopharmaceutical it is necessary to assess its brain regional distribution. Film contact autoradiography (AR) points such distributions to be evaluated on a fine anatomical scale, and avoids the inherent risk a microdissection experiments of missing interesting localization pattern. However, in vivo film AR may require a 1000-fold higher activity of a F-18 or I-123 radioligand than microdissection. In addition to health physics considerations, problems with receptor saturation can easily occur after injecting, say, 10 mCi into a 250g rat. A less commonly appreciated problem even with in vitro AR, using slide-mounted brain sections, is that it may be impossible to use sufficient F-18 to obtain acceptable images using film, because of receptor saturation. Phosphorimaging is superior in sensitivity to film by a factor of 10-50, and so relaxes constraints on injected activities and specific activities. Furthermore, it is also superior to film in terms of dynamic range and linearity of response. We have recently used phosphorimaging in two situations where film AR gave unsatisfactory results. (1) the novel cannabinoid CB1 receptor radioligand, I-123 AM281, was injected intravenously at 800 microcurie per rat. Animals were sacrificed at 2 h, frozen and whole body sections prepared. I-123 was clearly visualized in discrete brain areas (substantia nigra, globus pallidus, entopeduncular nucleus , hippocampus and cerebellum) consistent with the distribution of CB1 receptors previously demonstrated only in in vitro studies. (2) Rat brain sections were thaw mounted on gelatin/alum coated glass and incubated with the novel nicotinic acetylcholine receptor ligand F-18 2{prime}-fluoro-2{prime} nor-chloroepibatidine (1 nM).

  16. Normal physiologic and Benign foci with F-18 FDG avidity on PET/CT in patients with breast cancer

    Energy Technology Data Exchange (ETDEWEB)

    Park, Soon Ah; Lee, Kwang Man; Choi, Un Jong; Kim, Hun Soo; Kim, Hye Won; Song, Jeong Hoon [College of Medicine, Wonkwnag University, Iksan (Korea, Republic of)

    2010-12-15

    The aim of this study was to evaluate the physiologic and benign F-18 fluorodeoxyglucose (FDG) avid foci in patients with breast cancer. On 309 F-18 FDG PET/CT scans of 241 women with breast cancer, the hypermetabolic lesions compared with the surrounding normal region were evaluated retrospectively. Available reports of other relevant radiological imaging medical records, and follow-up PET/CT were reviewed for explanations of the abnormal uptake. Among the 70 physiologic foci, muscular uptake of the lower neck following the surgical and/or radiation therapy of ipsilateral breast (29%), hypermetabolic ovaries (16%) and uterine (10%) uptake during the ovulatory and menstrual phases during the normal menstrual cycle were identified, and also hypermetabolic brown fat in cold-induced thermogenesis (7%), non-specific bowel uptake (35%) were observed. Among the 147 benign lesions, sequelae of the chest wall and breasts following surgical and/or radiation therapy, were often observed (27%). Hypermetabolic thyroid glands were noted as adenomas and chronic thyroiditis (18%). Reactive hyperplasia of cervical or mediastinal lymph nodes (32%), degenerative osteoarthritis and healed fractures (15%), hypermetabolic benign lung lesions (6%) were observed. Altered physiologic and benign F-18 FDG uptake in the cervical muscle and chest wall following ipsilateral breast surgery or radiotherapy were common, and also normal physiologic uptake in ovary and uterus, brown fat, thyroid were considered as predominant findings in women patients with breast cancer. Knowledge of these findings might aid in the interpretation of FDG PET/CT in patients with breast cancer

  17. Monitoring of Tumor Response to Neoadjuvant Radio-Chemotherapy of Esophageal Carcinoma by F-18-FDG-PET

    Institute of Scientific and Technical Information of China (English)

    PeterTheissen; PaulM.Schneider; StephanE.Baldus; AlexandraJost; MarkusDietlein; RolfP.Miiller; ArnulfH.Hoelscher; HaraldSchicha

    2004-01-01

    Introduction: For clinical assessment of neoadjuvant radiochemotherapy of esophageal cancer reliable in-vivo methods are necessary. Therefore, the capabilities of F-18-Fluorodesoxyglucose-PET in comparison to histomorphological grading of tumor regression were studied. Methods: In 33 patients with locally advanced esophageal carcinoma (uT3, uN0-1, cM0) F-18-FDG-PET was performed before and 2 weeks after radiochemotherapy. All tumors were resected by transthoracic en-bloc esophagectomy 3-4 weeks after induction therapy. A subgroup of 11 patients underwent weekly PET scan during neoadjuvant therapy.PET was performed in a dedicated scanner 1.3 h after administration of 370 MBq F-18-FDG. Data analysis based on maximum SUV data derived from individual regions of interest in pre- and posttherapeutic images. PET data were compared to histomorphological grading parameters for tumor regression whithin the resected tissues. Results: The comparison of histopathological tumor regression after neoadjuvant therapy and PET SUV differences showed a significant x2 P-value of 0.006. There was a significant decrease of the SUV data from 9.14-3.5 to 4.3±1.9 (P<0.0001). In therapy responders SUV was diminished by 59% and in non-responders by 34 %. Longitudinal SUV measurement during neoadjuvant therapy showed a strong SUV decrease already after one and two weeks (P=0.021 and 0.003). Conclusion: The recent data of the FDG-PET follow-up after neoadjuvant therapy show that PET is able to predict therapy response.Longitudinal PET data advocate that it may be possible to recognize response also very early during radiochemotherapy.

  18. Synthesis of ferrocene-labeled steroids via copper-catalyzed azide-alkyne cycloaddition. Reactivity difference between 2β-, 6β- and 16β-azido-androstanes.

    Science.gov (United States)

    Fehér, Klaudia; Balogh, János; Csók, Zsolt; Kégl, Tamás; Kollár, László; Skoda-Földes, Rita

    2012-06-01

    Copper-catalyzed cycloaddition of steroidal azides and ferrocenyl-alkynes were found to be an efficient methodology for the synthesis of ferrocene-labeled steroids. At the same time, a great difference between the reactivity of 2β- or 16β-azido-androstanes and a sterically hindered 6β-azido steroid toward both ferrocenyl-alkynes and simple alkynes, such as phenylacetylene, 1-octyne, propargyl acetate and methyl propiolate, was observed.

  19. Design, Synthesis and Biological Evaluation of a Simplified Fluorescently Labeled Discodermolide as a Molecular Probe to Study the Binding of Discodermolide to Tubulin

    OpenAIRE

    Qi, Jun; Blanden, Adam R.; Bane, Susan; Kingston, David G. I.

    2011-01-01

    The design, synthesis, and biological evaluation of a simplified fluorescently labeled discodermolide analogue possessing a dimethylaminobenzoyl fluorophore has been achieved. Stereoselective Suzuki coupling, Horner–Wadsworth–Emmons reaction or the Wittig reaction comprised the key tactics for its construction. The analogue exhibited qualitatively similar activity to paclitaxel in a tubulin assembly assay, and it can thus be used as a fluorescent molecular probe to explore the local environme...

  20. Synthesis of biotin-labelled core glycans of GPI anchors and their application in the study of GPI interaction with pore-forming bacterial toxins.

    Science.gov (United States)

    Gao, Jian; Zhou, Zhifang; Guo, Jiatong; Guo, Zhongwu

    2017-06-06

    A convergent strategy was developed for the first-time synthesis of biotin-labeled GPI core glycans. These GPI conjugates are useful for various biological studies showcased by their application in the scrutiny of pore-forming bacterial toxin-GPI interaction, revealing that the phosphate group at the GPI inositol 1-O-position had a significant impact on GPI-toxin binding.

  1. Usefulness of F-18 FDG PET/CT in a case of Kaposi sarcoma with an unexpected bone lesion.

    Science.gov (United States)

    Morooka, Miyako; Ito, Kimiteru; Kubota, Kazuo; Yanagisawa, Kunio; Teruya, Katsuji; Hasuo, Kahehiro; Shida, Yoshitaka; Minamimoto, Rhogo; Kikuchi, Yoshimi; Oka, Shinichi

    2011-03-01

    Bone lesions of Kaposi sarcoma are rare. A 56-year-old man who was HIV positive and was diagnosed with Kaposi sarcoma on the basis of the results of a biopsy of skin lesions, underwent F-18 FDG PET/CT scan for detecting Kaposi sarcoma lesions and other AIDS-related diseases. An abnormal uptake was observed in the lumbar spine. MRI showed a diffuse enhanced spine lesion, and Ga-67 and ²⁰¹Tl scanning were negative. As a result, the lesion was considered to be a Kaposi sarcoma, and the shrinkage of the lesion was noted after the therapy for Kaposi sarcoma.

  2. Recurrent proliferating trichilemmal tumor with malignant change on the f-18 fluorodeoxyglucose position emission tomography/computed tomography

    Energy Technology Data Exchange (ETDEWEB)

    Moon, Eun Ha; Kim, Eun Ha; Kim, Young Jun; Yoo, Seol Bong; Nam, Kyung Hwa [Presbyterian Medical Center, Seonam University College of Medicine, Jeonju (Korea, Republic of)

    2016-06-15

    F-18 fluorodeoxyglucose (FDG) positron emission tomography/computed tomography scan has been used for the diagnosis, assessment of treatment response, and follow-up of various neoplasms. Proliferating trichilemmal cyst or tumor (PTT) is a rare neoplasm, originated from the outer root sheath of a hair follicle. Because this tumor has unpredictable biological and clinical behavior, the long-term clinical follow-up is necessary to detect metastasis or recurrence. We reported a case of recurrent malignant PTT on scalp that showed increased FDG uptake.

  3. Role of F18 fluorodeoxyglucose positron-emission tomography/computed tomography in the management of Askin's tumor.

    Science.gov (United States)

    Santhosh, Sampath; Kashyap, Raghava; Bhattacharya, Anish; Kumar Jindal, Surinder; Rai Mittal, Bhagwant

    2013-07-01

    A primitive neuroectodermal tumor (PNET) of the thoraco-abdominal region is one of a group of small round cell tumors usually found in children and young adults, originally described by Askin et al. Most cases arise in the soft-tissues of the thorax, but may rarely occur within the lung with the symptoms of chest wall pain, pleural effusion and dyspnea. The authors present two cases demonstrating the utility of F18 fluorodeoxyglucose positron-emission tomography/computed tomography in the staging and prognosis of PNET of the chest wall.

  4. Pretreatment F-18 FDG PET/CT Parameters to Evaluate Progression-Free Survival in Gastric Cancer

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Jeonghun; Lim, Seok Tae; Na, Chang Ju; Han, Yeonhee; Kim, Chanyoung; Jeong, Hwanjeong; Sohn, Myunghee [Chonbuk National Univ., Jeonju (Korea, Republic of)

    2014-03-15

    We performed this study to evaluate the predictive value of pretreatment F-18 FDG PET/CT for progression-free survival (PFS) in patients with gastric cancer. Of 321 patients with a diagnosis of gastric cancer, we retrospectively enrolled 97 patients (men:women = 61:36, age 59.8±13.2 years), who underwent pretreatment F-18 fluoro-2-deoxyglucose positron emission tomography/computed tomography (F-18 FDG PET/CT) from January 2009 to December 2009. Maximum standardized uptake value (SUVmax) was measured for each case with detectable primary lesions. In the remaining non-detectable cases, SUVmax was measured from the corresponding site seen on gastroduodenoscopy for analysis. In subgroup analysis, metabolic tumor volume (MTV) was measured in 50 patients with clearly distinguishable primary lesions. SUVmax, stage, depth of tumor invasion and presence of lymph node metastasis were analyzed in terms of PFS. Receiver operating characteristic (ROC) curves were used to find optimal cutoff values of SUVmax and MTV for disease progression. The relationship between SUVmax, MTV and PFS was analyzed using the Kaplan-Meier with log-rank test and Cox's proportional hazard regression methods. Of 97 patients, 15 (15.5 %) had disease progression. The mean follow-up duration was 29.6±10.2 months. The mean PFS of low SUVmax group (≤5.74) was significantly longer than that of the high SUVmax group (>5.74) (30.9±8.0 vs 24.3±13.6 months, p =0.008). In univariate analysis, stage (I vs II, III, IV), depth of tumor invasion (T1 vs T2, T3, T4), presence of lymph node metastasis and SUVmax (>5.74 vs ≤5.74) were significantly associated with recurrence. In multivariate analysis, high SUVmax (>5.74) was the only poor prognostic factor for PFS (p =0.002, HR 11.03, 95% CI 2.48.49.05). Subgroup multivariate analysis revealed that high MTV (>16.42) was the only poor prognostic factor for PFS (p =0.034, HR 3.59, 95 % CI 1.10.11.71). In gastric cancer, SUVmax measured by pretreatment F-18

  5. Role of F-18 FDG PET/CT in the management of infected abdominal aortic aneurysm due to salmonella

    Energy Technology Data Exchange (ETDEWEB)

    Choi, Seung Jin; Lee, Jin Soo; Cheong, Moon Hyun; Byun, Sung Su; Hyun, In Young [Inha University College of Medicine, Incheon (Korea, Republic of)

    2007-12-15

    We present a case of infected abdominal aortic aneurysm due to salmonella enteritidis. F-18 FDG PET/CT was performed to diagnosis and during follow-up after antibiotic treatment. Computed tomography (CT) is considered to be the best diagnostic imaging modality in infected aortic lesions. In this case, a combination of CT and FDG PET/CT provided accurate information for the diagnosis of infected abdominal aortic aneurysm. Moreover, FDG PET/CT made an important contribution of monitoring disease activity during antibiotic treatment.

  6. Synthesis and Complexation of Well-Defined Labeled Poly(N,N-dimethylaminoethyl methacrylates (PDMAEMA

    Directory of Open Access Journals (Sweden)

    Mark Billing

    2015-11-01

    Full Text Available We present the synthesis and characterization of well-defined polycationic copolymers containing thiazole dyes in the side chain. Atom transfer radical polymerization (ATRP was used for the copolymerization of 3-azidopropyl methacrylate (AzPMA and N,N-dimethylaminoethyl methacrylate (DMAEMA of different composition. Thiazole-based alkyne-functionalized dyes (e.g., 5-methyl-4-(prop-2-yn-1-yloxy-2-(pyridin-2-ylthiazole, (MPPT were afterwards covalently attached using copper catalyzed azide alkyne cycloadditions (CuAAC reaching contents of up to 9 mol % dye. Subsequent quaternization of the tertiary nitrogen of DMAEMA with strong methylation agents (e.g., methyl iodide led to permanently charged polyelectrolytes. The materials were characterized by size exclusion chromatography, as well as NMR- and UV/VIS-spectroscopy. Particular attention is paid to the spectroscopic properties of the dyes in the side chain upon environmental changes such as pH and salinity. We anticipate the application of such precisely functionalized polyelectrolytes as temperature- and pH-responsive sensors in biomedical applications, e.g., within interpolyelectrolyte complexes. Concerning the latter, first complex formation results are demonstrated.

  7. Solitary Plasmacytoma of the Sternum Mimicking Bone Metastasis in a Patient with a History of Breast Cancer Evaluated by F-18-FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Treglia, Giorgio; Luca, Giovanella [Oncology Institute of Southern Switzerland, Bellinzona (Switzerland); Barbara, Muoio; Carmelo, Caldarella [Catholic Univ., Rome (Italy)

    2014-06-15

    A 65-year-old woman with a history of breast cancer (stage T2N0M0 treated with left breast conservative therapy 7 years previously followed by hormone therapy) underwent fluorine-18-fluorodeoxyglucose positron emission tomography/computed tomography (F-18-FDG PET/CT) for restaging due to increased serum tumour markers levels (CA15-3, 37 U/ml and CEA, 8 ng/ml). The patient presented thoracic pain before performing F-18-FDG PET/CT. PET/CT demonstrated an area of increased F-18-FDG uptake corresponding to an osteolytic lesion occupying the upper sternum suspicious for bone metastasis. No other areas of abnormal F-18-FDG uptake were detected in the rest of the body. Based on this PET/CT finding, the patient performed biopsy of the sternal lesion. Histology demonstrated the presence of a sternal plasmacytoma and the patient was addressed to radiation therapy. The role of F-18-FDG PET/CT in patients with multiple myeloma is well known, whereas only some articles evaluated the usefulness of this method in patients with solitary plasmacytomas. In particular, F-18-FDG PET/CT may be useful in demonstrating the evolution of solitary plasmacytomas in multiple myeloma. In our case F-18-FDG PET/CT was useful in detecting a solitary plasmacytoma of the sternum mimicking bone metastasis in a patient with history of breast cancer, correctly addressing to further histological evaluation.

  8. Efficient synthesis of D-branched-chain amino acids and their labeled compounds with stable isotopes using D-amino acid dehydrogenase.

    Science.gov (United States)

    Akita, Hironaga; Suzuki, Hirokazu; Doi, Katsumi; Ohshima, Toshihisa

    2014-02-01

    D-Branched-chain amino acids (D-BCAAs) such as D-leucine, D-isoleucine, and D-valine are known to be peptide antibiotic intermediates and to exhibit a variety of bioactivities. Consequently, much effort is going into achieving simple stereospecific synthesis of D-BCAAs, especially analogs labeled with stable isotopes. Up to now, however, no effective method has been reported. Here, we report the establishment of an efficient system for enantioselective synthesis of D-BCAAs and production of D-BCAAs labeled with stable isotopes. This system is based on two thermostable enzymes: D-amino acid dehydrogenase, catalyzing NADPH-dependent enantioselective amination of 2-oxo acids to produce the corresponding D-amino acids, and glucose dehydrogenase, catalyzing NADPH regeneration from NADP(+) and D-glucose. After incubation with the enzymes for 2 h at 65°C and pH 10.5, 2-oxo-4-methylvaleric acid was converted to D-leucine with an excellent yield (>99 %) and optical purity (>99 %). Using this system, we produced five different D-BCAAs labeled with stable isotopes: D-[1-(13)C,(15)N]leucine, D-[1-(13)C]leucine, D-[(15)N]leucine, D-[(15)N]isoleucine, and D-[(15)N]valine. The structure of each labeled D-amino acid was confirmed using time-of-flight mass spectrometry and nuclear magnetic resonance analysis. These analyses confirmed that the developed system was highly useful for production of D-BCAAs labeled with stable isotopes, making this the first reported enzymatic production of D-BCAAs labeled with stable isotopes. Our findings facilitate tracer studies investigating D-BCAAs and their derivatives.

  9. Radiochemical synthesis of {sup 105g}Ag-labelled silver nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Ichedef, C., E-mail: cigdem_ch@yahoo.com; Simonelli, F.; Holzwarth, U. [Institute for Health and Consumer Protection, European Commission, Joint Research Centre (Italy); Bagaria, J. Piella; Puntes, V. F. [Institut Català de Nanotecnologia (ICN2) (Spain); Cotogno, G.; Gilliland, D.; Gibson, N. [Institute for Health and Consumer Protection, European Commission, Joint Research Centre (Italy)

    2013-11-15

    A method for synthesis of radiolabelled silver nanoparticles is reported. The method is based on proton activation of silver metal powder, enriched in {sup 107}Ag, with a 30.7 MeV proton beam. At this proton energy {sup 105g}Ag is efficiently created, mainly via the {sup 107}Ag(p,3n){sup 105}Cd → {sup 105g}Ag reaction. {sup 105g}Ag has a half-life of 41.29 days and emits easily detectable gamma radiation on decay to {sup 105}Pd. This makes it very useful as a tracing radionuclide for experiments over several weeks or months. Following activation and a period to allow short-lived radionuclides to decay, the powder was dissolved in concentrated nitric acid in order to form silver nitrate (AgNO{sub 3}), which was used to synthesise radiolabelled silver nanoparticles via the process of sodium borohydride reduction. For comparison, non-radioactive silver nanoparticles were synthesised using commercially supplied AgNO{sub 3} in order to check if the use of irradiated Ag powder as a starting material would alter in any way the final nanoparticle characteristics. Both nanoparticle types were characterised using dynamic light scattering, zeta-potential and X-ray diffraction measurements, while additionally the non-radioactive samples were analysed by transmission electron microscopy and UV–Vis spectrometry. A hydrodynamic diameter of about 16 nm was determined for both radiolabelled and non-radioactive nanoparticles, while the electron microscopy on the non-radioactive samples indicated that the physical size of the metal NPs was (7.3 ± 1.4) nm.

  10. An improved strategy for the synthesis of [18F]-labeled arabinofuranosyl nuclosides

    Science.gov (United States)

    Zhang, Hanwen; Cantorias, Melchor V.; Pillarsetty, NagaVaraKishore; Burnazi, Eva M.; Cai, Shangde; Lewis, Jason S.

    2012-01-01

    The expression of the herpes simplex virus type-1 thymidine kinase (HSV1-tk) gene can be imaged efficaciously using a variety of 2′-[18F]fluoro-2′-deoxy-1-b-D-arabinofuranosyl-uracil derivatives [[18F]-FXAU, X= I(iodo), E(ethyl), and M(methyl)]. However, the application of these derivatives in clinical and translational studies has been impeded by their complicated and long syntheses (3–5 h). To remedy these issues, in the study at hand we have investigated whether microwave or combined catalysts could facilitate the coupling reaction between sugar and nucleobase and, further, have probed the feasibility of establishing a novel approach for [18F]-FXAU synthesis. We have demonstrated that the rate of the trimethylsilyl trifluoromethanesulfonate (TMSOTf)-catalyzed coupling reaction between the 2-deoxy-sugar and uracil derivatives at 90°C can be significantly accelerated by microwave-driven heating or by the addition of Lewis acid catalyst (SnCl4). Further, we have observed that the stability of the α- and β-anomers of [18F]-FXAU derivatives differs during the hydrolysis step. Using the microwave-driven heating approach, overall decay-corrected radiochemical yields of 19–27% were achieved for [18F]-FXAU in 120 min at a specific activity of >22 MBq/nmol (595 Ci/mmol). Ultimately, we believe that these high yielding syntheses of [18F]-FIAU, [18F]-FMAU and [18F]-FEAU will facilitate routine production for clinical applications. PMID:22819195

  11. Synthesis of deuterium-labelled compounds for FOTEK project; Syntese af deuterium-maerkede forbindelser til FOeTEK projektet

    Energy Technology Data Exchange (ETDEWEB)

    Joergensen, O.; Egsgaard, H.; Larsen, E. [Forskningscenter Risoe, Roskilde (Denmark)

    1996-06-01

    In the FoTech project there have been utilized labelled compounds of stable isotopes as internal standards. Some of these compounds are commercially available ({sup 13}C-labelled PCB congeners, {sup 13}C-labelled diethylstilbestrol for determination of anabolic steroids). Others, like D{sub 9}-clenbuterol, D{sub 3}-clenbuterol, D{sub 3}-zeramol and D{sub 3}-dimetridazol have been synthesized. General aspects of deuterium compounds labelling are considered. (EG).

  12. Evaluation of glucose metabolic abnormality in postlingually deaf patients using F-18-FDG positron emission tomography and statistical parametric mapping

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Jae Sung; Lee, Dong Soo; Oh, Seung Ha; Kim, Chong Sun; Park, Kwang Suk; Chung, June Key; Lee, Myung Chul [College of Medicine, Seoul National Univ., Seoul (Korea, Republic of)

    2000-07-01

    We have previously reported the prognostic relevance of cross-modal cortical plasticity in prelingual deaf patients revealed by F-18-FDG PET and SPM analysis. In this study, we investigated metabolic abnormality in postlingual deaf patients, whose clinical features are different from prelingual deafness. Nine postlingual deaf patients (age: 30.5 {+-}14.0) were performed on F-18-FDG brain PET. We compared their PET images with those of age-matched 20 normal controls (age: 27.1 {+-}8.6), and performed correlation analysis to investigate the relationship between glucose metabolism and deaf duration using SPM99. Glucose metabolism of deaf patients was significantly (p<0.05, corrected) decreased in both anterior cingulate, inferior frontal cortices, and superior temporal cortices, and left hippocampus. Metabolism in both superior temporal cortices and association area in inferior parietal cortices showed significant (p<0.01, uncorrected) positive correlation with deaf duration. Decreased metabolism in hippocampus accompanied with hypometabolism in auditory related areas can be explained by recent finding of anatomical connectivity between them, and may be the evidence indicating their functional connectivity. Metabolism recovery in auditory cortex after long deaf duration suggests that cortical plasticity takes place also in postlingual deafness.

  13. Monitoring of the Formation and Development Process for Infection and Inflammation Using F-18 FDG, PET/CT

    Directory of Open Access Journals (Sweden)

    Türkan Ertay

    2015-02-01

    Full Text Available Objective: Many radiopharmaceuticals have been evaluated extensively in both preclinical and clinical studies as potential diagnostic agents to identify the sites of infection. There is a definite role of FDG-PET in diagnosis, extent of assessing the disease, evaluation of treatment response and disease activity in patients with infections and inflammation. The aim of the study, the process of formation and development of infection and inflammation is monitored using (18 F 2’-deoxy-2-fluoroD-glucose (F-18 FDG by Positron Emission Computed Tomography (PET-CT. Methods: In this study, sterile abscess was induced by using turpentine and infected abscess was induced by using Staphylococcus aureus atcc 25923 strain on rats. In the abscess formation on rats, three grups rats were used as sterile, infected and control grups. There were examined male White Wistar Rats, the clinical healthy animals were 150-220 gr body weight. Bacterial strain and rat model for abscess formation for infected abscess formation on rats (n=7, S. aureus 0.5 ml 107 CFU/ml was inoculated in the right arm of the rats as subcutaneous. For sterile abscess formation on rats (n=7 0.2-0.4 ml turpentine (sigma-aldrich was injected into the right arm of the rats as subcutaneous. In control group (n=6, 0.5 ml 0.9% NaCl was injected into the right arm of the rats as subcutaneous. First day imsaging was acquired 24 hours after inoculation of S.aureus and turpentine. 1 mCi 18F-FDG was injected intravenously via the tail vein. Prior to 18F-FDG injection, rats fasted at least 4 hours and well hydrated. Imaging was done using PET-CT (PHILIPS Gemini TF, beginning 1 hour following injection of 18F-FDG IV in the first day and at intervals of 24 hours for five days. First day imaging was performed 1. hour after IV injection of 18F-FDG to obtain optimum imaging time. PET/CT images were visually and semiquantitatively assessed. For semiquantitative analysis of the PET images, a region of interest

  14. Synthesis and pharmacokinetics of radioisotope labeled anti-malarial agent in Sprague-Dawley rats

    Energy Technology Data Exchange (ETDEWEB)

    Kannanpalli, Pradeep; Park, Sang Hyun [Korea Atomic Energy Research Institute, Daejeon (Korea, Republic of)

    2008-04-15

    Pyro naridine tetraphosphate is a new synthetic drug which is currently being investigated for use in the treatment of malaria. The main objective of this investigation was to synthesize [{sup 14}C]pyro naridine tetraphosphate and to determine its absorption, distribution, excretion and pharmacokinetics in to male and female Sprague-Dawley rats following a single oral administration (10 mg/kg). To overcome the disadvantages posed by the classical method, a novel and efficient method using microwave irradiation was employed for the synthesis of pyro naridine tetraphosphate. Use of microwave irradiation decreased the reaction time considerably, used less of the starting material and also increased the yield when compared with the classical method. [{sup 14}C]Pyro naridine tetraphosphate thus synthesized had a high degree of purity and showed satisfactory {sup 1}H NMR, {sup 13}C NMR, mass spectra (MS), infrared (IR) and elemental analysis data. The distribution of [{sup 14}C]pyro naridine tetraphosphate in various tissues like the blood, plasma, liver, lung, heart, spleen, kidney, brain, stomach, small intestine and large intestine were determined at 1, 4, 8, 24, 48, 96, 144, 192 and 240 h post administration of the drug to rats. Mass balance excretion of [{sup 14}C]pyro naridine tetraphosphate in urine, faeces and in breath as {sup 14}CO{sub 2} were also determined at different time intervals post administration of the drug. We observed that [{sup 14}C]pyro naridine tetraphosphate was readily absorbed and widely distributed within 1 h following oral administration as it was determined by the presence of radioactivity in various tissues investigated. The absorption, distribution and excretion of the drug was found to be gender independent as both male and female rats showed a similar pattern of radioactivity. [{sup 14}C]Pyro naridine tetraphosphate was absorbed mainly from the small intestine upon oral administration. The major route of excretion for [{sup 14}C

  15. Whey and casein labelled with L-[1-13C]-leucine and muscle protein synthesis: effect of resistance exercise and protein ingestion

    DEFF Research Database (Denmark)

    Reitelseder, Søren; Agergaard, Jakob; Doessing, Simon

    2011-01-01

    to a single bolus intake of whey or casein after performance of heavy resistance exercise. Young male individuals were randomly assigned to participate in two protein trials (n = 9) or one control trial (n = 8). Infusion of l-[1-(13)C]leucine was carried out, and either whey, casein (0.3 g/kg lean body mass......), or a noncaloric control drink was ingested immediately after exercise. l-[1-(13)C]leucine-labeled whey and casein were used while muscle protein synthesis (MPS) was assessed. Blood and muscle tissue samples were collected to measure systemic hormone and amino acid concentrations, tracer enrichments......, and myofibrillar protein synthesis. Western blots were used to investigate the Akt signaling pathway. Plasma insulin and branched-chain amino acid concentrations increased to a greater extent after ingestion of whey compared with casein. Myofibrillar protein synthesis was equally increased 1-6 h postexercise after...

  16. Synthesis and evaluation of {sup 18}f-labeled benzylideneaniline derivatives as new biomarkers for {beta}-amyloid imaging in Alzheimer's disease

    Energy Technology Data Exchange (ETDEWEB)

    B, Rai Ganeaha; Jeong, Jae Min; Lee, Yun Sang; Chang, Young Soo; Kim, Young Ju; Kim, Hyung Woo; Lee, Dong Soo; Chung, June Key; Lee, Myung Chul [Seoul National University College of Medicine, Seoul (Korea, Republic of)

    2005-07-01

    Noninvasive early detection of the A{beta} plaques in Alzheimer's disease (AD) brain may be useful tool for the treatment of AD patients. We herein describe the synthesis of {sup 18}F-labeled benzylideneaniline derivatives utilizing a novel labeling approach for imaging A{beta} plaques in AD patients. Condensation of [{sup 18}F] 4-fluorobenzaldehyde with various aromatic amines afforded {sup 18}F-labeled benzylideneaniline derivatives. The biodistribution of 18F-Iabeled benzylideneaniline derivatives was studied with ICR male mice. The binding affinities of the cold compounds to A{beta} (1-40) were determined using [{sup 125}I] 2-(3'-iodo-4-methylaminophenyl) benzothiazole as a reference standard. The radiochemical yields were 32-44% and radiochemical purities were above 99% after purification. Log P values of the compounds were 1.56-1.58. Some of the benzylideneaniline derivatives showed relatively high binding affinity to A{beta} (1-40) aggregates (Ki 149-304 nM). The {sup 18}F-labeled benzylideneaniline derivatives displayed high brain uptake ratio in normal mice (2.9-24.93). The study suggests that these {sup 18}F-labeled compounds may be suitable for A{beta} plaque imaging in AD patients.

  17. Prognostic significance and predictive performance of volume-based parameters of F-18 FDG PET/CT in squamous cell head and neck cancers

    Directory of Open Access Journals (Sweden)

    Sait Sager

    2014-01-01

    Conclusion: Metabolic tumor volume (MTV represents tumor burden, which shows F18-Fluorodeoxyglucose uptake and has a potential value in predicting short-term outcome and disease-free survival in patients with head and neck cancer.

  18. Tritium recovery as waste sub product in the Fluorine 18 production in a nuclear reactor; Recuperacion de tritio como subproducto de desecho en la produccion de F-18 en un reactor nuclear

    Energy Technology Data Exchange (ETDEWEB)

    Flores R, H.; Palma G, F.A.; Ramirez, F.M

    1990-09-15

    The tritium is a radioisotope that can be used to carry out basic as applied research. The current researches on the labelling of the organic molecules as well as its application in diagnostic, radiotherapy and hydrology among others confirm the before said. Due to their utility, they have been carried out studies to recover it of radioactive or nuclear waste as well as, to concentrate it of the natural water, the one which due to the nuclear tests in the last decades has gotten rich in tritium. In this work previous studies to recover the tritium coming from the process that was used to produce F-18 following the reaction {sup 6} Li (n, {alpha}) {sup 3} H, {sup 16} O (t, n) {sup 18} F in made up of lithium oxygenated, in the TRIGA Mark III Nuclear Reactor of the Nuclear Center of Mexico. The method consists on purifying by ion exchange the waste solutions where F-18 took place, to distill them and to concentrate them for an electrochemical method. It was already adapts a system reported to concentrate big volumes (approximately 250 ml) in such a way that could be used for small volumes. It was recovered 30% of the considered initial quantity of tritium. A modification to the proposed methodology will allow to recover the waste tritium in a percentage greater to 80%. (Author)

  19. Synthesis and evaluation of {sup 18}F-labeled benzylguanidine analogs for targeting the human norepinephrine transporter

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Hanwen; Huang, Ruimin; Pillarsetty, NagaVaraKishore; Thorek, Daniel L.J. [Memorial Sloan-Kettering Cancer Center (MSKCC), Department of Radiology, New York, NY (United States); Vaidyanathan, Ganesan [Duke University School of Medicine, Department of Radiology, Durham, NC (United States); Serganova, Inna [Memorial Sloan-Kettering Cancer Center (MSKCC), Department of Neurology, New York, NY (United States); Blasberg, Ronald G. [Memorial Sloan-Kettering Cancer Center (MSKCC), Department of Radiology, New York, NY (United States); Memorial Sloan-Kettering Cancer Center (MSKCC), Department of Neurology, New York, NY (United States); Memorial Sloan-Kettering Cancer Center (MSKCC), Molecular Pharmacology and Chemistry Program, New York, NY (United States); Lewis, Jason S. [Memorial Sloan-Kettering Cancer Center (MSKCC), Department of Radiology, New York, NY (United States); Memorial Sloan-Kettering Cancer Center (MSKCC), Molecular Pharmacology and Chemistry Program, New York, NY (United States); Molecular Pharmacology and Chemistry Program, SKI, Memorial Sloan-Kettering Cancer Center, Radiochemistry and Imaging Sciences Service, Department of Radiology, New York, NY (United States)

    2014-02-15

    Both {sup 131}I- and {sup 123}I-labeled meta-iodobenzylguanidine (MIBG) have been widely used in the clinic for targeted imaging of the norepinephrine transporter (NET). The human NET (hNET) gene has been imaged successfully with {sup 124}I-MIBG positron emission tomography (PET) at time points of >24 h post-injection (p.i.). {sup 18}F-labeled MIBG analogs may be ideal to image hNET expression at time points of <8 h p.i. We developed improved methods for the synthesis of known MIBG analogs, [{sup 18}F]MFBG and [{sup 18}F]PFBG and evaluated them in hNET reporter gene-transduced C6 rat glioma cells and xenografts. [{sup 18}F]MFBG and [{sup 18}F]PFBG were synthesized manually using a three-step synthetic scheme. Wild-type and hNET reporter gene-transduced C6 rat glioma cells and xenografts were used to comparatively evaluate the {sup 18}F-labeled analogs with [{sup 123}I]/[{sup 124}I]MIBG. The fluorination efficacy on benzonitrile was predominantly determined by the position of the trimethylammonium group. The para-isomer afforded higher yields (75 ± 7 %) than meta-isomer (21 ± 5 %). The reaction of [{sup 18}F]fluorobenzylamine with 1H-pyrazole-1-carboximidamide was more efficient than with 2-methyl-2-thiopseudourea. The overall radiochemical yields (decay-corrected) were 11 ± 2 % (n = 12) for [{sup 18}F]MFBG and 41 ± 12 % (n = 5) for [{sup 18}F]PFBG, respectively. The specific uptakes of [{sup 18}F]MFBG and [{sup 18}F]PFBG were similar in C6-hNET cells, but 4-fold less than that of [{sup 123}I]/[{sup 124}I]MIBG. However, in vivo [{sup 18}F]MFBG accumulation in C6-hNET tumors was 1.6-fold higher than that of [{sup 18}F]PFBG at 1 h p.i., whereas their uptakes were similar at 4 h. Despite [{sup 18}F]MFBG having a 2.8-fold lower affinity to hNET and approximately 4-fold lower cell uptake in vitro compared to [{sup 123}I]/[{sup 124}I]MIBG, PET imaging demonstrated that [{sup 18}F]MFBG was able to visualize C6-hNET xenografts better than [{sup 124}I

  20. Usefulness of F-18 FDG PET/CT in subcutaneous panniculitis-like T cell lymphoma: disease extent and treatment response evaluation

    OpenAIRE

    Kim, Jin-Suk; Jeong, Young Jin; Sohn, Myung-Hee; Jeong, Hwan-Jeong; Lim, Seok Tae; KIM, Dong Wook; Kwak, Jae-Yong; Yim, Chang-Yeol

    2012-01-01

    Background. Subcutaneous panniculitis-like T-cell lymphoma (SPTCL) is a rare form of cutaneous lymphomas, accounting for less than 1% of cases of non-Hodgkin’s lymphoma. Fluorine-18 fluorodeoxyglucose (F-18 FDG) positron-emission tomography/computed tomography (PET/CT) findings of SPTCL before and after treatment were rarely reported. Case report. We report a case of SPTCL in which F-18 FDG PET/CT showed increased FDG accumulations in numerous subcutaneous nodules without extracutaneous disea...

  1. Endometrial cancer with cervical extension mimicking dual concordant endometrial and cervical malignancy by F18 FDG PET and MRI

    Energy Technology Data Exchange (ETDEWEB)

    Yoon, Seok Nam [Kwandong Univ. College of Medicine, Seoul (Korea, Republic of)

    2012-09-15

    A 35 year old woman with endometrial cancer and cervical extension underwent F18 FDG PET CT and MRI studies after resection of a cervical mass presumed to be cervical myoma. The patient underwent cervical myomectomy and the histopathologic report revealed poorly differentiated invasive carcinoma. Cervical cancer was ruled out because the patient had no history of sexual intercourse and was negative for human papilloma virus infection. The patient underwent radical hysterectomy, bilateral salpingo oophorectomy, pelvic and para aortic lymph node dissection, and multiple biopsies. F18 FDG PET CT showed intense FDG uptake along the cervix wall. T2 weighted MRI also revealed a mass lesion with high SI involving the anterior and posterior lips of the uterine cervix. Another area of focal increased uptake above the endometrial lesion in the left pelvic cavity was observed on PET CT and MRI, possibly due to a functioning ovary. PET CT and MRI were interpreted as showing a dual concordant malignant lesion due to separated FDG uptakes and high SI without any connection between the cervical and endometrial lesions. F18 FDG PET CT showed intense FDG uptake along the endometrium. Given the patient's history and the fact that she was not menstruating at the time of imaging, this intense uptake was interpreted as another pathologic lesion, suggesting dual primary lesions. A suspected heterogeneous mass lesion along the endometrium suggesting concordant endometrial cancer was found on MRI. Endometrial cancer with cervical extension is sometimes difficult to differentiate from primary cervical cancer. The final histopathologic report showed poorly differentiated endometrial adenocarcinoma with cervical extension, although the FDG PET CT and MRI findings were suggestive of concordant cervical and endometrial cancer. Although histopathologic confirmation is necessary for final diagnosis, MRI and FDG PET CT studies may aid in the differential diagnosis. A metastatic cervical mass

  2. Comparison of diagnostic performance between interictal F-18-FDG PET and ictal Tc-99m-HMPAO SPECT in occipital lobe epilepsy

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Seok Ki; Lee, Dong Soo; Yeo, Jeong Seok; Lee, Sang Kun; Kim, Joo Yong; Jeong, Jae Min; Chung, June Key; Lee, Myung Chul [College of Medicine, Seoul National Univ., Seoul (Korea, Republic of)

    1999-02-01

    Interictal F-18-fluorodeoxyglucose (FDG) PET and ictal Tc-99m-HMPAO SPECT are found to be useful in localizing epileptogenic zones in neocortical lateral temporal or frontal lobe epilepsy. We investigated whether interictal F-18-FDG PET or ictal Tc-99m-HMPAO SPECT was useful to find epileptogenic zones in occipital lobe epilepsy (OLE). We reviewed patterns of hypometabolism in interictal F-18 FDG PET and of hyperfusion in ictal Tc-99m-HMPAO SPECT in 17 OLE patients (mean age=27{+-}6.8 year, M : F=10:7, injection time =30{+-}17 sec). OLE was diagnosed based on invasive electroencephalography (EEG) study, surgery and post-surgical outcome (Engel class I in all for average 14 months). Epileptogenic zones were correctly localized in 9 (60%) out of 15 patients by interictal F-18-FDG PET. Epiletogenic hemispheres were correctly lateralized in 14 patients (93%) . By ictal Tc-99m-HMPAO SPECT, epileptogenic hemispheres were correctly lateralized in 13 patients (76%), but localization was possible only in 3 patients (18%). Among patients who showed no abnormality with MR imaging and no correct localization with ictal Tc-99m-HMPAO SPECT, interictal F-18-FDG PET was helpful in 2 patients. Ictal Tc-99m-HMPAO SPECT was helpful in lateralization but not in localization in OLE. Interictal F-18-FDG PET was helpful for localization of epileptogenic zones even in patients with ambiguous MR of ictal SPECT findings.

