Radioisotope 45Ca labeling four calcium chemical compounds and tracing calcium bioavailability

International Nuclear Information System (INIS)

Zheng Hui; Zhen Rong; Niu Huisheng; Li Huaifen

2004-01-01

Objective: To build up a new method of the radioisotope 45 Ca labeling four calcium chemical compounds, observe and tracing bioavailability change of calcium labeled with radioisotope 45 Ca. Methods: The calcium gluconate (Ca-Glu), calcium citrate (Ca-Cit), calcium carbonate (Ca-Car) and calcium L-threonate (Ca-Thr)were labeled by radioisotope 45 Ca. Four calcium chemical compounds of 45 Ca labeling were used of calcium content 200 mg/kg in the rats and measure the absorption content and bioavailability of calcium in tissue of heart, lever spleen, stomach, kidney, brain, intestine, whole blood, urine, faeces. Results: 1) Radioisotope 45 Ca labeling calcium chemical compound has high radio intensity, more steady standard curve and recover rate. 2) The absorption of organic calcium chemical compounds is higher than the inorganic calcium chemical compound in the study of calcium bioavailability. Conclusion: The method of tracing with radioisotope 45 Ca labeling calcium chemical compounds has the characteristic of the sensitive, objective, accurate and steady in the study of calcium bioavailability

HAC and production of radioisotopes and labelled compounds

International Nuclear Information System (INIS)

Nozaki, T.

1984-01-01

In this paper, the author reviews different methods for the production of radioisotopes and labelled compounds that make use of hot atom reactions. Subsequently he discusses the production of radioisotopes for radiopharmaceuticals; enrichment of (n,γ) products, recoil labelling and related methods (neutron reaction products, cyclotron production, excitation labelling, radiation and discharge induced labelling). The final section offers a survey of radioisotope production using accelerators. Only a selection of the various conditions used in practical RI production is considered. (Auth.)

Studies on the preparation of radioactive labelled compounds

International Nuclear Information System (INIS)

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

1985-04-01

To deveolp 99 mTc instant labelling kits of dimercaptosuccinic acid (DMSA), glucoheptonic acid (GH), and tin colloid, molar ratios of the host compound to the stannous chloride, amount of the stannous chloride and pH were, respectively, controlled. The labelling yields and radiochemical purities were checked by means of a paper chromatography. Animal studies and clinical applications were also carried out. The results indicated that DMSA/SnCl 2 2H 2 O 3/1(mole/mole), SnCl 2 2H 2 O 410ug/ml/vial, pH 2.5, Ca GH/SnCl 2 2H 2 O 53/1(mole/mole), SnCl 2 2H 2 O 350 ug/ml/vial, pH 6.5, NaF 100ug/vial, SnCl 2 2H 2 O 150 ug/ml/vial, pH. 5.6 etc, were optimal conditions for the preparation of DMSA-, GH-, and tin colloid-kits, respectively. (Author)

Clinical applications of cells labelling

International Nuclear Information System (INIS)

Gonzalez, B.M.

1994-01-01

Blood cells labelled with radionuclides are reviewed and main applications are described. Red blood cell labelling by both random and specific principle. A table with most important clinical uses, 99mTc labelling of RBC are described pre tinning and in vivo reduction of Tc, in vitro labelling and administration of labelled RBC and in vivo modified technique. Labelled leucocytes with several 99mTc-complex radiopharmaceuticals by in vitro technique and specific monoclonal s for white cells(neutrofiles). Labelled platelets for clinical use and research by in vitro technique and in vivo labelling

131/123 iodine labeled benzamides for the detection of melanomas and metastases. Synthesis, labeling, animal experiences and preliminary clinical studies

International Nuclear Information System (INIS)

Pozzi, Oscar R.; Edreira, Martin M.; Castiglia, Silvia G.; Soroa, Victoria E.