  3. Rare Thyroid Cartilage and Diaphragm Metastases from Lung Cancer Visualized on F-18 FDG-PET/CT Imaging

    Directory of Open Access Journals (Sweden)

    Pelin Özcan Kara

    2011-08-01

    Full Text Available Positron emission tomography (PET with F-18 fluorodeoxyglucose (FDG has evolved as a useful imaging modality in the assessment of a variety of cancers, especially for tumor staging and post treatment monitoring. It provides metabolic information. Although, when used alone, relative lack of anatomic landmarks, is a major limitation of PET imaging, this limitation of PET imaging is overcome by the availability of integrated PET/CT imaging. PET and CT images are acquired in one procedure, yielding fused anatomical and functional data sets. Studies with integrated PET/CT imaging have shown promising results. In this case, we present an interesting integrated PET/CT imaging in a lung cancer patient with rare, diaphragm and thyroid cartilage metastases. (MIRT 2011;20:70-72

  4. Experience of Dual Time Point Brain F-18 FDG PET/CT Imaging in Patients with Infections Disease

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Dae Weung; Kim, Chang Guhn; Park, Soon Ah; Jung, Sang Ah [Wonkwang University School of Medicine, Iksan (Korea, Republic of)

    2010-06-15

    Dual time point FDG PET imaging (DTPI) has been considered helpful for discrimination of benign and malignant disease, and staging lymph node status in patients with pulmonary malignancy. However, DTPI for benign disease has been rarely reported, and it may show a better description of metabolic status and extent of benign infection disease than early imaging only. The authors report on the use F-18 fluorodeoxyglucose (FDG) positron emission tomography (PET)/computed tomography (CT) imaging with additional delayed imaging on a 52-year-old man with sparganosis and a 70-year-old man with tuberculous meningitis. To the best of our knowledge, this is the first report on dual time point PET/CT imaging in patients with cerebral sparganosis and tuberculous meningitis.

  5. F 18 FDG PET/CT Findings of Spontaneous Mesenteric Fibromatosis in a Patient with Gardner's Syndrome

    Energy Technology Data Exchange (ETDEWEB)

    Sohn, Myung Hee; Jeong, Young Jin; Lim, Seok Tae; Kim, Dong Wook; Jeong, Hwan Jeong; Yim, Chang Yeol [Chonbuk National Univ. Medical School and Hospital, Jeonju (Korea, Republic of)

    2011-06-15

    Gardner's syndrome (GS), a variant of familial adenomatous polyposis, is an autosomal dominant disease. Originally, Gardner described a syndrome consisting of hereditary intestinal polyposis With osteomas and multiple cutaneous and subcutaneous lesions. The syndrome was later modified by the addition of other features, such as dental abnormalities, abdominal fibromatosis, and a number of malignant tumors. the principal cutaneous lesions that have been described in GS are epidermoid cysts. Other cutaneous lesions include fibromas, lipomas, leiomyomas, neurofibromas, and pigmented skin lesions. Fibromatoses are histologically benign, but locally aggressive fibrous tumors consisting of mature fibroblasts within an extensive collagen matrix. Most cases are sporadic, but there is a clear association with familial adenomatous polyposis and GS, suggesting a link with a mutation of the APC gene on chromosome 5q22. Fibromatosis occurs in 3.5%-29% of patients with GS, and is more likely to be multiple and to involve the mesentery and abdominal wall rather than being an isolated form. Clinically, fibromatosis presents as a painless firm soft tissue mass. Most cases of fibromatosis are believed to be precipitated by surgical trauma, however, a few cases of spontaneous occurrence have been reported. In our patient, no history of abdominal surgery or trauma was present. In addition, an abdominal CT obtained 2 years ago revealed no abnormality. Although the radiological features of fibromatosis on CT or MR have been described in the literature, F 18 FDG PET or PET/CT findings are rarely reported. The F 18 FDG uptake in patients with fibromatosis ranged from low to moderate grade and was generally heterogenous with a few tiny foci of relatively intense uptake or relatively homogenous. The areas of higher FDG metabolism are likely to represent more cellular and mitotically active areas. Mesenteric fibromatosis has similar findings to extra abdominal lesions.

  6. Sci—Fri AM: Mountain — 04: Label-free Raman spectroscopy of single tumour cells detects early radiation-induced glycogen synthesis associated with increased radiation resistance

    Energy Technology Data Exchange (ETDEWEB)

    Matthews, Q; Lum, JJ [BC Cancer Agency — Vancouver Island Centre (Canada); Isabelle, M; Harder, S; Jirasek, A [Physics and Astronomy, University of Victoria (Australia); Brolo, AG [Chemistry, University of Victoria (Australia)

    2014-08-15

    Purpose: To use label-free Raman spectroscopy (RS) for early treatment monitoring of tumour cell radioresistance. Methods: Three human tumour cell lines, two radioresistant (H460, SF{sub 2} = 0.57 and MCF7, SF{sub 2} = 0.70) and one radiosensitive (LNCaP, SF{sub 2} = 0.36), were irradiated with single fractions of 2, 4, 6, 8 or 10 Gy. In additional experiments, H460 and MCF7 cells were irradiated under co-treatment with the anti-diabetic drug metformin, a known radiosensitizing agent. Treated and control cultures were analyzed with RS daily for 3 days post-treatment. Single-cell Raman spectra were acquired from 20 live cells per sample, and experiments were repeated in triplicate. The combined data sets were analyzed with principal component analysis using standard algorithms. Cells from each culture were also subjected to standard assays for viability, proliferation, cell cycle, and radiation clonogenic survival. Results: The radioresistant cells (H460, MCF7) exhibited a RS molecular radiation response signature, detectable as early as 1 day post-treatment, of which radiation-induced glycogen synthesis is a significant contributor. The radiosensitive cells (LNCaP) exhibited negligible glycogen synthesis. Co-treatment with metformin in MCF7 cells blocked glycogen synthesis, reduced viability and proliferation, and increased radiosensitivity. Conversely, metformin co-treatment in H460 cells did not produce these same effects; importantly, both radiation-induced synthesis of glycogen and radiosensitivity were unaffected. Conclusions: Label-free RS can detect early glycogen synthesis post-irradiation, a previously undocumented metabolic mechanism associated with tumour cell radioresistance that can be targeted to increase radiosensitivity. RS monitoring of intratumoral glycogen may provide new opportunities for personalized combined modality radiotherapy treatments.

  7. A fully automated two-step synthesis of an {sup 18}F-labelled tyrosine kinase inhibitor for EGFR kinase activity imaging in tumors

    Energy Technology Data Exchange (ETDEWEB)

    Kobus, D.; Giesen, Y.; Ullrich, R.; Backes, H. [Max Planck Institute for Neurological Research with Klaus-Joachim-Zuelch Laboratories of the Max Planck Society and the Faculty of Medicine of the University of Cologne, Cologne (Germany); Neumaier, B. [Max Planck Institute for Neurological Research with Klaus-Joachim-Zuelch Laboratories of the Max Planck Society and the Faculty of Medicine of the University of Cologne, Cologne (Germany)], E-mail: bernd.neumaier@nf.mpg.de

    2009-11-15

    Radiolabelled epidermal growth factor receptor (EGFR) tyrosine kinase (TK) inhibitors potentially facilitate the assessment of EGFR overexpression in tumors. Since elaborate multi-step radiosyntheses are required for {sup 18}F-labelling of EGFR-specific anilinoquinazolines we report on the development of a two-step click labelling approach that was adapted to a fully automated synthesis module. 6-(4-N,N-Dimethylaminocrotonyl)amido-4-(3-chloro-4-fluoro)phenylamino-7-{l_brace}3- [4-(2-[{sup 18}F]fluoroethyl)-2,3,4-triazol-1-yl]propoxy{r_brace}quinazoline ([{sup 18}F]6) was synthesized via Huisgen 1,3-dipolar cycloaddition between 2-[{sup 18}F]fluoroethylazide ([{sup 18}F]4) and the alkyne modified anilinoquinazoline precursor 5. PET images of PC9 tumor xenograft using the novel biomarker showed promising results to visualize EGFR overexpression.

  8. Predictive value of intratumoral heterogeneity of F-18 FDG uptake for characterization of thyroid nodules according to Bethesda categories of fine needle aspiration biopsy results.

    Science.gov (United States)

    Kim, Seong-Jang; Chang, Samuel

    2015-12-01

    The current study was aimed to investigate the clinical value of intratumoral heterogeneity of F-18 FDG uptake for characterization of thyroid nodule (TN) with inconclusive fine-needle aspiration biopsy (FNAB) results. The current study enrolled 200 patients who showed F-18 FDG incidentaloma and were performed FNAB. The intratumoral heterogeneity of F-18 FDG uptake was represented as the heterogeneity factor (HF), defined as the derivative (dV/dT) of a volume-threshold function for a primary tumor. The diagnostic and predictive values of HF and F-18 FDG PET/CT parameters were evaluated for characterization of inconclusive FNAB results. Among F-18 FDG PET/CT parameters, SUVmax, MTV, and TLG of malignant group were statistically higher than those of Bethesda category of suspicious malignant group. However, HF values were not statistically different between the groups of Bethesda categories (Kruskal-Wallis statistics, 9.924; p = 0.0774). In ROC analysis, when HF > 2.751 was used as cut-off value, the sensitivity and specificity for prediction of malignant TN were 100 % (95 % CI 69.2-100 %) and 60 % (95 % CI 42.1-76.1 %), respectively. The AUC was 0.826 (95 % CI 0.684-0.922) and standard error was 0.0648 (p F-18 FDG uptake represented by HF could be a predictor for characterization of TN with inconclusive FNAB results. Additional large population-based prospective studies are needed to validate the diagnostic utility of HF of F-18 FDG PET/CT.

  9. Design, Synthesis, EPR-Studies and Conformational Bias of Novel Spin-Labeled DCC-Analogues for the Highly Regioselective Labeling of Aliphatic and Aromatic Carboxylic Acids.

    Science.gov (United States)

    Gölz, Jan Philipp; NejatyJahromy, Yaser; Bauer, Mirko; Muhammad, Ashraf; Schnakenburg, Gregor; Grimme, Stefan; Schiemann, Olav; Menche, Dirk

    2016-07-04

    Novel types of spin-labeled N,N'-dicyclohexylcarbodiimides (DCC) are reported that bear a 2,2,6,6-tetramethylpiperidinyloxyl (TEMPO) residue on one side and different aromatic and aliphatic cyclohexyl analogues on the other side of the diimide core. These readily available novel reagents add efficiently to aliphatic and aromatic carboxylic acids, forming two possible spin-labeled amide derivatives with different radical distances of the resulting amide. The addition of aromatic DCC analogues proceeds with excellent selectivity, giving amides where the carboxylic acid is exclusively connected to the aromatic residue, while little or no selectivity was observed for the aliphatic congeners. The usefulness of these adducts in structural studies was demonstrated by EPR (electron paramagnetic resonance) measurements of biradical adducts of biphenyl-4,4'-dicarboxylic acids. These analyses also reveal high degrees of conformational bias for aromatic DCC derivatives, which further underlines the powerfulness of these novel reagents. This observation was further corroborated by quantum chemical calculations, giving a detailed understanding of the structural dynamics, while detailed information on the solid state structure of all novel reagents was obtained by X-ray structure analyses.

  10. Synthesis of ¹⁸O-labeled photosynthetically active chlorophylls at the 3- or 7-carbonyl group with high regioselectivity.

    Science.gov (United States)

    Morishita, Hidetada; Mizoguchi, Tadashi; Tamiaki, Hitoshi

    2010-09-01

    The 3- and 7-formyl groups of chlorophyll-d (Chl-d) and bacteriochlorophyll-e (BChl-e), respectively, were regioselectively labeled with an isotopically stable oxygen-18 (¹⁸O) atom to give 3¹-¹⁸O-labeled Chl-d and 7¹-¹⁸O-labeled BChl-e (ca. 90% ¹⁸O) by exchanging the carbonyl oxygen atoms in the presence of acidic H₂ ¹⁸O (ca. 95% ¹⁸O). Another photosynthetically active chlorophyll, BChl-a possessing the 3-acetyl group was treated under similar acidic conditions to afford a trace amount of 3¹-¹⁸O-labeled BChl-a and further demetallated compound, the corresponding 3¹-¹⁸O-labeled bacteriopheophytin-a as the major product with 55% ¹⁸O-degree. The FT-IR spectra of ¹⁸O-(un)labeled chlorophylls in the solution and the solid states showed that the 3- and 7-carbonyl stretching vibration modes moved to about a 30-cm⁻¹ lower wavenumber by ¹⁸O-labeling at the 3¹- and 7¹-oxo moieties. In artificial chlorosome-like self-aggregates of BChl-e, the ¹⁸O-labeled 7-carbonyl stretching mode was completely resolved from the specially hydrogen-bonded 13-C=O stretching mode, evidently indicating no interaction of the 7-CHO with other functional groups in the supramolecules.

  11. Synthesis and evaluation of a technetium-99m labeled cytotoxic bombesin peptide conjugate for targeting bombesin receptor-expressing tumors

    Energy Technology Data Exchange (ETDEWEB)

    Okarvi, Subhani M. [Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, MBC-03, PO Box 3354, Riyadh 11211 (Saudi Arabia)], E-mail: sokarvi@kfshrc.edu.sa; Al Jammaz, Ibrahim [Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, MBC-03, PO Box 3354, Riyadh 11211 (Saudi Arabia)

    2010-04-15

    Conjugation of the cytotoxic drugs to receptor-binding peptides is an attractive approach for the targeted delivery of cytotoxic peptide conjugates to tumor cells. In an attempt to develop an efficient peptide-based radiopharmaceutical for targeting bombesin (BN) receptor-expressing tumors (i.e., breast and prostate), we have prepared by solid-phase peptide synthesis, a novel BN analog derived from the universal sequence of BN and conjugated to a widely characterized antineoplastic agent, methotrexate (MTX). MTX-BN, after radiolabeling with {sup 99m}Tc via stannous-tartrate exchange, showed a good stability against cysteine and histidine transchelation as well as a high in vitro metabolic stability in human plasma. In vitro cell-binding and internalization on MDA-MB-231, MCF-7, T47-D breast cancer and PC-3 prostate cancer cell lines demonstrated high affinity and specificity of {sup 99m}Tc-MTX-BN towards both human breast and prostate cancer cells (binding affinities in nanomolar range). In addition, the radioconjugate displayed a significant internalization (values ranged between 19-35%) into the tumor cells. In vivo biodistribution and clearance kinetics in Balb/c mice are characterized by an efficient clearance from the blood and excretion mainly through the renal-urinary pathway with some elimination via the hepatobiliary system. In vivo tumor uptake in nude mice bearing MDA-MB-231 cells was 2.70{+-}0.44% ID/g at 1 h, whereas in nude mice with human epidermoid KB cells the accumulation in the tumor was found to be 1.48{+-}0.31% ID/g at 1 h post injection. The tumor uptake was always higher than in the blood and muscle, with good tumor retention and good tumor-to-blood and tumor-to-muscle ratios. The accumulation/retention in the major organs (i.e., lungs, stomach, liver, intestines, etc.) was low to moderate (<6% ID/g) in both healthy and tumor-bearing mice. However, the uptake/retention in the kidneys was rather high (up to 11.05{+-}1.80% ID/g), which is of a

  12. Design, synthesis and biological evaluation of a simplified fluorescently labeled discodermolide as a molecular probe to study the binding of discodermolide to tubulin.

    Science.gov (United States)

    Qi, Jun; Blanden, Adam R; Bane, Susan; Kingston, David G I

    2011-09-01

    The design, synthesis, and biological evaluation of a simplified fluorescently labeled discodermolide analogue possessing a dimethylaminobenzoyl fluorophore has been achieved. Stereoselective Suzuki coupling and Horner-Wadsworth-Emmons reaction comprised the key tactics for its construction. The analogue exhibited qualitatively similar activity to paclitaxel in a tubulin assembly assay, and it can thus be used as a fluorescent molecular probe to explore the local environment of the discodermolide binding site on tubulin. The results of fluorescence measurements on the tubulin-bound analogue are reported.

  13. Regioselective synthesis of isotopically labeled Δ9-tetrahydrocannabinolic acid A (THCA-A-D3) by reaction of Δ9-tetrahydrocannabinol-D3 with magnesium methyl carbonate.

    Science.gov (United States)

    Roth, Nadine; Wohlfarth, Ariane; Müller, Michael; Auwärter, Volker

    2012-10-10

    For the reliable quantification of Δ9-tetrahydrocannabinolic acid A (THCA-A), the biogenetic precursor of Δ9-tetrahydrocannabinol (THC), in biological matrices by LC-MS/MS and GC-MS(/MS), an isotopically labeled internal standard was synthesized starting from Δ9-tetrahydrocannabinol-D(3) (THC-D(3)). Synthesis strategy was based on a method reported by Mechoulam et al. in 1969 using magnesium methyl carbonate (MMC) as carboxylation reagent for the synthesis of cannabinoid acids. Preliminary experiments with THC to optimize yield of the product (THCA-A) resulted in the synthesis of the positional isomer tetrahydrocannabinolic acid B (THCA-B) as a byproduct. Using the optimized conditions for the desired isomer, THCA-A-D(3) was prepared and isolated with a yield of approx. 10% after two synthesis cycles. Isotope purity was estimated to be >99% by relative abundance of the molecular ions. The synthesized compound proved to be suitable as an internal standard for quantification of THCA-A in serum and hair samples of cannabis consumers.

  14. Investigation of the relationship between SLA-1 and SLA-3 gene expression and susceptibility to Escherichia coli F18 in post-weaning pigs.

    Science.gov (United States)

    Ye, L; Zi, C; Pan, Z Y; Zhu, J; Du, Z D; Zhu, G Q; Huang, X G; Bao, W B; Wu, S L

    2012-01-01

    Porcine post-weaning diarrhea and edema disease are principally caused by Escherichia coli strains that produce F18 adhesin. FUT1 genotyping and receptor binding studies divided piglets into E. coli F18-resistant and -sensitive groups, and the roles of SLA-1 and SLA-3 were investigated. SLA-1 and SLA-3 expression was detected in 11 pig tissues, with higher levels of SLA-1 in lung, immune tissues and gastrointestinal tract, and higher levels of SLA-3 also in lung and lymphoid tissues. Both genes were expressed higher in F18-resistant piglets, and their expression was positively correlated in different tissues; a negative correlation was observed in some tissues of F18-sensitive group, particularly in lung and lymphatic samples. Gene ontology and pathway analyses showed that SLA-1 and SLA-3 were involved in 37 biological processes, including nine pathways related to immune functions. These observations help to elucidate the relationship between SLA class I genes and E. coli F18-related porcine gastrointestinal tract diseases. Copyright © 2011 Elsevier Ltd. All rights reserved.

  15. Clinical implication of F-18 FDG PET/CT for differentiated thyroid cancer in patients with negative diagnostic iodine-123 scan and elevated thyroglobulin

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Seong-Jang [Department of Nuclear Medicine, Pusan National University Hospital, Busan (Korea, Republic of); Medical Research Institute, Pusan National University Hospital, Busan (Korea, Republic of)], E-mail: growthkim@daum.net; Lee, Tae Hong [Medical Research Institute, Pusan National University Hospital, Busan (Korea, Republic of); Department of Radiology, Pusan National University Hospital, Busan (Korea, Republic of); Kim, In-Ju; Kim, Yong-Ki [Department of Nuclear Medicine, Pusan National University Hospital, Busan (Korea, Republic of); Medical Research Institute, Pusan National University Hospital, Busan (Korea, Republic of)

    2009-04-15

    This study aims to investigate the usefulness of F-18 FDG PET/CT in differentiated thyroid cancer (DTC) with elevated serum thyroglobulin (Tg) but negative iodine-123 (I-123) scan. Methods: Twenty patients with histopathologically proven DTC, negative diagnostic I-123 scan, and elevated serum Tg levels were prospectively submitted to F-18 FDG PET/CT evaluation. The histopathologic findings consisted of 19 papillary thyroid cancers, 1 follicular thyroid cancer. Results: F-18 FDG PET/CT identified lesions in 18 out of 20 patients, giving a sensitivity of 90%. Thirteen of the 18 patients revealed limited loco-regional disease. Remaining 5 patients showed distant metastases, consisting of 4 patients with lung metastases and 1 patient with bone metastasis. Two patients revealed negative F-18 FDG PET/CT findings. Conclusion: F-18 FDG PET/CT is suitable for the detection and precise localization of loco-regional recurrences and distant metastases of DTC in patients with elevated serum Tg but negative I-123 whole body scan.

  16. 基于语言值的变权综合决策方法%Approach of Variable Weights Synthesis Decision Making Based on Linguistic Labels

    Institute of Scientific and Technical Information of China (English)

    李彦路; 李德清

    2012-01-01

    Multiplicative and additive operations between linguistic labels are given. By- applying extension principle and lattice similarity measures, the reasonability of the opera tions is proved. Based on the above works, a 2-tuple weighted synthesis decision model of pure linguistic label is proposed. Later, two transforming functions between linguistic set and the interval of [0, 1] are defined, the concept of linguistic utility vector of linguistic label is introduced. Furthermore, linguistic state variable weight vector is constructed by using utility vector of linguistic label and state variable weight vector of real number. Finally, two formulas for calculating variable weights based on linguistic labels and two variable weights synthesizing decision models are proposed.%给出一种新的语言值乘法和加法运算,同时利用扩展原理、格贴近度和择近原则等理论论证所给运算法则的科学性,在此基础上建立一个基于二元组的纯语言值加权综合决策模型.随后,在语言值与实数集[0,1]之间定义两个转换函数,由此引入语言值效用向量等概念,借助语言值效用向量和实数型状态变权向量导出语言值状态变权向量,进而建立相应的语言值变权公式和变权综合决策模型.

  17. Synthesis and in vivo distribution in rat brain of /sup 11/C-labelled N-alkylated ADTN derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Werf, J.F. van der; Vaalburg, W.; Korf, J.; Kuilman, T.; Wiegman, T. (Rijksuniversiteit Groningen (Netherlands). Hospital)

    1984-05-01

    A method for the rapid production and purification of /sup 11/C-labelled N-alkylated derivatives of the dopamine agonist 2-amino-6,7-dihydroxytetralin (ADTN) is described. The label is introduced by N-methylation with no-carrier-added /sup 11/CH/sub 3/I of the corresponding secondary amines via their lithium salts. Following systemic injection in rats a uniform distribution of radioactivity in the brain was found for both the labelled 2-(N-methyl-N-n-propylamino)- and 2-(N,N-dimethylamino)-6,7-dihydroxytetralin.

  18. Synthesis and in vivo distribution in rat brain of /sup 11/C-labelled N-alkylated ADTN derivatives

    Energy Technology Data Exchange (ETDEWEB)

    van der Werf, J.F.; Vaalburg, W.; Korf, J.; Kuilman, T.; Wiegman, T.

    1984-05-01

    A method for the rapid production and purification of /sup 11/C-labelled N-alkylated derivatives of the dopamine agonist 2-amino-6,7-dihydroxytetralin (ADTN) is described. The label is introduced by N-methylation with no-carrier-added /sup 11/CH/sup 3/I of the corresponding secondary amines via their lithium salts. Following systemic injection in rats a uniform distribution of radioactivity in the brain was found for both the labelled 2-(N-methyl-N-n-propylamino)- and 2-(N,N-dimethylamino)-6,7-dihydroxytetralin.

  19. Perylene-labeled silica nanoparticles: synthesis and characterization of three novel silica nanoparticle species for live-cell imaging.

    Science.gov (United States)

    Blechinger, Julia; Herrmann, Rudolf; Kiener, Daniel; García-García, F Javier; Scheu, Christina; Reller, Armin; Bräuchle, Christoph

    2010-11-05

    The increasing exposure of humans to nanoscaled particles requires well-defined systems that enable the investigation of the toxicity of nanoparticles on the cellular level. To facilitate this, surface-labeled silica nanoparticles, nanoparticles with a labeled core and a silica shell, and a labeled nanoparticle network-all designed for live-cell imaging-are synthesized. The nanoparticles are functionalized with perylene derivatives. For this purpose, two different perylene species containing one or two reactive silica functionalities are prepared. The nanoparticles are studied by transmission electron microscopy, widefield and confocal fluorescence microscopy, as well as by fluorescence spectroscopy in combination with fluorescence anisotropy, in order to characterize the size and morphology of the nanoparticles and to prove the success and homogeneity of the labeling. Using spinning-disc confocal measurements, silica nanoparticles are demonstrated to be taken up by HeLa cells, and they are clearly detectable inside the cytoplasm of the cells.

  20. Bitemporal hypometabolism in Creutzfeldt-Jakob Disease measured by positron emission tomography with (F-18)2-fluorodeoxyglucose

    Energy Technology Data Exchange (ETDEWEB)

    Friedland, R.P.; Budinger, T.F.; Prusiner, S.B.; Jagust, W.J.

    1984-01-01

    It is well established that Creutzfeldt-Jakob Disease (CJD) is caused by a slow infectious agent similar to the scrapie prion. However, the pathogenesis of this infection is poorly understood. Positron emission tomography (PET) was performed on a 54 year old male subject with autopsy confirmed CJD using (F-18)2-fluorodeoxyglucose (FDG) and the Donner 280-crystal tomograph. An x-ray computed tomographic study of the brain performed 4 days prior to PET was normal. In the PET study the frontal to temporal cortex difference of activity densities was 30% on the left and 12% on the right, reflecting temporal hypometabolism. The left-right temporal cortex difference of activity density was 25%, documenting marked hemispheric asymmetry. These findings are similar to those previously obtained in PET-FDG studies of patients with clinically defined Alzheimer's Disease (AD) and are distinctly different from PET-FDG finding in patients with other dementing illnesses or in healthy aged subjects. Recent work has demonstrated extensive biological similarities between CJD, scrapie and AD. The similarities in the regional metabolic alterations between CJD and AD provide additional evidence for the hypothesis that AD is caused by a slow infectious (prion-like) pathogen.

  1. False-positive axillary lymph node on F-18 FDG PET/CT due to moxibustion therapy

    Energy Technology Data Exchange (ETDEWEB)

    Jeong, Shin Young; Lee, Sang Woo; Ahn, Byeong Cheol; Lee, Jae Tae [Kyungpook National University Hospital, Daegu (Korea, Republic of); Seo, Ji Hyoung [Inje University Haeundae Paik Hospital, Busan (Korea, Republic of)

    2010-12-15

    A 30-year-old female was diagnosed with papillary thyroid cancer and underwent total thyroidectomy and high-dose radioiodine ablation. F-18 fluorodeoxyglucose (FDG) positron emission tomography/computed tomography (PET/CT) for recurrence detection of thyroid carcinoma was performed at 3 years after total thyroidectomy. Moxibustion is a traditional Chinese medicine therapy using moxa or the mugwort herb. Moxibustion is the burning of a small, thimble-sized, smoldering plug of dried leaves such as moxa or mugwort on the skin at an acupuncture point. Acupuncture and moxibustion induce hyperemia and a local inflammatory reaction. Complications associated with moxibustion such as skin bums or infection of the site have been reported previously. False-positive FDG uptake in PET may result from inflammation, infection, and variations in physiological uptake. In the present case, the hypermetabolic axillary lymph node disappeared without any treatment. Well-known of false-positive FDG uptake in axillary lymph noes such as arthritis of the upper extremity, extravasation of injected FDG, and vaccination were not found. Thus, left axillary lymph node uptake was

  2. Determining degradation and synthesis rates of arabidopsis proteins using the kinetics of progressive 15N labeling of two-dimensional gel-separated protein spots.

    Science.gov (United States)

    Li, Lei; Nelson, Clark J; Solheim, Cory; Whelan, James; Millar, A Harvey

    2012-06-01

    The growth and development of plant tissues is associated with an ordered succession of cellular processes that are reflected in the appearance and disappearance of proteins. The control of the kinetics of protein turnover is central to how plants can rapidly and specifically alter protein abundance and thus molecular function in response to environmental or developmental cues. However, the processes of turnover are largely hidden during periods of apparent steady-state protein abundance, and even when proteins accumulate it is unclear whether enhanced synthesis or decreased degradation is responsible. We have used a (15)N labeling strategy with inorganic nitrogen sources coupled to a two-dimensional fluorescence difference gel electrophoresis and mass spectrometry analysis of two-dimensional IEF/SDS-PAGE gel spots to define the rate of protein synthesis (K(S)) and degradation (K(D)) of Arabidopsis cell culture proteins. Through analysis of MALDI-TOF/TOF mass spectra from 120 protein spots, we were able to quantify K(S) and K(D) for 84 proteins across six functional groups and observe over 65-fold variation in protein degradation rates. K(S) and K(D) correlate with functional roles of the proteins in the cell and the time in the cell culture cycle. This approach is based on progressive (15)N labeling that is innocuous for the plant cells and, because it can be used to target analysis of proteins through the use of specific gel spots, it has broad applicability.

  3. Synthesis of RNAs with up to 100 Nucleotides Containing Site-Specific 2-methylseleno Labels for use in X-ray Crystallography

    Energy Technology Data Exchange (ETDEWEB)

    Hobartner,C.; Rieder, R.; Kreutz, C.; Puffer, B.; Lang, K.; Polonskaia, A.; Serganov, A.; Micura, R.

    2005-01-01

    The derivatization of nucleic acids with selenium is a new and highly promising approach to facilitate their three-dimensional structure determination by X-ray crystallography. Here, we report a comprehensive study on the chemical and enzymatic syntheses of RNAs containing 2'-methylseleno (2'-Se-methyl) nucleoside labels. Our approach includes the first synthesis of an appropriate purine nucleoside phosphoramidite building block. Most importantly, a substantially changed RNA solid-phase synthesis cycle, comprising treatment with threo-1, 4-dimercapto-2, 3-butanediol (DTT) after the oxidation step, is required for a reliable strand elongation. This novel operation allows for the chemical syntheses of multiple Se-labeled RNAs in sizes that can typically be achieved only for nonmodified RNAs. In combination with enzymatic ligation, biologically important RNA targets become accessible for crystallography. Exemplarily, this has been demonstrated for the Diels-Alder ribozyme and the add adenine riboswitch sequences. We point out that the approach documented here has been the chemical basis for the very recent structure determination of the Diels-Alder ribozyme which represents the first novel RNA fold that has been solved via its Se-derivatives.

  4. Value of Bone Scan in Addition to F-18 FDG PET/CT and Characteristics of Discordant Lesions between F-18 FDG PET/CT and Bone Scan in the Spinal Bony Metastasis

    Energy Technology Data Exchange (ETDEWEB)

    Jun, Sung Min; Nam, Hyun Yeol; Kim, In Ju; Kim, Yong Ki [Pusan National University Hospital, Pusan (Korea, Republic of); Kim, Ju Sung [College of Medical Life Science, Silla University, Pusan (Korea, Republic of)

    2008-06-15

    Our purpose was to evaluate spinal bony metastasis which could be missed on an F-18 FDG PET/CT (FDG PET/CT) alone, and to characterize discordant metastatic lesions between FDG PET/CT and bone scan. FDG PET/CT and bone scans of 43 patients with spinal bony metastasis were analyzed retrospectively. A McNemar test was performed comparing the FDG PET/CT alone to the FDG PET/CT plus bone scan in the spinal bony metastases. A one-way chi-square test was performed to characterize the metastases that were missed on the FDG PET/CT alone. To evaluate discordant lesions between FDG PET/CT and bone scan, we performed logistic regression analyses. The independent variables were sites (cervical, thoracic, and lumbar), size (large and small), and maximum SUVs, and the dependant variable was bone scan uptake (positive and negative MDP uptake). A significant difference was found between the FDG PET/CT alone and the FDG PET/CT combined with the bone scan (p<0.01). Using the FDG PET/CT only, diffuse osteoblastic metastasis was missed with a significantly higher frequency (p=0.04). In the univariate analysis, cervical vertebra and small size were related to negative MDP uptake, and thoracic vertebra and large size were related to positive MDP uptake. However, in the multivariate analysis, only the large size was related to positive MDP uptake. A bone scan in addition to the FDG PET/CT increased the ability to evaluate spinal bony metastases, especially for diffuse osteoblastic metastasis. Large metastasis was related to positive bone scan uptake in spinal bony metastasis.

  5. Unexpected second primary malignancies detected by f-18 FDG PET/CT during follow-up for primary malignancy: Two case report

    Energy Technology Data Exchange (ETDEWEB)

    Bang, Ji In; Lee, Eun Seong; Kim, Tae Sung; Kim, Seok Ki [Nuclear Medicine, Research Institute and Hospital, National Cancer Center, Goyang (Korea, Republic of)

    2015-03-15

    As the survival rate of cancer patients has increased over the last few decades, the risk of cancer survivors developing second primary malignancies has gained attention. We report two rare cases of second primary hematologic malignancy detected by 18F-fluorodeoxyglucose (F-18 FDG) positron emission tomography/computed tomography (PET/CT) during follow-up for primary solid malignancies. Acute lymphoblastic leukemia developed in a breast cancer patient and non-Hodgkin lymphoma in an anal cancer patient. F-18 FDG PET/CT findings led to the diagnosis of unexpected second primary hematologic malignancy in cancer survivors in these two cases.

  6. Development of pharmaceuticals with radioactive rhenium for cancer therapy. Production of {sup 186}Re and {sup 188}Re, synthesis of labeled compounds and their biodistributions

    Energy Technology Data Exchange (ETDEWEB)

    NONE

    1998-03-01

    Production of the radioactive rhenium isotopes {sup 186}Re and {sup 188}Re, and synthesis of their labeled compounds have been studied together with the biodistributions of the compounds. This work was carried out by the Working Group on Radioactive Rhenium, consisting of researchers of JAERI and some universities, in the Subcommittee for Production and Radiolabeling under the Consultative Committee of Research on Radioisotopes. For {sup 186}Re, production methods by the {sup 185}Re(n,{gamma}){sup 186}Re reaction in a reactor and by the {sup 186}W(p,n){sup 186}Re reaction with an accelerator, which can produce nocarrier-added {sup 186}Re, have been established. For {sup 188}Re, a production method by the double neutron capture reaction of {sup 186}W, which produces a {sup 188}W/{sup 188}Re generator, has been established. For labeling of bisphosphonate, DMSA, DTPA, DADS, aminomethylenephosphonate and some monoclonal antibodies with the radioactive rhenium isotopes, the optimum conditions, including pH, the amounts of reagents and so on, have been determined for each compound. The biodistributions of each of the labeled compounds in mice have been also obtained. (author)

  7. Development of F-18 Labeled Radiotracers for PET Imaging of Brain Alpha-1 Noradrenergic Receptors: Potential PTSD Vulnerability and Diagnostic Biomarkers

    Science.gov (United States)

    2012-09-01

    by the NIMH Psychoactive Drug Screening Pro-gram (PDSP). The HEAT analog exhibing the best profile of α1NAR vs. off-target neurotransmitter receptor... drug that blocks excessive stimulation of CNS α1NARs (13)] robustly reduces combat-related nightmares and sleep disturbance and improves overall CSS...to this question, we developed a chiral -HPLC method for the separation of the optical isomers of 2-Fluoro-HEAT [#2], as illustrated in Figure 3. In

  8. Fluorine F 18 Fluorodopa-Labeled PET Scan in Planning Surgery and Radiation Therapy in Treating Patients With Newly Diagnosed High- or Low-Grade Malignant Glioma

    Science.gov (United States)

    2016-10-10

    Adult Anaplastic Astrocytoma; Adult Anaplastic Ependymoma; Adult Anaplastic Oligodendroglioma; Adult Brain Stem Glioma; Adult Diffuse Astrocytoma; Adult Ependymoma; Adult Giant Cell Glioblastoma; Adult Glioblastoma; Adult Gliosarcoma; Adult Mixed Glioma; Adult Myxopapillary Ependymoma; Adult Oligodendroglioma; Adult Pilocytic Astrocytoma; Adult Pineal Gland Astrocytoma; Adult Subependymal Giant Cell Astrocytoma; Adult Subependymoma

  9. [Microbial synthesis of deuterium labelled L-phenylalanine with different levels of isotopic enrichment by facultative methylotrophic bacterium Brevibacterium methylicum with RMP assimilation of carbon].

    Science.gov (United States)

    Mosin, O V; Shvets, V I; Skladnev, D A; Ignatov, I

    2014-01-01

    The preparative microbial synthesis of amino acids labelled with stable isotopes, including deuterium ( 2 H), suitable for biomedical applications by methylotrophic bacteria was studied using L-phenylalanine as example. This amino acid is secreted by Gram-negative aerobic facultative methylotrophic bacteria Brevibacterium methylicum, assimilating methanol via ribulose-5-monophosphate (RMP) cycle of assimilation of carbon, The data on adaptation of L-phenylalanine secreted by methylotrophic bacterium В. methylicum to the maximal concentration of deuterium in the growth medium with 98% 2 Н 2 O and 2% [ 2 Н]methanol, and biosynthesis of deuterium labelled L-phenylalanine With different levels of enrichment are presented. The strain was adapted by means of plating initial cells on firm (2% agarose) minimal growth media with an increasing gradient of 2 Н 2 O concentration from 0; 24.5; 49.0; 73.5 up to 98% 2 Н 2 O followed by subsequent selection of separate colonies stable to the action of 2 Н 2 O. These colonies were capable to produce L-phenylalanine. L-phenylalanine was extracted from growth medium by extraction with isopropanol with the subsequent crystallization in ethanol (output 0.65 g/l). The developed method of microbial synthesis allows to obtain deuterium labelled L-phenylalanine with different levels of isotopic enrichment, depending on concentration of 2 Н 2 O in growth media, from 17% (on growth medium with 24,5% 2 Н 2 O) up to 75% (on growth medium with 98% 2 Н 2 O) of deuterium in the molecule that is confirmed with the data of the electron impact (EI) mass- spectrometry analysis of methyl ethers of N-dimethylamino(naphthalene)-5-sulfochloride (dansyl) phenylalanine in these experimental conditions.

  10. Incidental tenosynovial huge cell tumors of the flexor hallucis longus muscle: seldom differential diagnosis of metabolic lesions using F18-FDG PET/CT; Inzidenteller tenosynovialer Riesenzelltumor des Musculus flexor hallucis longus. Seltene Differenzialdiagnose stoffwechselaktiver Laesionen in der F-18-FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Koestner, W.; Daemmrich, M.; Derlin, T.