1999-01-01

Radioiodine labeled benzamides are being studied as radiopharmaceuticals for the detection of melanomas and metastases. With this purpose the synthesis and labeling of N-(2-diethylaminoethyl)-3-[ 131 I]-4-methoxybenzamide (IMBA) has been carried out. Tissue distribution of the labeled compound has been studied in C 57 mice, showing a fast renal excretion. The labeled benzamide was also injected in mice with previously induced subcutaneous melanomas and lung metastases using B 16-F0 murine melanoma cells. The tumors show a good uptake of the labeled benzamide. The melanoma/other tissues uptake ratio is suitable for scintigraphic detection. Clinical studies in patients are under way. (author)

Biokinetics and dosimetry of radioactively labelled organic C-14 compounds

International Nuclear Information System (INIS)

Krins, A.; Sahre, P.; Schoenmuth, T.

2003-12-01

The report starts with summarising research work and the resulting scientific information in connection with the dosimetry of C-14 labelled organic compounds. Biokinetic models are developed for compounds such as benzene, phenol, aniline, nitrobenzene, and a selection of pharmaceuticals, in order to show the radioactivity distribution after administration of the C-14 labelled substances. Based on the those models, dose coefficients and excretion rates are derived. The following synoptic view of the available data library leads on to a discussion of various aspects, as eg. the question of whether and how monitoring for detection of incorporation of C-14 administered with labelled organic compounds is possible. None of the questions and aspects arising in connection with this subject can be adequately dealt with in the present document, but concepts and methods are presented which permit an interpretation of radioactivity excretion data measured after incorporation of C-14 labelled organic substances. (orig./CB) [de

Some methods for labelling organic compounds by deuterium

International Nuclear Information System (INIS)

Moustapha, C.

1988-01-01

The rapid growth of knowledge in the fields of biochemistry, physiology, and molecular biology reflects to a considerable degree the utilization of stable isotopes (specially deuterium) in the study of chemical reactions and fragmentation mechanisms in mass spectrometry, as well as in the pharmacological and biological studies. Organic compounds maybe labelled by deuterium through classic organic reactions by using special deuterated solvents and reagents. This article discusses some reactions, with examples on how to prepare labelled compounds with high isotopic purety. These reactions are: exchange reactions in acid and alkaline media (the exchange in the chromatographic column in liquid and gas phases, the exchange in homogenous medium), reduction reactions of functional groups as well as saturation of the double bounds by deuterium using hydrogenation catalystes, electrochemical reactions using KOLBE, and photochemical reactions. This article also deals with spectroscopic properties of deuterium and the methods which are used to identify its compounds such as infrared, nuclear magnetic resonance, and mass spectroscopy. 37 refs., 2 figs

Production of radionuclides and preparation of labelled compounds. Nuclear chemical technology

International Nuclear Information System (INIS)

Anon.

1976-01-01

A general review is presented of methods of producing radionuclide preparations and labelled compounds, such as their production from natural raw materials, from a nuclear reactor, a particle accelerator, and using radioisotope generators. Also described are the fundamental kinetic relations of nuclear reactions. Basic methods are surveyed of obtaining labelled compounds by chemical synthesis, biosynthesis, exchange reactions, recoil reactions, by the Wilzbach method and the Szillard-Chalmers reaction. (L.K.)

Preparation of 125I labelled compound

International Nuclear Information System (INIS)

Rafii, H.; Beiki, D.; Matlubi, M.; Jalilian, A.R.; Motamedi, F.; Karimian, A.R.; Najafi, R.; Babaei, M.; Kamali Dehghan, M.; Shah-Hossaini, G.R.; Shafahi, S.K.; Keshavarzi, F.

2002-01-01

Iodinated compounds with 131 I, 125 I and 123 I have been widely used for biochemical function studies. In conjunction with SPECT, [ 123 I] labelled proteins have various diagnostic and therapeutic applications in nuclear medicine. In this study, synthesis and quality control of [ 18 F]radiofluorinated and radioiodinated of some proteins and peptides as well as their biological behaviors are considered to be investigated. (author)

Metabolism of [14C]bicarbonate by Streptococcus lactis: identification and distribution of labelled compounds

International Nuclear Information System (INIS)

Hillier, A.J.; Jago, G.R.

1978-01-01

Streptococcus lactis C10, grown in tryptone-yeast extract-lactose broth containing [ 14 C] bicarbonate, incorporated radioactivity into the protein and nucleic acid fractions of the cell as well as into compounds which were excreted by the organism into the growth medium. Aspartic acid was the first compound to be labelled and was the only amino acid labelled in the cell protein. All 4 bases were labelled in the cell RNA. Aspartic, succunuc and lactic acids were the radioactive compounds excreted into the growth medium. (U.K.)