    2016-03-15

    Tenosynovial huge cell tumors are seldom benign tumors in extremities originating from bone joint synovia and tendon sheats. In F18-FDG PET/CT imaging the tenosynovial huge cell tumors show increased metabolic activity and can trigger false diagnoses.

  11. CLONING, EXPRESSION, PURIFICATION AND IMMUNOLOGICAL CHARACTERISTICS OF DER F18 FROM DUST HOUSE MITE DERMATOPHA GOIDES FARINAE%粉尘螨Der f18变应原的克隆表达、纯化及免疫学特性鉴定

    Institute of Scientific and Technical Information of China (English)

    朱永烽; 刘志刚; 高波

    2008-01-01

    通过对纯培养的粉尘螨提取总RNA,采用RT-PCR方法有效地扩增出Der f18片段,将Der f18连接到pET-24a表达载体上并转化到表达菌BL21(DE3)中,得到重组质粒pET-Der f18和重组工程菌.重组工程菌经IPTG诱导培养,高效表达出Der f18蛋白,SDS-PAGE结果显示表达产物约为52 kDa.表达产物经亲和层析纯化,用Western blot方法检测免疫学活性,结果表明目的蛋白具有良好的免疫原性.

  12. Synthesis of [1-{sup 11}C]octanoic acid, [{sup 11}C]raclopride and [{sup 11}C]nicergoline with a general-purpose automated synthesis apparatus of {sup 11}C-labeled radiopharmaceuticals

    Energy Technology Data Exchange (ETDEWEB)

    Yajima, Kazuyosi; Kawashima, Hidefumi; Cui, Ying-she; Hashimoto, Naoto; Miyake, Yoshihiro [National Cardiovascular Center, Suita, Osaka (Japan)

    1997-06-01

    We have developed a general-purpose automated synthesis apparatus of {sup 11}C-labeled radiopharmaceuticals for PET, which can be adopted to both one-pot and two-or-more-pot reactions. The features of the apparatus were shown in the successful preparation of [(1-{sup 11})C]octanoic acid in a one-pot reaction and [{sup 11}C]raclopride and [{sup 11}C]nicergoline in two-pot reactions, the latter being a novel radiopharmaceutical. (author).

  13. Prevalencia de antigenos fimbriales f4 y f18 en cerditos lactantes y destetados diarreicos en la provincia de Villa Clara, Cuba (Prevalence of f4 and f18 fimbrial antigens in diarrheal nursing and weaned piglets of the province of Villa Clara.

    Directory of Open Access Journals (Sweden)

    Castillo Cuenca. Julio César

    2012-06-01

    Full Text Available RESUMENEl presente trabajo se realizó con el objetivo de determinar la prevalencia de antígenos fimbriales F4 y F18 en cerditos lactantes y destetados diarreicos de la Provincia de Villa Clara.SUMMARYThe present work was carried out with the objective of determining the prevalence of F4 and F18 fimbrial antigens in diarrheal nursing and weaned piglets of the Province of Villa Clara.

  14. Cognition and amyloid load in Alzheimer disease imaged with florbetapir F 18(AV-45) positron emission tomography.

    Science.gov (United States)

    Rosenberg, Paul B; Wong, D F; Edell, S L; Ross, J S; Joshi, A D; Brašić, J R; Zhou, Y; Raymont, V; Kumar, A; Ravert, H T; Dannals, R F; Pontecorvo, M J; Skovronsky, D M; Lyketsos, C G

    2013-03-01

    To examine the association between regional brain uptake of a novel amyloid positron emission tomography (PET) tracer florbetapir F 18 ([(18)F]-AV-45) and cognitive performance in a pilot study. Cross-sectional comparison of [(18)F]-AV-45 in AD patients versus controls. Three specialty memory clinics. Eleven participants with probable Alzheimer disease (AD) by NINDS/ADRDA criteria and 15 healthy comparison (HC) participants. Participants underwent PET imaging following a 370 MBq (10 mCi) intravenous administration of [(18)F]-AV-45. Regional/cerebellar standardized uptake value ratios (SUVRs) were calculated. Cognition was assessed using Mini-Mental State Examination, Alzheimer's Disease Assessment Scale-Cognitive subscale (ADAS-Cog), Wechsler Logical Memory IA (immediate recall) test (LMIA), and verbal category fluency. Greater [(18)F]-AV-45 SUVR was associated with poorer performance on all cognitive tests. In the HC group, occipital, parietal, precuneus, temporal, and cortical average SUVR was associated with greater ADAS-Cog, and greater anterior cingulate SUVR was associated with lower LMIA. Two HC participants had [(18)F]-AV-45 cortical/cerebellar SUVR greater than 1.5, one of whom had deficits in episodic recall and on follow-up met criteria for amnestic mild cognitive impairment. [(18)F]-AV-45 SUVR in several brain regions was associated with worse global cognitive performance particularly in HC, suggesting its potential as a marker of preclinical AD. Copyright © 2013 American Association for Geriatric Psychiatry. Published by Elsevier Inc. All rights reserved.

  15. Synthesis of carbon nanohorns/chitosan/quantum dots nanocomposite and its applications in cells labeling and in vivo imaging

    Energy Technology Data Exchange (ETDEWEB)

    Li, Jing; He, Zhe [Chemistry Department, Northeastern University, Shenyang 110819 (China); Guo, Changrun [College of Life Sciences, Jilin University, Changchun 130023 (China); Wang, Liping, E-mail: wanglp@jlu.edu.cn [College of Life Sciences, Jilin University, Changchun 130023 (China); Xu, Shukun, E-mail: xushukun46@126.com [Chemistry Department, Northeastern University, Shenyang 110819 (China)

    2014-01-15

    Due to the unique optical and chemical features of quantum dots and the special structural advantages of carbon nanohorns, it is highly desirable to synthesize nanohorns/quantum dots nanocompsite which can be applied in cell labeling and in vivo imaging. Here, we report a new method which uses chitosan as connector to synthesize nanohorns/chitosan/quantum dots fluorescent nanocomposite. Further more, the synthesized nanocomposite demonstrated strong red fluorescence and had been successfully used in Hela cells labeling and in vivo imaging of Caenorhabditis elegans (C. elegans). -- Highlights: Carbon nanohorn/chitosan/QDs nanocomposite was prepared by covalent linkage The nanocomposite was successfully used in the labeling of HeLa cells The nanocomposite was used for in vivo imaging with C. elegans as animal mode.

  16. New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-affinity γ-Hydroxybutyrate (GHB) Binding Sites

    OpenAIRE

    Vogensen, Stine B.; Marek, Aleš; Bay, Tina; Wellendorph, Petrine; Kehler, Jan; Bundgaard, Christoffer; Frølund, Bente; Pedersen, Martin H. F.; Clausen, Rasmus P.

    2013-01-01

    3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA, 1) is a potent ligand for the high-affinity GHB binding sites in the CNS. An improved synthesis of 1 together with a very efficient synthesis of [3H]-1 is described. The radiosynthesis employs in situ generated lithium trimethoxyborotritide. Screening of 1 against different CNS targets establishes a high selectivity and we demonstrate in vivo brain penetration. In vitro characterization of [3H]-1 binding shows high specificity to the high-affin...

  17. Evaluation of Response to Therapy in a Patient with Lung Cancer: Correlation of Sclerotic Bone Lesions with F 18 FDG PET/CT and Bone Scintigraphy

    Directory of Open Access Journals (Sweden)

    Filiz Özülker

    2011-04-01

    Full Text Available A 64-year-old male patient with small cell lung cancer underwent Fluorine-18 fluorodeoxyglucose (F 18 FDG positron emission tomography (PET/CT scan which revealed multiple F 18 FDG uptake in the spine, both humeri, ribs, pelvis and proximal long bones. There was no obvious lytic or sclerotic bone destruction accompanying these lesions on CT component of the study. After the patient received six courses of chemotherapy a repeat F 18 FDG-PET/CT was performed for evaluation of therapy response. The PET/CT showed the presence of multiple sclerotic lesions on CT without FDG uptake, corresponding to the bone lesions on the previous PET/CT scan. A concomitant Tc 99m Methylene diphosphonate (Tc 99m MDP bone scintigraphy (BS revealed no pathologically increased Tc 99m MDP uptake in the skeletal system. The FDG avid lesions in the skeletal system, which were not sclerotic initially, were transformed into FDG non-avid sclerotic lesions after chemotherapy. This was attributed to the direct effect of previous successful therapy for bone metastases, leading to the transformation of metabolically active disease, into blastic metabolically inactive metastases. In conclusion, a F 18 FDG negative bone lesion, which is sclerotic on CT, may represent post-treatment osteoblastic change rather than active tumor and BS might play a role in the discrimination of these two situations. (MIRT 2011; 20: 29-33

  18. Effect of increased serotonin levels on [F-18] MPPF binding in rat brain : Fenfluramine vs the combination of citalopram and ketanserin

    NARCIS (Netherlands)

    de Haes, JIU; Cremers, TIFH; Bosker, FJ; Postema, F; Timersma-Wegman, TD; den Boer, JA

    2005-01-01

    [F-18]MPPF is a selective serotonin-1A (5-HT1A) receptor antagonist and may be used to measure changes in the functional levels of serotonin (5-HT). The technique is based on the assumption that the injected radiolabeled ligand competes for the same receptor as the endogenous transmitter. Results fr

  19. Tumor imaging with 2 sigma-receptor ligands, F-18-FE-SA5845 and C-11-SA4503 : A feasibility study

    NARCIS (Netherlands)

    van Waarde, A; Buursma, AR; Hospers, GAP; Kawamura, K; Kobayashi, T; Ishii, K; Oda, K; Ishiwata, K; Vaalburg, W; Elsinga, PH

    2004-01-01

    Our objective was to study 2 radioligands for visualization of sigma-receptors with PET. Methods: Two radioligands--sigma(1)-selective C-11-1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine (C-11-SA4503) and nonsubtype-selective 1-(4-2'-F-18-fluoroethoxy-3-methoxyphenethyl)-4-(3-(4-fluoropheny

  20. PET STUDIES WITH L-[1-C-11]TYROSINE, L-[METHYL-C-11]METHIONINE AND F-18 FLUORODEOXYGLUCOSE IN PROLACTINOMAS IN RELATION TO BROMOCRYPTINE TREATMENT

    NARCIS (Netherlands)

    DAEMEN, BJG; ZWERTBROEK, R; ELSINGA, PH; PAANS, AMJ; DOORENBOS, H; VAALBURG, W

    1991-01-01

    Aspects of metabolism in prolactinomas were investigated by positron emission tomography using L-[1-C-11]tyrosine, L-[methyl-C-11]methionine and F-18-fluorodeoxyglucose (18FDG). Using L-[1-C-11]tyrosine, four patients were monitored prior to and 18 h after an injection of 50 mg bromocryptine. At 18

  1. Detection and grading of soft tissue sarcomas of the extremities with F-18-3 '-fluoro-3 '-deoxy-L-thymidine

    NARCIS (Netherlands)

    Cobben, DCP; Elsinga, PH; Suurmeijer, AJH; Vaalburg, W; Maas, B; Jager, PL; Hoekstra, HJ

    2004-01-01

    Purpose: The aim of the study was to investigate the feasibility of F-18-3'-fluoro-3'-deoxy-L-thymidine positron emission tomography (FLT-PET) for the detection and grading of soft tissue sarcoma (STS). Experimental Design: Nineteen patients with 20 STSs of the extremities were scanned, using attenu

  2. Residual F-18-FDG-PET Uptake 12 Weeks After Stereotactic Ablative Radiotherapy for Stage I Non-Small-Cell Lung Cancer Predicts Local Control

    NARCIS (Netherlands)

    Bollineni, Vikram Rao; Widder, Joachim; Pruim, Jan; Langendijk, Johannes A.; Wiegman, Erwin M.

    2012-01-01

    Purpose: To investigate the prognostic value of [F-18]fluorodeoxyglucose positron emission tomography (FDG-PET) uptake at 12 weeks after stereotactic ablative radiotherapy (SABR) for stage I non-small-cell lung cancer (NSCLC). Methods and Materials: From November 2006 to February 2010, 132 medically

  3. SPM analysis of brain perfusion SPECT and F-18 FDG PET in the Korean autosomal dominant nocturnal frontal lobe epilepsy family

    Energy Technology Data Exchange (ETDEWEB)

    Won, Kyoung Sook; Zeon, Seok Kil [Keimyung University Dongsan Medical Center, Daegu (Korea, Republic of)

    2004-07-01

    This study attempted to investigate the specific pattern of brain perfusion and glucose metabolism in the Korean autosomal dominant nocturnal frontal lobe epilepsy (ADNFLE) family. Using Tc-99m ECD brain perfusion SPECT. we assessed brain perfusion in 6 patients at interictal period and 5 patients at ictal period. Interictal F-18 FDG PET was performed on 6 affected family members. The scans were statistically analyzed by using statistical parametric mapping (SPM99). The data of the affected family members were compared to those of the control subjects. Interictal F-18 FDG PET SPM group analysis showed decreased glucose metabolism over the left middle and superior frontal gyri and the left central regions including the anterior parietal lobe. There was a less pronounced decrease in glucose uptake in the right anterior superior frontal gyrus. Interictal brain perfusion SPECT SPM group analysis showed similar pattern of decreased perfusion compared to those of interictal F-18 FDG PET. Ictal brain perfusion SPECT SPM group analysis revealed increased perfusion over the left pre-and postcentral gyri and less pronounced increased perfusion in the right postcentral gyrus. lnterictal F -18 PET and brain perfusion SPECT SPM group analysis suggest that major abnormalities of ADNFLE family are in the left frontal lobe. These findings may be helpful to elucidate the pathophysiological mechanism of this rare disease entity.

  4. Predicting Response to Neoadjuvant Chemoradiotherapy in Esophageal Cancer with Textural Features Derived from Pretreatment F-18-FDG PET/CT Imaging

    NARCIS (Netherlands)

    Beukinga, Roelof J.; Hulshoff, Jan B.; van Dijk, Lisanne V.; Muijs, Christina T.; Burgerhof, Johannes G. M.; Kats-Ugurlu, Gursah; Slart, Riemer H. J. A.; Slump, Cornelis H.; Mul, Veronique E. M.; Plukker, John Th. M.

    Adequate prediction of tumor response to neoadjuvant chemoradiotherapy (nCRT) in esophageal cancer (EC) patients is important in a more personalized treatment. The current best clinical method to predict pathologic complete response is SUVmax in F-18-FDG PET/ CT imaging. To improve the prediction of

  5. Microcontroladores PIC F18: estudio y aplicación a la gestión de un aparcamiento de turismos

    OpenAIRE

    Verdejo Garrido, David

    2015-01-01

    En este trabajo de fin de grado se lleva a cabo un estudio de la familia de microcontroladores PIC F18 de Microchip. Departamento de Tecnología Electrónica Grado en Ingeniería en Electrónica Industrial y Automática

  6. Multiple skeletal muscle metastases in a case of transitional cell carcinoma of bladder detected by F-18 FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Kashyap, Raghava; Mittal, Bhagwant Rai; Chakraborty, Dhritiman; Bhattacharya, Anish; Singh, Baljinder [Institute of Medical Education and Research, Chandigarh (India)

    2010-12-15

    We present a case of poorly differentiated muscle invasive transitional cell carcinoma in a 64-year-old male diagnosed with FDG-avid mass in the urinary bladder wall and multiple skeletal muscles visualised on F-18 FDG PET/CT

  7. Synthesis of /sup 14/C- and /sup 3/H-labeled fluoxetine, a selective serotonin uptake inhibitor

    Energy Technology Data Exchange (ETDEWEB)

    Robertson, D.W.; Krushinski, J.H.; Wong, D.T.; Kau, D.

    1987-11-01

    Fluoxetine (N-methyl-..gamma..-(4-(trifluoromethyl)phenoxy) benzenepropanamine) is a potent, highly selective serotonin uptake inhibitor that is useful in treating a variety of major psychiatric derangements. We have synthesized this compound in /sup 14/C- and /sup 3/H-labeled forms. The tritium label was introduced in the final step by catalytic dehalogenation of the brominated fluoxetine precursor. Reaction conditions could be controlled such that catalytic hydrogenolysis of the labile C-O benzylic bond was minimized. Following HPLC purification, (/sup 3/H)-fluoxetine was obtained in a state of high radiochemical purity (98%) and specific activity (20.4 Ci/mmol). The /sup 14/C-label was introduced in the final step via a nucleophilic aromatic substitution reaction between the sodium salt of ..cap alpha..-(2-(methylamino)ethyl)benzenemethanol and uniformly ring-labeled p-chlorobenzotrifluoride. Following purification by flash chromatography, (/sup 14/C)-fluoxetine was obtained in 98.3% radiochemical purity with a specific activity of 5.52 mCi/mmol.

  8. Synthesis of [sup 14]C-labelled sodium pariprazole (E3810). [Anti-ulcer agent; ATPase inhibitor

    Energy Technology Data Exchange (ETDEWEB)

    Tagami, Katsuya; Chiku, Shigeru; Sohda, Shigeru (Eisai Co., Ltd., Ibaraki (Japan). Tsukuba Research Labs.)

    1993-09-01

    Sodium pariprazole (E3810), an inhibitor of H[sup +],K[sup +]-ATPase, was synthesized labelled with carbon-14, starting from 2-mercapto[2-[sup 14]C]-benzimidazole with a specific activity of 888 MBq/mmol. It was obtained in 49.3% radiochemical yield with a radiochemical purity of more than 98%. (author).

  9. Universal chitosan-assisted synthesis of Ag-including heterostructured nanocrystals for label-free in situ SERS monitoring.

    Science.gov (United States)

    Cai, Kai; Xiao, Xiaoyan; Zhang, Huan; Lu, Zhicheng; Liu, Jiawei; Li, Qin; Liu, Chen; Foda, Mohamed F; Han, Heyou

    2015-12-07

    A universal chitosan-assisted method was developed to synthesize various Ag-including heterostructured nanocrystals, in which chelation probably plays a vital role. The as-prepared Ag/Pd heterostructured nanocrystals show outstanding properties when used as bifunctional nanocomposites in label-free in situ SERS monitoring of Pd-catalyzed reaction.

  10. Diagnostic Performance of F-18 FDG PET/CT in Patients with Cancer of Unknown Primary: Additional Benefit over CT-Based Conventional Work up

    Directory of Open Access Journals (Sweden)

    Mehrdad Bakhshayeshkaram

    2016-01-01

    Full Text Available Background: In the era of well-developed site-specific treatment strategies in cancer, identification of occult primary is of paramount importance in CUP patients. Furthermore, exact determination of the extent of the disease may help in optimizing treatment planning. The aim of the present study was to investigate additional value of F-18 FDG PET/CT in patients with cancer of unknown primary (CUP as an appropriate imaging tool in early phase of initial standard work up.Materials and Methods: Sixty-two newly diagnosed CUP patients with inconclusive diagnostic CT scan of chest, abdomen and pelvis referring for F-18 FDG PET/CT were enrolled in this study. Standard of reference was defined as histopathology, other diagnostic procedures and a 3-month formal clinical follow up. The results of PET/CT were categorized as suggestion for primary site and additional metastasis and classified as true positive, false positive, false negative and true negative. The impact of additional metastasis revealed by F-18 FDG PET/CT on treatment planning and the time contribution of F-18 FDG PET/CT in diagnostic pathway was investigated.Results: Sixty-two patients with mean age of 62 (30 men, 32 women, PET/CT correctly identified primary origin in 32% with false positive rate of 14.8%. No primary lesion was detected after negative PET/CT according to standard of reference. Sensitivity, Specificity and accuracy were 100%, 78% and 85%, respectively. Additional metastatic site was found in 56% with 22% impact on treatment planning. Time contribution for PET/CT was 10% of total diagnostic pathway.Conclusion: Providing higher detection rate of primary origin with excellent diagnostic performance, shortening the diagnostic pathway and improving treatment planning, F-18 FDG PET/CT may play a major role in diagnostic work up of CUP patients and may be recommended as an alternative imaging tool in early phase of investigation.

  11. New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-affinity γ-Hydroxybutyrate (GHB) Binding Sites

    Science.gov (United States)

    Vogensen, Stine B.; Marek, Aleš; Bay, Tina; Wellendorph, Petrine; Kehler, Jan; Bundgaard, Christoffer; Frølund, Bente; Pedersen, Martin H.F.; Clausen, Rasmus P.

    2013-01-01

    3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA, 1) is a potent ligand for the high-affinity GHB binding sites in the CNS. An improved synthesis of 1 together with a very efficient synthesis of [3H]-1 is described. The radiosynthesis employs in situ generated lithium trimethoxyborotritide. Screening of 1 against different CNS targets establishes a high selectivity and we demonstrate in vivo brain penetration. In vitro characterization of [3H]-1 binding shows high specificity to the high-affinity GHB binding sites. PMID:24053696

  12. New synthesis and tritium labeling of a selective ligand for studying high-affinity γ-hydroxybutyrate (GHB) binding sites.

    Science.gov (United States)

    Vogensen, Stine B; Marek, Aleš; Bay, Tina; Wellendorph, Petrine; Kehler, Jan; Bundgaard, Christoffer; Frølund, Bente; Pedersen, Martin H F; Clausen, Rasmus P

    2013-10-24

    3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA, 1) is a potent ligand for the high-affinity GHB binding sites in the CNS. An improved synthesis of 1 together with a very efficient synthesis of [(3)H]-1 is described. The radiosynthesis employs in situ generated lithium trimethoxyborotritide. Screening of 1 against different CNS targets establishes a high selectivity, and we demonstrate in vivo brain penetration. In vitro characterization of [(3)H]-1 binding shows high specificity to the high-affinity GHB binding sites.

  13. New Synthesis and Tritium Labeling of a Selective Ligand for Studying High-Affinity γ-Hydroxybutyrate (GHB) Binding Sites

    DEFF Research Database (Denmark)

    Vogensen, Stine B.; Marek, Ales; Bay, Tina

    2013-01-01

    3-Hydroxycyclopent-1-enecarboxylic acid (HOCPCA, 1) is a potent ligand for the high-affinity GHB binding sites in the CNS. An improved synthesis of 1 together with a very efficient synthesis of [3H]-1 is described. The radiosynthesis employs in situ generated lithium trimethoxyborotritide....... Screening of 1 against different CNS targets establishes a high selectivity, and we demonstrate in vivo brain penetration. In vitro characterization of [3H]-1 binding shows high specificity to the high-affinity GHB binding sites....

  14. Synthesis and characterization of C@CdS dots in aqueous solution and their application in labeling human gastric carcinoma cells

    Energy Technology Data Exchange (ETDEWEB)

    Dong, Wei, E-mail: dongwei5873@126.com [Shenyang Medical College, Department of Chemistry (China); Zhou, Siqi [Fengtian Hospital Affiliated to Shenyang Medical College, ICU (China); Dong, Yan [Shenyang Pharmaceutical University, Experiment Center of Traditional Chinese Medicine Department (China); Wang, Jingwen; Liu, Shuang; Zhu, Pengxia [Shenyang Medical College, Department of Chemistry (China)

    2015-03-15

    Colloidal carbon spheres coated with cadmium sulfide nanoparticle quantum dots (C@CdS dots) with the particle size smaller than 50 nm were synthesized by an aqueous approach. The effects of different reaction times, temperatures, and pH values were carefully investigated to optimize the synthesis conditions. The as-prepared C@CdS dots were linked with mouse anti-human carcinoembryonic antigen antibody and goat anti-mouse immunoglobulin (IgG) to directly and indirectly label fixed human gastric carcinoma cells, respectively. The cytotoxicity of the C@CdS dots was also tested using the human gastric carcinoma cells. No apparent cytotoxicity was observed, which suggested the potential application of the as-prepared C@CdS dots in bioimaging.

  15. A semi-preparative enzymic synthesis of malonyl-CoA from [14C]acetate and 14CO2: labelling in the 1, 2 or 3 position.

    Science.gov (United States)

    Roughan, G

    1994-06-01

    A semi-preparative enzymic synthesis of [1-14C]malonyl-CoA from [1-14C]acetate and bicarbonate, and of [3-14C]malonyl-CoA from Na2(14)CO3 and acetate, was achieved by using chloroplasts rapidly isolated from 7-8-day-old pea shoots. Around 70% of the [1-14C]acetate was converted into malonyl-CoA in 2-3 h, and the specific radioactivity of [3-14C]malonyl-CoA synthesized in the system was 25-30 Ci/mol. Reactions were monitored and labelled products were purified by h.p.l.c.

  16. Design and Synthesis of an 18F-Labeled Version of Phenylethyl Orvinol ([18F]FE-PEO for PET-Imaging of Opioid Receptors

    Directory of Open Access Journals (Sweden)

    Gjermund Henriksen

    2012-09-01

    Full Text Available The semisynthetic oripavine derivative phenethyl orvinol (PEO, a full agonist at opioid receptors (OR, is an attractive structural motif for developing 18F-labeled PET tracers with a high degree of sensitivity for competition between endogenous and exogenous OR-ligands. The target cold reference compound 6-O-(2-fluoroethyl-6-O-desmethylphenylethyl orvinol (FE-PEO was obtained via two separate reaction routes. A three-step synthesis was developed for the preparation of a tosyloxyethyl precursor (TE-TDPEO, the key precursor for a direct, nucleophilic radiofluorination to yield [18F]FE-PEO. The developed radiosynthesis provides the target compound in relevantly high yield and purity, and is adaptable to routine production.

  17. Synthesis of organic substances labelled with {sup 14}C and {sup 35}S; Syntheses de molecules organiques marquees par le carbone-14 et le soufre-35

    Energy Technology Data Exchange (ETDEWEB)

    Pichat, L. [Commissariat a l' Energie Atomique, Saclay (France). Centre d' Etudes Nucleaires

    1958-07-01

    After a brief history of the development of the Section des Molecules marquees of the Frenchmic Energy Commission, the author gives an outline of the synthesis of the following labelled compounds: benzene {sup 14}C-6; phenyl-p-fluorophenyl, thienyl-2 {beta} alanines {beta} {sup 14}C; noradrenaline {beta} {sup 14}C (arterenol {beta} {sup 14}C), dotriacontane {sup 14}C-16-17, aminoethane sulfinic acid (hypotaurine {sup 35}S). (author)Fren. [French] Apres un bref historique du developpement de la Section des Molecules marquees du Commissariat a l'Energie Atomique fran is, l'auteur donne un resume des syntheses des composes marques suivants: benzene {sup 14}C-6; phenyl-p-fluorophenyl, thienyl-2 {beta} alamines {beta} {sup 14}C; noradrenaline {beta} {sup 14}C (arterenol {beta} {sup 14}C), dotriacontane {sup 14}C-16-17, acide aminoethane sulfinique (hypotaurine {sup 35}S). (auteur)

  18. Synthesis and characterization of C@CdS dots in aqueous solution and their application in labeling human gastric carcinoma cells

    Science.gov (United States)

    Dong, Wei; Zhou, Siqi; Dong, Yan; Wang, Jingwen; Liu, Shuang; Zhu, Pengxia

    2015-03-01

    Colloidal carbon spheres coated with cadmium sulfide nanoparticle quantum dots (C@CdS dots) with the particle size smaller than 50 nm were synthesized by an aqueous approach. The effects of different reaction times, temperatures, and pH values were carefully investigated to optimize the synthesis conditions. The as-prepared C@CdS dots were linked with mouse anti-human carcinoembryonic antigen antibody and goat anti-mouse immunoglobulin (IgG) to directly and indirectly label fixed human gastric carcinoma cells, respectively. The cytotoxicity of the C@CdS dots was also tested using the human gastric carcinoma cells. No apparent cytotoxicity was observed, which suggested the potential application of the as-prepared C@CdS dots in bioimaging.

  19. Synthesis of novel {sup 68}Ga-labeled amino acid derivatives for positron emission tomography of cancer cells

    Energy Technology Data Exchange (ETDEWEB)

    Shetty, Dinesh [Department of Nuclear Medicine, Institute of Radiation Medicine, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Cancer Research Institute, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Department of Radiation Applied Life Science, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Jeong, Jae Min, E-mail: jmjng@snu.ac.k [Department of Nuclear Medicine, Institute of Radiation Medicine, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Cancer Research Institute, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Department of Radiation Applied Life Science, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Ju, Chang Hwan [Cancer Research Institute, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University, Seoul (Korea, Republic of); Lee, Yun-Sang [Department of Nuclear Medicine, Institute of Radiation Medicine, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Department of Radiation Applied Life Science, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Jeong, Seo Young [Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University, Seoul (Korea, Republic of); Choi, Jae Yeon; Yang, Bo Yeun [Department of Nuclear Medicine, Institute of Radiation Medicine, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Cancer Research Institute, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of); Department of Radiation Applied Life Science, Seoul National University College of Medicine, Seoul 110-744 (Korea, Republic of)

    2010-11-15

    Objectives: We developed amino acid derivatives of 1,4,7,10-tetraazacyclododecane-1,7-diacetic acid (DO2A) and 1,4,7,10-tetraazacyclododecane-1,4,7,-triacetic acid (DO3A) that can be labeled with {sup 68}Ga, and we investigated their basic biological properties. Materials and methods: Alanine derivatives of DO2A and DO3A were synthesized by regiospecific nucleophilic attack of DO2tBu and DO3tBu on the {beta}-position of Boc-L-serine-{beta}-lactone, followed by acid hydrolysis. Also, homoalanine derivatives were synthesized by reacting with the protected bromo derivative of homoalanine, which was synthesized from N-Cbz-L-homoserine lactone. Further catalytic reduction and acid cleavage of protected groups resulted in the required products. All derivatives were labeled with {sup 68}Ga. Cell uptake assays were carried out in Hep3B (human hepatoma) and U87MG (human glioma) cell lines at 37{sup o}C. Positron emission tomography (PET) imaging studies were performed using balb/c mice xenografted with CT-26 (mouse colon cancer). Results: All compounds were labeled with >97% efficiency. According to in vitro studies, the labeled amino acid derivatives showed significantly greater uptakes than the control ({sup 68}Ga 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) in cancer cells. Small animal PET images for labeled compounds showed high tumor uptake, as well as kidney and bladder uptakes, at 30 min postinjection. {sup 68}Ga-DO3A-homoalanine showed the highest standardized uptake value ratio (3.9{+-}0.3), followed by {sup 68}Ga-DO2A-alanine (3.1{+-}0.2), {sup 68}Ga-DO3A-alanine (2.8{+-}0.2) and {sup 68}Ga-DO2A-homoalanine (2.3{+-}0.2). Conclusion: These derivatives were found to have high labeling efficiencies, high stabilities, high tumor cell uptakes, high tumor/nontumor xenograft uptakes and low nonspecific uptake in normal organs, except for the kidneys. However, the uptake mechanism of these derivatives remains unclear, and uptake via specific amino acid

  20. Facile synthesis of carbon-11-labeled arylpiperazinylthioalkyl derivatives as new PET radioligands for imaging of 5-HT{sub 1A}R

    Energy Technology Data Exchange (ETDEWEB)

    Gao Mingzhang; Wang Min [Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-208, Indianapolis, IN 46202-2111 (United States); Zheng Qihuang, E-mail: qzheng@iupui.edu [Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, L3-208, Indianapolis, IN 46202-2111 (United States)

    2012-03-15

    Carbon-11-labeled arylpiperazinylthioalkyl derivatives, 2-((4-(4-(2-[{sup 11}C]methoxyphenyl)piperazin-1-yl)butyl)thio)benzo[d]oxazole ([{sup 11}C]5a), 2-((4-(4-(2-[{sup 11}C]methoxyphenyl)piperazin-1-yl)butyl)thio)-5,7-dimethylbenzo [d]oxazole ([{sup 11}C]5c), 2-((4-(4-(2-[{sup 11}C]methoxyphenyl)piperazin-1-yl)butyl)thio)benzo[d]thiazole ([{sup 11}C]5e), 2-((6-(4-(2-[{sup 11}C]methoxyphenyl)piperazin-1-yl)hexyl)thio)benzo[d]oxazole ([{sup 11}C]5g), 2-((6-(4-(2-[{sup 11}C]methoxyphenyl)piperazin-1-yl)hexyl)thio)-5,7-dimethylbenzo [d]oxazole ([{sup 11}C]5i), and 2-((6-(4-(2-[{sup 11}C]methoxyphenyl)piperazin-1-yl)hexyl)thio)benzo[d]thiazole ([{sup 11}C]5k), were prepared from their corresponding phenol precursors with [{sup 11}C]CH{sub 3}OTf through O-[{sup 11}C]methylation and isolated by a simplified solid-phase extraction (SPE) method using a Sep-Pak Plus C18 cartridge in 50-60% (n=5) radiochemical yields based on [{sup 11}C]CO{sub 2} and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 23 min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 277.5{+-}92.5 GBq/{mu}mol (n=5). - Highlights: Black-Right-Pointing-Pointer New arylpiperazinylthioalkyl derivatives were synthesized. Black-Right-Pointing-Pointer New carbon-11-labeled arylpiperazinylthioalkyl derivatives were synthesized. Black-Right-Pointing-Pointer Simplified solid-phase extraction (SPE) method was employed in radiosynthesis.

  1. Metabolism of nonessential N-15-labeled amino acids and the measurement of human whole-body protein synthesis rates

    Science.gov (United States)

    Stein, T. P.; Settle, R. G.; Albina, J. A.; Melnick, G.; Dempsey, D. T.

    1991-01-01

    Eight N-15-labeled nonessential amino acids plus (N-15)H4Cl were administered over a 10-h period to four healthy adult males using a primed-constant dosage regimen. The amount of N-15 excreted in the urine and the urinary ammonia, hippuric acid, and plasma alanine N-15 enrichments were measured. There was a high degree of consistency across subjects in the ordering of the nine compounds based on the fraction of N-15 excreted.

  2. Metabolism of nonessential N-15-labeled amino acids and the measurement of human whole-body protein synthesis rates

    Science.gov (United States)

    Stein, T. P.; Settle, R. G.; Albina, J. A.; Melnick, G.; Dempsey, D. T.

    1991-01-01

    Eight N-15-labeled nonessential amino acids plus (N-15)H4Cl were administered over a 10-h period to four healthy adult males using a primed-constant dosage regimen. The amount of N-15 excreted in the urine and the urinary ammonia, hippuric acid, and plasma alanine N-15 enrichments were measured. There was a high degree of consistency across subjects in the ordering of the nine compounds based on the fraction of N-15 excreted.

  3. Methanol synthesis via CO₂ hydrogenation over a Au/ZnO catalyst: an isotope labelling study on the role of CO in the reaction process.

    Science.gov (United States)

    Hartadi, Yeusy; Widmann, Daniel; Behm, R Jürgen

    2016-04-28

    Methanol synthesis for chemical energy storage, via hydrogenation of CO2 with H2 produced by renewable energies, is usually accompanied by the undesired formation of CO via the reverse water-gas shift reaction. Aiming at a better mechanistic understanding of methanol formation from CO2/H2 on highly selective supported Au/ZnO catalysts we have investigated the role of CO in the reaction process using isotope labelling experiments. Using (13)C-labelled CO2, we found for reaction at 5 bar and 240 °C that (i) the methanol formation rate is significantly higher in CO2-containing gas mixtures than in a CO2-free mixture and (ii) in mixtures containing both CO2 and CO methanol formation from CO increases with the CO content up to 1% CO, and then remains at 20% of the total methanol formation up to a CO2/CO ratio of 1/1, making CO2 the preferred carbon source in these mixtures. A shift in the preferred carbon source for MeOH from CO2 towards CO is observed with increasing reaction temperatures between 240 °C and 300 °C. At even higher temperatures CO is expected to become the dominant carbon source. The consequences of these findings for the application of Au/ZnO catalysts for chemical storage of renewable energies are discussed.

  4. One-pot synthesis of quantum dot-labeled hydrophilic molecularly imprinted polymer nanoparticles for direct optosensing of folic acid in real, undiluted biological samples.

    Science.gov (United States)

    Yang, Yaqiong; Wang, Zhengzheng; Niu, Hui; Zhang, Huiqi

    2016-12-15

    A facile and efficient one-pot approach for the synthesis of quantum dot (QD)-labeled hydrophilic molecularly imprinted polymer (MIP) nanoparticles for direct optosensing of folic acid (FA) in the undiluted bovine and porcine serums is described. Hydrophilic macromolecular chain transfer agent-mediated reversible addition-fragmentation chain transfer (RAFT) precipitation polymerization was used to implement the molecular imprinting of FA in the presence of CdTe quantum dots (QDs). The resulting FA-imprinted polymer nanoparticles with surface-grafted hydrophilic poly(glyceryl monomethacrylate) brushes and QDs labeling not only showed outstanding specific molecular recognition toward FA in biological samples, but also exhibited good photostability, rapid binding kinetics, and obvious template binding-induced fluorescence quenching. These characteristics make them a useful fluorescent chemosensor for directly and selectively optosensing FA in the undiluted bovine and porcine serums, with its limit of detection being 0.025μM and average recoveries ranging from 98% to 102%, even in the presence of several interfering compounds. This advanced fluorescent MIP chemosensor is highly promising for rapid quantification of FA in such applications as clinical diagnostics and food analysis.

  5. Synthesis, Radiolabelling and In Vitro Characterization of the Gallium-68-, Yttrium-90- and Lutetium-177-Labelled PSMA Ligand, CHX-A''-DTPA-DUPA-Pep

    Directory of Open Access Journals (Sweden)

    Benjamin Baur

    2014-04-01

    Full Text Available Since prostate-specific membrane antigen (PSMA has been identified as a diagnostic target for prostate cancer, many urea-based small PSMA-targeting molecules were developed. First, the clinical application of these Ga-68 labelled compounds in positron emission tomography (PET showed their diagnostic potential. Besides, the therapy of prostate cancer is a demanding field, and the use of radiometals with PSMA bearing ligands is a valid approach. In this work, we describe the synthesis of a new PSMA ligand, CHX-A''-DTPA-DUPA-Pep, the subsequent labelling with Ga-68, Lu-177 and Y-90 and the first in vitro characterization. In cell investigations with PSMA-positive LNCaP C4-2 cells, KD values of ≤14.67 ± 1.95 nM were determined, indicating high biological activities towards PSMA. Radiosyntheses with Ga-68, Lu-177 and Y-90 were developed under mild reaction conditions (room temperature, moderate pH of 5.5 and 7.4, respectively and resulted in nearly quantitative radiochemical yields within 5 min.

  6. Synthesis of [{sup 18}F]-labelled nebivolol as a β{sub 1}-adrenergic receptor antagonist for PET imaging agent

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Taek Soo; Park, Jeong Hoon; Lee, Jun Young; Yang, Seung Dae [Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute (KAERI), Jeongeup (Korea, Republic of); Chang, Dong Jo [College of pharmacy, Sunchon National University, Suncheon (Korea, Republic of)

    2017-02-15

    Selective β{sub 1}-agonist and antagonists are used for the treatment of cardiac diseases including congestive heart failure, angina pectoris and arrhythmia. Selective β{sub 1}-antagonists including nebivolol have high binding affinity on β{sub 1}-adrenergic receptor, not β{sub 2}-receptor mainly expressed in smooth muscle. Nebivolol is one of most selective β{sub 1}-blockers in clinically used β{sub 1}- blockers including atenolol and bisoprolol. We tried to develop clinically useful cardiac PET tracers using a selective β{sub 1}-blocker. Nebivolol is C{sub 2}-symmetric and has two chromane moiety with a secondary amino alcohol and aromatic fluorine. We adopted the general synthetic strategy using epoxide ring opening reaction. Unlike formal synthesis of nebivolol, we prepared two chromane building blocks with fluorine and iodine which was transformed to diaryliodonium salt for labelling of {sup 18}F. Two epoxide building blocks were readily prepared from commercially available chromene carboxylic acids (1, 8). Then, the amino alcohol building block (15) was prepared by ammonolysis of epoxide (14) followed by coupling reaction with the other building block, epoxide (7). Diaryliodonium salt, a precursor for {sup 18}F-aromatic substitution, was synthesized in moderate yield which was readily subjected to {sup 18}F-aromatic substitution to give {sup 18}F-labelled nebivolol.

  7. Chemo-Enzymatic Synthesis of (13)C Labeled Complex N-Glycans As Internal Standards for the Absolute Glycan Quantification by Mass Spectrometry.

    Science.gov (United States)

    Echeverria, Begoña; Etxebarria, Juan; Ruiz, Nerea; Hernandez, Álvaro; Calvo, Javier; Haberger, Markus; Reusch, Dietmar; Reichardt, Niels-Christian

    2015-11-17

    Methods for the absolute quantification of glycans are needed in glycoproteomics, during development and production of biopharmaceuticals and for the clinical analysis of glycan disease markers. Here we present a strategy for the chemo-enzymatic synthesis of (13)C labeled N-glycan libraries and provide an example for their use as internal standards in the profiling and absolute quantification of mAb glycans by matrix-assisted laser desorption ionization-time-of-flight (MALDI-TOF) mass spectrometry. A synthetic biantennary glycan precursor was (13)C-labeled on all four amino sugar residues and enzymatically derivatized to produce a library of 15 glycan isotopologues with a mass increment of 8 Da over the natural products. Asymmetrically elongated glycans were accessible by performing enzymatic reactions on partially protected UV-absorbing intermediates, subsequent fractionation by preparative HPLC, and final hydrogenation. Using a preformulated mixture of eight internal standards, we quantified the glycans in a monoclonal therapeutic antibody with excellent precision and speed.

  8. 产志贺毒素样大肠杆菌F18ab菌毛操纵子基因的体外非诱导系统的表达和鉴定%Cloning and expression of F18 fimbrial operon gene cluster from Shiga-like toxigenic E.coli(SLTEC) using non-induced expression system

    Institute of Scientific and Technical Information of China (English)

    吴娟; 朱春红; 郁磊; 羊扬; 朱军; 舒燕; 包文斌; 吴圣龙; Dieter M Schifferli; 朱国强

    2012-01-01

    The fed operon gene cluster encoding the F18ab-serotype fimbriae was amplified by Expand Long Template PCR using the genomic DNA template from Shiga-like toxigenic E.coli reference strain 107/86.The predicted PCR products with the restriction enzyme sites at each end were digested and then cloned into the expression vector pBR322,the recombinant plasmid pBR322-fed with the inserts of the whole fed gene clusters were constructed and screened,further confirmed by the means of combination with both restriction endonuclease analysis and sequencing.The fimbriae F18ab were isolated and purified from the recombinant E.coli SE5000(pBR322-fed),and only a single major band of protein with size of approximately 15 000 was visualized in Coomassie blue-stained gels after SDS-PAGE,and this protein band was recognized positively by the polyclonal sera against fimbriae F18ab in Western-blotting assay.The results in agglutination assay showed that the polyclonal sera,purified IgG,and monoclonal antibody(Mab) directed against the major subunit of F18ab fimbriae(FedF),F18ab fimbriae from the reference strain E.coli 107/86 reacted to the recombinant E.coli SE5000 expressing the fimbriae F18ab,respectively.Small intestine epithelial cells from the susceptible piglets with the genotypes of FUT1 gene M307GG were prepared and tested for the adherence to the recombinant E.coli SE5000(pBR322-fed) under the microscopic examination.Adhesion and adhesion inhibition test showed the recombinant E.coli SE5000(pBR322-fed) could adhere to the jejunal epithelial cells in vitro as the reference strain E.coli 107/86 did.The polyclonal anti-sera directed against fimbriae F18ab can efficiently inhibit the fimbriae-mediated susceptible piglet jejunal epithelial cells adherence to the recombinant E.coli SE5000(pBR322-fed) and reference strain E.coli 107/86.%以产志贺毒素样大肠杆菌(SLTEC)F18ab血清型标准菌株107/86基因组DNA为模板,利用PCR技术成功扩增出编码F18ab完整菌

  9. Food Labels

    Science.gov (United States)

    ... Surgery? Choosing the Right Sport for You Shyness Food Labels KidsHealth > For Teens > Food Labels Print A ... have at least 95% organic ingredients. continue Making Food Labels Work for You The first step in ...

  10. Synthesis of highly fluorescent and thio-linkers stabilize gold quantum dots and nano clusters in DMF for bio-labeling

    Energy Technology Data Exchange (ETDEWEB)

    Rastogi, Shiva K., E-mail: srastogi@uidaho.edu [University of Idaho, Department of Chemistry (United States); Denn, Benjamin D.; Branen, A. Larry [University of Idaho, Coeur D' Alene, Biosensors and Nanotechnology Application Laboratory (BNAL) (United States)

    2012-01-15

    This study demonstrates a one versus two-step synthesis of fluorescent gold quantum dots (F-AuQDs) and nano clusters (F-AuNCs) functionalized with thiolated organic linkers using reduction of gold precursor in N,N Prime -dimethylformamide in 1 h of reaction. The F-AuQDs and F-AuNCs show fluorescence emission at 425 {+-} 5 nm upon excitation at 345 {+-} 5 nm of wavelength, with good water solubility and stability. Five different thiolated organic binary linkers consisting of various functional groups including: carboxylic acid, hydroxyl, and aromatic amine, were conjugated with the F-AuQDs and F-AuNCs. The formation mechanism and functionalization of the F-AuQDs and F-AuNCs was characterized using UV-vis absorption spectra, UV-vis light, fluorescent emission spectra, pH, TEM, and FTIR. The fluorescence emission of the F-AuQDs and F-AuNCs is greatly dependent on the thio-linker. This novel one-step approach provides facile and fast synthesis of F-AuQDs and F-AuNCs over the two-step method, with less than 5 h of reaction and workup compared to more than 28 h of reaction for the two-step approach. These thio-linker functionalized F-AuQDs and F-AuNCs have a wide application in fluorescent labeling of biomolecules, optical devices, imaging, energy transfer, and biosensing.

  11. Synthesis of a potent and selective (18)F-labeled delta-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging.

    Science.gov (United States)

    Ryu, Eun Kyoung; Wu, Zhanhong; Chen, Kai; Lazarus, Lawrence H; Marczak, Ewa D; Sasaki, Yusuke; Ambo, Akihiro; Salvadori, Severo; Ren, Chuancheng; Zhao, Heng; Balboni, Gianfranco; Chen, Xiaoyuan

    2008-03-27

    Identification and pharmacological characterization of two new selective delta-opioid receptor antagonists, derived from the Dmt-Tic pharmacophore, of potential utility in positron emission tomography (PET) imaging are described. On the basis of its high delta selectivity, H-Dmt-Tic--Lys(Z)-OH (reference compound 1) is a useful starting point for the synthesis of (18)F-labeled compounds prepared by the coupling of N-succinimidyl 4-[ (18)F]fluorobenzoate ([(18)F]SFB) with Boc-Dmt-Tic--Lys(Z)-OH under slightly basic conditions at 37 degrees C for 15 min, deprotection with TFA, and HPLC purification. The total synthesis time was 120 min, and the decay-corrected radiochemical yield of [(18)F]- 1 was about 25-30% ( n = 5) starting from [(18)F]SFB ( n = 5) with an effective specific activity about 46 GBq/micromol. In vitro autoradiography studies showed prominent uptake of [ (18)F]- 1 in the striatum and cortex with significant blocking by 1 and UFP-501 (selective delta-opioid receptor antagonist), suggesting high specific binding of [(18)F]- 1 to delta-opioid receptors. Noninvasive microPET imaging studies revealed the absence of [(18)F]- 1 in rat brain, since it fails to cross the blood-brain barrier. This study demonstrates the suitability of [ (18)F]- 1 for imaging peripheral delta-opioid receptors.

  12. Synthesis of deuterium-labelled methylphenidate, p-hydroxy-methylphenidate, ritalinic acid and p-hydroxyritalinic acid

    Energy Technology Data Exchange (ETDEWEB)

    Patrick, K.; Kilts, C.; Breese, G. (North Carolina Univ., Chapel Hill (USA). School of Medicine)

    1982-04-01

    The synthesis of threo-dl-methylphenidate (Ritalin 1), threo-dl-p-hydroxy-methylphenidate (3), threo-dl-ritalinic acid (2), and threo-dl-p-hydroxyritalinic acid (4) with deuterium incorporated in the piperidine ring is described. These compounds were synthesized for use as internal standards for mass fragmentographic assays of methylphenidate and its metabolites. The synthetic scheme described resulted in less than 0.05% /sup 2/H/sub 0/ in the piperidine ring in any of the preparations.

  13. Malignant extrarenal rhabdoid tumor of the spine: staging and evaluation of response to therapy with F-18 FDG PET/CT.

    Science.gov (United States)

    Makis, William; Ciarallo, Anthony; Hickeson, Marc

    2011-07-01

    Malignant extrarenal rhabdoid tumor (ERRT) is a very rare type of soft-tissue sarcoma with a reported incidence of 0.3% of all soft-tissue sarcomas. Only 7 cases of spinal malignant ERRT have been reported in the literature, and to our knowledge, F-18 FDG PET/CT imaging for staging and evaluation of response to therapy for these tumors has not been previously described. This is a case of an 8-month-old boy with malignant ERRT of the spine, who was staged with F-18 FDG PET/CT, and had his tumor burden assessed with PET/CT after chemotherapy, which altered the subsequent chemotherapy regimen.

  14. Synthesis of Fluorine-18 Labeled Glucose-Lys-Arg-Gly-Asp-D-Phe as a Potential Tumor Imaging Agent

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Kyo Chul; Kim, Ji Sun; Sung, Hyun Ju; Jung, Jae Ho; An, Gwang Il; Chi, Dae Yoon [Korea Institute of Radiological and Medical Sciences, Seoul (Korea, Republic of); Lee, Byung Chul; Moon, Byung Seok; Choi, Tae Hyun; Chuna, Kwon Soo [Inha Univ., Inchon (Korea, Republic of)

    2005-07-01

    The {alpha}{sub v}{beta}{sub 3} integrin is an important receptor affecting tumor growth, metastatic potential on proliferating endothelial cells as well as on tumor cells of various origin, tumor-induced angiogenesis could be blocked by antagonizing the {alpha}{sub v}{beta}{sub 3} integrin with RGD. Therefore, {alpha}{sub v}{beta}{sub 3} integrin is a target for angiogenesis imaging that might be useful in assessing tumor-induced angiogenesis and identifying tumor metastasis. To design potent radiotracer for imaging angiogenesis containing a cRGD moiety should include low hepatic uptake in vivo. Tripeptide Arg-Gly-Asp (RGD), naturally existed in extracellular matrix proteins, is known to be the primary binding site of the {alpha}{sub v}{beta}{sub 3} integrin. The imaging of {alpha}{sub v}{beta}{sub 3} receptor expression will give the information of the metastatic ability of the tumor which is not available by [{sup 18}F]FDG. Our interest in developing new radiopharmaceuticals for in vivo visualization of angiogenesis has led us to synthesize derivatives of cRGD (cyclic arginineglycine-aspartic acid) that contains glucose moiety. Because sugar-protein interaction is a key step in metastasis and angiogenesis, it has also been proposed to play an intriguing role in imaging of tumor. We designed and synthesized two fluorine-18 labeled RGD glycopeptides . N-fluorobenzyl-diaminobutane-N'-glucose-Lys-Arg-Gly-Asp-D-Phe ([{sup 18}F]fluorobenzyl-glucose-KRGDf, and Nfluorobenzoyl- diaminobutane-N'-glucose-Lys-Arg-Gly-Asp-D-Phe ([{sup 18}F]fluorobenzoyl-glucose-KRGDf, from same precursor as a diagnostic tumor imaging agent for positron emission tomography (PET). Fluorine-18 labeled cRGD glycopeptides were prepared using two different simple labeling methods: one is reductive alkylation of an amine with [{sup 18}F]fluorobenzaldehyde and the other is amide condensation with [{sup 18}F]fluorobenzoic acid.

  15. Continuous-Flow Synthesis of Deuterium-Labeled Antidiabetic Chalcones: Studies towards the Selective Deuteration of the Alkynone Core

    Directory of Open Access Journals (Sweden)

    Sándor B. Ötvös

    2016-03-01

    Full Text Available Flow chemistry-based syntheses of deuterium-labeled analogs of important antidiabetic chalcones were achieved via highly controlled partial C≡C bond deuteration of the corresponding 1,3-diphenylalkynones. The benefits of a scalable continuous process in combination with on-demand electrolytic D2 gas generation were exploited to suppress undesired over-reactions and to maximize reaction rates simultaneously. The novel deuterium-containing chalcone derivatives may have interesting biological effects and improved metabolic properties as compared with the parent compounds.

  16. Pancreatic tuberculosis: Evaluation of therapeutic response using F-18 fluoro-2-deoxy-D-glucose positron emission tomography/computed tomography.

    Science.gov (United States)

    Santhosh, Sampath; Bhattacharya, Anish; Rana, Surinder Singh; Bhasin, Deepak Kumar; Srinivasan, Radhika; Mittal, Bhagwant Rai

    2014-10-01

    F-18 fluoro-2-deoxy-D-glucose positron emission tomography/computed tomography (FDG PET/CT) is a functional imaging technique that monitors glucose metabolism in tissues. Pulmonary tuberculosis (TB) has been reported to show intense uptake of FDG, with a decrease in metabolism of the tuberculous lesions after successful anti-tubercular treatment (ATT). The authors present a patient with pancreatic TB and demonstrate the usefulness of FDG PET/CT in monitoring the response to ATT.

  17. Insufficiency of Bone Scintigraphy in Vertebral Lesions of Langerhans Cell Histiocytosis Compared to F-18 Fluorodeoxyglucose Positron Emission Tomography/Computed Tomography and Diagnostic Computed Tomography

    Science.gov (United States)

    Koç, Zehra Pınar; Şimşek, Selçuk; Akarsu, Saadet; Balcı, Tansel Ansal; Onur, Mehmet Ruhi; Kepenek, Ferat

    2015-01-01

    Langerhans cell histiocytosis (LCH) is a benign disorder related to the histiocytes which can infiltrate bone tissue. The most effective method for demonstrating severity of this disease is PET/CT and bone scintigraphy might show bone lesions. We present a seventeen year old male patient with disseminated LCH presented with exophtalmos and having multiple vertebral lesions which were identified by F-18 FDG PET/CT scan and diagnostic CT but not in the bone scintigraphy. PMID:25800594

  18. Insufficiency of Bone Scintigraphy in Vertebral Lesions of Langerhans Cell Histiocytosis Compared to F-18 Fluorodeoxyglucose Positron Emission Tomography/Computed Tomography and Diagnostic Computed Tomography

    Directory of Open Access Journals (Sweden)

    Zehra Pınar Koç

    2015-02-01

    Full Text Available Langerhans cell histiocytosis (LCH is a benign disorder related to the histiocytes which can infiltrate bone tissue. The most effective method for demonstrating severity of this disease is PET/CT and bone scintigraphy might show bone lesions. We present a seventeen year old male patient with disseminated LCH presented with exophtalmos and having multiple vertebral lesions which were identified by F-18 FDG PET/CT scan and diagnostic CT but not in the bone scintigraphy

  19. Histomorphometric characteristics of immune cells in small intestine of pigs perorally immunized with vaccine candidate F18ac+ nonenterotoxigenic E. coli strain

    Directory of Open Access Journals (Sweden)

    I. Valpotic

    2009-12-01

    Full Text Available Colidiarrhea and colienterotoxemia caused by F4+ and/or F18+ enterotoxigenic E. coli (ETEC strains are the most prevalent infections of suckling and weaned pigs. Here we tested the immunogenicity and protective effectiveness of attenuated F18ac+ non-ETEC vaccine candidate strain against challenge infection with F4ac+ ETEC strain by quantitative phenotypic analysis of small intestinal leukocyte subsets in weaned pigs. We also evaluated levamisole as an immune response modifier (IRM and its adjuvanticity when given in the combination with the experimental vaccine. The pigs were parenterally immunized with either levamisole (at days -2, -1 and 0 or with levamisole and perorally given F18ac+ non-ETEC strain (at day 0, and challenged with F4ac+ ETEC strain 7 days later. At day 13 the pigs were euthanatized and sampled for immunohistological/histomorphometrical analyses. Lymphoid CD3+, CD45RA+, CD45RC+, CD21+, IgA+ and myeloid SWC3+ cell subsets were identified in jejunal and ileal epithelium, lamina propria and Peyer’s patches using the avidin-biotin complex method, and their numbers were determined by computer-assisted histomorphometry. Quantitative immunophenotypic analyses showed that levamisole treated pigs had highly increased numbers of jejunal CD3+, CD45RC+ and SWC3+ cells (p<0.05 as compared to those recorded in nontreated control pigs. In the ileum of these pigs we have recorded that only CD21+ cells were significantly increased (p<0.01. The pigs that were treated with levamisole adjuvanted experimental vaccine had significantly increased numbers of all tested cell subsets in both segments of the small intestine. It was concluded that levamisole adjuvanted F18ac+ non-ETEC vaccine was a requirement for the elicitation of protective gut immunity in this model; nonspecific immunization with levamisole was less effective, but confirmed its potential as an IRM.

  20. The Effect of Patient Age on Standardized Uptake Value-Hounsfield Unit Values of Male Genitourinery Structures In F-18 FDG PET/CT

    Directory of Open Access Journals (Sweden)

    Berrin Çavuşoğlu

    2011-12-01

    Full Text Available Objective: Relation between patient age and Hounsfield Unit (HU,which is the linear attenuation coefficient, and Standardized Uptake Values (SUV which is the amount of 18F-fluorodeoxyglucose (F-18 FDG uptake, measured in the areas of interest drawn to prostate, seminal vesicles and testicles in F-18 FDG Positron Emission Tomography/Computed Tomography (PET/CT images was investigated. Material and Methods: Mean and maximum SUV and HU values were recorded from the areas of interest (min 12 mm in diameter which showed FDG uptake in prostate, seminal vesicles and testicles from F-18 FDG PET-CT images of 21 male patients under 40 years without genitourinary cancer. The effect of patient age to SUV and HU values was examined with Pearson correlation test using SPSS program. Results: There was a negative insignificant correlation between patient age and SUV and HU values for prostate. For seminal vesicles, correlation between patient age and SUV values and HUmax were positive but insignificant, while correlation with HUmean was significant (r=0.459, p=0.00. Correlation between patient age and SUVmax and SUVmean values were significant for testicles (r=0.506, p=0.002 and r=0.467, p=0.005, respectively but the correlation between patient age and HUmax and HUmean values was not significant. Conclusion: F-18 FDG uptake in testicles in males increases with age until 40, suggesting an increase in metabolic rate. The significant correlation between age and mean HU values is probably caused by thickening of the tissue without an increase in glucose metabolism in seminal vesicles. In prostate, the effect of patient age to SUV and HU values was not observed until the age 40. (MIRT 2011;20:104-107

  1. Amyloid deposition detected with florbetapir F 18 (18F-AV-45) is related to lower episodic memory performance in clinically normal older individuals

    Science.gov (United States)

    Sperling, Reisa A.; Johnson, Keith A.; Doraiswamy, P. Murali; Reiman, Eric M.; Fleisher, Adam S.; Sabbagh, Marwan; Sadowsky, Carl; Carpenter, Alan; Davis, Mat; Lu, Ming; Flitter, Matthew; Joshi, Abhinay; Clark, Christopher M.; Grundman, Michael; Mintun, Mark; Skovronsky, Daniel; Pontecorvo, Michael

    2012-01-01

    The objective of this study was to evaluate the relationship of amyloid burden, as assessed by florbetapir F 18 (18F-AV-45) amyloid PET, and cognition in healthy older control subjects (HC). Seventy-eight HC subjects were assessed with a brief cognitive test battery and PET imaging with florbetapir F 18. A standard uptake value ratio (SUVr) was computed for mean data from six cortical regions using a whole cerebellum reference region. Scans were also visually rated as amyloid positive (Aβ+) or amyloid negative (Aβ−) by three readers. Higher SUVr correlated with lower immediate memory (r=−0.33; p=0.003) and delayed recall scores (r=−0.25; p=0.027). Performance on immediate recall was also lower in the visually rated Aβ+ compared to Aβ− HC (p=0.04), with a similar trend observed in delayed recall (p=0.06). These findings support the hypothesis that higher amyloid burden is associated with lower memory performance among clinically normal older subjects. Longitudinal follow-up is ongoing to determine whether florbetapir F 18 may also predict subsequent cognitive decline. PMID:22878163

  2. Synthesis and biosynthesis of {sup 13}C-, {sup 15}N-labeled deoxynucleosides useful for biomolecular structural determinations

    Energy Technology Data Exchange (ETDEWEB)

    Ashburn, D.A.; Garcia, K.; Hanners, J.L.; Silks, L.A. III; Unkefer, C.J. [Los Alamos National Laboratory, NM (United States)

    1994-12-01

    Currently, there is a great emphasis on elucidating the structure, function, and dynamics of DNA. Much of the research involved in this study uses nuclear magnetic resonance (NMR) spectroscopy. Effective use of NMR spectroscopy for DNA molecules with mw > 10,000 requires stable isotope enrichment. We present strategies for site-specific isotopic labeling of the purine bases adenosine and guanosine and the biosynthesis of (U-{sup 13}C, {sup 15}N) DNA from methylotropic bacteria. With commercially available 6-chloropurine, an effective two-step route leads to 2{prime}-deoxy-(amino-{sup 15}N)adenosine (dA). The resulting d(amino-{sup 15}N)A is used in a series of reactions to synthesize 2{prime}-deoxy-(2-{sup 13}C,1,amino-{sup 15}N{sub 2})guanosine or any combination thereof. An improved biosynthesis of labeled DNA has been accomplished using Methylobacterium extorquens AS1. Each liter of growth medium contains 4 g of methanol to yield 1 g of lyophilized cells. As much as 200 mg of RNA per liter of culture has been obtained. We are currently developing large-scale isolation protocols. General synthetic pathways to oligomeric DNA will be presented.

  3. Synthesis and biological evaluation of (68) Ga-labeled Pteroyl-Lys conjugates for folate receptor-targeted tumor imaging.

    Science.gov (United States)

    Zhang, Xuran; Yu, Qian; He, Yingfang; Zhang, Chun; Zhu, Hua; Yang, Zhi; Lu, Jie

    2016-07-01

    In order to develop novel (68) Ga-labeled PET tracers for folate receptor imaging, two DOTA-conjugated Pteroyl-Lys derivatives, Pteroyl-Lys-DOTA and Pteroyl-Lys-DAV-DOTA, were designed, synthesized and radiolabeled with (68) Ga. Biological evaluations of the two radiotracers were performed with FR-positive KB cell line and athymic nude mice bearing KB tumors. Both (68) Ga-DOTA-Lys-Pteroyl and (68) Ga-DOTA-DAV-Lys-Pteroyl exhibited receptor specific binding in KB cells in vitro. The tumor uptake values of (68) Ga-DOTA-Lys-Pteroyl and (68) Ga-DOTA-DAV-Lys-Pteroy were 10.06 ± 0.59%ID/g and 11.05 ± 0.60%ID/g at 2 h post-injection, respectively. Flank KB tumor was clearly visualized with (68) Ga-DOTA-DAV-Lys-Pteroyl by Micro-PET imaging at 2 h post-injection, suggesting the feasibility of using (68) Ga-labeled Pteroyl-Lys conjugates as a novel class of FR targeted probes.

  4. Design, synthesis and evaluation of (18)F-labeled cationic carbonic anhydrase IX inhibitors for PET imaging.

    Science.gov (United States)

    Zhang, Zhengxing; Lau, Joseph; Zhang, Chengcheng; Colpo, Nadine; Nocentini, Alessio; Supuran, Claudiu T; Bénard, François; Lin, Kuo-Shyan

    2017-12-01

    Carbonic anhydrase IX (CA-IX) is a marker for tumor hypoxia, and its expression is negatively correlated with patient survival. CA-IX represents a potential target for eliminating hypoxic cancers. We synthesized fluorinated cationic sulfonamide inhibitors 1-3 designed to target CA-IX. The binding affinity for CA-IX ranged from 0.22 to 0.96 μM. We evaluated compound 2 as a diagnostic PET imaging agent. Compound 2 was radiolabeled with (18)F in 10 ± 4% decay-corrected radiochemical yield with 85.1 ± 70.3 GBq/μmol specific activity and >98% radiochemical purity. (18)F-labeled 2 was stable in mouse plasma at 37 °C after 1 h incubation. PET/CT imaging was conducted at 1 h post-injection in a human colorectal cancer xenograft model. (18)F-labeled 2 cleared through hepatobiliary and renal pathways. Tumor uptake was approximately 0.41 ± 0.06% ID/g, with a tumor-to-muscle ratio of 1.99 ± 0.25. Subsequently, tumor xenografts were visualized with moderate contrast. This study demonstrates the use of a cationic motif for conferring isoform selectively for CA-IX imaging agents.

  5. An improved method for the synthesis of mercurated dUTP. Enzymic synthesis of Hg-labelled DNA of high molecular weight suitable for use in an image based DNA sequencing strategy.

    Science.gov (United States)

    Bridgman, A J; Petersen, G B

    1996-01-01

    The development of high-resolution scanning-probe microscopes has reawakened interest in the possibility of sequencing large nucleic acid molecules by direct imaging. Such an approach would be facilitated by the availability of effective methods for increasing contrast by labelling specific nucleotides, and the utility of introducing mercury atoms into complete DNA molecules through the enzymic polymerisation of mercurated pyrimidine deoxynucleoside triphosphates has been re-investigated. A simplified and improved method for the synthesis of a heat- and thiol-stable, mercurated derivative of deoxyuridine triphosphate in high yield and the incorporation of this precursor into full-length copies of a single-stranded phage M13 template are described. The DNA product has been fully characterised and the quantitative and specific replacement of thymidylic acid residues by the mercurated analogue demonstrated.

  6. One-Pot Synthesis of Biocompatible CdSe/CdS Quantum Dots and Their Applications as Fluorescent Biological Labels

    OpenAIRE

    Huang Hai; Wu Yulian; Zhai Chuanxin; Zhang Hui; Du Ning; Chen Bingdi; Yang Deren

    2011-01-01

    Abstract We developed a novel one-pot polyol approach for the synthesis of biocompatible CdSe quantum dots (QDs) using poly(acrylic acid) (PAA) as a capping ligand at 240°C. The morphological and structural characterization confirmed the formation of biocompatible and monodisperse CdSe QDs with several nanometers in size. The encapsulation of CdS thin layers on the surface of CdSe QDs (CdSe/CdS core–shell QDs) was used for passivating the defect emission (650 nm) and enhancing the ...

  7. Atmospheric histories and growth trends of C4F10, C5F12, C6F14, C7F16 and C8F18

    Directory of Open Access Journals (Sweden)

    R. F. Weiss

    2012-02-01

    Full Text Available The first atmospheric observations and trends are presented for the high molecular weight perfluorocarbons (PFCs: decafluorobutane (C4F10, dodecafluoropentane (C5F12, tetradecafluorohexane (C6F14, hexadecafluoroheptane (C7F16 and octadecafluorooctane (C8F18. Their atmospheric histories are based on measurements of 38 Northern Hemisphere and 46 Southern Hemisphere archived air samples collected between 1973 to 2011 using the Advanced Global Atmospheric Gases Experiment (AGAGE "Medusa" preconcentration gas chromatography-mass spectrometry systems. A new calibration scale was prepared for each PFC, with estimated accuracies of 6.8% for C4F10, 7.8% for C5F12, 4.0% for C6F14, 6.6% for C7F16 and 7.9% for C8F18. Based on our observations the 2011 globally averaged dry air mole fractions of these heavy PFCs are: 0.18 parts-per-trillion (ppt, i.e., parts per 1012 for C4F10, 0.12 ppt for C5F12, 0.28 ppt for C6F14, 0.12 ppt for C7F16 and 0.09 ppt for C8F18. These atmospheric mole fractions combine to contribute to a global average radiative forcing of 0.35 mW m−2, which is 3.6% of the total PFC radiative forcing. The globally averaged mean atmospheric growth rates of these PFCs during 1973–2011 are 4.58 parts per quadrillion (ppq, i.e., parts per 1015 per year (yr for C4F10, 3.29 ppq yr−1 for C5F12, 7.50 ppq yr−1 for C6F14, 3.19 ppq yr−1 for C7F16 and 2.51 ppq yr−1 for C8F18. The growth rates of the heavy perfluorocarbons were largest in the early 1990s for C4F10 and C5F12 and in the mid-to-late 1990s for C6F14, C7F16 and C8F18. The more recent slow down in the growth rates of the high molecular weight PFCs suggests that emissions are declining as compared to the 1980s and 1990s. Nevertheless continued monitoring of these potent, extremely long-lived greenhouse gases is necessary to verify that global PFC emissions continue to decline.

  8. Clinical Usefulness of F-18 FDG PET/CT in papillary thyroid cancer with negative radioiodine scan and elevated thyroglobulin level or positive anti-thyroglobulin antibody

    Energy Technology Data Exchange (ETDEWEB)

    Choi, Su Jung; Jung, Kyung Pyo; Lee, Sun Seong; Park, Yun Soo; Lee, Seok Mo [Dept. of Nuclear Medicine, Busan Paik Hospital, Inje University College of Medicine, Busan (Korea, Republic of); Bae, Sang Kyun [Dept. of Nuclear Medicine, Haeundae Paik Hospital, Inje University College of Medicine, Busan (Korea, Republic of)

    2016-06-15

    Elevated thyroglobulin (Tg) levels, along with a negative radioiodine scan, present a clinical problem for the diagnosis of recurrence in papillary thyroid cancer (PTC) patients. The purpose of this study was to assess (1) the usefulness of 18F-fluorodeoxyglucose (F-18 FDG) positron emission tomography (PET)/computed tomography (CT) for PTC patients with negative diagnostic radioiodine scan and elevated serum Tg level or positive anti-thyroglobulin antibody (TgAb), and (2) the effect of endogenous thyroid stimulating hormone (TSH) stimulation (ETS) on detecting recurrence in these circumstances. Eighty-four patients with negative diagnostic radioiodine scan and elevated serum Tg or positive TgAb under ETS were included. Correlation with clinicopathological features and recurrence, detectability of FDG PET/CT and cut-off value of serum Tg for recurrence in PTC patients with these circumstance were assessed. In addition, detectability of F-18 FDG PET/CT under ETS and suppression were compared. In Cox regression analysis, only serum Tg level was significantly associated with recurrence (P<0.001, HR  = 1.13; 95 % CI, 1.061–1.208). The cut-off level of Tg was 21.5 ng/mL (AUC, 0.919; P < 0.001) for discriminating the recurrence in the patients with positive PET/CT finding. The sensitivity, specificity, PPV, NPV, and accuracy of F-18 FDG PET/CT for detecting recurrence were 64 %, 94 %, 86 %, 81 %, and 83 %. In the analysis of F-18 FDG PET/CT under ETS, the sensitivity, specificity, PPV, NPV and accuracy was 64 %, 94 %, 88 %, 81 % and 83 %. Those under TSH suppression were 67 %, 92 %, 80 %, 85 % and 83 %. F-18 FDG PET/CT, although less sensitive, showed high specificity, PPV, NPV, and accuracy and therefore can be useful for the patients with negative diagnostic radioiodine scan and elevated serum Tg or positive TgAb. In addition, FDG PET/CT under ETS does not seem to have an additive role in detecting recurrence in these patients.

  9. Atmospheric histories and growth trends of C4F10, C5F12, C6F14, C7F16 and C8F18

    Directory of Open Access Journals (Sweden)

    R. F. Weiss

    2012-05-01

    Full Text Available Atmospheric observations and trends are presented for the high molecular weight perfluorocarbons (PFCs: decafluorobutane (C4F10, dodecafluoropentane (C5F12, tetradecafluorohexane (C6F14, hexadecafluoroheptane (C7F16 and octadecafluorooctane (C8F18. Their atmospheric histories are based on measurements of 36 Northern Hemisphere and 46 Southern Hemisphere archived air samples collected between 1973 to 2011 using the Advanced Global Atmospheric Gases Experiment (AGAGE "Medusa" preconcentration gas chromatography-mass spectrometry systems. A new calibration scale was prepared for each PFC, with estimated accuracies of 6.8% for C4F10, 7.8% for C5F12, 4.0% for C6F14, 6.6% for C7F16 and 7.9% for C8F18. Based on our observations the 2011 globally averaged dry air mole fractions of these heavy PFCs are: 0.17 parts-per-trillion (ppt, i.e., parts per 1012 for C4F10, 0.12 ppt for C5F12, 0.27 ppt for C6F14, 0.12 ppt for C7F16 and 0.09 ppt for C8F18. These atmospheric mole fractions combine to contribute to a global average radiative forcing of 0.35 mW m−2, which is 6% of the total anthropogenic PFC radiative forcing (Montzka and Reimann, 2011; Oram et al., 2012. The growth rates of the heavy perfluorocarbons were largest in the late 1990s peaking at 6.2 parts per quadrillion (ppq, i.e., parts per 1015 per year (yr for C4F10, at 5.0 ppq yr−1 for C5F12 and 16.6 ppq yr−1 for C6F14 and in the early 1990s for C7F16 at 4.7 ppq yr−1 and in the mid 1990s for C8F18 at 4.8 ppq yr−1. The 2011 globally averaged mean atmospheric growth rates of these PFCs are subsequently lower at 2.2 ppq yr−1 for C4F10, 1.4 ppq yr−1 for C5F12, 5.0 ppq yr−1 for C6F14, 3.4 ppq yr−1 for C7F16 and 0.9 ppq yr−1 for C8F18. The more recent slowdown in the growth rates suggests that emissions are declining as compared to the 1980s and 1990s.

  10. 6-[F-18]Fluoro-L-Dihydroxyphenylalanine Positron Emission Tomography Is Superior to Conventional Imaging with I-123-Metaiodobenzylguanidine Scintigraphy, Computer Tomography, and Magnetic Resonance Imaging in Localizing Tumors Causing Catecholamine Excess

    NARCIS (Netherlands)

    Fiebrich, Helle-Brit; Brouwers, Adrienne H.; Kerstens, Michiel N.; Pijl, Milan E. J.; Kema, Ido P.; de Jong, Johan R.; Jager, Pieter L.; Elsinga, Philip H.; Dierckx, Rudi A. J. O.; van der Wal, Jacqueline E.; Sluiter, Wim J.; de Vries, Elisabeth G. E.; Links, Thera P.

    2009-01-01

    Context: Catecholamine excess is rare, but symptoms may be life threatening. Objective: The objective of the study was to investigate the sensitivity of 6-[F-18]fluoro-L-dihydroxyphenylalanine positron emission tomography (F-18-DOPAPET), compared with I-123-metaiodobenzylguanidine (I-123-MIBG) scint

  11. Diagnostic Performance of F-18-FDG PET and PET/CT for the Detection of Recurrent Esophageal Cancer After Treatment with Curative Intent : A Systematic Review and Meta-Analysis

    NARCIS (Netherlands)

    Goense, Lucas; van Rossum, Peter S. N.; Reitsma, Johannes B.; Lam, Marnix G. E. H.; Meijer, Gert J.; van Vulpen, Marco; Ruurda, Jelle P.; van Hillegersberg, Richard

    The aim of this study was to assess the diagnostic performance of F-18-FDG PET and integrated F-18-FDG PET/CT for diagnosing recurrent esophageal cancer after initial treatment with curative intent. Methods: The PubMed, Embase, and Cochrane library were systematically searched for all relevant

  12. Simultaneous Synthesis and Biotinylation of Proteins Using Puromycin-Based Labeling Technology for Fabrication of Protein Array Chip

    Science.gov (United States)

    Kumal, Subhashini Raj; Biyani, Manish; Ueno, Shingo; Akagi, Takanori; Ichiki, Takanori

    2013-06-01

    Protein arrays represent a class of devices that are of growing importance in the field of proteomics. These arrays enable screening of a large amount of proteins in a short time and at a lower cost. Here we present a method to fabricate protein array using biotin-conjugated puromycin to simultaneously synthesize and label proteins followed by immobilization onto streptavidin-functionalized surface based on the noncovalent biotin-streptavidin interaction. This method demonstrates the fabrication of protein array based on cell-free transcription/translation system using unmodified DNA as a starting genetic material. As a consequence, the procedure of protein arraying has been greatly simplified over the conventional approaches that require tedious and multi-step reactions. Further, an integrated approach of micro reactor array technology makes this method very simple and robust for achieving high-density protein arrays.

  13. Synthesis of N-succinimidyl 4-[{sup 76}Br]bromobenzoate and its use in conjugation labelling of macromolecules

    Energy Technology Data Exchange (ETDEWEB)

    Yngve, U.; Hedberg, E. [Uppsala Univ., Dept. of Organic Chemistry, Uppsala (Sweden); Loevqvist, A.; Tolmachev, V. [Uppsala Univ., Dept. of Radiation Science, Uppsala (Sweden); Laangstroem, B. [Uppsala Univ. PET Centre, Uppsala (Sweden)

    1999-11-01

    The {sup 76}Br radiobromination of proteins and modified oligonucleotides by the use of N-succinimidyl 4-[{sup 76}Br]bromobenzoate are described. The labelled N-succinimidyl bromobenzoate was synthesised from the corresponding trimethyltin compound, N-succinimidyl 4-trimethylstannylbenzoate, in 45-60% isolated radiochemical yield with a specific radioactivity of 20-200 GBq {mu}mol{sup -1}. The use of N-succinimidyl 4-[{sup 76}Br]bromobenzoate in conjugation with the proteins human serum albumin and chromogranin and with 5`-hexylamino-modified oligodeoxynucleotides (ODN) and its phosphorothioate analogues (S-ODN), is described. The oligonucleotide sequence chosen for this work is an antisense sequence for the m-RNA encoding for chromogranin in rat. (au) 27 refs.

  14. Synthesis of deuterium-labelled substrates for the study of oleuropein biosynthesis in Olea europaea callus cultures.

    Science.gov (United States)

    Serrilli, Anna Maria; Maggi, Agnese; Casagrande, Valentina; Bianco, Armandodoriano

    2016-01-01

    We propose the cell culture approach to investigate oleuropein (1) biogenesis in Olea europaea L. We suggest employing olive callus cultures to identify the iridoidic precursor of oleuropein. In fact, we confirmed that callus cells from olive shoot explants are able to produce key secoiridoid as 1. To enable this approach, we synthesised and characterised deuterium-labelled iridoidic precursors belonging both to the loganin and the 8-epiloganin series. These iridoids are [7,8-(2)H2]-7-deoxy-8-epi-loganin (2(D)), [8,10-(2)H2]-8-epi-loganin (4(D)) and [7,8-(2)H2]-7-deoxy-loganin (3(D)).

  15. Dansyl-labeled anionic amphiphile with a hexadecanoic carbon chain: synthesis and detection for shape transitions in organized molecular assemblies.

    Science.gov (United States)

    Gao, Lining; Xia, Huiyun; Wang, Xiaoman; Li, Li; Chen, Huaxin

    2015-03-15

    The probing properties of a new fluorophore-labeled anionic surfactant, sodium 16-(N-dansyl)aminocetylate (16-DAN-ACA) were investigated systematically in molecular assemblies, especially in the transitions between micelles and vesicles. 16-DAN-ACA can efficiently differentiate the two different aggregate types in mixed cationic and anionic surfactant systems. The fluorescence anisotropy of 16-DAN-ACA was found to be sensitive for directly detecting the micellar growth in micelles containing oppositely charged surfactants; both cationic cetyltrimethylammonium bromide (CTAB) systems and anionic sodium dodecyl sulfate (SDS) systems were studied. The results indicated that the 16-DAN-ACA is a good fluorescent probe for differentiating the different aggregates, and even more can be used to detect the micellar growth.