Synthesizing labeled compounds

International Nuclear Information System (INIS)

London, R.E.; Matwiyoff, N.A.; Unkefer, C.J.; Walker, T.E.

1983-01-01

A metabolic study is presented of the chemical reactions provided by isotopic labeling and NMR spectroscopy. Synthesis of 13 C-labeled D-glucose, a 6-carbon sugar, involves adding a labeled nitrile group to the 5-carbon sugar D-arabinose by reaction with labeled hydrogen cyanide. The product of this reaction is then reduced and hydrolyzed to a mixture of the labeled sugars. The two sugars are separated by absorption chromotography. The synthesis of 13 C-labeled L-tyrosine, an amino acid, is also presented

3. Production of radionuclides, preparation and handling of labelled compounds

International Nuclear Information System (INIS)

Toelgyessy, J.

1981-01-01

The preparation of natural radioactive compounds and the manufacture of artificial radionuclides, the labelling of organic compounds, and the methods of radioactive substance separation are described. The principles are shown of handling radioactive materials and a brief description is given of the stability, packaging and storage of radiopharmaceuticals. (J.P.)

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).

Radio-labelled quaternary compounds and their diagnostic use

International Nuclear Information System (INIS)

Woo, D.V.

1984-01-01

Radio-labelled compounds having a lipophilic cation, which are quaternary ammonium, phosphonium or arsonium halides, in which the halide is a chloride, bromide or iodide, and in which the four quaternary substituents are independently selected from Csub(1-3) alkyl, phenyl and benzyl, at least two substituents being phenyl or benzyl, and one phenyl or benzyl substituent carrying a ring-substituent selected from 123 I, 125 I, 131 I, 77 Br, 82 Br and 18 F. Such compounds can be administered by injection, and a radio-image of the myocardium obtained. (author)

Synthesis of uniformly labelled organic compounds by polymerization of 14C ethylene

International Nuclear Information System (INIS)

Dauphin, J.-F.

1972-01-01

The synthesis of 14 C uniformly labelled compounds is described. By polymerization of 14 C ethylene, linear olefins with a double bond at α position were obtained. From these olefins, uniformly labelled alkanes, alcohols and acids were prepared [fr

Extraction of carbon 14-labeled compounds from plant tissue during processing for electron microscopy

International Nuclear Information System (INIS)

Coetzee, J.; van der Merwe, C.F.

1989-01-01

Loss of 14 C-labeled compounds from bean leaf tissue was monitored during all the stages of routine specimen preparation. No significant differences in extraction were associated with the use of acetone, ethanol, or dioxane as dehydration fluids. Fixation at low temperature increased the loss of label. Prolonged fixation in glutaraldehyde increased the loss, but fixation in osmium solutions for periods as long as 4 hr had no influence on extraction. Buffer rinses and dehydration fluids caused appreciable amounts of label to be extracted. The use of propylene oxide as transition fluid resulted in low extraction. Some embedding media caused the loss of small amounts of labeled compounds, but one of the media tested (LR-white) extracted significant amounts of label

Process for the production of 14C-labelled compounds

International Nuclear Information System (INIS)

Oldham, K.G.; Carr, N.G.

1978-01-01

The patent describes the production of 14 C-labelled compounds from solution with the aid of algae. A microorganism of the Anacystic species is used, preferably Anacystis nidulans which is also known as 'Indiana 625'. The experiments and their results are described in detail. (UWI) [de

Dynamics of growth/mature-related substances in vegetables using specific triple labeled compound

International Nuclear Information System (INIS)