  16. Synthesis and evaluation of the racemate and individual enantiomers of C-11 labeled methylphenidate as radioligands for the presynaptic dopaminergic neuron

    Energy Technology Data Exchange (ETDEWEB)

    Ding, Y.S.; Fowler, J.S.; Volkow, N.D. [Brookhaven National Lab., Upton, NY (United States)] [and others

    1994-05-01

    Methylphenidate (MP, ritalin) is a psychostimulant drug widely used to treat attention deficit hyperactivity disorder and narcolepsy. Its therapeutic properties are attributed to inhibition of the dopamine (DA) transporter enhancing synaptic DA. MP has two chiral centers and is marketed as the dl-threo racemic form. However, its pharmacological activity is believed due solely to the d-enantiomer. We have synthesized [{sup 11}C]d,l-threo-methylphenidate ([{sup 11}C]MP) in order to examine its pharmacokinetics in vivo and to examine its suitability as a radioligand for PET studies of the presynaptic DA neuron. [{sup 11}C]MP was prepared by O-{sup 11}C-alkylation of a protected derivative of ritalinic acid with labeled methyl iodide. Serial studies at baseline and after treatment with methylphenidate (0.5 mg/kg, 20 min prior); GBR 12909 (1.5 mg/kg; 30 min prior); tomoxetine (1.5 mg/kg, 20 min prior) and citalopram (2.0 mg/kg, 30 min prior) were performed to assess non-specific binding and binding to the DA, norepinephrine and serotonin transporters respectively. Only MP and GBR 12909 changed the SR/CB distribution volume ratio (decrease of 38 and 37% respectively) demonstrating selectivity for DA transporters over other monoamine transporters. We then pursued the synthesis of enantiomerically pure C-{sup 11} labeled d- and l-MP by using enantiomerically pure protected d- and l-ritalinic acids as precursors. A striking difference in SR/CB ratio (3.3 and 1.1 for d- and l-respectively at 1 hr. after i.v. injections) strongly suggests that the pharmacological specificity of MP resides entirely in the d-isomer and the binding of l-isomer was mostly non-specific. Further evaluations are underway. Radioligand reversibility, selectivity and the fact that MP is an approved drug are advantages of using [{sup 11}C]MP.

  17. Co-precipitation of DEAE-dextran coated SPIONs: how synthesis conditions affect particle properties, stem cell labelling and MR contrast.

    Science.gov (United States)

    Barrow, Michael; Taylor, Arthur; García Carrión, Jaime; Mandal, Pranab; Park, B Kevin; Poptani, Harish; Murray, Patricia; Rosseinsky, Matthew J; Adams, Dave J

    2016-09-01

    Superparamagnetic iron oxide nanoparticles (SPIONs) are widely used as contrast agents for stem cell tracking using magnetic resonance imaging (MRI). The total mass of iron oxide that can be internalised into cells without altering their viability or phenotype is an important criterion for the generation of contrast, with SPIONs designed for efficient labelling of stem cells allowing for an increased sensitivity of detection. Although changes in the ratio of polymer and iron salts in co-precipitation reactions are known to affect the physicochemical properties of SPIONs, particularly core size, the effects of these synthesis conditions on stem cell labelling and magnetic resonance (MR) contrast have not been established. Here, we synthesised a series of cationic SPIONs with very similar hydrodynamic diameters and surface charges, but different polymer content. We have investigated how the amount of polymer in the co-precipitation reaction affects core size and modulates not only the magnetic properties of the SPIONs but also their uptake into stem cells. SPIONs with the largest core size and lowest polymer content presented the highest magnetisation and relaxivity. These particles also had the greatest uptake efficiency without any deleterious effect on either the viability or function of the stem cells. However, for all particles internalised in cells, the T2 and T2(*) relaxivity was independent of the SPION's core size. Our results indicate that the relative mass of iron taken up by cells is the major determinant of MR contrast generation and suggest that the extent of SPION uptake can be regulated by the amount of polymer used in co-precipitation reactions. Copyright © 2016 John Wiley & Sons, Ltd.

  18. Improved synthesis of anti-[{sup 18}F]FACBC: improved preparation of labeling precursor and automated radiosynthesis

    Energy Technology Data Exchange (ETDEWEB)

    McConathy, Jonathan; Voll, Ronald J.; Yu Weiping; Crowe, Ronald J.; Goodman, Mark M. E-mail: mgoodma@emory.edu

    2003-06-01

    The non-natural amino acid anti-1-amino-3-[{sup 18}F]fluorocyclobutyl-1-carboxylic acid (FACBC) has shown promise for tumor imaging with positron emission tomography. An improved synthesis of the precursor of anti-[{sup 18}F]FACBC has been devised which demonstrates high stereoselectivity and suitability for large-scale preparations. An automated radiosynthesis has been developed which provides anti-[{sup 18}F]FACBC in 24% decay-corrected yield. Additionally, the major non-radioactive species present in doses of anti-[{sup 18}F]FACBC has been identified as anti-1-amino-3-hydroxycyclobutane-1-carboxylic acid. Together, these results are important steps towards the routine production of anti-[{sup 18}F]FACBC for human use.

  19. One-pot green synthesis of N-doped carbon quantum dots for cell nucleus labelling and copper (Ⅱ) detection.

    Science.gov (United States)

    Ci, Jiliang; Tian, Ye; Kuga, Shigenori; Niu, Zhongwei; Wu, Min; Huang, Yong

    2017-09-21

    The doping of nitrogen into carbon quantum dots was vitally important for improvement of fluorescence performance. However, the synthesis of nitrogen-doped carbon quantum dots (N-CQDs) was usually conducted under strong acid and high temperature, which would result in the environmental pollution and energy consumption. Herein, the N-CQDs were prepared by a mild one-pot hydrothermal process. The hydrothermal reaction temperature was adjusted to control the particle size, N/C atomic ratio and quantum yield. The products were water-soluble with narrow particle size distribution and good dispersion stability in wide pH range. The N-CQDs could penetrate into HeLa cell nucleus without any further functionalization. Moreover, the fluorescence of N-CQDs could be selectively quenched by Cu2+, suggesting application of detecting Cu2+ in human plasma. © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  20. SLA-DQA基因在F18大肠杆菌抗性和敏感性断奶仔猪间的差异表达分析%The Differential Expression of SLA-DQA Gene between Weaning Piglets Resistant or Sensitive to Escherichia coli F18

    Institute of Scientific and Technical Information of China (English)

    訾臣; 刘璐; 苏先敏; 杜子栋; 黄雪根; 杨建生; 孙寿永; 吴圣龙; 包文斌

    2012-01-01

    运用荧光定量PCR方法分析SLA-DQA基因在苏太猪F18大肠杆菌病抗性和敏感性资源群体中各个组织的分布和表达水平,以及在抗性组和敏感组中的表达差异,以探讨SLA-DQA基因在断奶仔猪抗大肠杆菌F18 菌株感染中发挥的作用.试验结果显示,SLA-DQA基因在所检测的11个组织中均有表达,并呈现相似的表达规律,在肺、脾和淋巴结中的表达量较高,在空肠、十二指肠和胸腺中也有中度的表达.SLA-DQA基因在抗性组个体各个组织中的表达量普遍高于敏感性个体,而且在肺、脾、淋巴结、空肠和十二指肠5个组织中,SLA-DQA基因在抗性组个体中的表达量显著高于敏感性个体(P<0.05).由此可见,当断奶仔猪受到大肠杆菌毒素侵扰后,SLA-DQA基因较高的表达量有利于SLA-Ⅱ类抗原分子的合成,SLA-DQA基因虽然不是针对由大肠杆菌F18菌株造成的断奶仔猪腹泻和水肿病的直接免疫因子,但是在断奶仔猪受大肠杆菌F18菌株病原菌侵袭后引起的一系列生理变化和应答过程中发挥着重要的作用.%The mRNA expression of SLA-DQA was assayed by real-time PCR in 11 different tissues in order to analyze the differential expression between resistant and sensitive post-weaning Sutai piglets invaded with ETEC F18 aiming to explore the role of SLA-DQA gene in the resistance against ETEC F18. The results showed that the SLA-DQA gene was broadly expressed in 11 tissues with a similar expression rule. The expression level was the highest in thymus, lung and lymph nodes. The expression level was moderate in the jejunum, duodenum and spleen. The mRNA expression of SLA-DQA gene in resistant piglets was higher than that in sensitive piglets generally. In lymph node, lung, spleen, jejunum and duodenum, the mRNA expression level of SLA-DQA gene in resistant piglets were significant higher than that in sensitive piglets (P< 0. 05). The analysis suggest that higher expression level

  1. Design, synthesis and evaluation of (18)F-labeled bradykinin B1 receptor-targeting small molecules for PET imaging.

    Science.gov (United States)

    Zhang, Zhengxing; Kuo, Hsiou-Ting; Lau, Joseph; Jenni, Silvia; Zhang, Chengcheng; Zeisler, Jutta; Bénard, François; Lin, Kuo-Shyan

    2016-08-15

    Two fluorine-18 ((18)F) labeled bradykinin B1 receptor (B1R)-targeting small molecules, (18)F-Z02035 and (18)F-Z02165, were synthesized and evaluated for imaging with positron emission tomography (PET). Z02035 and Z02165 were derived from potent antagonists, and showed high binding affinity (0.93±0.44 and 2.80±0.50nM, respectively) to B1R. (18)F-Z02035 and (18)F-Z02165 were prepared by coupling 2-[(18)F]fluoroethyl tosylate with their respective precursors, and were obtained in 10±5 (n=4) and 22±14% (n=3), respectively, decay-corrected radiochemical yield with >99% radiochemical purity. (18)F-Z02035 and (18)F-Z02165 exhibited moderate lipophilicity (LogD7.4=1.10 and 0.59, respectively), and were stable in mouse plasma. PET imaging and biodistribution studies in mice showed that both tracers enabled visualization of the B1R-positive HEK293T::hB1R tumor xenografts with better contrast than control B1R-negative HEK293T tumors. Our data indicate that small molecule antagonists can be used as pharmacophores for the design of B1R-targeting PET tracers.

  2. 猪TLR4基因在F18大肠杆菌抗性型和敏感型资源群体间的差异表达分析%Differentiation of Porcine TLR4 Gene mRNA Expression between Resistant and Sensitive Resource Populations to ETEC F18

    Institute of Scientific and Technical Information of China (English)

    包文斌; 潘章源; 朱璟; 叶兰; 杜子栋; 蔡家嘉; 黄小国; 朱国强; 吴圣龙

    2011-01-01

    本研究旨在检测TLR4基因mRNA在猪各个组织的分布以及在F18大肠杆菌抗性型和敏感型群体间差异表达水平,为探讨该基因在免疫识别和F18大肠杆菌抗性中发挥的作用提供理论依据.本试验运用SYBR Green Ⅰ实时荧光定量PCR技术进行定量测定.首先,各取8头35日龄F18大肠杆菌抗性型和敏感型苏太仔猪组织样,包括心脏、肝脏、脾脏等11个组织,提取总RNA,以GAPDH基因为内参基因,进行实时荧光定量PCR.对TLR4基因mR-NA进行均一化处理,利用荧光阈值(Ct值)计算TLR4基因mRNA在各个组织以及F18大肠杆菌抗性型和敏感型群体间表达量.结果显示,TLR4 mRNA在猪各种组织中广泛表达,在肺、淋巴结、肾脏和脾脏等免疫器官中表达量较高,F18大肠杆菌敏感型的TLR4基因表达量普遍高于抗性型个体的表达量,在各个组织中(除胃外)TLR4表达量差异倍数从1.083到2.980不等;在肺、淋巴结、肾脏和胸腺组织中,F18大肠杆菌敏感型的TLR4基因表达量显著高于抗性型个体的表达量(P<0.05).本研究结果表明,TLR4基因通过天然免疫识别机制对猪F18大肠杆菌病等革兰氏阴性疾病有一定的影响,TLR4基因表达量的下调与F18大肠杆菌的抗性具有一定程度的关系.%This study was conducted to detect the expression of TLR4 gene in variOus tissues of pig, and then to analyze the expression difference between resistant and sensitive resource populations to ETEC F18, which aimed to discuss the role that TLR4 gene played in immunity and resistance to ETEC F18. Porcine TLR4 mRNA was amplified by SYBR-GreenⅠ semi-quantitativeRT-PCR, total RNA was extracted from 11 organizations of sixteen 35-day-old piglets (eight ETEC F18 resistant piglets and eight F18 sensitive piglets) including heart, liver, spleen, and so on. Using GAPDH as an inner control gene, the relative TLR4 gene mRNA expression level in various tissues and then in resistant and

  3. Global emission estimates and radiative impact of C4F10, C5F12, C6F14, C7F16 and C8F18

    Directory of Open Access Journals (Sweden)

    R. G. Prinn

    2012-05-01

    Full Text Available Global emission estimates based on new atmospheric observations are presented for the acylic high molecular weight perfluorocarbons (PFCs: decafluorobutane (C4F10, dodecafluoropentane (C5F12, tetradecafluorohexane (C6F14, hexadecafluoroheptane (C7F16 and octadecafluorooctane (C8F18. Emissions are estimated using a 3-dimensional chemical transport model and an inverse method that includes a growth constraint on emissions. The observations used in the inversion are based on newly measured archived air samples that cover a 39-yr period, from 1973 to 2011, and include 36 Northern Hemispheric and 46 Southern Hemispheric samples (Ivy et al., 2012. The derived emission estimates show that global emission rates were largest in the 1980s and 1990s for C4F10 and C5F12, and in the 1990s for C6F14,C7F16 and C8F18. After a subsequent decline, emissions have remained relatively stable, within 20%, for the last 5 yr. Bottom-up emission estimates are available from the Emission Database for Global Atmospheric Research version 4.2 (EDGARv4.2 for C4F10, C5F12, C6F14 and C7F16, and inventories of C4F10, C5F12 andC6F14 are reported to the United Nations' Framework Convention on Climate Change (UNFCCC by Annex 1 countries that have ratified the Kyoto Protocol. The atmospheric measurement based emission estimates are 20 times larger than EDGARv4.2 for C4F10 and over three orders of magnitude for C5F12. The derived emission estimates for C6F14 largely agree with the bottom-up estimates from EDGARv4.2. Moreover, the C7F16 emission estimates are comparable to those of EDGARv4.2 at their peak in the 1990s, albeit significant underestimation for the other time periods. There are no bottom-up emission estimates for C8F18, thus the emission rates reported here are the first for C8F18. The reported inventories for C4F10, C5F12 and C6F14 to UNFCCC are five to ten times lower than those estimated in this study. In addition, we present measured infrared absorption spectra for C

  4. Global emission estimates and radiative impact of C4F10, C5F12, C6F14, C7F16 and C8F18

    Science.gov (United States)

    Ivy, D. J.; Rigby, M.; Baasandorj, M.; Burkholder, J. B.; Prinn, R. G.

    2012-08-01

    Global emission estimates based on new atmospheric observations are presented for the acylic high molecular weight perfluorocarbons (PFCs): decafluorobutane (C4F10), dodecafluoropentane (C5F12), tetradecafluorohexane (C6F14), hexadecafluoroheptane (C7F16) and octadecafluorooctane (C8F18). Emissions are estimated using a 3-dimensional chemical transport model and an inverse method that includes a growth constraint on emissions. The observations used in the inversion are based on newly measured archived air samples that cover a 39-yr period, from 1973 to 2011, and include 36 Northern Hemispheric and 46 Southern Hemispheric samples. The derived emission estimates show that global emission rates were largest in the 1980s and 1990s for C4F10 and C5F12, and in the 1990s for C6F14, C7F16 and C8F18. After a subsequent decline, emissions have remained relatively stable, within 20%, for the last 5 yr. Bottom-up emission estimates are available from the Emission Database for Global Atmospheric Research version 4.2 (EDGARv4.2) for C4F10, C5F12, C6F14 and C7F16, and inventories of C4F10, C5F12 and C6F14 are reported to the United Nations' Framework Convention on Climate Change (UNFCCC) by Annex 1 countries that have ratified the Kyoto Protocol. The atmospheric measurement-based emission estimates are 20 times larger than EDGARv4.2 for C4F10 and over three orders of magnitude larger for C5F12 (with 2008 EDGARv4.2 estimates for C5F12 at 9.6 kg yr-1, as compared to 67±53 t yr-1 as derived in this study). The derived emission estimates for C6F14 largely agree with the bottom-up estimates from EDGARv4.2. Moreover, the C7F16 emission estimates are comparable to those of EDGARv4.2 at their peak in the 1990s, albeit significant underestimation for the other time periods. There are no bottom-up emission estimates for C8F18, thus the emission rates reported here are the first for C8F18. The reported inventories for C4F10, C5F12 and C6F14 to UNFCCC are five to ten times lower than those

  5. The value of F-18 fluorodeoxyglucose positron emission tomography/computed tomography in asymptomatic examinees with unexplained elevated blood carcinoembryonic antigen levels

    Energy Technology Data Exchange (ETDEWEB)

    Li, Wenfeng [The First Affiliated Hospital of Wenzhou Medical University, Laboratory for Advanced Interdisciplinary Research, Institutes of Translational Medicine, Wenzhou (China); The First Affiliated Hospital of Wenzhou Medical University, Department of Radiation Oncology, Wenzhou (China); Yin, Weiwei [The First Affiliated Hospital of Wenzhou Medical University, Division of PET/CT, Department of Radiology, Wenzhou (China); Ou, Rongying [The First Affiliated Hospital of Wenzhou Medical University, Laboratory for Advanced Interdisciplinary Research, Institutes of Translational Medicine, Wenzhou (China); The First Affiliated Hospital of Wenzhou Medical University, Department of Gynaecology and Obstetrics, Wenzhou (China); Chen, Ting; Xiong, Lingling; Xu, Yunsheng [The First Affiliated Hospital of Wenzhou Medical University, Laboratory for Advanced Interdisciplinary Research, Institutes of Translational Medicine, Wenzhou (China); The First Affiliated Hospital of Wenzhou Medical University, Department of Dermatovenereology, Wenzhou (China); Cheng, Dezhi; Xie, Deyao [The First Affiliated Hospital of Wenzhou Medical University, Laboratory for Advanced Interdisciplinary Research, Institutes of Translational Medicine, Wenzhou (China); The First Affiliated Hospital of Wenzhou Medical University, Department of Cardiothoracic Surgery, Wenzhou (China); Zheng, Xiangwu; Zhao, Liang [The First Affiliated Hospital of Wenzhou Medical University, Laboratory for Advanced Interdisciplinary Research, Institutes of Translational Medicine, Wenzhou (China); The First Affiliated Hospital of Wenzhou Medical University, Division of PET/CT, Department of Radiology, Wenzhou (China); The First Affiliated Hospital of Wenzhou Medical University, Institutes of Intelligent and Molecular Imaging, Wenzhou (China)

    2016-04-15

    Cancer is still a clinical challenge, with many efforts invested in order to achieve timely detection. Unexplained elevated blood carcinoembryonic antigen levels are occasionally observed in an asymptomatic population and considered as a risk factor of cancers. The purpose of this study was to determine the validity of 18 F-fluorodeoxyglucose-positron emission tomography/computed tomography (F-18 FDG-PET/CT) for detecting cancer in an asymptomatic population with an unexplained elevation in blood carcinoembryonic antigen (CEA) levels. This retrospective study included a total of 1920 asymptomatic examinees conducted from August 2011 through September 2013. The participants underwent CEA assay and conventional medical imaging (CEA-conventional), or CEA assay and F-18 FDG-PET/CT (CEA-PET/CT). The validity of conventional medical imaging and CEA-PET/CT scanning for detecting cancer and early-stage cancer in an asymptomatic population with an unexplained elevation in blood CEA levels were evaluated. Sensitivity, specificity, cancer detection rate, missed cancer detection rate, early-stage cancer detection rate, and early-stage cancer ratio using the CEA-PET/CT scanning were 96.6 %, 100 %, 10.4 %, 0.4 %, 3.7 %, and 34.5 %, respectively. In contrast, the corresponding values obtained using the conventional medical imaging were 50.6 % (P < 0.0001), 100 % (P > 0.9999), 50.6 % (P < 0.0001), 99.9 % (P = 0.055), 2.6 % (P < 0.0001), 2.5 % (P = 0.04), 0.7 % (P = 0.0004), and 14.5 % (P = 0.002), respectively. The F-18 FDG-PET/CT scanning significantly improved the validity of the cancer detection program in the asymptomatic population with an unexplained elevation in CEA levels. (orig.)

  6. Nerve Sheath Tumors in Neurofibromatosis Type 1: Assessment of Whole-Body Metabolic Tumor Burden Using F-18-FDG PET/CT.

    Directory of Open Access Journals (Sweden)

    Johannes Salamon

    Full Text Available To determine the metabolically active whole-body tumor volume (WB-MTV on F-18-fluorodeoxyglucose positron emission tomography/computed tomography (F-18-FDG PET/CT in individuals with neurofibromatosis type 1 (NF1 using a three-dimensional (3D segmentation and computerized volumetry technique, and to compare PET WB-MTV between patients with benign and malignant peripheral nerve sheath tumors (PNSTs.Thirty-six NF1 patients (18 patients with malignant PNSTs and 18 age- and sex-matched controls with benign PNSTs were examined by F-18-FDG PET/CT. WB-MTV, whole-body total lesion glycolysis (WB-TLG and a set of semi-quantitative imaging-based parameters were analyzed both on a per-patient and a per-lesion basis.On a per-lesion basis, malignant PNSTs demonstrated both a significantly higher MTV and TLG than benign PNSTs (p < 0.0001. On a per-patient basis, WB-MTV and WB-TLG were significantly higher in patients with malignant PNSTs compared to patients with benign PNSTs (p < 0.001. ROC analysis showed that MTV and TLG could be used to differentiate between benign and malignant tumors.WB-MTV and WB-TLG may identify malignant change and may have the potential to provide a basis for investigating molecular biomarkers that correlate with metabolically active disease manifestations. Further evaluation will determine the potential clinical impact of these PET-based parameters in NF1.

  7. Synthesis of carbon-14 labelled cis-malonato [(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane] platinum(II) (SKI 2053R)

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Dae-Kee; Kim, Youngseok; Rim, Jonggill; Kim, Ganghyeok; Gam, Jongsik; Song, Sungkun; Yoo, Kwanghee; Kim, Key H. (Sunkyong Industries, Kyungki-Do (Korea, Republic of). Life Science Research Center)

    1994-02-01

    The synthesis of [sup 14]C-labelled cis-malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolan e]platinum(II) from [1,4-[sup 14]C] D-tartaric acid is described. The overall radiochemical yield of the product in a eight-step sequence was 23.8% and radiochemical purity was 98.5%. (author).

  8. Synthesis and evaluation of a bromine-76-labeled PPAR{gamma} antagonist 2-bromo-5-nitro-N-phenylbenzamide

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Hsiaoju [Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110 (United States); Finck, Brian N. [Department of Internal Medicine, Division of Geriatrics and Nutritional Science, Washington University School of Medicine, St. Louis. MO 63110 (United States); Jones, Lynne A. [Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110 (United States); Welch, Michael J. [Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110 (United States); Mach, Robert H. [Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110 (United States)]. E-mail: rhmach@mir.wustl.edu

    2006-10-15

    Peroxisome proliferator activated-receptor gamma (PPAR{gamma}) binds to peroxisome receptor response elements with its heterodimeric partner, retinoid X receptor, and regulates downstream gene expression. PPAR{gamma} transcriptionally modulates fat metabolism, and receptor agonists have been developed to treat type II diabetes. PPAR{gamma} is also overexpressed in some tumor cell lines and primary tumors, including breast and prostate tumors. Two PPAR{gamma} antagonists, 2-chloro-5-nitro-N-phenylbenzamide (GW9662) and 2-chloro-5-nitro-N-pyridin-4-yl-benzamide (T0070907), represent good lead compounds for radiotracer development. In the current study, four additional halogen substituted analogs were synthesized and evaluated in a whole cell screening assay for PPAR{gamma} binding activity. Two bromine-containing analogs having EC{sub 5} values <5 nM were chosen for bromine-76 radiolabeling. Bromine-76-labeled 2-bromo-5-nitro-N-phenyl-benzamide was selected for subsequent in vitro and in vivo studies due to its superior radiolabeling yield ({approx}70%) and the well-characterized pharmacological properties of its analog GW9662. An in vitro stability study showed that 40% of the compound remained intact in plasma and about 25% in whole blood after 30 min. Biodistribution studies in MDA-MB-435 human breast tumor-bearing nude mice were carried out at 5 min, 30 min, 2 h and 24 h post injection of the radiotracer. Although in vivo metabolite studies demonstrated rapid compound degradation, at least 10% of the parent compound was delivered to the tumor. We are currently exploring second generation analogs of these lead compounds for the development of radiolabeled antagonists of the PPAR{gamma} receptor.

  9. Synthesis of fluorescent label, DBD-beta-proline, and the resolution efficiency for chiral amines by reversed-phase chromatography.

    Science.gov (United States)

    Min, Jun Zhe; Toyo'oka, Toshimasa; Kato, Masaru; Fukushima, Takeshi

    2005-01-01

    DBD-d(and l)-beta-proline, new fluorescent chiral derivatization reagents, were synthesized from the reaction of 4-(N,N-dimethylaminosulfonyl)-7- fl uoro-2,1,3-benzoxadiazole (DBD-F) with beta-proline. The racemic mixture synthesized was separated by a chiral stationary phase (CSP) column, Chiralpak AD-H, with n-hexane-EtOH-TFA-diethylamine (70:30:0.1:0.1) as the mobile phase. The dl-forms were decided according to the results obtained from a circular dichroism (CD) detector after separation by the CSP column. The fractionated enantiomers reacted with chiral amine to produce a couple of diastereomers. The labeling proceeded in the presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) and pyridine as the activation reagents. The reaction conditions were mild and no racemization occurred during the diastereomer formation. The resulting diastereomers fluoresced at around 570 nm (excitation at around 460 nm). Good linearity of the calibration curves was obtained in the range 1-75 pmol and the detection limits on chromatogram were less than 1 pmol. The separability of the diastereomers was compared with the diastereomers derived from DBD-d(or l)-proline. The resolution values (Rs) obtained from the diastereomers of three chiral amines with DBD-d(or l)-beta-proline were higher than those derived from DBD-d(or l)-proline, e.g. dl-phenylalanine methylester (dl-PAME), 2.23 vs 1.37; (R)(S)-1-phenylethylamine [(R)(S)-PEA], 2.09 vs 1.13; and (R)(S)-1-(1-naphthyl)ethylamines [(R)(S)-NEA], 5.19 vs 1.23. The results suggest that the position of COOH group on pyrrolidine moiety in the structures is one of the important factors for the efficient separation of a couple of the diastereomers.

  10. Synthesis, uptake mechanism characterization and biological evaluation of {sup 18}F labeled fluoroalkyl phenylalanine analogs as potential PET imaging agents

    Energy Technology Data Exchange (ETDEWEB)

    Wang Limin [Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104 (United States); Qu Wenchao; Lieberman, Brian P.; Ploessl, Karl [Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104 (United States); Kung, Hank F., E-mail: kunghf@gmail.co [Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104 (United States); Department of Pharmacology, University of Pennsylvania, Philadelphia, PA 19104 (United States)

    2011-01-15

    Introduction: Amino acids based tracers represent a promising class of tumor metabolic imaging agents with successful clinical applications. Two new phenylalanine derivatives, p-(2-[{sup 18}F]fluoroethyl)-L-phenylalanine (FEP, [{sup 18}F]2) and p-(3-[{sup 18}F]fluoropropyl)-L-phenylalanine (FPP, [{sup 18}F]3) were synthesized and evaluated in comparison to clinically utilized O-(2-[{sup 18}F]fluoroethyl)-L-tyrosine (FET, [{sup 18}F]1). Methods: FEP ([{sup 18}F]2) and FPP ([{sup 18}F]3) were successfully synthesized by a rapid and efficient two-step nucleophilic fluorination of tosylate precursors and deprotection reaction. In vitro cell uptake studies were carried out in 9L glioma cells. In vivo studies, 9L tumor xenografts were implanted in Fisher 344 rats. Results: FEP ([{sup 18}F]2) and FPP ([{sup 18}F]3) could be efficiently labeled within 90 min with good enantiomeric purity (>95%), good yield (11-37%) and high specific activity (21-69 GBq/{mu}mol). Cell uptake studies showed FEP had higher uptake than FPP as well as reference ligand FET ([{sup 18}F]1). Uptake mechanism studies suggested that FEP is a selective substrate for system L and prefers its subtype LAT1. In vivo biodistribution studies demonstrated FEP had specific accumulation in tumor cells and tumor to background ratio reached 1.45 at 60 min. Small animal positron emission tomography (PET) imaging studies showed FEP was comparable to FET for imaging rats bearing 9L tumor model. FEP had high uptake in 9L tumor compared to surrounding tissue and was quickly excreted through urinary tract. Conclusion: Biological evaluations indicate that FEP ([{sup 18}F]2) is a potential useful tracer for tumor imaging with PET.

  11. Synthesis of BODIPY derivatives substituted with various bioconjugatable linker groups: a construction kit for fluorescent labeling of receptor ligands.

    Science.gov (United States)

    Heisig, Fabian; Gollos, Sabrina; Freudenthal, Sven J; El-Tayeb, Ali; Iqbal, Jamshed; Müller, Christa E

    2014-01-01

    The goal of the present study was to design small, functionalized green-emitting BODIPY dyes, which can readily be coupled to target molecules such as receptor ligands, or even be integrated into their pharmacophores. A simple two-step one-pot procedure starting from 2,4-dimethylpyrrole and ω-bromoalkylcarboxylic acid chlorides was used to obtain new ω-bromoalkyl-substituted BODIPY fluorophores (1a-1f) connected via alkyl spacers of different length to the 8-position of the fluorescent dye. The addition of radical inhibitors reduced the amount of side products. The ω-bromoalkyl-substituted BODIPYs were further converted to introduce various functional groups: iodo-substituted dyes were obtained by Finkelstein reaction in excellent yields; microwave-assisted reaction with methanolic ammonia led to fast and clean conversion to the amino-substituted dyes; a hydroxyl-substituted derivative was prepared by reaction with sodium ethylate, and thiol-substituted BODIPYs were obtained by reaction of 1a-1f with potassium thioacetate followed by alkaline cleavage of the thioesters. Water-soluble derivatives were prepared by introducing sulfonate groups into the 2- and 6-position of the BODIPY core. The synthesized BODIPY derivatives showed high fluorescent yields and appeared to be stable under basic, reducing and oxidative conditions. As a proof of concept, 2-thioadenosine was alkylated with bromoethyl-BODIPY 1b. The resulting fluorescent 2-substituted adenosine derivative 15 displayed selectivity for the A3 adenosine receptor (ARs) over the other AR subtypes, showed agonistic activity, and may thus become a useful tool for studying A3ARs, or a lead structure for further optimization. The new functionalized dyes may be widely used for fluorescent labeling allowing the investigation of biological targets and processes.

  12. Synthesis, dynamic NMR characterization and XRD studies of novel N,N’-substituted piperazines for bioorthogonal labeling

    Directory of Open Access Journals (Sweden)

    Constantin Mamat

    2016-11-01

    Full Text Available Novel, functionalized piperazine derivatives were successfully synthesized and fully characterized by 1H/13C/19F NMR, MS, elemental analysis and lipophilicity. All piperazine compounds occur as conformers resulting from the partial amide double bond. Furthermore, a second conformational shape was observed for all nitro derivatives due to the limited change of the piperazine chair conformation. Therefore, two coalescence points were determined and their resulting activation energy barriers were calculated using 1H NMR. To support this result, single crystals of 1-(4-nitrobenzoylpiperazine (3a, monoclinic, space group C2/c, a = 24.587(2, b = 7.0726(6, c = 14.171(1 Å, β = 119.257(8°, V = 2149.9(4 Å3, Z = 4, Dobs = 1.454 g/cm3 and the alkyne derivative 4-(but-3-yn-1-yl-1-(4-fluorobenzoylpiperazine (4b, monoclinic, space group P21/n, a = 10.5982(2, b = 8.4705(1, c = 14.8929(3 Å, β = 97.430(1°, V = 1325.74(4 Å3, Z = 4, Dobs = 1.304 g/cm3 were obtained from a saturated ethyl acetate solution. The rotational conformation of these compounds was also verified by XRD. As proof of concept for future labeling purposes, both nitropiperazines were reacted with [18F]F–. To test the applicability of these compounds as possible 18F-building blocks, two biomolecules were modified and chosen for conjugation either using the Huisgen-click reaction or the traceless Staudinger ligation.

  13. Synthesis and evaluation of tetraphosphonates labelled with {sup 212}Bi, {sup 212}Pb and {sup 165}Er

    Energy Technology Data Exchange (ETDEWEB)

    Hassfjell, S.P

    1997-08-01

    The main goal of this work has been to achieve a synthesis of radiolabelled phosphonates for the improvement of diagnostic and therapy of osteoblastic osteosarcoma and sclerotic bone metastases. {sup 212}Bi-DOTMP is shown to be an in vivo stable bone seeking radiopharmaceutical with a potential for a {alpha}-particle therapy of the above mentioned diseases. It has biodistribution characteristics similar to {sup 153}Sm-EDTMP, which is now formally approved in several countries, most recently in the US. {sup 212}Pb-DOTMP is also a promising candidate having the advantage of increasing the effective half life of the {alpha}-emitter, although loss of some of the in vivo generated {sup 212}Bi may be a problem. A generator has been developed for the production of the {alpha}-emitting radionuclide {sup 212}Bi and its parent nuclide {sup 212}Pb. The generator is based on the emanation of {sup 220}Rn from ({sup 228}Th)barium stearate. The decay product of {sup 220}Rn, {sup 212}Pb deposits on the walls of a polyethylene bottle, and can be wasted off with distilled water. The generator shows no leakage of any long-lived parent nuclides, is easy to operate and has a high degree of radiation safety.

  14. Synthesis of carbon-11 labelled SCH 39166, a new selective dopamine D-1 receptor ligand, and preliminary PET investigations

    Energy Technology Data Exchange (ETDEWEB)

    Halldin, Christer; Farde, Lars; Sedvall, Goeran (Karolinska Hospital, Stockholm (Sweden). Dept. of Psychiatry and Psychology); Barnett, Allen (Schering-Plough Corp., Bloomfield, NJ (USA))

    1991-01-01

    SCH 39166 ((-)-trans-6,7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-N-methyl-5H-benzo(d)naphtho-(2,1-b)azepine ) is a new more selective dopamine D-1 receptor antagonist than the widely used SCH 23390. ({sup 11}C)SCH 39166 was prepared by N-methylation of the desmethyl compound SCH 40853 ((-)-trans-6,7,7a,8,9,13b-hexahydro-3-chloro-2-hydroxy-5H-benzo(d)naphtho -(2,1-b)azepine) with ({sup 11}C)methyl iodide. Reaction in acetone with subsequent straight-phase semi-preparative HPLC resulted in 20-30% radiochemical yield (from EOB and decay-corrected) with a total synthesis time of 35-40 min and a radiochemical purity >99%. The specific activity obtained at EOS was about 1500 Ci/mmol (55 GBq/{mu}mol). ({sup 11}C)SCH 39166 was injected into a Cynomolgus monkey. PET-analysis demonstrated accumulation in the striatum, a region known to have a high density of dopamine D-1 receptors. In a displacement experiment, radioactivity in the striatum was markedly reduced after injection of 6 mg unlabelled SCH 23390, thus demonstrating the specificity and reversibility of ({sup 11}C)SCH 39166 binding to dopamine D-1 receptors. (author).

  15. A case of dedifferentiated liposarcoma showing a biphasic pattern on 2-deoxy-2-F18- fluoro-D-glucose positron emission tomography/ computed tomography

    Directory of Open Access Journals (Sweden)

    Manabu Hoshi

    2013-04-01

    Full Text Available Integrated 2-deoxy-2-F18-fluoro-D-glucose positron emission tomography combined with computed tomography (FDG-PET/CT has been used in the field of soft tissue sarcoma. We report an 81-year-old man with dedifferentiated liposarcoma in the left thigh, which was composed of well-differentiated liposarcoma and pleomorphic malignant fibrous histiocytoma. As well as other radiological modalities, FDG-PET was able to demonstrate a biphasic signal pattern composed of well-differentiated liposarcoma and dedifferentiated area, being consistent with the histological grade of malignancy.

  16. Aeropropulsive characteristics of Mach numbers up to 2.2 of axisymmetric and nonaxisymmetric nozzles installed on an F-18 model

    Science.gov (United States)

    Capone, F. J.

    1982-01-01

    An investigation to determine the aeropropulsive characteristics of nonaxisymmetric nozzles on an F-18 jet effects model was conducted in the Langley 16-foot transonic tunnel and the AEDC 16-foot supersonic wind tunnel. The performance of a two dimensional convergent-divergent nozzle, a single expansion ramp nozzle, and a wedge nozzle was compared with that of the baseline axisymmetric nozzle. Test data were obtained at static conditions and at Mach numbers from 0.60 to 2.20 at an angle of attack of 0 deg. Nozzle pressure ratio was varied from jet-off to about 20.

  17. Suppression of isotope scrambling in cell-free protein synthesis by broadband inhibition of PLP enymes for selective 15N-labelling and production of perdeuterated proteins in H2O.

    Science.gov (United States)

    Su, Xun-Cheng; Loh, Choy-Theng; Qi, Ruhu; Otting, Gottfried

    2011-05-01

    Selectively isotope labelled protein samples can be prepared in vivo or in vitro from selectively labelled amino acids but, in many cases, metabolic conversions between different amino acids result in isotope scrambling. The best results are obtained by cell-free protein synthesis, where metabolic enzymes are generally less active, but isotope scrambling can never be suppressed completely. We show that reduction of E. coli S30 extracts with NaBH(4) presents a simple and inexpensive way to achieve cleaner selective isotope labelling in cell-free protein synthesis reactions. The purpose of the NaBH(4) is to inactivate all pyridoxal-phosphate (PLP) dependent enzymes by irreversible reduction of the Schiff bases formed between PLP and lysine side chains of the enzymes or amino groups of free amino acids. The reduced S30 extracts retain their activity of protein synthesis, can be stored as well as conventional S30 extracts and effectively suppress conversions between different amino acids. In addition, inactivation of PLP-dependent enzymes greatly stabilizes hydrogens bound to α-carbons against exchange with water, minimizing the loss of α-deuterons during cell-free production of proteins from perdeuterated amino acids in H(2)O solution. This allows the production of highly perdeuterated proteins that contain protons at all exchangeable positions, without having to back-exchange labile deuterons for protons as required for proteins that have been synthesized in D(2)O.