Yamato, Yoichi; Hamano, Megumi; Yamazaki, Hiroko; Miura, Hiroyuki

2000-01-01

To progress physiological studies of vegetables, development of biosynthetic method for production of triple labeled compounds was attempted in this study and such method for vegetables using specifically labeled sugars was examined. As a sugar compound, 6-C 14 -glucose (14-CG) and 1-H 3 -glucose (3-HG) were given to culture medium for cells derived from tomato embryonic axis and the changes of these compounds were monitored. Tomato embryonic cells were harvested 20 and 44 hours after the addition of 14-CG or 3-CG into the culture medium the cells. The cells were homogenized and the supernatant after centrifugation was applied onto HPLC. Radio analyzer revealed major two peaks in the chromatography of the sugar fraction from the cells after 20 hours from the addition of 14-CG. One was the peak of glucose, itself and the other was estimated to be that of fructose based on the retention time. Whereas in the elution pattern of the sugar fraction after 44 hours from the addition, a peak of sucrose was found along with the peak of glucose. These results indicate that C 14 in 14-CG but not H 3 in 3-HG was transferred into fructose after the metabolism in tomato. Moreover, in both elution patterns, there was a peak positioned at the same retention time, indicating that the compound in this peak was produced from either of 14-CG or 3-HG. Therefore, it is thought that H 3 and C 14 double-labeled compound could be produced from the cell culture added with both labeled compounds; 14-CG and 3-HG. (M.N.)

Improvement of organic compounds labelling method with the use of thermally activated tritium gas

International Nuclear Information System (INIS)

Nejman, L.A.; Smolyakov, V.S.; Antropova, L.P.

1982-01-01

Use of a support (various types of papers) is recommended for organic compounds labelling by tritium gas activated at a hot tungsten filament. This improvement increases chemical and radiochemical yields and makes the experiment simpler and faster. Generally labelled triethyloxonium tetra-fluoroborate, ethyl-p-aminobenzoate, p-aminobenzoic acid (Na-salt), A-factor (a natural regulator of streptomycin biosynthesis), decapeptide angiotensin I, phospholipid 1, 2 - dimyristoyl-sn-glycero-3--phosphocholine and E. coli tRNAs have been prepared by this method. Molar radioactivity of the labelled compounds is in the range of 1-200 GBg/mmole [ru

Some aspects of the analysis of labelled organic compounds by gas radiochromatography

International Nuclear Information System (INIS)

Heise, K.H.; Gorner, Ch.; Bubner, M.

1977-01-01

The first experience with the analysis of tritium-and 14 C-labelled compounds by gas radiochromatography are reported. The instrumental arrangement is described where, on the chromatograph output, the radioactive compounds are burnt, and the radioactive gases are measured by scintillation detectors in a coincidence circuit

Studies on the preparation of labelled compounds for γ scintigraphy use

International Nuclear Information System (INIS)

Kim, Jae Rok; Awh, Ok Doo; Park, Kyung Bae; Han, Kwang Hee; Park, Woong Woo

1990-02-01

To develop Tc-99m labelling kits of hepatobiliary agents such as IOTIDA and IODIDA, the raw materials were synthesized and the conditions for labelling were optimized. Similar experiments were also conducted for I-131 MIBG of diagnostic use and for stannous MDP, the typical in-vivo labelling agent for RBC. The synthesis yield of IOTIDA and IODIDA were 42 % and 50 %, respectively from the starting materials 2,3,6-trimethylaniline and 2,6-diethylaniline. It has been confirmed that Tc-99m labelling yield of IDA compounds were almost quantitative under optimized conditions and they were excreted mostly through hepatobiliary track. MIBG were synthesized 62 % yield from m-iodobenzylaminehydrochloride and labelled with I-131 almost quantitatively (>98 %). It has been confirmed that p-aminobenzoic acid is an effrective antioxidant for the Tc-99m-MDP. (author)

Labelling of some organic compounds with radioiodine and technetium-99m

Energy Technology Data Exchange (ETDEWEB)

Bayoumy, A A M

1994-07-01

Amino acids have received significant attention in the evaluation of serotonergic and dopaminergic functions in the central nervous system. the wide distribution of {gamma}-cameras and SPECT create an increasing need for appropriated labelled radiopharmaceuticals . {sup 99m}Tc and {sup 123}I are the most important radionuclides for this purpose. In order to avoid pharmacological and toxicological effects, the radiolabelled compounds must be often produced with high specific activity. In the first part of this thesis, the work is therefore focused on labelling methods with no carrier added radioiodine. The radioiodinated analogues of two amino acids were chosen as model compounds of research. L-m-tyrosine is potentially useful for the evaluation of dopamine metabolism in Parkinson's disease, while L -{alpha} -methyl tyrosine is a well known indicator of amino acid transport useful for tumor studies.