  18. Suppression of isotope scrambling in cell-free protein synthesis by broadband inhibition of PLP enymes for selective {sup 15}N-labelling and production of perdeuterated proteins in H{sub 2}O

    Energy Technology Data Exchange (ETDEWEB)

    Su Xuncheng; Loh, Choy-Theng; Qi Ruhu; Otting, Gottfried, E-mail: gottfried.otting@anu.edu.au [Australian National University, Research School of Chemistry (Australia)

    2011-05-15

    Selectively isotope labelled protein samples can be prepared in vivo or in vitro from selectively labelled amino acids but, in many cases, metabolic conversions between different amino acids result in isotope scrambling. The best results are obtained by cell-free protein synthesis, where metabolic enzymes are generally less active, but isotope scrambling can never be suppressed completely. We show that reduction of E. coli S30 extracts with NaBH{sub 4} presents a simple and inexpensive way to achieve cleaner selective isotope labelling in cell-free protein synthesis reactions. The purpose of the NaBH{sub 4} is to inactivate all pyridoxal-phosphate (PLP) dependent enzymes by irreversible reduction of the Schiff bases formed between PLP and lysine side chains of the enzymes or amino groups of free amino acids. The reduced S30 extracts retain their activity of protein synthesis, can be stored as well as conventional S30 extracts and effectively suppress conversions between different amino acids. In addition, inactivation of PLP-dependent enzymes greatly stabilizes hydrogens bound to {alpha}-carbons against exchange with water, minimizing the loss of {alpha}-deuterons during cell-free production of proteins from perdeuterated amino acids in H{sub 2}O solution. This allows the production of highly perdeuterated proteins that contain protons at all exchangeable positions, without having to back-exchange labile deuterons for protons as required for proteins that have been synthesized in D{sub 2}O.

  19. Visualization of small glottic laryngeal cancer using methyl-labeled C-11-methionine positron emission tomography

    NARCIS (Netherlands)

    Wedman, Jan; Pruim, J.; Langendijk, J. A.; van der Laan, B. F. A. M.

    2009-01-01

    Despite abundant literature on the use of PET in head and neck cancer, a little is known about the visualization of small laryngeal cancer. Moreover, most literature deals with the radiopharmaceutical F-18-fludeoxyglucose (FDG), whereas only a few papers address the use of C-11 labeled amino acids.

  20. Visualization of small glottic laryngeal cancer using methyl-labeled C-11-methionine positron emission tomography

    NARCIS (Netherlands)

    Wedman, Jan; Pruim, J.; Langendijk, J. A.; van der Laan, B. F. A. M.

    2009-01-01

    Despite abundant literature on the use of PET in head and neck cancer, a little is known about the visualization of small laryngeal cancer. Moreover, most literature deals with the radiopharmaceutical F-18-fludeoxyglucose (FDG), whereas only a few papers address the use of C-11 labeled amino acids.

  1. Semi-Quantitative Calculations of Primary Tumor Metabolic Activity Using F-18 FDG PET/CT as a Predictor of Survival in 92 Patients With High-Grade Bone or Soft Tissue Sarcoma

    DEFF Research Database (Denmark)

    Andersen, Kim Francis; Fuglo, Hanna Maria; Rasmussen, Sine Hvid;

    2015-01-01

    To assess the prognostic value of primary tumor metabolic activity in patients with high-grade bone sarcomas (BS) or soft tissue sarcomas (STS) using F-18 FDG PET/CT. A single-site, retrospective study including 92 patients with high-grade BS or STS. Pretreatment F-18 FDG PET/CT scan was performed...... metabolic activity with pretherapeutic SUVmax using F-18 FDG PET/CT demonstrates independent properties beyond histologic grading for prediction of survival in patients with high-grade STS, but not with high-grade BS....

  2. F-18 high alpha research vehicle surface pressures: Initial in-flight results and correlation with flow visualization and wind-tunnel data

    Science.gov (United States)

    Fisher, David F.; Banks, Daniel W.; Richwine, David M.

    1990-01-01

    Pressure distributions measured on the forebody and the leading-edge extensions (LEX's) of the NASA F-18 high alpha research vehicle (HARV) were reported at 10 and 50 degree angles of attack and at Mach 0.20 to 0.60. The results were correlated with HARV flow visualization and 6-percent scale F-18 wind-tunnel-model test results. The general trend in the data from the forebody was for the maximum suction pressure peaks to first appear at an angle of attack (alpha) of approximately 19 degrees and increase in magnitude with angle of attack. The LEX pressure distribution general trend was the inward progression and increase in magnitude of the maximum suction peaks up to vortex core breakdown and then the decrease and general flattening of the pressure distribution beyond that. No significant effect of Mach number was noted for the forebody results. However, a substantial compressibility effect on the LEX's resulted in a significant reduction in vortex-induced suction pressure as Mach number increased. The forebody primary and the LEX secondary vortex separation lines, from surface flow visualization, correlated well with the end of pressure recovery, leeward and windward, respectively, of maximum suction pressure peaks. The flight to wind-tunnel correlations were generally good with some exceptions.

  3. Imaging patients with breast and prostate cancers using combined 18F NaF/18F FDG and TOF simultaneous PET/ MRI

    Energy Technology Data Exchange (ETDEWEB)

    Iagaru, Andrei; Minamimoto, Ryogo; Jamali, Mehran; Barkodhodari, Amir; Gambhir, Sanjiv Sam; Vasanawala, Shreyas [Stanford University, Department of Radiology, Division of Nuclear Medicine and Molecular Imaging (United States)

    2015-05-18

    Here we prospectively compared the combined 18F NaF/18F FDG PET/ MRI against 99mTc-MDP in patients with breast and prostate cancers. Twelve patients referred for 99mTc-MDP bone scans were prospectively enrolled from Oct 14 - Jan 15. The cohort included 6 men with prostate cancer and 6 women with breast cancer, 41 – 85 year-old (average 63 ± 15). 18F NaF (0.7-2.2 mCi, mean: 1.33 mCi) and 18F FDG (3.9-5.2 mCi, mean: 4.6 mCi) were subsequently injected from separate syringes. The PET/MRI was done 6-12 days (average 9.3 ± 3.2) after bone scan. The whole body MRI protocol consisted of T2-weighted, DWI, and contrast-enhanced T1-weighted imaging. Lesions detected with each test were tabulated and the results were compared. All patients tolerated the PET/MRI exam, and PET image quality was diagnostic despite the marked reduction in the administered dosage of radiopharmaceuticals (80% less for 18F NaF and 67% less for 18F FDG). Five patients had no bone metastases identified on either scans. Bone scintigraphy and PET/MRI showed osseous metastases in 7 patients, but more numerous bone findings were noted on PET/MRI than on bone scintigraphy in 3 patients. Lesions outside the skeleton were identified by PET/MRI in 2 patients. The combined 18F NaF/18F FDG PET/MRI is superior to 99mTc-MDP scintigraphy for evaluation of skeletal disease extent. Further, it detected extra- skeletal disease that may change the management of these patients, while allowing a significant reduction in radiation exposure from lower dosages of PET radiopharmaceuticals administered. A combination of 18F NaF/18F FDG PET/MRI may provide the most accurate staging of patients with breast and prostate cancers prior to the start of treatment.

  4. Nutrition Labeling

    DEFF Research Database (Denmark)

    Grunert, Klaus G

    2013-01-01

    because consumers will avoid products that the label shows to be nutritionally deficient, but also because food producers will try to avoid marketing products that appear, according to the label, as nutritionally problematic, for example, because of a high content of saturated fat or salt. Nutrition......Nutrition labeling refers to the provision of information on a food product’s nutritional content on the package label. It can serve both public health and commercial purposes. From a public health perspective, the aim of nutrition labeling is to provide information that can enable consumers...... to make healthier choices when choosing food products. Nutrition labeling is thus closely linked to the notion of the informed consumer, that chooses products according to their aims, on the basis of the information at their disposal. Because many consumers are assumed to be interested in making healthy...

  5. Nutrition Labeling

    DEFF Research Database (Denmark)

    Grunert, Klaus G

    2013-01-01

    because consumers will avoid products that the label shows to be nutritionally deficient, but also because food producers will try to avoid marketing products that appear, according to the label, as nutritionally problematic, for example, because of a high content of saturated fat or salt. Nutrition......Nutrition labeling refers to the provision of information on a food product’s nutritional content on the package label. It can serve both public health and commercial purposes. From a public health perspective, the aim of nutrition labeling is to provide information that can enable consumers...... to make healthier choices when choosing food products. Nutrition labeling is thus closely linked to the notion of the informed consumer, that chooses products according to their aims, on the basis of the information at their disposal. Because many consumers are assumed to be interested in making healthy...

  6. Pattern of cerebral glucose metabolism on F-18 FDG brain PET during vomiting and symptom free periods in cyclic vomiting syndrome

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Yu Kyeong; Lee, Dong Soo; Kang, Eun Joo; Seo, Jeong Kee; Yeo, Jeong Seok; Chung, June Key; Lee, Myung Chul [College of Medicine, Seoul National Univ., Seoul (Korea, Republic of)

    2001-06-01

    Cyclic Vomiting Syndrome (CVS) is characterized by recurrent, periodic, self-limiting vomiting. However, its pathogenesis is not yet established. We investigated the changes of the cerebral glucose metabolism using F-18 FDG during the vomiting attack and symptom free period in two children with CVS. FDG PET study showed the markedly increased metabolism in both temporal lobes and also in the medulla and cerebellum during the vomiting period. Also, FDG PET showed the decreased metabolism in the parieto-occipital and occipital areas during the in vomiting period. The area with decreased metabolism seemed to be related with the region showing abnormalities in EEG and perfusion SPECT studies. We expect that what we observed would be a helpful finding in clarifying the pathogenesis of the CVS.

  7. F-18 high alpha research vehicle surface pressures - Initial in-flight results and correlation with flow visualization and wind-tunnel data

    Science.gov (United States)

    Fisher, David F.; Banks, Daniel W.; Richwine, David M.

    1990-01-01

    Flight tests with the NASA F-18 high-alpha research vehicle (HARV) have yielded pressure distributions at angles of attack from 10 to 50 deg, at Mach 0.23 to 0.6, at five fuselage forebody stations and three on the leading-edge extensions (LEXs). Correlations are made between these data and both previously obtained HARV flow visualizations and wind tunnel model test results. The general trend is one in which the forebody's maximum suction pressure peaks increase in magnitude, after their first appearance at alpha of about 19 deg, with increasing alpha. LEX pressure-distribution trends involve the inward progression of the maximum suction peaks, an increase in the magnitude of the maximum pressure peaks up to pressure core breakdown, and the decrease and general flattening of the pressure distribution beyond the LEX primary vortex breakdown.

  8. Preserved Glucose Metabolism of Deep Cerebellar Nuclei in a Case of Multiple System Atrophy with Predominant Cerebellar Ataxia: F-18 Fluorodeoxyglucose Positron Emission Tomography Study

    Directory of Open Access Journals (Sweden)

    Oh Dae Kwon

    2010-10-01

    Full Text Available The cerebellar glucose metabolism of multiple system atrophy with predominant cerebellar ataxia (MSA-C is known to be decreased but is not defined among areas of cerebellum. We encountered a 54-year-old man who developed dizziness and progressive ataxia followed by urinary incontinence and orthostatic hypotension, all of those symptoms progressed relentlessly and the symptoms responded poorly to levodopa therapy. Visual analysis and statistical parametric mapping analysis of F-18 fluorodeoxyglucose positron emission tomography showed hypometabolism of both cerebellar hemisphere, severe at cortical area, and pons. There was clear sparing of deep cerebellar nuclei. Our report, as we know, shows the first case of preserved glucose metabolism of deep cerebellar nuclei relative to cerebellar cortex in an MSA-C patient.

  9. Age- and Sex-Associated Changes in Cerebral Glucose Metabolism in Normal Healthy Subjects: Statistical Parametric Mapping Analysis of F-18 Fluorodeoxyglucose Brain Positron Emission Tomography

    Energy Technology Data Exchange (ETDEWEB)

    Kim, In-Ju; Kim, Seong-Jang; Kim, Yong-Ki (Dept. of Nuclear Medicine, Pusan National Univ. Hospital, Busan (Korea); Medical Research Institute, Pusan National Univ., Busan (Korea)). e-mail: growthkim@daum.net/growthkim@pusan.ac.kr)

    2009-12-15

    Background: The age- and sex-associated changes of brain development are unclear and controversial. Several previous studies showed conflicting results of a specific pattern of cerebral glucose metabolism or no differences of cerebral glucose metabolism in association with normal aging process and sex. Purpose: To investigate the effects of age and sex on changes in cerebral glucose metabolism in healthy subjects using fluorine-18 fluorodeoxyglucose (F-18 FDG) brain positron emission tomography (PET) and statistical parametric mapping (SPM) analysis. Material and Methods: Seventy-eight healthy subjects (32 males, mean age 46.6+-18.2 years; 46 females, mean age 40.6+-19.8 years) underwent F-18 FDG brain PET. Using SPM, age- and sex-associated changes in cerebral glucose metabolism were investigated. Results: In males, a negative correlation existed in several gray matter areas, including the right temporopolar (Brodmann area [BA] 38), right orbitofrontal (BA 47), left orbitofrontal gyrus (BA 10), left dorsolateral frontal gyrus (BA 8), and left insula (BA 13) areas. A positive relationship existed in the left claustrum and left thalamus. In females, negative changes existed in the left caudate body, left temporopolar area (BA 38), right orbitofrontal gyri (BA 47 and BA 10), and right dorsolateral prefrontal cortex (BA 46). A positive association was demonstrated in the left subthalamic nucleus and the left superior frontal gyrus. In white matter, an age-associated decrease in FDG uptake in males was shown in the left insula, and increased FDG uptake was found in the left corpus callosum. The female group had an age-associated negative correlation of FDG uptake only in the right corpus callosum. Conclusion: Using SPM, we found not only similar areas of brain, but also sex-specific cerebral areas of age-associated changes of FDG uptake

  10. The differentiation of malignant and benign musculoskeletal tumors by F-18 FDG PET/CT studies-determination of maxSUV by analysis of ROC curve

    Energy Technology Data Exchange (ETDEWEB)

    Kong, Eun Jung; Cho, Ihn Ho; Chun, Kyung Ah; Won, Kyu Chang; Lee, Hyung Woo; Choi, Jun Heok; Shin, Duk Seop [Yeungnam University College of Medicine, Daegu (Korea, Republic of)

    2007-12-15

    We evaluated the standard uptake value (SUV) of F-18 FDG at PET/CT for differentiation of benign from malignant tumor in primary musculoskeletal tumors. Forty-six tumors (11 benign and 12 malignant soft tissue tumors, 9 benign and 14 malignant bone tumors) were examined with F-18 FDG PET/CT (Discovery ST, GE) prior to tissue diagnosis. The maxSUV(maximum value of SUV) were calculated and compared between benign and malignant lesions. The lesion analysis was based on the transverse whole body image. The maxSUV with cutoff of 4.1 was used in distinguishing benign from malignant soft tissue tumor and 3.05 was used in bone tumor by ROC curve. There was a statistically significant difference in maxSUV between benign (n = 11; maxSUV 3.4 {+-} 3.2) and malignant (n = 12; maxSUV 14.8 {+-} 12.2) lesion in soft tissue tumor ({rho} = 0.001). Between benign bone tumor (n = 9; maxSUV 5.4 {+-} 4.0) and malignant bone tumor (n = 14; maxSUV 7.3 {+-} 3.2), there was not a significant difference in maxSUV. The sensitivity and specificity for differentiating malignant from benign soft tissue tumor was 83% and 91%, respectively. There were four false positive malignant bone tumor cases to include fibrous dysplasia, Langerhans-cell histiocytosis (n = 2) and osteoid osteoma. Also, one false positive case of malignant soft tissue tumor was nodular fasciitis. The maxSUV was useful for differentiation of benign from malignant lesion in primary soft tissue tumors. In bone tumor, the low maxSUV correlated well with benign lesions but high maxSUV did not always mean malignancy.

  11. Optimizing the interval between G-CSF therapy and F-18 FDG PET imaging in children and young adults receiving chemotherapy for sarcoma

    Energy Technology Data Exchange (ETDEWEB)

    Trout, Andrew T.; Sharp, Susan E.; Gelfand, Michael J. [Cincinnati Children' s Hospital Medical Center, Department of Radiology, Cincinnati, OH (United States); Turpin, Brian K. [Cincinnati Children' s Hospital Medical Center, Cancer and Blood Diseases Institute, Division of Oncology, Cincinnati, OH (United States); Zhang, Bin [Cincinnati Children' s Hospital Medical Center, Division of Biostatistics and Epidemiology, Cincinnati, OH (United States)

    2015-07-15

    Granulocyte colony-stimulating factors (G-CSF) speed recovery from chemotherapy-induced myelosuppression but the marrow stimulation they cause can interfere with interpretation of F-18 fluorodeoxyglucose positron emission tomography (F-18 FDG PET) exams. To assess the frequency of interfering G-CSF-induced bone marrow activity on FDG PET imaging in children and young adults with Ewing sarcoma and rhabdomyosarcoma and to define an interval between G-CSF administration and FDG PET imaging that limits marrow interference. Blinded, retrospective review of FDG PET exams performed in patients treated with long-acting G-CSF as part of their chemotherapeutic regimen. Exams were subjectively scored by two reviewers (R1 and R2) who assessed the level of marrow uptake of FDG and measured standardized uptake values in the marrow, liver, spleen and blood pool. FDG PET findings were correlated with time since G-CSF administration and with blood cell counts. Thirty-eight FDG PET exams performed in 17 patients were reviewed with 47.4% (18/38) of exams having marrow uptake of FDG sufficient to interfere with image interpretation. Primary predictors of marrow uptake of FDG were patient age (P = 0.0037) and time since G-CSF exposure (P = 0.0028 for subjective marrow uptake of FDG, P = 0.008 [R1] and P = 0.004 [R2] for measured maximum standardized uptake value (SUVmax)). The median interval between G-CSF administration and PET imaging in cases with marrow activity considered normal or not likely to interfere was 19.5 days (range: 7-55 days). In pediatric and young adult patients with Ewing sarcoma and rhabdomyosarcoma, an interval of 20 days between administration of the long-acting form of G-CSF and FDG PET imaging should limit interference by stimulated marrow. (orig.)

  12. Synthesis and pre-clinical evaluation of a new class of high-affinity {sup 18}F-labeled PSMA ligands for detection of prostate cancer by PET imaging

    Energy Technology Data Exchange (ETDEWEB)

    Kelly, James; Amor-Coarasa, Alejandro; Williams, Clarence; Ponnala, Shashikanth [Weill Cornell Medicine, Division of Radiopharmaceutical Sciences and Molecular Imaging Innovations Institute, Department of Radiology, New York, NY (United States); Nikolopoulou, Anastasia [Weill Cornell Medicine, Division of Radiopharmaceutical Sciences and Molecular Imaging Innovations Institute, Department of Radiology, New York, NY (United States); Weill Cornell Medicine, Citigroup Biomedical Imaging Center, New York, NY (United States); Kim, Dohyun [Weill Cornell Medicine, Citigroup Biomedical Imaging Center, New York, NY (United States); Babich, John W. [Weill Cornell Medicine, Division of Radiopharmaceutical Sciences and Molecular Imaging Innovations Institute, Department of Radiology, New York, NY (United States); Weill Cornell Medicine, Citigroup Biomedical Imaging Center, New York, NY (United States); Weill Cornell Medicine, Meyer Cancer Center, New York, NY (United States)

    2017-04-15

    Current clinical imaging of PSMA-positive prostate cancer by positron emission tomography (PET) mainly features {sup 68}Ga-labeled tracers, notably [{sup 68}Ga]Ga-PSMA-HBED-CC. The longer half-life of fluorine-18 offers significant advantages over Ga-68, clinically and logistically. We aimed to develop high-affinity PSMA inhibitors labeled with fluorine-18 as alternative tracers for prostate cancer. Six triazolylphenyl ureas and their alkyne precursors were synthesized from the Glu-urea-Lys PSMA binding moiety. PSMA affinity was determined in a competitive binding assay using LNCaP cells. The [{sup 18}F]triazoles were isolated following a Cu(I)-catalyzed click reaction between the alkynes and [{sup 18}F]fluoroethylazide. The {sup 18}F-labeled compounds were evaluated in nude mice bearing LNCaP tumors and compared to [{sup 68}Ga]Ga-PSMA-HBED-CC and [{sup 18}F]DCFPyL. Biodistribution studies of the two tracers with the highest imaged-derived tumor uptake and highest PSMA affinity were undertaken at 1 h, 2 h and 4 h post-injection (p.i.), and co-administration of PMPA was used to determine whether uptake was PSMA-specific. F-18-labeled triazolylphenyl ureas were prepared with a decay-corrected RCY of 20-40 %, >98 % radiochemical and chemical purity, and specific activity of up to 391 GBq/μmol. PSMA binding (IC{sub 50}) ranged from 3-36 nM. The position of the triazole influenced tumor uptake (3 > 4 > 2), and direct conjugation of the triazole with the phenylurea moiety was preferred to insertion of a spacer group. Image-derived tumor uptake ranged from 6-14 %ID/g at 2 h p.i., the time of maximum tumor uptake; uptake of [{sup 68}Ga]Ga-PSMA-HBED-CC and [{sup 18}F]DCFPyL was 5-6 %ID/g at 1-3 h p.i., the time of maximum tumor uptake. Biodistribution studies of the two most promising compounds gave maximum tumor uptakes of 10.9 ± 1.0 % and 14.3 ± 2.5 %ID/g, respectively, as compared to 6.27 ± 1.44 %ID/g for [{sup 68}Ga]Ga-PSMA-HBED-CC. Six [{sup 18}F

  13. Sustainability Labeling

    NARCIS (Netherlands)

    Dam, van Y.K.

    2017-01-01

    Sustainability labeling originated from a need to protect the identity of alternative systems of food production and to increase market transparency. From the 1980s onwards sustainability labeling has changed into a policy instrument replacing direct government regulation of the food market, and a

  14. Optimization of the synthesis of a high specific activity 125{sup I}-labelled hapten for radioimmunoassays; Optimizacion de un metodo de preparacion de un radiohapteno-125''I para ria de alta actividad especifica

    Energy Technology Data Exchange (ETDEWEB)

    Suraez, C.; Paz, D.; Simon, M. A.; Romero del Hombrebueno, B.

    1994-07-01

    In this first report it is described the synthesis, separation and purification of the 2-radioiodinated histamine- I-labelled histamine by a mixed anhydride reaction. About 75% incorporation of I{sup -}125, from Na{sup 1}25I, was achieved with a molecular ratio of 1:1 mixed anhydride:histamine. The radiochemical purity of the conjugate by TLC was > 99% and its theoretical specific activity, 3850 {mu}Ci/{mu}g. Dissolved in ethanol and held at -20 degree centigree under darkness decomposition on storage didn't exceed 1% per month. (Author) 13 refs.

  15. Stereoselective synthesis of (2S,3R)-α-hydroxy-β-amino acids (AHBAs): valinoctin A, (2S,3R)-3-amino-2-hydroxydecanoic acid, and a fluorescent-labeled (2S,3R)-AHBA.

    Science.gov (United States)

    Deshmukh, Sharad Chandrakant; Talukdar, Pinaki

    2014-11-21

    We report the stereoselective synthesis of an alkynyl side-chain containing (2S,3R)-α-hydroxy-β-amino acid ((2S,3R)-AHBA) analogues. The Cu(I)-catalyzed reactions of (R)-glyceraldehyde acetonide and dibenzylamine with terminal alkynes provided the corresponding (2S,3R)-α-amino alcohols with good-to-excellent diastereoselectivity. Subsequent chemical transformations provided easy access to the alkynyl side-chain containing (2S,3R)-AHBAs. The utility of the methodology was demonstrated by the stereoselective synthesis of valinoctin A and (2S,3R)-3-amino-2-hydroxydecanoic acid ((2S,3R)-AHDA). Photophysical properties and cell permeability of a pyrene-labeled (2S,3R)-AHBA were also determined.

  16. Discordant Findings of Skeletal Metastasis Between Tc99m MDP Bone Scans and F18 FDG PET/CT Imaging for Advanced Breast and Lung Cancers—Two Case Reports and Literature Review

    Directory of Open Access Journals (Sweden)

    Yu-Wen Chen

    2007-12-01

    Full Text Available Traditionally, Tc99m methyl diphosphate (MDP bone scintigraphy provides high-sensitivity detection of skeletal metastasis from breast and lung cancers in regular follow-up. Fluorodeoxyglucose (FDG positron emission tomography/computed tomography (PET/CT, based on the glucose metabolism of malignant cells, plays a role in describing rumor growth, proliferation of neoplasm and the extent of metastasis. In general, concordant findings of skeletal metastasis are seen on both types of image, especially in cases of breast and lung cancer. However, there were extremely discordant findings of skeletal metastasis between bone scans and F18 FDG PET/CT imaging in two cases among 300 consecutive F18 FDG PET/CT follow-up exams of patients with malignancies, during the past year, in our center. Both cases, one of breast cancer and one of lung cancer, had negative bone scintigraphic findings, but a diffusely high grade of F18 FDG avid marrow infiltration in the axial spine, leading to the diagnosis of stage IV disease in both cases. Owing to variant genetic aberrance of malignance, F18 FDG PET/CT reveals direct evidence of diffuse, rapid neoplasm metabolism in the bone marrow of the spine, but not of secondary osteoblastic reactions in vivo. F18 FDG PET/CT should always be employed in the follow-up of patients with malignancies.

  17. Brain metabolism in patients with vegetative state after post-resuscitated hypoxic-ischemic brain injury: statistical parametric mapping analysis of F-18 fluorodeoxyglucose positron emission tomography

    Institute of Scientific and Technical Information of China (English)

    Yong Wook Kim; Hyoung Seop Kim; Young-Sil An

    2013-01-01

    Background Hypoxic-ischemic brain injury (HIBI) after cardiopulmonary resuscitation is one of the most devastating neurological conditions that causing the impaired consciousness.However,there were few studies investigated the changes of brain metabolism in patients with vegetative state (VS) after post-resuscitated HIBI.This study aimed to analyze the change of overall brain metabolism and elucidated the brain area correlated with the level of consciousness (LOC) in patients with VS after post-resuscitated HIBI.Methods We consecutively enrolled 17 patients with VS after HIBI,who experienced cardiopulmonary resuscitation.Overall brain metabolism was measured by F-18 fluorodeoxyglucose positron emission tomography (F-18 FDG PET) and we compared regional brain metabolic patterns from t7 patients with those from 15 normal controls using voxel-by-voxel based statistical parametric mapping analysis.Additionally,we correlated the LOC measured by the JFK-coma recovery scale-revised of each patient with brain metabolism by covariance analysis.Results Compared with normal controls,the patients with VS after post-resuscitated HIBI revealed significantly decreased brain metabolism in bilateral precuneus,bilateral posterior cingulate gyrus,bilateral middle frontal gyri,bilateral superior parietal gyri,bilateral middle occipital gyri,bilateral precentral gyri (PFEw correctecd <0.0001),and increased brain metabolism in bilateral insula,bilateral cerebella,and the brainstem (PFEw correctecd <0.0001).In covariance analysis,the LOC was significantly correlated with brain metabolism in bilateral fusiform and superior temporal gyri (P uncorrected <0.005).Conclusions Our study demonstrated that the precuneus,the posterior cingulate area and the frontoparietal cortex,which is a component of neural correlate for consciousness,may be relevant structure for impaired consciousness in patient with VS after post-resuscitated HIBI.In post-resuscitated HIBI,measurement of brain

  18. Characteristics of Metastatic Mediastinal Lymph Nodes of Non-Small Cell Lung Cancer on Preoperative F-18 FDG PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Ah Young; Choi, Su Jung; Jung, Kyung Pyo; Park, Ji Sun; Lee, Seok Mo; Bae, Sang Kyun [Inje Univ. College of Medicine, Gimhae (Korea, Republic of)

    2014-03-15

    The aim of this study was to evaluate the characteristics of PET and CT features of mediastinal metastatic lymph nodes on F-18 FDG PET/CT and to determine the diagnostic criteria in nodal staging of non-small cell lung cancer. One hundred four non-small cell lung cancer patients who had preoperative F-18 FDG PET/CT were included. For quantitative analysis, the maximum SUV of the primary tumor, maximum SUV of the lymph nodes (SUVmax), size of the lymph nodes, and average Hounsfield units (aHUs) and maximum Hounsfield units (mHUs) of the lymph nodes were measured. The SUVmax, SUV ratio of the lymph node to blood pool (LN SUV/blood pool SUV), SUV ratio of the lymph node to primary tumor (LN SUV/primary tumor SUV), size, aHU, and mHU were compared between the benign and malignant lymph nodes. Among 372 dissected lymph node stations that were pathologically diagnosed after surgery, 49 node stations were malignant and 323 node stations benign. SUVmax, LN SUV/blood pool SUV, and size were significantly different between the malignant and benign lymph node stations (P <0.0001). However, there was no significant difference in LN SUV/primary tumor SUV (P =0.18), mHU (P =0.42), and aHU (P =0.98). Using receiver-operating characteristic curve analyses, there was no significant difference among these three variables (SUVmax, LN SUV/blood pool SUV, and size). The optimal cutoff values were 2.9 for SUVmax, 1.4 for LN SUV/blood pool SUV, and 5 mm for size. When the cutoff value of SUVmax≥2.9 and size≥5 mm were used in combination, the positive predictive value was 44.2%, and the negative predictive value was 90.9 %. When we evaluated the results based on the histology of the primary tumor, the negative predictive value was 92.3 % in adenocarcinoma (cutoff values of SUVmax≥2.3 and size≥5 mm) and 97.2 % in squamous cell carcinoma (cutoff values of SUVmax≥3.6 and size≥8 mm), separately. In the lymph node staging of non-small cell lung cancer, SUVmax, LN SUV/blood pool SUV

  19. Synthesis of aromatic (13)C/(2)H-α-ketoacid precursors to be used in selective phenylalanine and tyrosine protein labelling.

    Science.gov (United States)

    Lichtenecker, R J

    2014-10-14

    Recent progress in protein NMR spectroscopy revealed aromatic residues to be valuable information sources for performing structure and motion analysis of high molecular weight proteins. However, the applied NMR experiments require tailored isotope labelling patterns in order to regulate spin-relaxation pathways and optimize magnetization transfer. We introduced a methodology to use α-ketoacids as metabolic amino acid precursors in cell-based overexpression of phenylalanine and/or tyrosine labelled proteins in a recent publication, which we have now developed further by providing synthetic routes to access the corresponding side-chain labelled precursors. The target compounds allow for selective introduction of (13)C-(1)H spin systems in a highly deuterated chemical environment and feature alternating (12)C-(13)C-(12)C ring-patterns. The resulting isotope distribution is especially suited to render straightforward (13)C spin relaxation experiments possible, which provide insight into the dynamic properties of the corresponding labelled proteins.

  20. Flight-Determined Subsonic Longitudinal Stability and Control Derivatives of the F-18 High Angle of Attack Research Vehicle (HARV) with Thrust Vectoring

    Science.gov (United States)

    Iliff, Kenneth W.; Wang, Kon-Sheng Charles

    1997-01-01

    The subsonic longitudinal stability and control derivatives of the F-18 High Angle of Attack Research Vehicle (HARV) are extracted from dynamic flight data using a maximum likelihood parameter identification technique. The technique uses the linearized aircraft equations of motion in their continuous/discrete form and accounts for state and measurement noise as well as thrust-vectoring effects. State noise is used to model the uncommanded forcing function caused by unsteady aerodynamics over the aircraft, particularly at high angles of attack. Thrust vectoring was implemented using electrohydraulically-actuated nozzle postexit vanes and a specialized research flight control system. During maneuvers, a control system feature provided independent aerodynamic control surface inputs and independent thrust-vectoring vane inputs, thereby eliminating correlations between the aircraft states and controls. Substantial variations in control excitation and dynamic response were exhibited for maneuvers conducted at different angles of attack. Opposing vane interactions caused most thrust-vectoring inputs to experience some exhaust plume interference and thus reduced effectiveness. The estimated stability and control derivatives are plotted, and a discussion relates them to predicted values and maneuver quality.

  1. Three-dimensional texture analysis of contrast enhanced CT images for treatment response assessment in Hodgkin lymphoma: Comparison with F-18-FDG PET

    Energy Technology Data Exchange (ETDEWEB)

    Knogler, Thomas; El-Rabadi, Karem; Weber, Michael; Karanikas, Georgios; Mayerhoefer, Marius E., E-mail: marius.mayerhoefer@meduniwien.ac.at [Department of Biomedical Imaging and Image-guided Therapy, Medical University of Vienna, Waehringer Guertel 18-20, Vienna 1090 (Austria)

    2014-12-15

    Purpose: To determine the diagnostic performance of three-dimensional (3D) texture analysis (TA) of contrast-enhanced computed tomography (CE-CT) images for treatment response assessment in patients with Hodgkin lymphoma (HL), compared with F-18-fludeoxyglucose (FDG) positron emission tomography/CT. Methods: 3D TA of 48 lymph nodes in 29 patients was performed on venous-phase CE-CT images before and after chemotherapy. All lymph nodes showed pathologically elevated FDG uptake at baseline. A stepwise logistic regression with forward selection was performed to identify classic CT parameters and texture features (TF) that enable the separation of complete response (CR) and persistent disease. Results: The TF fraction of image in runs, calculated for the 45° direction, was able to correctly identify CR with an accuracy of 75%, a sensitivity of 79.3%, and a specificity of 68.4%. Classical CT features achieved an accuracy of 75%, a sensitivity of 86.2%, and a specificity of 57.9%, whereas the combination of TF and CT imaging achieved an accuracy of 83.3%, a sensitivity of 86.2%, and a specificity of 78.9%. Conclusions: 3D TA of CE-CT images is potentially useful to identify nodal residual disease in HL, with a performance comparable to that of classical CT parameters. Best results are achieved when TA and classical CT features are combined.

  2. The use of quantitative PCR for identification and quantification of Brachyspira pilosicoli, Lawsonia intracellularis and Escherichia coli fimbrial types F4 and F18 in pig feces

    DEFF Research Database (Denmark)

    Ståhl, Marie; Kokotovic, Branko; Hjulsager, Charlotte Kristiane

    2011-01-01

    than the earlier used method due to improvements in DNA extraction. In addition, as samples were not analysed for all four pathogen agents by traditional diagnostic methods, many samples were found positive for agents that were not expected on the basis of age and case history. The use of quantitative...... the spiking experiments were 102 bacteria/g feces for BpiloqPCR and Laws-qPCR, 103 CFU/g feces for F4-qPCR and F18-qPCR. The PCR efficiency for all four qPCR assays was between 0.91 and 1.01 with R2 above 0.993. Standard curves, slopes and elevation, varied between assays and between measurements from pure...... DNA from reference strains and feces spiked with the respective strains. The linear ranges found for spiked fecal samples differed both from the linear ranges from pure culture of the reference strains and between the qPCR tests. The linear ranges were five log units for F4- qPCR, and Laws-qPCR, six...

  3. Diffuse Hypermetabolism at Bone Marrow in F-18 FDG PET/CT: Correlation with Bone Marrow Biopsy and Complete Blood Cell Counts

    Energy Technology Data Exchange (ETDEWEB)

    Kang, Yun Hee; Lim, Seok Tae; Jeong, Young Jin; Kim, Dong Wook; Jeong, Hwan Jeong; Sohn, Myung Hee [Chonbuk National University Medical School, Jeonju (Korea, Republic of)

    2009-02-15

    Increased FDG uptake in the bone marrow has been reported in patients taking erythropoietin or granulocyte-colony stimulating factor (G-CSF). The aim of this study is to investigate the correlation between F-18 FDG uptake in the bone marrow and bone marrow finding, hematological parameters. Twenty patients who had diffuse FDG uptake at the bone marrow and received hematological examinations, bone marrow biopsy within 10 days before or after PET/CT were enrolled in this study. Among them, 11 patients were excluded; 4 patients received G-CSF or erythropoietin before PET/CT. Seven patients showed definite pathology in a bone marrow biopsy. The parameters included the measurement of WBC, hemoglobin, platelet and cellularity of the bone marrow. Bone marrow FDG uptake was correlated with a low hemoglobin but not WBC, platelet. Histopathologic findings in marrow biopsies were various: normal finding (n=3), hyperplasia of granulocytic cells (n=2), eosinophilic hyperplasia (n=1), reactive lymphoid nodules (n=1), hypercelluar marrow (n=1), hypocelluar marrow (n=1). All patients except two, showed normal marrow celluarity. FDG uptake by bone marrow correlated with anemia but not WBC, platelet, bone marrow cellularity.

  4. Predictive Role of Functional Visceral Fat Activity Assessed by Preoperative F-18 FDG PET/CT for Regional Lymph Node or Distant Metastasis in Patients with Colorectal Cancer.

    Directory of Open Access Journals (Sweden)

    Kisoo Pahk

    Full Text Available To investigate the role of functional visceral fat activity assessed by preoperative F-18 fluorodeoxyglucose positron emission tomography/computed tomography (18F-FDG PET/CT in colorectal cancer (CRC for predicting regional lymph node (LN or distant metastasis.We evaluated 131 patients with newly diagnosed CRC. They all underwent pre-operative 18F-FDG PET/CT and surgery. Functional fat activity was measured by maximum standardized uptake value (SUVmax using 18F-FDG PET/CT. Functional visceral fat activity was measured by SUVmax of visceral fat/SUVmax of subcutaneous fat (V/S ratio. Mann-Whitney U test, χ2 test, Fisher's exact test, receiver-operating characteristic (ROC analysis, Spearrman's correlation coefficient, and uni- and multivariate logistic regression statistical analyses were done.Patients with higher V/S ratio displayed a significantly higher rate of regional LN (p = 0.004 and distant metastasis (p<0.001. In addition, V/S ratio was the only factor that was significantly associated with distant metastasis. An optimal cut-off V/S ratio of 1.88 was proposed for predicting distant metastasis with a sensitivity of 84.6% and specificity of 78.8% (area under the curve: 0.86; p<0.0001.Functional visceral fat activity is significantly associated with distant metastasis in CRC patients. Furthermore, V/S ratio can be useful as a complementary factor in predicting distant metastasis.

  5. Volume-Based F-18 FDG PET/CT Imaging Markers Provide Supplemental Prognostic Information to Histologic Grading in Patients With High-Grade Bone or Soft Tissue Sarcoma

    DEFF Research Database (Denmark)

    Andersen, Kim Francis; Fuglo, Hanna Maria; Rasmussen, Sine Hvid;

    2015-01-01

    The aim of the study is to assess the prognostic value of different volume-based calculations of tumor metabolic activity in the initial assessment of patients with high-grade bone sarcomas (BS) and soft tissue sarcomas (STS) using F-18 FDG PET/CT.A single-site, retrospective study from 2002...... to 2012 including 92 patients with histologically verified high-grade BS (N = 37) or STS (N = 55). All patients underwent a pretreatment F-18 FDG PET/CT scan. Clinical data were registered. Measurements of the accuracy of metabolic tumor volume with a preset threshold of 40% of the maximum standardized.......05, HR 3.37 [95% CI 1.02-11.11]). No significant results were demonstrated for MTV40%.Volume-based F-18 FDG PET/CT imaging markers in terms of pretreatment estimation of TLG provide supplemental prognostic information to histologic grading, with significant independent properties for prediction...

  6. Low molecular weight poly (2-dimethylamino ethylmethacrylate) polymers with controlled.positioned fluorescent labeling: Synthesis, characterization and in vitro interaction with human endothelial cells

    DEFF Research Database (Denmark)

    Flebus, Luca; Lombart, Francois; Sevrin, Chantal

    2015-01-01

    ) fluorescent labeled PDMAEMA of low molecular weight (Mw) (below 15 kDa), controlling the position and density of fluorescein.The second goal was to analyze the possible difference in uptake and subcellular distribution of this labeled FF polycation between human umbilical vein endothelial cells (HUVEC) and h...... to a minor cytotoxicity compared to the higher ones.As main conclusion this study highlights the similitude in cell trafficking of FF PDMAEMA and data previously reported for PDMAEMA/DNA complexes....

  7. Flow cytometric measurement of RNA synthesis based on bromouridine labelling and combined with measurement of DNA content or cell surface antigen

    DEFF Research Database (Denmark)

    Jensen, P O; Larsen, J; Larsen, J K

    1993-01-01

    that RNA synthesis increased within the first 24 hours of phytohemagglutinin (PHA) stimulation, reaching a maximum at 48 hours, when cells had entered the cell cycle. Using a new method for flow cytometric dual parameter analysis of BrUrd incorporation and a cell surface antigen, spontaneous RNA synthesis...