Radioiodine and its labelled compounds

International Nuclear Information System (INIS)

Robles, Ana Maria

1994-01-01

Chemical characteristics and their nuclear characteristics, types of labelled molecules,labelling procedures, direct labelling with various oxidizing agents, indirect labelling with various conjugates attached to protein molecules, purification and quality control. Iodination damage.Safe handling of labelling procedures with iodine radioisotopes.Bibliography

Adsorption chromatographic separation of radioiodine-labelled compounds using binary eluents

International Nuclear Information System (INIS)

Toth, G.

1980-01-01

An adsorption chromatographic method using Sephadex LH-20 dextran gel as adsorbent and water-organic solvent binary eluents was developed for the systematic separation of low molecular weight radioiodine-labelled substances like iodothyronines, iodobenzoic acids and iodotyrosine methyl ester derivatives of prostaglandins, steroids etc. The adsorbed iodine compounds were separated by water-organic solvent mixture, and the order of the compounds is in accordance with the increasing number of iodine substituents per molecule. A method is reported which enables the calculation of the eluent strength of the water-organic solvent eluents. (author)

Radioiodine-labelled compounds previously or currently used for tumour localization

International Nuclear Information System (INIS)

Beierwaltes, W.H.

1976-01-01

131 I-labelled human serum albumin, though not used for tumour localization today, is an excellent ''standard'' with which to compare uptake of ''tumour-specific'' radiolabelled compounds. 131 I-labelled fibrinogen and antibodies to fibrinogen have a non-specific uptake in tumours. Nungester, Beierwaltes and Knorpp are credited by Mahaley as first treating a human for cancer with 131 I-labelled antibody globulins (malignant melanoma). Although many theoretical problems remain in obtaining diagnostic localization of 131 I-IgG, Quinones, Mizejewski and Beierwaltes demonstrated the uptake of 131 I-labelled immune antibodies in Syrian hamster cheeck pouch with chorionic gonadotropic hormone as the specific tumour-associated antigen. This model was then used successfully by Goldenberg and Hoffer for demonstrating colon carcinoma by using antibodies to carcinoembryonic antigen. A 131 I-labelled chloroquine analogue, synthesized by Counsell, has been demonstrated by Beierwaltes et al. to concentrate diagnostically and therapeutically in the malignant melanotic melanoma. 131 I-19-iodocholesterol, synthesized by Counsell, has been demonstrated by Beierwaltes et al. to concentrate diagnostically in the human adrenal cortex. It has many unique diagnostic capabilities not available with other routine diagnostic methods available today. (author)

The metabolism and dosimetry of carbon-14 labelled compounds

International Nuclear Information System (INIS)

Crawley, F.E.H.

1977-01-01

The number of compounds labelled at high specific activity with carbon-14 has greatly increased over the last few years. There are limited biological data available to enable an assessment of the internal radiation dose and to identify the critical tissues after an intake of such compounds. The ICRP consider two Model Systems for deriving dose. Both Models assume a total elimination of the carbon-14 in the breath and only bone or whole body as critical tissues and are not representative of the majority of the compounds now available. A research programme has been established to study the rate of excretion and tissue distribution of selected carbon-14 labelled compounds in the rat after intravenous injection, pulmonary and gastric intubation and skin absorption. These metabolic data have been used to calculate the committed dose equivalent and maximum permissible annual intake (MPAI) for various tissues in man on the assumption that the experimental data obtained in the rat are true for man. To date potassium 14 C-cyanide and 14 C-methanol have been studied. The values for the MPAI's derived from the doses to individual tissues are more restrictive than values calculated from the whole body doses. The MPAI calculated from excretion data in terms of whole body dose is 31 mCi for 14 C-cyanide and 25 mCi for 14 C-methanol. However, the critical tissue for 14 C-cyanide is the stomach with an MPAI of 1.5 mCi based on a dose of 10.7 rem mCi -1 . This was an order of magnitude greater than the dose to any other region of the GI tract and 5 times that to the testis. The critical organs for 14 C-methanol are the testis (MPAI 2.5 mCi) for males and the ovaries (MPAI 6.2 mCi) for females

Clinical applications of cells labelling; Aplicaciones clinicas del marcado de celulas

Energy Technology Data Exchange (ETDEWEB)

Gonzalez, B M [Instituto Nacional de Pediatria (Mexico)

1994-12-31

Blood cells labelled with radionuclides are reviewed and main applications are described. Red blood cell labelling by both random and specific principle. A table with most important clinical uses, 99mTc labelling of RBC are described pre tinning and in vivo reduction of Tc, in vitro labelling and administration of labelled RBC and in vivo modified technique. Labelled leucocytes with several 99mTc-complex radiopharmaceuticals by in vitro technique and specific monoclonal s for white cells(neutrofiles). Labelled platelets for clinical use and research by in vitro technique and in vivo labelling.

Aziridines in the synthesis of 11C- and 18F-labelled compounds

International Nuclear Information System (INIS)

Gillings, N.M.

1998-01-01

Racemic [4- 11 C]aspartic acid, [4- 11 C]asparagine and 2,4-diamino[4- 11 C]butyric acid were synthesised by the ring-opening of an N-activated aziridine-2-carboxylate with 11 C]cyanide, followed by preparative HPLC and hydrolysis/reduction. These labelled amino acids arise from nucleophilic attack at the β-carbon of the aziridine ring. A radioactive by-product of ca. 25% was attributed to the product of α-attack. Several N-activated 2-aryl aziridines were synthesised for the attempted synthesis of β-[ 18 F] fluorophenylalanine and β-[ 18 F]fluorodopa. Ring-opening with [ 18 F]fluoride showed no evidence of β-fluorinated products and it is proposed that attack occurs exclusively at the α-carbon, giving the corresponding α-[ 18 F]fluoro-β-amino acids. Further evidence for this was the reaction of the β-unsubstituted N-activated aziridine-2-carboxylate with [ 18 F]fluoride. This reaction was totally regiospecific and afforded exclusively the α-substituted product, α-[ 18 F]fluoro-β-alanine. Aziridine precursors were resolved by chiral HPLC. On labelling the chiral aziridines, however, racemic 11 C- and 18 F-labelled amino acids were obtained. This was attributed to racemisation of the initially formed ring-opened products. The use of [ 11 C]methyl lithium as a nucleophile for aziridine ring-opening was investigated. Reaction was expected to occur at low temperature, thus potentially avoiding racemisation. No products corresponding to aziridine ring-opening with [ 11 C]methyl lithium were, however, observed. A difluorinated analogue of amphetamine was synthesised by fluorination of an azirine (via an aziridine). This racemic compound was resolved as its chiral tartarate salts and subsequently labelled by methylation with [ 11 C]methyl iodide, giving the novel compound β, β-difluoro[N-methyl- 11 C]methamphetamine in high specific activity for in vivo binding studies using positron emission tomography. The non-radioactive reference compound was also

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

International Nuclear Information System (INIS)

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

1981-01-01

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

Deuterium- and tritium-labelled compounds. Applications in the life sciences

International Nuclear Information System (INIS)

Atzrodt, Jens; Derdau, Volker; Kerr, William J.; Reid, Marc

2018-01-01

Hydrogen isotopes are unique tools for identifying and understanding biological and chemical processes. Hydrogen isotope labelling allows for the traceless and direct incorporation of an additional mass or radioactive tag into an organic molecule with almost no changes in its chemical structure, physical properties, or biological activity. Using deuterium-labelled isotopologues to study the unique mass-spectrometric patterns generated from mixtures of biologically relevant molecules drastically simplifies analysis. Such methods are now providing unprecedented levels of insight in a wide and continuously growing range of applications in the life sciences and beyond. Tritium ( 3 H), in particular, has seen an increase in utilization, especially in pharmaceutical drug discovery. The efforts and costs associated with the synthesis of labelled compounds are more than compensated for by the enhanced molecular sensitivity during analysis and the high reliability of the data obtained. In this review, advances in the application of hydrogen isotopes in the life sciences are described. (copyright 2018 Wiley-VCH Verlag GmbH and Co. KGaA, Weinheim)

Cu2+-labeled dansyl compounds as fluorescent and PET probes for imaging apoptosis.