  8. Toward a biorelevant structure of protein kinase C bound modulators: design, synthesis, and evaluation of labeled bryostatin analogues for analysis with rotational echo double resonance NMR spectroscopy.

    Science.gov (United States)

    Loy, Brian A; Lesser, Adam B; Staveness, Daryl; Billingsley, Kelvin L; Cegelski, Lynette; Wender, Paul A

    2015-03-18

    Protein kinase C (PKC) modulators are currently of great importance in preclinical and clinical studies directed at cancer, immunotherapy, HIV eradication, and Alzheimer's disease. However, the bound conformation of PKC modulators in a membrane environment is not known. Rotational echo double resonance (REDOR) NMR spectroscopy could uniquely address this challenge. However, REDOR NMR requires strategically labeled, high affinity ligands to determine interlabel distances from which the conformation of the bound ligand in the PKC-ligand complex could be identified. Here we report the first computer-guided design and syntheses of three bryostatin analogues strategically labeled for REDOR NMR analysis. Extensive computer analyses of energetically accessible analogue conformations suggested preferred labeling sites for the identification of the PKC-bound conformers. Significantly, three labeled analogues were synthesized, and, as required for REDOR analysis, all proved highly potent with PKC affinities (∼1 nM) on par with bryostatin. These potent and strategically labeled bryostatin analogues are new structural leads and provide the necessary starting point for projected efforts to determine the PKC-bound conformation of such analogues in a membrane environment, as needed to design new PKC modulators and understand PKC-ligand-membrane structure and dynamics.

  9. Synthesis and application of a N-1' fluorescent biotinyl derivative inducing the specific carboxy-terminal dual labeling of a novel RhoB-selective scFv.

    Science.gov (United States)

    Chaisemartin, L; Chinestra, P; Favre, G; Blonski, C; Faye, J C

    2009-05-20

    The fluorescent site-specific labeling of protein would provide a new, easy-to-use alternative to biochemical and immunochemical methods. We used an intein-mediated strategy for covalent labeling of the carboxy-terminal amino acid of a RhoB-selective scFv previously isolated from a phage display library (a human synthetic V(H) + V(L) scFv phage library). The scFv fused to the Mxe intein was produced in E. coli and purified and was then labeled with a newly synthesized fluorescent biotinyl cysteine derivative capable of inducing scFv-Mxe intein splicing. In this study, we investigated the splicing and labeling properties of various amino acids in the hinge domain between scFv and Mxe under thiol activation. In this dual labeling system, the fluorescein is used for antibody detection and biotin is used for purification, resulting in a high specific activity for fluorescence. We then checked that the purified biotinylated fluorescent scFv retained its selectivity for RhoB without modification of its affinity.

  10. C11-acetate and F-18 FDG PET for men with prostate cancer bone metastases: relative findings and response to therapy.

    Science.gov (United States)

    Yu, Evan Y; Muzi, Mark; Hackenbracht, Joy A; Rezvani, Brian B; Link, Jeanne M; Montgomery, Robert Bruce; Higano, Celestia S; Eary, Janet F; Mankoff, David A

    2011-03-01

    This study tested the feasibility of C11-acetate (acetate) positron emission tomography (PET) imaging to assess response to therapy in men with bone metastatic prostate cancer and compared results for disease detection and response evaluation with F-18 fluorodeoxyglucose (FDG) PET. Men with ≥3 prostate cancer bone metastases identified by Tc-99m methylene diphosphonate (MDP) bone scintigraphy and/or computed tomography were enrolled in a prospective study of serial acetate and FDG PET imaging. Patients were imaged before and 6 to 12 weeks after initial androgen deprivation therapy for new metastatic prostate cancer or first-line chemotherapy with docetaxel for castration-resistant prostate cancer. Qualitative assessment and changes in the tumor:normal uptake ratio were used to assess response by both acetate and FDG PET. In addition, the detection of bone metastases pretherapy was compared for acetate and FDG PET. A total of 8 patients with documented bone metastases were imaged, of which 6 were imaged both pre- and post-therapy. Acetate PET detected bone metastases in all 8 patients, whereas FDG PET detected lesions in 6 of the 7 imaged patients. Acetate PET generally detected more metastases with a higher tumor:normal uptake ratio. Qualitative and quantitative assessments of post-treatment response correlated with composite clinical designations of response, stable disease, or progression in 6 of 6 and 5 of 6 by acetate and 4 of 5 and 3 of 5 by FDG PET, respectively. In this pilot study, results indicate that acetate PET holds promise for response assessment of prostate cancer bone metastases and is complementary to FDG PET in bone metastasis detection.

  11. Is [F-18]-fluorodeoxyglucose FDG-PET/CT better than CT alone for the preoperative lymph node staging of muscle invasive bladder cancer?

    Energy Technology Data Exchange (ETDEWEB)

    Uttam, Mete; Pravin, Nayak; Anish, Bhattacharya; Nandita, Kakkar; Arup, Mandal, E-mail: uttam_mete@yahoo.com [PGIMER, Chandigarh, (India)

    2016-03-15

    Objective: To evaluate whether the use of [F-18]-FDG-PET/CT can accurately predict pelvic lymph node metastasis in patients with muscle invasive TCC of the bladder undergoing radical cystectomy. Materials and methods: Fifteen patients with muscle invasive bladder cancer had undergone FDG-PET/CT scan from the skull base to the mid-thighs after IV injection of 6.5MBq (Mega-Becquerel)/Kg of FDG. After intravenous hydration IV furosemide was given to overcome the difficulties posed by urinary excretion of {sup 18}F-FDG. PET/ CT data were analyzed as PET and CT images studied separately as well as fused PET/ CT images. The imaging findings were correlated with the histopathology of the nodes (gold standard). Results: CT and FDG-PET had demonstrated positive lymph nodes in 9 & 8 patients respectively. Among the 15 patients 3 had documented metastasis on histopathology. Both CT and PET could detect the nodes in all these 3 patients (100% sensitivity). Nodes were histologically negative amongst 6&5 patients who had node involvement by CT and PET respectively. Therefore, specificity, positive predictive value (PPV) & negative predictive value (NPV) for CT and PET/CT were 50%, 33.3%, 100% and 58.3%, 37.5%, 100% respectively. Conclusion: The theoretical advantage of this cutting edge technology for whole body imaging has not been translated into clinical practice as we found minimal advantage of combined FDG-PET/CT over CT alone for nodal staging of muscle invasive bladder cancer. This may be due to substantial overlap between standardized uptake values (SUVs) from active inflammatory processes with those of malignant lesion. (author)

  12. Multiphase CT scanning and different intravenous contrast media concentrations in combined F-18-FDG PET/CT: Effect on quantitative and clinical assessment

    Energy Technology Data Exchange (ETDEWEB)

    Rebiere, Marilou, E-mail: Marilou.Rebiere@rwth-aachen.de [Department of Nuclear Medicine, University Hospital RWTH Aachen, Pauwelsstrasse 30, 52057 Aachen (Germany); Verburg, Frederik A., E-mail: fverburg@ukaachen.de [Department of Nuclear Medicine, University Hospital RWTH Aachen, Pauwelsstrasse 30, 52057 Aachen (Germany); Department of Nuclear Medicine, Maastricht University Medical Center, P. Debeylaan 25, 6202 AZ Maastricht (Netherlands); Palmowski, Moritz, E-mail: mpalmowski@ukaachen.de [Department of Nuclear Medicine, University Hospital RWTH Aachen, Pauwelsstrasse 30, 52057 Aachen (Germany); Department of Radiology, University Hospital RWTH Aachen, Pauwelsstrasse 30, 52057 Aachen (Germany); Department of Experimental Molecular Imaging, University Hospital RWTH Aachen, Pauwelsstrasse 30, 52057 Aachen (Germany); Krohn, Thomas, E-mail: tkrohn@ukaachen.de [Department of Nuclear Medicine, University Hospital RWTH Aachen, Pauwelsstrasse 30, 52057 Aachen (Germany); Pietsch, Hubertus, E-mail: hubertus.pietsch@bayer.com [Contrast Media Research, Bayer Pharma AG, Muellerstr. 178, 13353 Berlin (Germany); Kuhl, Christiane K., E-mail: ckuhl@ukaachen.de [Department of Radiology, University Hospital RWTH Aachen, Pauwelsstrasse 30, 52057 Aachen (Germany); Mottaghy, Felix M., E-mail: fmottaghy@ukaachen.de [Department of Nuclear Medicine, University Hospital RWTH Aachen, Pauwelsstrasse 30, 52057 Aachen (Germany); Department of Nuclear Medicine, Maastricht University Medical Center, P. Debeylaan 25, 6202 AZ Maastricht (Netherlands); Behrendt, Florian F., E-mail: fbehrendt@ukaachen.de [Department of Nuclear Medicine, University Hospital RWTH Aachen, Pauwelsstrasse 30, 52057 Aachen (Germany)

    2012-08-15

    Purpose: To evaluate the influence of multiphase CT scanning and different intravenous contrast media on contrast enhancement, attenuation correction and image quality in combined PET/CT. Material and methods: 140 patients were prospectively enrolled for F-18-FDG-PET/CT including a low-dose unenhanced, arterial and venous contrast enhanced CT. The first (second) 70 patients, received contrast medium with 370 (300) mg iodine/ml. The iodine delivery rate (1.3 mg/s) and total iodine load (44.4 g) were identical for both groups. Contrast enhancement and maximum and mean standardized FDG uptake values (SUVmax and SUVmean) were determined for the un-enhanced, arterial and venous PET/CT at multiple anatomic sites and PET reconstructions were visually evaluated. Results: Arterial contrast enhancement was significantly higher for the 300 mg/ml contrast medium compared to 370 mg I/ml at all anatomic sites. Venous enhancement was not different between the two contrast media. SUVmean and SUVmax were significantly higher for the contrast enhanced compared to the non-enhanced PET/CT at all anatomic sites (all P < 0.001). Tracer uptake was significantly higher in the arterial than in the venous PET/CT in the arteries using both contrast media (all P < 0.001). No differences in tracer uptake were found between the contrast media (all P > 0.05). Visual assessment revealed no relevant differences between the different PET reconstructions. Conclusions: There is no relevant qualitative influence on the PET scan from the use of different intravenous contrast media in its various phases in combined multiphase PET/CT. For quantitative analysis of tracer uptake it is required to use an identical PET/CT protocol.

  13. [F-18]2-fluoro-2-deoxyglucose (FDG) positron emission tomography after limb salvage surgery: post-surgical appearance, attenuation correction and local complications

    Energy Technology Data Exchange (ETDEWEB)

    Gelfand, Michael J.; Sharp, Susan E. [Cincinnati Children' s Hospital Medical Center, Department of Radiology, Nuclear Medicine Division, Cincinnati, OH (United States)

    2015-08-15

    Metal endoprostheses and internal fixation devices cause significant artifacts on CT after limb salvage surgery; positron emission tomography (PET) images should be evaluated for artifacts. (1) To describe [F-18]2-fluoro-2-deoxyglucose (FDG) PET uptake patterns after limb salvage surgery. (2) To determine whether metal endoprostheses and fixation hardware cause significant artifacts on CT attenuation-corrected PET that interfere with diagnostic use of PET/CT after limb salvage surgery. We reviewed 92 studies from 18 patients ages 5-21 years. Diagnoses were osteogenic sarcoma in 14, Ewing sarcoma in 3, and malignant peripheral nerve sheath tumor originating in bone in 1. Nine patients had distal femur/knee endoprostheses, five had lower-extremity bone allografts secured by large metal plates and four had upper-extremity limb salvage procedures. Maximum standardized uptake value was calculated at lower-extremity soft-tissue-endoprosthesis interfaces. In 15 patients with PET/CT imaging, the first PET/CT scan after limb salvage surgery was reviewed for metal artifacts on CT images and for artifacts at locations on PET corresponding to the CT metal artifacts. Increased FDG uptake was consistently present at soft-tissue interfaces with endoprostheses, allografts and internal fixation devices, with little or no FDG uptake at cemented endoprosthesis-bone interfaces. Maximum standardized uptake value at margins of femur/knee endoprostheses ranged from 1.4 to 5.7. In four patients with distal femur/knee endoprostheses, minimal artifact was noted on attenuation-corrected PET images, but image interpretation was not affected. In the other 11 patients who had CT attenuation correction, we detected no artifacts caused by the attenuation correction. CT attenuation correction did not cause artifacts that affected interpretation of attenuation-corrected PET images. (orig.)

  14. Synthesis of a Potent Aminopyridine-Based nNOS-Inhibitor by Two Recent No-Carrier-Added (18)F-Labelling Methods.

    Science.gov (United States)

    Drerup, Christian; Ermert, Johannes; Coenen, Heinz H

    2016-09-01

    Nitric oxide (NO), an important multifunctional signaling molecule, is produced by three isoforms of NO-synthase (NOS) and has been associated with neurodegenerative disorders. Selective inhibitors of the subtypes iNOS (inducible) or nNOS (neuronal) are of great interest for decoding neurodestructive key factors, and (18)F-labelled analogues would allow investigating the NOS-function by molecular imaging with positron emission tomography. Especially, the highly selective nNOS inhibitor 6-((3-((3-fluorophenethylamino)methyl)phenoxy)methyl)-4-methylpyridin-2-amine (10) lends itself as suitable compound to be (18)F-labelled in no-carrier-added (n.c.a.) form. For preparation of the (18)F-labelled nNOS-Inhibitor [(18)F]10 a "build-up" radiosynthesis was developed based on a corresponding iodonium ylide as labelling precursor. The such activated phenethyl group of the compound was efficiently and regioselectively labelled with n.c.a. [(18)F]fluoride in 79% radiochemical yield (RCY). After conversion by reductive amination and microwave assisted displacement of the protecting groups, the desired nNOS-inhibitor was obtained in about 15% total RCY. Alternatively, for a simplified "late-stage" (18)F-labelling procedure a corresponding boronic ester precursor was synthesized and successfully used in a newer, copper(II) mediated n.c.a. (18)F-fluoro-deboroniation reaction, achieving the same total RCY. Thus, both methods proved comparatively suited to provide the highly selective NOS-inhibitor [(18)F]10 as probe for preclinical in vivo studies.

  15. Enabling minimal invasive parathyroidectomy for patients with primary hyperparathyroidism using Tc-99m-sestamibi SPECT-CT, ultrasound and first results of F-18-fluorocholine PET-CT

    NARCIS (Netherlands)

    Kluijfhout, Wouter P.; Vorselaars, WM; Vriens, Menno R.; Borel Rinkes, IHM; Valk, GD; de Keizer, B

    Objective: Assessment of the diagnostic value of ultrasound (US), single photon-emission computed tomography-computed tomography (SPECT-CT) and F-18-fluorocholine (FCH) PET-CT for preoperative localization of hyper-functioning parathyroid(s) in order to create a more efficient diagnostic pathway and

  16. Synthesis, biodistribution and effects of farnesyltransferase inhibitor therapy on tumour uptake in mice of 99mTc labelled epidermal growth factor.

    NARCIS (Netherlands)

    Cornelissen, B.; Kersemans, V.; Burvenich, I.; Oltenfreiter, R.; Heyden, J.L. van der; Boerman, O.C.; Wiele, C. van de; Slegers, G.

    2005-01-01

    OBJECTIVE: The goal of this study was to develop a 99mTc labelled human epidermal growth factor (hEGF) for the in-vivo prediction of cancer cell response to farnesyltransferase inhibitor (FTI) therapy. This is based on the observation that internalization of EGF receptors is inhibited by FTIs. METHO

  17. Synthesis of deuterium-labelled peptido-aminobenzophenone (4-chloro-2-(2'-chlorobenzoyl)-N-(glycylglycyl)-N-methyl-anilide) and its metabolites

    Energy Technology Data Exchange (ETDEWEB)

    Hashimoto, S.; Takahashi, S. (Shionogi and Co. Ltd., Osaka (Japan). Research Lab.)

    1982-07-01

    Deuterium-labelled peptido-aminobenzophenone (4-chloro-2-(2'-chlorobenzoyl)-N-(glycylglycl)-N-methylanilide, 1) and its benzodiazepine-metabolites were prepared for use as internal standards in the quantification of the peptido-aminobenzophenone, chlorodiazepam, lormetazepam, chlorodesmethyldiazepam, and lorazepam at low levels in human plasma by selected ion monitoring.

  18. Synthesis and positron emission tomography studies of C-11 labeled isotopomers and metabolites of GTS-21, a partial α7 nicotinic cholinergic agonist drug

    Science.gov (United States)

    Kim, Sung Won; Ding, Yu-Shin; Alexoff, David; Patel, Vinal; Logan, Jean; Lin, Kuo-Shyan; Shea, Colleen; Muench, Lisa; Xu, Youwen; Carter, Pauline; King, Payton; Constanzo, Jasmine R.; Ciaccio, James A.; Fowler, Joanna S.

    2009-01-01

    Introduction GTS-21 ((3E)-3-[(2,4-dimethoxyphenyl)methylene]-3,4,5,6-tetrahydro-2,3′-bipyridine), a partial α7 nicotinic acetylcholine receptor agonist drug, has recently been shown to improve cognition in schizophrenia and Alzheimer’s disease. One of its two major demethylated metabolites, 4-OH-GTS-21, has been suggested to contribute to its therapeutic effects. Methods We labeled GTS-21 in two different positions with carbon-11 ([2-methoxy-11C]GTS-21 and [4-methoxy-11C]GTS-21) along with two corresponding demethylated metabolites ([2-methoxy-11C]4-OH-GTS-21 and [4-methoxy-11C]2-OH-GTS-21) for pharmacokinetic studies in baboons and mice with PET. Results Both [2-methoxy-11C]GTS-21 and [4-methoxy-11C]GTS-21 showed similar initial high rapid uptake in baboon brain, peaking from 1–3.5 min (0.027–0.038 %ID/cc) followed by rapid clearance (t1/2 <15 min), resulting in low brain retention by 30 min. However, after 30 min, [2-methoxy-11C]GTS-21 continued to clear while [4-methoxy-11C]GTS-21 plateaued, suggesting the entry of a labeled metabolite into the brain. Comparison of the pharmacokinetics of the two labeled metabolites confirmed expected higher brain uptake and retention of [4-methoxy-11C]2-OH-GTS-21 (the labeled metabolite of [4-methoxy-11C]GTS-21) relative to [2-methoxy-11C]4-OH-GTS-21 (the labeled metabolite of [2-methoxy-11C]GTS-21) which had negligible brain uptake. Ex vivo studies in mice showed that GTS-21 is the major chemical form in the mouse brain. Whole body dynamic PET imaging in baboon and mouse showed that the major route of excretion of C-11 is through the gallbladder. Conclusions The major findings are (1) extremely rapid uptake and clearance of [2-methoxy-11C]GTS-21 from the brain which may need to be considered in developing optimal dosing of GTS-21 for patients, and (2) significant brain uptake of 2-OH-GTS-21, suggesting that it might contribute to the therapeutic effects of GTS-21. This study illustrates the value of comparing

  19. Synthesis and positron emission tomography studies of C-11-labeled isotopomers and metabolites of GTS-21, a partial {alpha}7 nicotinic cholinergic agonist drug

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Sung Won [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States) and Department of Chemistry, State University of New York at Stony Brook, Stony Brook, NY 11794-3400 (United States)]. E-mail: swkim@bnl.gov; Ding Yushin [Department of Chemistry, State University of New York at Stony Brook, Stony Brook, NY 11794-3400 (United States); Department of Radiology, Yale University School of Medicine, New Haven, CT 06520-8048 (United States); Alexoff, David [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Patel, Vinal [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Logan, Jean [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Lin, K.-S. [Department of Radiology, University of Pittsburgh, Pittsburgh, PA 15213 (United States); Shea, Colleen [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Muench, Lisa [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Xu Youwen [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Carter, Pauline [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); King, Payton [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Constanzo, Jasmine R. [Department of Chemistry, Fordham University, Bronx, NY 10458 (United States); Ciaccio, James A. [Department of Chemistry, Fordham University, Bronx, NY 10458 (United States); Fowler, Joanna S. [Medical Department, Brookhaven National Laboratory, Upton, NY 11973 (United States); Department of Chemistry, State University of New York at Stony Brook, Stony Brook, NY 11794-3400 (United States); Department of Psychiatry, Mount Sinai School of Medicine, New York, NY 10029 (United States)

    2007-07-15

    Introduction: (3E)-3-[(2,4-dimethoxyphenyl)methylene]-3,4,5,6-tetrahydro-2,3'-bipyridine (GTS-21), a partial {alpha}7 nicotinic acetylcholine receptor agonist drug, has recently been shown to improve cognition in schizophrenia and Alzheimer's disease. One of its two major demethylated metabolites, 4-OH-GTS-21, has been suggested to contribute to its therapeutic effects. Methods: We labeled GTS-21 in two different positions with carbon-11 ([2-methoxy-{sup 11}C]GTS-21 and [4-{sup 11}C]GTS-21) along with two corresponding demethylated metabolites ([2-methoxy-{sup 11}C]4-OH-GTS-21 and [4-methoxy-{sup 11}C]2-OH-GTS-21) for pharmacokinetic studies in baboons and mice with positron emission tomography (PET). Results: Both [2-{sup 11}C]GTS-21 and [4-methoxy-{sup 11}C]GTS-21 showed similar initial high rapid uptake in baboon brain, peaking from 1 to 3.5 min (0.027-0.038%ID/cc) followed by rapid clearance (t {sub 1/2}<15 min), resulting in low brain retention by 30 min. However, after 30 min, [2-methoxy-{sup 11}C]GTS-21 continued to clear while [4-methoxy-{sup 11}C]GTS-21 plateaued, suggesting the entry of a labeled metabolite into the brain. Comparison of the pharmacokinetics of the two labeled metabolites confirmed expected higher brain uptake and retention of [4-methoxy-{sup 11}C]2-OH-GTS-21 (the labeled metabolite of [4-methoxy-{sup 11}C]GTS-21) relative to [2-methoxy-{sup 11}C]4-OH-GTS-21 (the labeled metabolite of [2-methoxy-{sup 11}C]GTS-21), which had negligible brain uptake. Ex vivo studies in mice showed that GTS-21 is the major chemical form in the mouse brain. Whole-body dynamic PET imaging in baboon and mouse showed that the major route of excretion of C-11 is through the gallbladder. Conclusions: The major findings are as follows: (a) extremely rapid uptake and clearance of [2-methoxy-{sup 11}C]GTS-21 from the brain, which may need to be considered in developing optimal dosing of GTS-21 for patients, and (b) significant brain uptake of 2-OH-GTS-21

  20. Stereoselective synthesis of stable isotope labeled L-[alpha]-amino acids: synthesis of L-[4-[sup 13]C] and L-[3,4,-[sup 13]C[sub 2

    Energy Technology Data Exchange (ETDEWEB)

    Lodwig, S.N. (Centralia College, WA (United States). Science Div.); Unkefer, C.J. (Los Alamos National Lab., NM (United States))

    1992-02-01

    We have developed a stereoselective route to isotopically labeled L-aspartic acid using L-serine as a chiral precursor. Labeled serine, prepared biosynthetically was N-protected by conversion to the N-t-Boc derivative. (N-t-Boc)-[3-[sup 13]C]Serine is cyclized to its [beta]-lactone which was treated with potassium [[sup 13]C]cyanide to yield L-[beta]-[3,4-[sup 13]C[sub 2

  1. Synthesis of 125I Labeled Estradiol-17-Hemisuccinate and Its Binding Study to Estrogen Receptors Using Scintillation Proximity Assay Method

    Directory of Open Access Journals (Sweden)

    Y. Susilo

    2012-12-01

    Full Text Available Research was carried out to obtain a selective ligand which strongly bind to estrogen receptors through determination of binding affinity of estradiol-17β-hemisuccinate. Selectivity of these compounds for estrogen receptor was studied using Scintillation Proximity Assay (SPA method. Primary reagents required in the SPA method including radioligand and receptor, the former was obtained by labeling of estradiol-17β-hemisuccinate with 125I, while MCF7 was used as the receptor. The labeling process was performed by indirect method via two-stage reaction. In this procedure, first step was activation of estradiol-17β-hemisuccinate using isobutylchloroformate and tributylamine as a catalist, while labeling of histamine with 125I was carried out using chloramin-T method to produce 125I-histamine. The second stage was conjugation of activated estradiol-17β-hemisuccinate with 125I-histamine. The product of estradiol-17β-hemisuccinate labeled 125I was extracted using toluene. Furtherly, the organic layer was purified by TLC system. Characterization of estradiol-17β-hemisuccinate labeled 125I from this solvent extraction was carried out by determining its radiochemical purity and the result was obtained using paper electrophoresis and TLC were 79.8% and 84.4% respectively. Radiochemical purity could be increased when purification step was repeated using TLC system, the result showed up to 97.8%. Determination of binding affinity by the SPA method was carried out using MCF7 cell lines which express estrogen receptors showed the value of Kd at 7.192 x 10-3 nM and maximum binding at 336.1 nM. This low value of Kd indicated that binding affinity of estradiol-17β-hemisuccinate was high or strongly binds to estrogen recepto

  2. Food labels

    DEFF Research Database (Denmark)

    Selsøe Sørensen, Henrik; Clement, Jesper; Gabrielsen, Gorm

    2012-01-01

    The food industry develops tasty and healthy food but fails to deliver the message to all consumers. The consumers’ background knowledge is essential for how they find and decode relevant elements in the cocktail of signs which fight for attention on food labels. In this exploratory study, we find...... evidence for dividing consumers into two profiles: one relying on general food knowledge and another using knowledge related to signpost labels. In a combined eyetracking and questionnaire survey we analyse the influence of background knowledge and identify different patterns of visual attention...... for the two consumer profiles. This underlines the complexity in choosing and designing the ‘right’ elements for a food package that consumers actually look at and are able to make rational use of. In spite of any regulation of food information provided by authorities, consumers will still be confronted...

  3. Quantitative assessment of simultaneous F-18 FDG PET/MRI in patients with various types of hepatic tumors: Correlation between glucose metabolism and apparent diffusion coefficient.

    Science.gov (United States)

    Kong, Eunjung; Chun, Kyung Ah; Cho, Ihn Ho

    2017-01-01

    Metabolism and water diffusion may have a relationship or an effect on each other in the same tumor. Knowledge of their relationship could expand the understanding of tumor biology and serve the field of oncologic imaging. This study aimed to evaluate the relationship between metabolism and water diffusivity in hepatic tumors using a simultaneous positron emission tomography/magnetic resonance imaging (PET/MRI) system with F-18 fluorodeoxyglucose (FDG) and to reveal the metabolic and diffusional characteristics of each type of hepatic tumor. Forty-one patients (mean age 63 ± 13 years, 31 male) with hepatic tumors (18 hepatocellular carcinoma [HCC], six cholangiocarcinoma [CCC], 10 metastatic tumors, one neuroendocrine malignancy, and six benign lesions) underwent FDG PET/MRI before treatment. Maximum standard uptake (SUVmax) values from FDG PET and the apparent diffusion coefficient (ADC) from the diffusion-weighted images were obtained for the tumor and their relationships were examined. We also investigated the difference in SUVmax and ADC for each type of tumor. SUVmax showed a negative correlation with ADC (r = -0.404, p = 0.009). The median of SUVmax was 3.22 in HCC, 6.99 in CCC, 6.30 in metastatic tumors, and 1.82 in benign lesions. The median of ADC was 1.039 × 10-3 mm/s2 in HCC, 1.148 × 10-3 mm/s2 in CCC, 0.876 × 10-3 mm/s2 in metastatic tumors, and 1.323 × 10-3 mm/s2 in benign lesions. SUVmax was higher in metastatic tumors than in benign lesions (p = 0.023). Metastatic tumors had a lower ADC than CCC (p = 0.039) and benign lesions (p = 0.004). HCC had a lower ADC than benign lesions, with a suggestive trend (p = 0.06). Our results indicate that SUVmax is negatively correlated with ADC in hepatic tumors, and each group of tumors has different metabolic and water diffusivity characteristics. Evaluation of hepatic tumors by PET/MRI could be helpful in understanding tumor characteristics.

  4. The Clinical Value of Dual Time Point F-18 FDG PET/CT Imaging for the Differentiation of Colonic Focal Uptake Lesions

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Jin Suk; Lim, Seok Tae; Jeong, Young Jin; Kim, Dong Wook; Jeong, Hwan Jeong; Sohn, Myung Hee [Chonbuk National University Medical School and Hospital, Jeonju (Korea, Republic of)

    2009-08-15

    F-18 FDG can be accumulated in the liver, bowel, kidney, urinary tract, and muscles physiologically. The aim of this study was to evaluate the clinical value of dual time point 18F-FDG PET/CT imaging for the differentiation of the colonic focal uptake lesions. One hundred thirty two patients (M:F=77:55, Age 62.8{+-}11.6 years) underwent {sup 18}F-FDG PET/CT at two time points, prospectively: early image at 50-60 min and delayed image at 4-4.5 hours after the intravenous injection of {sup 18}F-FDG. Focally increased uptake lesions on early images but disappeared or shifted on delayed images defined a physiological uptake. For the differential evaluation of persistent focal uptake lesions on delayed images, colonoscopy and histopathologic examination were performed. SUVmax changes between early and delayed images were also compared. Among the 132 patients, 153 lesions of focal colonic uptake were detected on early images of {sup 18}F-FDG PET/CT. Of these, 72 (47.1%) lesions were able to judge with physiological uptake because the focal increased uptake disappeared from delayed image. Among 81 lesions which was showed persistent increased uptake in delayed image, 61 (75.3%) lesions were confirmed as the malignant tumor and 14 (17.3%) lesions were confirmed as the benign lesions including adenoma and inflammatory disease. Remaining 6 (7.4%) lesions were confirmed as the physiological uptake because there was no particular lesion in the colonoscopy. In the malignant lesions, the calculated dual time point change for SUVmax ({delta}%SUVmax) was 20.8%{+-}18.7%, indicating a significant increase in SUVmax between the two point (p<0.01). In contrast, the change in SUVmax for the non-malignant lesions including benign lesions and physiological uptake was -13.7%{+-}24.2%. For the differentiation of the malignant and non-malignant focal colonic uptake lesions, {delta}%SUVmax was the most effective parameter, and the cut-off value using -5% provided the best sensitivity

  5. TU-G-BRA-07: Characterization of Tumor Proliferation During Successive Cycles of Anti-Angiogenic Therapy Using [F-18]FLT PET/CT

    Energy Technology Data Exchange (ETDEWEB)

    Scarpelli, M; Perlman, S; Harmon, S; Perk, T; Scully, P; Bruce, J; Liu, G; Jeraj, R [University of Wisconsin, Madison, WI (United States)

    2015-06-15

    Purpose: Studies have shown cessation of anti-angiogenic treatment during the first cycle of therapy resulted in rebound of tumor proliferation (flare). This study characterized proliferation dynamics during the first and third cycle of anti-angiogenic treatment using [F-18]FLT PET. Methods: Thirteen patients with various solid cancers were treated with Axitinib (Pfizer, Inc) at a dose of 5mg orally, twice daily, on contiguous three-week cycles with intermittent dosing (two-weeks-on/one-week-off). All patients received three FLT PET/CT scans during cycle 1 (C1): at baseline (C1D0), peak Axitinib concentration (C1D14), and the end of washout (C1D21). Ten patients received up to an additional three scans at corresponding time points during cycle 3 (C3). Lesions were identified by a nuclear medicine physician and manually contoured. Tumor burden was quantified using standard SUV metrics. Correlations between imaging metrics across C1 and C3 were calculated using the Spearman correlation. Results: At C1 peak drug concentration 11/13 patients had decreases in SUVtotal, with median decrease of 50% (change from C1D0 to C1D14). At C3 peak drug concentration 7/7 patients had decreases in SUVtotal, with median decrease of 20% (C3D0 to C3D14). Proliferative flare during C1 washout (>20% increase from C1D14 to C1D21) occurred in 9/13 patients, with median SUVtotal increase of 190%. Flare was also seen in C3 for 5/5 patients, with median SUVtotal increase of 70% (change from C3D14 to C3D21). Correlations were found between changes in imaging metrics across C1 and C3, notably the change in SUVtotal from C1D0 to C1D21 and the change in SUVtotal from C1D0 to C3D0 (ρ = 0.80). Conclusion: Measurements of SUVtotal showed that both patient response to treatment and flare were evident in both cycles of treatment. Correlation between changes in SUVtotal across C1 and C3 suggest early time points could be used to characterize patient response in later cycles. Research funded in part by

  6. Synthesis of deuterium-labelled 5'-O-[N-(Salicyl)sulfamoyl]adenosine (Sal-AMS-d(4)) as an internal standard for quantitation of Sal-AMS.

    Science.gov (United States)

    Gupte, Amol; Subramanian, Murali; Remmel, Rory P; Aldrich, Courtney C

    2008-02-01

    5'-O-[N-(Salicyl)sulfamoyl]adenosine (Sal-AMS, 1) is a potent inhibitor of the bifunctional enzyme salicyl-AMP ligase in Mycobacterium tuberculosis. This inhibitor acts by disrupting the biosynthesis of the mycobactin siderophores that are essential for the process of iron acquisition. To aid with in vitro metabolism and in vivo pharmacokinetic studies of Sal-AMS, a stable deuterium-labelled Sal-AMS analog (Sal-AMS-d(4)) was synthesized. This deuterium-labelled analog was used as an internal standard to conduct in vitro plasma and microsomal stability studies. Sal-AMS was found to be stable for 24 h in human plasma and 1 h in human liver microsomes at 37 degrees C.

  7. Chemical synthesis of glycoproteins with the specific installation of gradient enriched 15N-labeled amino acids for getting insight into glycoprotein behavior.

    Science.gov (United States)

    Kajihara, Yasuhiro; Nguyen, Minh Hien; Izumi, Masayuki; Sato, Hajime; Okamoto, Ryo

    2017-03-09

    We propose a novel partially 15N-labelling method for the amide backbone of a synthetic glycoprotein. By use of a chemical approach utilizing SPPS and NCL, we inserted thirteen 15N-labeled amino acids at specific positions of the protein backbone, while intentionally varying the enrichment of 15N atoms. This idea enables us to discriminate even the same type of amino acid based on the intensities of 1H-15N HSQC signals, thus allowing us to understand the dynamics of the local conformation of a synthetic homogeneous glycoprotein. Results suggested that the attachment of an oligosaccharide of either a bi-antennary complex-type or a high-mannose-type did not disturb protein conformation. However, T1 values suggested that the oligosaccharide influenced dynamics at the local conformation. Temperature-varied CD spectra and T1 values clearly indicated that oligosaccharides appeared to inhibit protein fluctuation or, in other words, stabilize protein structure.

  8. Synthesis of O-[{sup 11}C]acetyl CoA, O-[{sup 11}C]acetyl-L-carnitine, and L-[{sup 11}C]carnitine labelled in specific positions, applied in PET studies on rhesus monkey

    Energy Technology Data Exchange (ETDEWEB)

    Jacobson, Gunilla B.; Watanabe, Yasuyoshi; Valind, Sven; Kuratsune, Hirohiko; Laangstroem, Bengt

    1997-07-01

    The syntheses of L-carnitine, O-acetyl CoA, and O-acetyl-L-carnitine labelled with {sup 11}C at the 1- or 2-position of the acetyl group or the N-methyl position of carnitine, using the enzymes acetyl CoA synthetase and carnitine acetyltransferase, are described. With a total synthesis time of 45 min, O-[1-{sup 11}C]acetyl CoA and O-[2-{sup 11}C]acetyl CoA was obtained in 60-70% decay-corrected radiochemical yield, and O-[1-{sup 11}C]acetyl-L-carnitine and O-[2-{sup 11}C]acetyl-L-carnitine in 70-80% yield, based on [1-{sup 11}C]acetate or [2-{sup 11}C]acetate, respectively. By an N-methylation reaction with [{sup 11}C]methyl iodide, L-[methyl-{sup 11}C]carnitine was obtained within 30 min, and O-acetyl-L-[methyl-{sup 11}C]carnitine within 40 min, giving a decay-corrected radiochemical yield of 60% and 40-50%, respectively, based on [{sup 11}C]methyl iodide. Initial data of the kinetics of the different {sup 11}C-labelled L-carnitine and acetyl-L-carnitines in renal cortex of anaesthetized monkey (Macaca mulatta) are presented.

  9. CdTe/CdS-MPA quantum dots as fluorescent probes to label yeast cells: synthesis, characterization and conjugation with Concanavalin A

    Science.gov (United States)

    Kato, Ilka T.; Santos, Camila C.; Benetti, Endi; Tenório, Denise P. L. A.; Cabral Filho, Paulo E.; Sabino, Caetano P.; Fontes, Adriana; Santos, Beate S.; Prates, Renato A.; Ribeiro, Martha S.

    2012-03-01

    Candida albicans is the most frequent human opportunistic pathogenic fungus and one of the most important causes of nosocomial infections. In fact, diagnosis of invasive candidiasis presents unique problems. The aim of this work was to evaluate, by fluorescence image analysis, cellular labeling of C. albicans with CdTe/CdS quantum dots conjugated or not to concanavalin A (ConA). Yeast cells were incubated with CdTe/CdS quantum dots (QD) stabilized with mercaptopropionic acid (MPA) (emission peak at 530 nm) for 1 hour. In the overall study we observed no morphological alterations. The fluorescence microscopic analysis of the yeast cells showed that the non-functionalized QDs do not label C. albicans cells, while for the QD conjugated to ConA the cells showed a fluorescence profile indicating that the membrane was preferentially marked. This profile was expected since Concanavalin A is a protein that binds specifically to terminal carbohydrate residues at the membrane cell surface. The results suggest that the QD-labeled Candida cells represent a promising tool to open new possibilities for a precise evaluation of fungal infections in pathological conditions.

  10. Introduction to Pesticide Labels

    Science.gov (United States)

    Pesticide product labels provide critical information about how to safely and legally handle and use pesticide products. Unlike most other types of product labels, pesticide labels are legally enforceable. Learn about pesticide product labels.

  11. Food Label and You

    Medline Plus

    Full Text Available ... Products Food Home Food Ingredients, Packaging & Labeling Labeling & Nutrition The Food Label and You — Video Share Tweet ... FDA has issued final changes to update the Nutrition Facts label for packaged foods. For more information, ...

  12. Synthesis of [13C4]-labeled ∆9-Tetrahydrocannabinol and 11-nor-9-Carboxy-∆9-tetrahydrocannabinol as Internal Standards for Reducing Ion Suppressing/Alteration Effects in LC/MS-MS Quantification

    Directory of Open Access Journals (Sweden)

    Morten Karlsen

    2014-09-01

    Full Text Available (−-∆9-Tetrahydrocannabinol is the principal psychoactive component of the cannabis plant and also the active ingredient in some prescribed drugs. To detect and control misuse and monitor administration in clinical settings, reference samples of the native drugs and their metabolites are needed. The accuracy of liquid chromatography/mass spectrometric quantification of drugs in biological samples depends among others on ion suppressing/alteration effects. Especially, 13C-labeled drug analogues are useful for minimzing such interferences. Thus, to provide internal standards for more accurate quantification and for identification purpose, synthesis of [13C4]-∆9-tetrahydro-cannabinol and [13C4]-11-nor-9-carboxy-∆9-tetrahydrocannabinol was developed via [13C4]-olivetol. Starting from [13C4]-olivetol the synthesis of [13C4]-11-nor-9-carboxy-∆9-tetrahydrocannabinol was shortened from three to two steps by employing nitromethane as a co-solvent in condensation with (+-apoverbenone.