Science.gov (United States)

Han, Junyan; Wang, Xukui; Yu, MeiXiang

2016-11-15

Compound DNSTT-Cu 2+ , a novel chelate of Cu 2+ with DOTA conjugated to a fluorescent dansyl fragment, is developed for imaging cell apoptosis. Apoptotic U-87MG cells could be selectively visualized by the fluorescence of DNSTT-Cu 2+ from cytoplasm of cells, confirmed by the fluorescence of apoptosis cells co-labeled with Alexa Fluor 568-labeled annexin V, a conventional probe for selectively labeling membranes of apoptosis cells. A radioactive 64 Cu 2 + analog, DNSTT- 64 Cu 2+ , was easily synthesized, providing a potential PET probe for imaging apoptosis in vivo. Copyright © 2016 Elsevier Ltd. All rights reserved.

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

International Nuclear Information System (INIS)

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

1984-01-01

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

Synthesis and analysis of 14C-labelled butyltin compounds

International Nuclear Information System (INIS)

Kloetzer, D.

1976-01-01

This paper deals with methods for the synthesis of 14 C-labelled analoga of the important biocides tributyltin oxide, tributyltin benzoate, tributyltin salicylate and tributyltin fluoride as well as dibutyltin oxide. The radioactive starting substance butylbromide-1- 14 C is treated with sodium and monobutyltin chloride or tin tetrachloride to form a mixture of radioactive butyltin compounds from which the substance desired is separated. A system satisfactorily meeting the conditions for thin-layer radiochromatography is presented. (author)

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.

Increase in the specific radioactivity of tritium-labeled compounds obtained by tritium thermal activation method

International Nuclear Information System (INIS)

Badun, G.A.; Chernysheva, M.G.; Ksenofontov, A.L.

2012-01-01

A method of tritium introduction into different types of organic molecules that is based on the interaction of atomic tritium with solid organic target is described. Tritium atoms are formed on the hot W-wire, which is heated by the electric current. Such an approach is called 'tritium thermal activation method'. Here we summarize the results of labeling globular proteins (lysozyme, human and bovine serum albumins); derivatives of pantothenic acid and amino acids; ionic surfactants (sodium dodecylsulfate and alkyltrimethylammonium bromides) and nonionic high-molecular weight surfactants - pluronics. For the first time it is observed that if the target-compound is fixed and its radicals are stable the specific radioactivity of the labeled product can be drastically increased (up to 400 times) when the target temperature is ca. 295 K compared with the results obtained at 77 K. The influence of labeling parameters as tritium gas pressure, exposure time and W-wire temperature was tested for each target temperature that results in the optimum labeling conditions with high specific radioactivity and chemical yield of the resulting compound. (orig.)

Deuterium- and tritium-labelled compounds. Applications in the life sciences

Energy Technology Data Exchange (ETDEWEB)

Atzrodt, Jens; Derdau, Volker [Isotope Chemistry and Metabolite Synthesis, Integrated Drug Discovery, Medicinal Chemistry, Frankfurt (Germany); Kerr, William J.; Reid, Marc [Department of Pure and Applied Chemistry, WestCHEM, University of Strathclyde, Glasgow (United Kingdom)

2018-02-12

Hydrogen isotopes are unique tools for identifying and understanding biological and chemical processes. Hydrogen isotope labelling allows for the traceless and direct incorporation of an additional mass or radioactive tag into an organic molecule with almost no changes in its chemical structure, physical properties, or biological activity. Using deuterium-labelled isotopologues to study the unique mass-spectrometric patterns generated from mixtures of biologically relevant molecules drastically simplifies analysis. Such methods are now providing unprecedented levels of insight in a wide and continuously growing range of applications in the life sciences and beyond. Tritium ({sup 3}H), in particular, has seen an increase in utilization, especially in pharmaceutical drug discovery. The efforts and costs associated with the synthesis of labelled compounds are more than compensated for by the enhanced molecular sensitivity during analysis and the high reliability of the data obtained. In this review, advances in the application of hydrogen isotopes in the life sciences are described. (copyright 2018 Wiley-VCH Verlag GmbH and Co. KGaA, Weinheim)

Copper-catalyzed oxidative desulfurization-oxygenation of thiocarbonyl compounds using molecular oxygen: an efficient method for the preparation of oxygen isotopically labeled carbonyl compounds.