  13. On Online Labeling with Polynomially Many Labels

    DEFF Research Database (Denmark)

    Babka, Martin; Bulánek, Jan; Cunat, Vladimír

    2012-01-01

    In the online labeling problem with parameters n and m we are presented with a sequence of nkeys from a totally ordered universe U and must assign each arriving key a label from the label set {1,2,…,m} so that the order of labels (strictly) respects the ordering on U. As new keys arrive it may be...

  14. Synthesis and tritium labeling of the highly potent mast cell-degranulating substance P analog H-Arg-Pro-Lys-Pro-NH-C sub 12 H sub 25

    Energy Technology Data Exchange (ETDEWEB)

    Bienert, M.; Oehlke, J.; Niedrich, H. (Academy of Sciences of GDR, Berlin (Germany, F.R.). Inst. of Drug Research); Mittag, E. (Zentralinstitut fuer Kernforschung, Rossendorf (Germany, F.R.))

    1990-12-01

    Tritium labeling of the mast cell degranulating substance P analog H-Arg-Pro-Lys(3,4-{sup 3}H-Pro)-NH-C{sub 12}H{sub 25} by catalytic saturation of the dehydroproline (Dhp{sup 1}) double bond is described. Catalytic tritiation in water afforded the radioactive analog with a specific activity of 1.07 TBq/mmol. Tenfold enhancement of the catalyst-to-substrate ratio resulted in a reduced specific activity of 0.74 TBq/mmol. (author).

  15. Synthesis and biological evaluation of I-125/I-123-labelled analogues of citalopram and escitalopram as potential radioligands for imaging of the serotonin transporter

    DEFF Research Database (Denmark)

    Madsen, Jacob; Elfving, Betina; Frokjaer, Vibe G.

    2011-01-01

    Two novel radioligands for the serotonin transporter (SERT), [I-125]{3-[5-iodo-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-1-yl]-propyl}-dimethylamine ([I-125]-2) and S-[I-125]{3-[5-iodo-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-1-yl]-propyl}-dimethylamine ([I-125]-(S)-2) were synthesized in a ...... of the radioligand in imaging cortical SERT distribution in vivo. These data suggest that the iodine-labelled derivatives of citalopram and escitalopram are not superior to another SPECT tracer for the SERT, namely [I-123] ADAM....

  16. Synthesis and evaluation of a fluorine-18 labeled antisense oligonucleotide as a potential PET tracer for iNOS mRNA expression

    Energy Technology Data Exchange (ETDEWEB)

    Vries, Erik F.J. de E-mail: e.f.j.de.vries@pet.azg.nl; Vroegh, Joke; Dijkstra, Gerard; Moshage, Han; Elsinga, Philip H.; Jansen, Peter L.M.; Vaalburg, Willem

    2004-07-01

    Inducible NO synthase (iNOS) is overexpressed in inflammatory bowel diseases. An antisense oligonucleotide with good hybridization properties for iNOS mRNA was selected using RT-PCR. The oligonucleotide was reliably labeled with fluorine-18 using N-(4-[{sup 18}F]fluorobenzyl)-2-bromoacetamide. Cellular uptake and efflux of oligonucleotide complexed with FuGENE-6 were rapid, unlike naked oligonucleotide, which hardly accumulated. However, neither uptake nor efflux showed any selectivity for iNOS expressing cells. The oligonucleotide showed a high level of non-specific binding, which may have obscured its specific hybridization to iNOS mRNA.

  17. Synthesis and characterization of (68)Ga-labeled curcumin and curcuminoid complexes as potential radiotracers for imaging of cancer and Alzheimer's disease.

    Science.gov (United States)

    Asti, Mattia; Ferrari, Erika; Croci, Stefania; Atti, Giulia; Rubagotti, Sara; Iori, Michele; Capponi, Pier C; Zerbini, Alessandro; Saladini, Monica; Versari, Annibale

    2014-05-19

    Curcumin (CUR) and curcuminoids complexes labeled with fluorine-18 or technetium-99m have recently shown their potential as diagnostic tools for Alzheimer's disease. Gallium-68 is a positron-emitting, generator-produced radionuclide, and its properties can be exploited in situ in medical facilities without a cyclotron. Moreover, CUR showed a higher uptake in tumor cells compared to normal cells, suggesting potential diagnostic applications in this field. In spite of this, no studies using labeled CUR have been performed in this direction, so far. Herein, (68)Ga-labeled complexes with CUR and two curcuminoids, namely diacetyl-curcumin (DAC) and bis(dehydroxy)curcumin (bDHC), were synthesized and characterized by means of experimental and theoretical approaches. Moreover, a first evaluation of their affinity to synthetic β-amyloid fibrils and uptake by A549 lung cancer cells was performed to show the potential application of these new labeled curcuminoids in these diagnostic fields. The radiotracers were prepared by reacting (68)Ga(3+) obtained from a (68)Ge/(68)Ga generator with 1 mg/mL curcuminoids solutions. Reaction parameters (precursor amount, reaction temperature, and pH) were optimized to obtain high and reproducible radiochemical yield and purity. Stoichiometry and formation of the curcuminoid complexes were investigated by matrix-assisted laser desorption ionization time-of-flight mass spectrometry, NMR, ultraviolet-visible, and fluorescence spectroscopy on the equivalent (nat)Ga-curcuminoids (nat = natural) complexes, and their structure was computed by theoretical density functional theory calculations. The analyses evidenced that CUR, DAC, and bDHC were predominantly in the keto-enol form and attested to Ga(L)2(+) species formation. Identity of the (68)Ga(L)2(+) complexes was confirmed by coelution with the equivalent (nat)Ga(L)2(+) complexes in ultrahigh-performance liquid chromatography analyses.(68)Ga(CUR)2(+), (68)Ga(DAC)2(+), and (68)Ga(bDHC)2

  18. Evaluation of F-18-labeled 5-iodocytidine ({sup 18}F-FIAC) as a new potential positron emission tomography probe for herpes simplex virus type 1 thymidine kinase imaging

    Energy Technology Data Exchange (ETDEWEB)

    Chan, Pei-Chia; Wu, Chun-Yi; Chang, Wen-Yi; Chang, Wei-Ting [Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, Taipei, 11221, Taiwan (China); Alauddin, Mian [Department of Experimental Diagnostic Imaging, MD Anderson Cancer Center, University of Texas, TX, 77054 (United States); Liu, Ren-Shan [Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, Taipei, 11221, Taiwan (China); Department of Nuclear Medicine, Faculty of Medicine, National Yang-Ming University, Taipei, 11221, Taiwan (China); Department of Nuclear Medicine and National PET/Cyclotron Center, Taipei Veterans General Hospital, Taipei, 11217, Taiwan (China); Lin, Wuu-Jyh [Institute of Nuclear Energy Research, Atomic Energy Council, Taoyuan, 32546, Taiwan (China); Chen, Fu-Du [College of Health and Leisure Science, TransWorld University, Yunlin, 64063, Taiwan (China); Chen, Chuan-Lin, E-mail: clchen2@ym.edu.tw [Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, Taipei, 11221, Taiwan (China); Wang, Hsin-Ell, E-mail: hewang@ym.edu.tw [Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming University, Taipei, 11221, Taiwan (China)

    2011-10-15

    Objective: Herpes simplex virus type 1 thymidine kinase (HSV1-tk) gene in combination with radiolabeled nucleoside substrates is the most widely used reporter system. This study characterized 1-(2'-deoxy-2'-[{sup 18}F]fluoro-{beta}-D-arabinofuranosyl)-5-iodocytosine ({sup 18}F-FIAC) as a new potential positron emission tomography (PET) probe for HSV1-tk gene imaging and compared it with 2'-deoxy-2'-[{sup 18}F]fluoro-5-iodo-1-{beta}-D-arabinofuranosyluracil ({sup 18}F-FIAU) and 2'-deoxy-2'-[{sup 18}F]fluoro-5-ethyl-1-{beta}-D-arabinofuranosyluracil({sup 18}F-FEAU) (thymidine analogues) in an NG4TL4-WT/STK sarcoma-bearing mouse model. Methods: A cellular uptake assay, biodistribution study, radioactive metabolites assay and microPET imaging of NG4TL4-WT/STK tumor-bearing mice post administration of {sup 18}F-FIAC, {sup 18}F-FIAU and {sup 18}F-FEAU were conducted to characterize the biological properties of these tracers. Results: Highly specific uptake of {sup 18}F-FIAC, {sup 18}F-FIAU and {sup 18}F-FEAU in tk-transfected [tk(+)] cells was observed. The tk(+)-to-tk(-) cellular uptake ratio after a 2-h incubation was 66.6{+-}25.1, 76.3{+-}18.2 and 247.2{+-}37.2, respectively. In biodistribution studies, {sup 18}F-FIAC showed significant tk(+) tumor specificity (12.6; expressed as the tk(+)-to-tk(-) tumor uptake ratio at 2 h postinjection) comparable with {sup 18}F-FIAU (15.8) but lower than {sup 18}F-FEAU (48.0). The results of microPET imaging also revealed the highly specific accumulation of these three radioprobes in the NG4TL4-tk(+) tumor. Conclusion: Our findings suggested that the cytidine analogue {sup 18}F-FIAC is a new potential PET probe for the imaging of HSV1-tk gene expression. {sup 18}F-FIAC may be regarded as the prodrug of {sup 18}F-FIAU in vivo.

  19. Evaluation of elastix-based propagated align algorithm for VOI- and voxel-based analysis of longitudinal F-18-FDG PET/CT data from patients with non-small cell lung cancer (NSCLC)

    OpenAIRE

    Kerner, Gerald S. M. A.; Fischer, Alexander; Koole, Michel J. B.; Pruim, Jan; Groen, Harry J M

    2015-01-01

    Background: Deformable image registration allows volume of interest (VOI)- and voxel-based analysis of longitudinal changes in fluorodeoxyglucose (FDG) tumor uptake in patients with non-small cell lung cancer (NSCLC). This study evaluates the performance of the elastix toolbox deformable image registration algorithm for VOI and voxel-wise assessment of longitudinal variations in FDG tumor uptake in NSCLC patients. Methods: Evaluation of the elastix toolbox was performed using F-18-FDG PET/CT ...

  20. Comparison of the Prognostic Value of F-18 Pet Metabolic Parameters of Primary Tumors and Regional Lymph Nodes in Patients with Locally Advanced Cervical Cancer Who Are Treated with Concurrent Chemoradiotherapy.

    Directory of Open Access Journals (Sweden)

    Gun Oh Chong

    Full Text Available This study investigated the metabolic parameters of primary tumors and regional lymph nodes, as measured by pre-treatment F-18 fluorodeoxyglucose positron emission tomography/computed tomography (F-18 FDG PET/CT to compare the prognostic value for the prediction of tumor recurrence. This study also identified the most powerful parameter in patients with locally advanced cervical cancer treated with concurrent chemoradiotherapy.Fifty-six patients who were diagnosed with cervical cancer with pelvic and/or paraaortic lymph node metastasis were enrolled in this study. Metabolic parameters including the maximum standardized uptake value (SUVmax, the metabolic tumor volume (MTV, and total lesion glycolysis (TLG of the primary tumors and lymph nodes were measured by pre-treatment F-18 FDG PET/CT. Univariate and multivariate analyses for disease-free survival (DFS were performed using the clinical and metabolic parameters.The metabolic parameters of the primary tumors were not associated with DFS. However, DFS was significantly longer in patients with low values of nodal metabolic parameters than in those with high values of nodal metabolic parameters. A univariate analysis revealed that nodal metabolic parameters (SUVmax, MTV and TLG, paraaortic lymph node metastasis, and post-treatment response correlated significantly with DFS. Among these parameters, nodal SUVmax (hazard ratio [HR], 4.158; 95% confidence interval [CI], 1.1-22.7; p = 0.041 and post-treatment response (HR, 7.162; 95% CI, 1.5-11.3; p = 0.007 were found to be determinants of DFS according to a multivariate analysis. Only nodal SUVmax was an independent pre-treatment prognostic factor for DFS, and the optimal cutoff for nodal SUVmax to predict progression was 4.7.Nodal SUVmax according to pre-treatment F-18 FDG PET/CT may be a prognostic biomarker for the prediction of disease recurrence in patients with locally advanced cervical cancer.

  1. Synthesis and Application of Four Fluorescence Labeled Nucleotides Through Disulfide as Reversible Terminators in DNA Sequencing by Synthesis%四色荧光标记二硫键可逆终端的合成及在DNA合成测序中的应用

    Institute of Scientific and Technical Information of China (English)

    汤道年; 江敏; 李小卫; 康亚妮; 伍新燕; 龚兵; 邵志峰; 赵小东; 沈玉梅

    2014-01-01

    分别以5-碘-2'-脱氧尿苷、5-碘-2'-脱氧胞苷、7-去氮-7-碘-2'-脱氧腺苷及7-去氮-7-碘-2'-脱氧鸟苷为原料,以二硫键为可裂解连接单元,通过多步反应合成了四色荧光标记不同碱基的脱氧核糖核苷酸;研究了该类荧光标记核苷酸作为可逆终端在DNA合成测序中的应用。所得产物结构经1 H NMR,31 P NMR及HRMS表征,并对其进行了DNA高通量测序的测试。结果表明,该类荧光标记核苷酸作为DNA合成测序的可逆终端能够满足高通量测序的生化反应要求,具有较好的应用前景。%DNA sequencing is one of the important means of biological research. The development of accurate and high-throughput DNA-sequencing methods has a strong impact on biomedical research. Sequencing by synthesis( SBS) approaches is one of the most important techniques of DNA sequencing. A series of SBS methods have been investigated and implemented. In SBS methods, the principal thing is to synthesize four fluorescently labelled cyclic reversible terminators as the sequencing reagents. These cyclic reversible termina-tors need to connect the fluorescein through a cleavable linker. In chemical biology, disulfide bridges, which are known to be efficiently and rapidly cleaved by mild reducing agents, have been used in a wide range of ap-plications including drug delivery, functional and structural proteomics, DNA and tumor imaging. The disul-fide-based cleavable linker is commonly used due to its rapid cleavage and straightforward synthesis. In this work, starting from 5-iodo-2'-deoxyuridine, 5-iodo-2'-deoxycyridine, 7-deazo-7-iodo-2'-deoxyadenosine and 7-deazo-7-iodo-2'-deoxyguanosine, four kinds of fluorescence labelled necleotides with four different bases through disulfide were synthesized and characterized. The synthesized fluorescence labelled nucleotides can be recognized and accepted by an identified DNA polymerase, incorporated faithfully into DNA strand, followed by

  2. Update of the BIPM comparison BIPM.RI(II)-K1.F-18 of activity measurements of the radionuclide 18F to include the 2010 result of the LNE-LNHB (France)

    Science.gov (United States)

    Michotte, C.; Ratel, G.; Courte, S.; Cassette, P.; Moune, M.

    2016-01-01

    Since 2001, six national metrology institutes (NMI) have submitted seven samples of known activity of 18F to the International Reference System (SIR) for activity comparison at the Bureau International des Poids et Mesures (BIPM), with comparison identifier BIPM.RI(II)-K1.F-18. The values of the activity submitted were between about 1 MBq and 18 MBq. The primary standardization result for the LNE-LNHB, France, replaces their earlier result of 2002 and the key comparison reference value (KCRV) has been recalculated. In the frame of the BIPM.RI(II)-K4.F18 comparison, the NPL updated their result in the KCDB. Consequently there are now five results in the BIPM.RI(II)-K1.F-18 comparison. The degrees of equivalence between each equivalent activity measured in the SIR and the updated KCRV have been calculated and the results are given in the form of a table. A graphical presentation is also given. Main text To reach the main text of this paper, click on Final Report. Note that this text is that which appears in Appendix B of the BIPM key comparison database kcdb.bipm.org/. The final report has been peer-reviewed and approved for publication by the CCRI, according to the provisions of the CIPM Mutual Recognition Arrangement (CIPM MRA).

  3. Azido-iodo-N-benzyl derivatives of threo-methylphenidate (Ritalin, Concerta): Rational design, synthesis, pharmacological evaluation, and dopamine transporter photoaffinity labeling.

    Science.gov (United States)

    Lapinsky, David J; Velagaleti, Ranganadh; Yarravarapu, Nageswari; Liu, Yi; Huang, Yurong; Surratt, Christopher K; Lever, John R; Foster, James D; Acharya, Rejwi; Vaughan, Roxanne A; Deutsch, Howard M

    2011-01-01

    In contrast to tropane-based compounds such as benztropine and cocaine, non-tropane-based photoaffinity ligands for the dopamine transporter (DAT) are relatively unexplored. Towards addressing this knowledge gap, ligands were synthesized in which the piperidine nitrogen of 3- and 4-iodomethylphenidate was substituted with a benzyl group bearing a photoreactive azide. Analog (±)-3a demonstrated modest DAT affinity and a radioiodinated version was shown to bind covalently to rat striatal DAT and hDAT expressed in cultured cells. Co-incubation of (±)-3a with nonradioactive d-(+)-methylphenidate or (-)-2-β-carbomethoxy-3-β-(4-fluorophenyl)tropane (β-CFT, WIN-35,428, a cocaine analog) blocked DAT labeling. Compound (±)-3a represents the first successful example of a DAT photoaffinity ligand based on the methylphenidate scaffold. Such ligands are expected to assist in mapping non-tropane ligand-binding pockets within plasma membrane monoamine transporters.

  4. Synthesis of polymer-bound 6-mercuric carboxylate DOPA precursors and solid phase labelling method of 6-radioiodinated L-DOPA.

    Science.gov (United States)

    Kawai, K; Ohta, H; Channing, M A; Kubodera, A; Eckelman, W C

    1996-01-01

    In order to avoid separating unreacted mercury precursor and other mercury-containing compounds after the halodemercuration of a 6-mercury DOPA precursor, we developed a polymer-bound mercury precursor for the preparation of 6-halogenated DOPA. In this study, polymer-bound 6-mercuric carboxylate DOPA derivatives were synthesized from ion-exchange resin and Merrifield-type resin. Iododemercuration of polymer-bound 6-mercuric carboxylate DOPA derivatives gave higher yields (49-54%) compared with monomeric 6-mercuric trifluoroacetate protected DOPA. The radioiodination of the resin with no-carrier added iodine-125 afforded protected 6-[125I]I-L-DOPA with labelling efficiency of 92-97% with both polymer-bound 6-mercuric carboxylate DOPA derivatives.

  5. Synthesis and Biological Evaluation of Novel 99mTc(CO3-Labeled Thymidine Analogs as Potential Probes for Tumor Proliferation Imaging

    Directory of Open Access Journals (Sweden)

    Xiaojiang Duan

    2016-04-01

    Full Text Available Achieving a 99mTc labeled thymidine radiotracer for single photon emission tomography (SPECT is considered to be of interest. In this study, four novel thymidine analogs, 6a, 6b, 6c and 6d, were successfully synthesized via “click reaction” route and then radiolabeled using a [99mTc(CO3]+ core to prepare the corresponding 99mTc(CO3 complexes in high yields. These complexes were hydrophilic and had good in vitro stability. Biodistribution of these complexes in mice bearing S180 tumors showed that all of them exhibited accumulation in the tumors, suggesting that they would be potential tumor imaging agents.

  6. A Label-Free Microelectrode Array Based on One-Step Synthesis of Chitosan–Multi-Walled Carbon Nanotube–Thionine for Ultrasensitive Detection of Carcinoembryonic Antigen

    Directory of Open Access Journals (Sweden)

    Huiren Xu

    2016-07-01

    Full Text Available Carcinoembryonic antigen (CEA has been an extensively used tumor marker responsible for clinical early diagnosis of cervical carcinomas, and pancreatic, colorectal, gastric and lung cancer. Combined with micro-electro mechanical system (MEMS technology, it is important to develop a novel immune microelectrode array (MEA not only for rapid analysis of serum samples, but also for cell detection in vitro and in vivo. In this work, we depict a simple approach to modify chitosan–multi-walled carbon nanotubes–thionine (CS–MWCNTs–THI hybrid film through one-step electrochemical deposition and the CS-MWCNTs-THI hybrid films are successfully employed to immobilize anti-CEA for fabricating simple, label-free, and highly sensitive electro-chemical immune MEAs. The detection principle of immune MEA was based on the fact that the increasing formation of the antigen-antibody immunocomplex resulted in the decreased response currents and the relationship between the current reductions with the corresponding CEA concentrations was directly proportional. Experimental results indicated that the label-free MEA had good selectivity and the limit of detection for CEA is 0.5 pg/mL signal to noise ratio (SNR = 3. A linear calibration plot for the detection of CEA was obtained in a wide concentration range from 1 pg/mL to 100 ng/mL (r = 0.996. This novel MEA has potential applications for detecting CEA for the research on cancer cells and cancer tissue slices as well as for effective early diagnosis.

  7. Synthesis and sensing integration: A novel enzymatic reaction modulated Nanoclusters Beacon (NCB) "Illumination" strategy for label-free biosensing and logic gate operation.

    Science.gov (United States)

    Hong, Lu; Zhou, Fu; Wang, Guangfeng; Zhang, Xiaojun

    2016-12-15

    A novel fluorescent label-free "turn-on" NAD(+) and adenosine triphosphate (ATP) biosensing strategy is proposed by fully exploiting ligation triggered Nanocluster Beacon (NCB). In the presence of the target, the split NCB was brought to intact, which brought the C-rich sequence and enhancer sequence in close proximity resulting in the lightening of dark DNA/AgNCs ("On" mode). Further application was presented for logic gate operation and aptasensor construction. The feasibility was investigated by Ultraviolet-visible spectroscopy (UV-vis), Fluorescence, lifetime and High Resolution Transmission Electron Microscopy (HRTEM) etc. The strategy displayed good performance in the detection of NAD(+) and ATP, with the detection limit of 0.002nM and 0.001mM, the linear range of 10-1000nM and 0.003-0.01mM, respectively. Due to the DNA/AgNCs as fluorescence reporter, the completely label-free fluorescent strategy boasts the features of simplicity and low cost, and showing little reliance on the sensing environment. Meanwhile, the regulation by overhang G-rich sequence not relying on Förster energy transfer quenching manifests the high signal-to-background ratios (S/B ratios). This method not only provided a simple, economical and reliable fluorescent NAD(+) assay but also explored a flexible G-rich sequence regulated NCB probe for the fluorescent biosensors. Furthermore, this sensing mode was expanded to the application of a logic gate design, which exhibited a high performance for not only versatile biosensors construction but also for molecular computing application. Copyright © 2016 Elsevier B.V. All rights reserved.

  8. Synthesis and in Vivo Biological Evaluation of (68)Ga-Labeled Carbonic Anhydrase IX Targeting Small Molecules for Positron Emission Tomography.

    Science.gov (United States)

    Sneddon, Deborah; Niemans, Raymon; Bauwens, Matthias; Yaromina, Ala; van Kuijk, Simon J A; Lieuwes, Natasja G; Biemans, Rianne; Pooters, Ivo; Pellegrini, Paul A; Lengkeek, Nigel A; Greguric, Ivan; Tonissen, Kathryn F; Supuran, Claudiu T; Lambin, Philippe; Dubois, Ludwig; Poulsen, Sally-Ann

    2016-07-14

    Tumor hypoxia contributes resistance to chemo- and radiotherapy, while oxygenated tumors are sensitive to these treatments. The indirect detection of hypoxic tumors is possible by targeting carbonic anhydrase IX (CA IX), an enzyme overexpressed in hypoxic tumors, with sulfonamide-based imaging agents. In this study, we present the design and synthesis of novel gallium-radiolabeled small-molecule sulfonamides targeting CA IX. The compounds display favorable in vivo pharmacokinetics and stability. We demonstrate that our lead compound, [(68)Ga]-2, discriminates CA IX-expressing tumors in vivo in a mouse xenograft model using positron emission tomography (PET). This compound shows specific tumor accumulation and low uptake in blood and clears intact to the urine. These findings were reproduced in a second study using PET/computed tomography. Small molecules investigated to date utilizing (68)Ga for preclinical CA IX imaging are scarce, and this is one of the first effective (68)Ga compounds reported for PET imaging of CA IX.

  9. Aqueous synthesis of type-II CdTe/CdSe core-shell quantum dots for fluorescent probe labeling tumor cells.

    Science.gov (United States)

    Zeng, Ruosheng; Zhang, Tingting; Liu, Jincheng; Hu, Song; Wan, Qiang; Liu, Xuanming; Peng, Zhiwei; Zou, Bingsuo

    2009-03-04

    In this paper, we report a two-step aqueous synthesis of highly luminescent CdTe/CdSe core/shell quantum dots (QDs) via a simple method. The emission range of the CdTe/CdSe QDs can be tuned from 510 to 640 nm by controlling the thickness of the CdSe shell. Accordingly, the photoluminescence quantum yield (PL QY) of CdTe/CdSe QDs with an optimized thickness of the CdSe shell can reach up to 40%. The structures and compositions of the core/shell QDs were characterized by transmission electron microscopy, x-ray diffraction, and x-ray photoelectron spectroscopy experiments, and their formation mechanism is discussed. Furthermore, folate conjugated CdTe/CdSe QDs in Hela cells were assessed with a fluorescence microscope. The results show that folate conjugated CdTe/CdSe QDs could enter tumor cells efficiently.

  10. Studies toward labeling cytisine with [11C]phosgene: rapid synthesis of a delta-lactam involving a new chemoselective lithiation-annulation method.

    Science.gov (United States)

    Rouden, Jacques; Seitz, Thomas; Lemoucheux, Laurent; Lasne, Marie-Claire

    2004-05-28

    With the aim of the radiolabeling of cytisine, a potent agonist of nicotinic receptors, with [(11)C]phosgene, the rapid synthesis of a lactam model of our target has been studied. The key step of the delta-lactam formation is a new chemoselective lithiation-annulation method, under high dilution, of a suitable piperidinylcarbamoyl chloride. This precursor was obtained from (2-hydroxyethyl)piperidine in a linear synthetic sequence involving a Corey-Fuchs olefination of the corresponding aldehyde, followed by a selective reduction, using a diimide equivalent, of an iodoalkyne into a (Z)-iodopropene piperidine. This alkene served as main precursor to study the cyclization according to several procedures using phosgene as the required carbonylating reagent.

  11. Rapid synthesis and in vitro and in vivo evaluation of folic acid derivatives labeled with fluorine-18 for PET imaging of folate receptor-positive tumors

    Energy Technology Data Exchange (ETDEWEB)

    Jammaz, I. Al, E-mail: jammaz@kfshrc.edu.sa; Al-Otaibi, B.; Amer, S.; Okarvi, S.M.

    2011-10-15

    In an attempt to visualize folate receptors that overexpress on many cancers, [{sup 18}F]-fluorobenzene and pyridinecarbohydrazide-folate/methotrexate conjugates ([{sup 18}F]-1, [{sup 18}F]-2-folates and [{sup 18}F]-8, [{sup 18}F]-9-MTXs) were synthesized by the nucleophilic displacement reactions using ethyl-trimethylammonium-benzoate and pyridinecarboxylate precursors. The intermediates ethyl [{sup 18}F]-fluorinated benzene and pyridine esters were reacted with hydrazine to produce the [{sup 18}F]-fluorobenzene and pyridinecarbohydrazides, followed by coupling with N-hydroxysuccinimide-folate/MTX. Radiochemical yields were greater than 80% (decay corrected), with total synthesis time of less than 45 min. Radiochemical purities were always greater than 97% without high-performance liquid chromatography purification. These synthetic approaches hold considerable promise as rapid and simple method for the radiofluorination of folate derivatives with high radiochemical yield in short synthesis time. In vitro tests on KB cell line showed that significant amount of the radioconjugates were associated with cell fractions, and in vivo characterization in normal Balb/c mice revealed rapid blood clearance of these radioconjugates with excretion predominantly by the urinary and partially by the hepatobiliary systems. Biodistribution studies in nude mice bearing human KB cell line xenografts demonstrated significant tumor uptake and favorable biodistribution profile for [{sup 18}F]-2-folate over the other conjugates. The uptake in the tumors was blocked by excess coinjection of folic acid, suggesting a receptor-mediated process. Micro-positron emission tomography images of nude mice bearing human KB cell line xenografts confirmed these observations. These results demonstrate that [{sup 18}F]-2-folate may be useful as molecular probe for detecting and staging of folate receptor-positive cancers, such as ovarian cancer and their metastasis as well as monitoring tumor response

  12. Synthesis and in vitro/in vivo evaluation of novel mono- and trivalent technetium-99m labeled ghrelin peptide complexes as potential diagnostic radiopharmaceuticals.

    Science.gov (United States)

    Koźmiński, Przemysław; Gniazdowska, Ewa

    2015-01-01

    Ghrelin is an endogenous hormone present in blood. It is released from the oxyntic cells (X/A-like cells) of the stomach and fundus and can exist in two forms: as an acylated and des-acylated ghrelin. Ghrelin is an endogenous ligand of the growth hormone receptor (growth hormone secretagogue receptor, GHS-R). Overexpression of GHS-R1a receptor was identified in cells of different types of tumors (e.g. pituitary adenoma, neuroendocrine tumors of the thyroid, lung, breast, gonads, prostate, stomach, colorectal, endocrine and non-endocrine pancreatic tumors). This fact suggests that gamma radionuclide labeled ghrelin peptide may be considered as a potential diagnostic radiopharmaceutical. Ghrelin peptide labeled with mono- and trivalent technetium-99m complexes, (99m)Tc-Lys-GHR, has been prepared on the n.c.a. scale. The physicochemical (stability, charge, shape, lipophilicity) and biological (receptor affinity, biodistribution) properties of the conjugates have been studied relevant to use the conjugates as receptor-based diagnostic radiopharmaceuticals. The obtained conjugates [(99m)Tc(CO)3LN,O(CN-Lys-GHR)](+), (99m)Tc(CO)3LS,O(CN-Lys-GHR) and (99m)Tc(NS3)(CN-Lys-GHR) show different shape, charge, lipophilicity and two of them, (99m)Tc(CO)3LS,O(CN-Lys-GHR) and (99m)Tc(NS3)(CN-Lys-GHR), high stability in neutral aqueous solutions, even in the presence of excess concentration of histidine/cysteine competitive standard ligands or human serum. The in vitro binding affinity of (99m)Tc-Lys-GHR conjugates with respect to growth hormone secretagogue receptor (GHS-R1a) present on DU-145 cells was in the range of IC50 from 45 to 54 nM. The conjugate (99m)Tc(CO)3LS,O(CN-Lys-GHR) exhibited excretion route by the liver and kidney in comparable degree, while the more lipophilic conjugate (99m)Tc(NS3)(CN-Lys-GHR)-mainly by the liver. Basing on the results concerning physicochemical and biochemical properties, the conjugates (99m)Tc(CO)3LS,O(CN-Lys-GHR) and (99m)Tc(NS3)(CN

  13. Food Label and You

    Medline Plus

    Full Text Available ... Vaccines, Blood & Biologics Animal & Veterinary Cosmetics Tobacco Products Food Home Food Ingredients, Packaging & Labeling Labeling & Nutrition The Food Label and You — Video Share Tweet Linkedin Pin ...

  14. Deuterium-labelled N-acyl-l-homoserine lactones (AHLs) - inter-kingdom signalling molecules - synthesis, structural studies, and interactions with model lipid membranes

    Energy Technology Data Exchange (ETDEWEB)

    Jakubczyk, Dorota [Institute of Organic Chemistry, Karlsruhe Institute of Technology, Karlsruhe (Germany); Institute of Functional Interfaces, Karlsruhe Institute of Technology, Eggenstein-Leopoldshafen (Germany); Barth, Christoph; Anastassacos, Frances; Koelsch, Patrick; Schepers, Ute [Institute of Toxicology and Genetics, Karlsruhe Institute of Technology, Eggenstein-Leopoldshafen (Germany); Kubas, Adam; Fink, Karin [Institute of Nanotechnology, Karlsruhe Institute of Technology, Eggenstein-Leopoldshafen (Germany); Brenner-Weiss, Gerald [Institute of Functional Interfaces, Karlsruhe Institute of Technology, Eggenstein-Leopoldshafen (Germany); Braese, Stefan [Institute of Organic Chemistry, Karlsruhe Institute of Technology, Karlsruhe (Germany)

    2012-04-15

    N-Acyl-l-homoserine lactones (AHLs) are synthesized by Gram-negative bacteria. These quorum-sensing molecules play an important role in the context of bacterial infection and biofilm formation. They also allow communication between microorganisms and eukaryotic cells (inter-kingdom signalling). However, very little is known about the entire mechanism of those interactions. Precise structural studies are required to analyse the different AHL isomers as only one form is biologically most active. Theoretical studies combined with experimental infrared and Raman spectroscopic data are therefore undertaken to characterise the obtained compounds. To mimic interactions between AHL and cell membranes, we studied the insertion of AHL in supported lipid bilayers, using vibrational sum-frequency-generation spectroscopy. Deuterium-labelled AHLs were thus synthesized. Starting from readily available deuterated fatty acids, a two-step procedure towards deuterated N-acyl-l-homoserine lactones with varying chain lengths is described. This included the acylation of Meldrum's acid followed by amidation. Additionally, the detailed analytical evaluation of the products is presented herein. (orig.)

  15. Enzymic synthesis of steroid sulphates. XI. Study of the oestrogen binding site of oestrogen sulphotransferase by affinity labelling with 4-mercuri-17beta-oestradiol.

    Science.gov (United States)

    Dodsworth, A I; Jackson, D E

    1975-04-19

    Oistrogen sulphotransferase (3"-phosphoadenylylsulphate: oestrone sulphotransferase, EC 2.8.2.4) contains asingle sulphydryl group thought to be at, or near, the oestrogen-binding site. 4-mercuri-17beta-oestradiol, the activity of the enzyme decreased with increasing concentration of the oestrogen derivative. However, some 40% of the activity remained when all the sulphydryl had reacted to form mercaptide. Formation of mercaptide was only marginally decreased in the presence of the substrate 17beta-oestradiol. Other steroids, such as 11-deoxycorticosterone and testosterone, which are non-substrates for the enzyme, were more effective than 17beta-oestradiol in inhibiting mercaptide formation. Bovine serum albumin also reacted with 4-mercure-17beta-oestradiol and the effects of various steroids on mercaptide formation by the affinity label closely paralleled those found for the enzyme. 2t is concluded that the single sulphydryl group in the enzyme is not directly involved in the binding of oestrogen at the active site but is perhaps in closer proximity to a second site capable of binding certain non-substrate steroids.

  16. Synthesis, characterization and biological evaluation of a well dispersed suspension of gallium-68-labeled magnetic nanosheets of graphene oxide for in vivo coincidence imaging

    Energy Technology Data Exchange (ETDEWEB)

    Fazaeli, Yousef; Feizi, Shahzad [Nuclear Science and Technology Research Institute, Karaj (Iran, Islamic Republic of). Radiation Application Research School; Rahighi, Reza [Sharif Univ. of Technology, Tehran (Iran, Islamic Republic of). Dept. of Physics; Tayyebi, Ahmad [Sharif Univ. of Technology, Tehran (Iran, Islamic Republic of). Dept. of Engineering

    2017-03-01

    Graphene oxide (GO) nanosheets were hybridized with Fe{sub 3}O{sub 4} nanoparticles (NPs) to form magnetic GO (MGO) and were further labeled by [{sup 68}Ga]GaCl{sub 3} as a potential drug delivery system. Paper chromatography, Fourier transform infra red (FTIR) spectroscopy, low-angle X-ray diffraction (XRD), CHN and atomic force microscopy (AFM) were utilized to characterize the trinary composite ([{sup 68}Ga] rate at MGO). Biological evaluations of the prepared nanocomposite were performed in normal Sprague Dawley rats and it was found to be a possible host for theranostic radiopharmaceuticals. The results showed that the grafting of Fe{sub 3}O{sub 4} NPs on nanocomposite reduced the unwanted liver and spleen uptakes and increased the ratio of kidney/liver uptake from 0.037 to 1.07, leading to the fast removal of radioactive agent and less imposed radiation to patients. The high level of hydrogen bonding caused by the presence of functional groups is responsible for this effect. Considering the accumulation of the tracer in vital organs of rat (especially brain), efficient iron oxide grafting, fast wash-out, the short half-life gallium-68 and less imposed radiation doses to patients, this nanocomposite could be a suitable candidate for positron emission tomography (PET) studies and imaging applications.

  17. Synthesis of [{sup 123}I]iodine labelled imidazo[1,2-b] pyridazines as potential probes for the study of peripheral benzodiazepine receptors using SPECT

    Energy Technology Data Exchange (ETDEWEB)

    Katsifis, A.; Mattner, F.; Dikic, B. [Radiopharmaceuticals Div. ANSTO, Menai, NSW (Australia); Barlin, G. [Div. of Neurosciences, John Curtin School of Medical Research, Australian National Univ., Canberra (Australia)

    2004-07-01

    The pyridazines 3-acetamidomethyl-6-chloro-2-(4'-iodophenyl)imidazo[1,2-b]pyridazine 1 (IC{sub 50} = 1.6 nM) and 3-benzamidomethyl-6-iodo-2-(4'-t-butylphenyl)imidazo[1,2-b] pyridazine 2 (IC{sub 50} = 4.2 nM), are high affinity and selective ligands for the peripheral benzodiazepine receptors (PBR) compared to the central benzodiazepine counterparts. The [{sup 123}I]1 and [{sup 123}I]2 labelled analogues of these compounds were subsequently synthesised for the potential study of the PBR in vivo using SPECT. Radioiodination of [{sup 123}I]1 was achieved by iododestannylation of the corresponding tributyl tin precursor with Na[{sup 123}I] in the presence of peracetic acid or chloramine-T and the product isolated by C-18 RP HPLC. Radioiodination of [{sup 123}I]2 was achieved by copper assisted bromine [{sup 123}I]iodine exchange of the corresponding bromo precursor in the presence of acetic acid and sodium bisulfate as reducing agent at 200 C. Purification of the crude products were achieved by semi-preparative C-18 RP HPLC to give the products in radiochemical yields > 90%. The products were obtained in > 97% chemical and radiochemical purity and with specific activities > 180 GBq/{mu}mol. (orig.)

  18. Synthesis and biological evaluation of one novel technetium-99m-labeled nitroquipazine derivative as an imaging agent for serotonin transporter

    Energy Technology Data Exchange (ETDEWEB)

    Guo Yunhang; Chen Xiangji; Jia Hongmei; Ji Xinmin [Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875 (China); Liu Boli [Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875 (China)], E-mail: liuboli@bnu.edu.cn

    2008-12-15

    Imaging of serotonin transporter (SERT) by positron emission tomography (PET) or single-photon emission-computed tomography (SPECT) in humans would provide useful information in diagnosis and therapy of several neurodegenerative and neuropsychiatric disorders. 6-Nitroquipazine is a highly potent and selective inhibitor of the SERT. For the development of new {sup 99m}Tc-labeled 6-nitroquipazine derivatives as SERT imaging agents, novel [N-[2-((3-(4-(6-nitroquinolin-2-yl)piperazin-1-yl)propyl)(2-mercaptoethyl) amino]-acetyl-2-aminoethanethiolato] [{sup 99m}Tc]technetium (V) oxide ({sup 99m}Tc-MAMA-3-PQ) and its rhenium analog were synthesized and characterized. {sup 99m}Tc-MAMA-3-PQ displayed high initial brain uptake (0.52% ID/organ at 2 min post-injection (pi)) and relatively fast washout in mice (0.09% ID/organ at 60 min pi). The regional brain distribution studies in rats showed high-specific binding ratios at 60 min pi. Maximum regional contrast ratio observed for thalamus/cerebellum was 2.94, followed by 2.62 for hypothalamus/cerebellum. These encouraging results lead us to further explore its derivatives as new imaging agents for the SERT in the brain.

  19. Synthesis and Evaluation of 18F-labeled Pyridaben Analogues for Myocardial Perfusion Imaging in Mice, Rats and Chinese mini-swine

    Science.gov (Uni