Science.gov (United States)

Shibahara, Fumitoshi; Suenami, Aiko; Yoshida, Atsunori; Murai, Toshiaki

2007-06-21

A novel copper-catalyzed oxidative desulfurization reaction of thiocarbonyl compounds, using molecular oxygen as an oxidant and leading to formation of carbonyl compounds, has been developed, and the utility of the process is demonstrated by its application to the preparation of a carbonyl-18O labeled sialic acid derivative.

Isotopically modified compounds

International Nuclear Information System (INIS)

Kuruc, J.

2009-01-01

In this chapter the nomenclature of isotopically modified compounds in Slovak language is described. This chapter consists of following parts: (1) Isotopically substituted compounds; (2) Specifically isotopically labelled compounds; (3) Selectively isotopically labelled compounds; (4) Non-selectively isotopically labelled compounds; (5) Isotopically deficient compounds.

131/123 iodine labeled benzamides for the detection of melanomas and metastases. Synthesis, labeling, animal experiences and preliminary clinical studies; Benzamidas marcadas con 131/123 iodo para deteccion de melanomas y metastasis. Sintesis, marcacion, estudio en animales y primeros estudios clinicos

Energy Technology Data Exchange (ETDEWEB)

Pozzi, Oscar R; Edreira, Martin M; Castiglia, Silvia G [Comision Nacional de Energia Atomica, Ezeiza (Argentina). Dept. de Radioquimica; Zarlenga, Ana C; Arashiro, Jorge G; Parma, P [Instituto de Oncologia Angel H. Roffo, Buenos Aires (Argentina); Soroa, Victoria E [Hospital Clinicas Jose de San Martin, Buenos Aires (Argentina)

1999-07-01

Radioiodine labeled benzamides are being studied as radiopharmaceuticals for the detection of melanomas and metastases. With this purpose the synthesis and labeling of N-(2-diethylaminoethyl)-3-[{sup 131}I]-4-methoxybenzamide (IMBA) has been carried out. Tissue distribution of the labeled compound has been studied in C 57 mice, showing a fast renal excretion. The labeled benzamide was also injected in mice with previously induced subcutaneous melanomas and lung metastases using B 16-F0 murine melanoma cells. The tumors show a good uptake of the labeled benzamide. The melanoma/other tissues uptake ratio is suitable for scintigraphic detection. Clinical studies in patients are under way. (author)

Ior-CEA-1: Labelling, quality control and clinical evaluation

International Nuclear Information System (INIS)

Pimentel, G.J.

1998-01-01

Within the Co-ordinated Programme on Labelling, Quality Control and Evaluation of Monoclonal Antibodies, the IAEA has made a great effort to expand efficient labelling methods, mainly those with radioisotopes which have been used for radioimmunoscintigraphy. In this sense, more recently 99 Tc m has been mostly employed in the majority of the investigations due to its ideal physical characteristics. Efficient labelling of monoclonal antibodies depends on a number of factors including the method and way of the label incorporation into the protein. During the last years several direct labelling approaches have been developed, which led to attain simple and inexpensive methods for medical practice, as well as safe and stable techniques which bring accurate and good quality images. Accordingly, this paper describes the results obtained during last five years which come from the comparison among different labelling systems, passing through the quality control to test the labelled monoclonal stability and the protein bioreactivity, to continue in the clinical evaluation of ior-CEA-1, as well as the evaluation of other antibodies. Up to now we have evaluated more than 70 patients with the anti-CEA monoclonal antibody (ior-CEA-1), examined in different clinical assays such as: pilot, phase I-II and extensive phase III-IV trials, whose results are encouraging. It confirms that the employed labelling approach was safe and adequate

Aziridines in the synthesis of {sup 11}C- and {sup 18}F-labelled compounds

Energy Technology Data Exchange (ETDEWEB)

Gillings, N.M

1998-07-01

Racemic [4-{sup 11}C]aspartic acid, [4-{sup 11}C]asparagine and 2,4-diamino[4-{sup 11}C]butyric acid were synthesised by the ring-opening of an N-activated aziridine-2-carboxylate with [{sup 11}C]cyanide, followed by preparative HPLC and hydrolysis/reduction. These labelled amino acids arise from nucleophilic attack at the {beta}-carbon of the aziridine ring. A radioactive by-product of ca. 25% was attributed to the product of {alpha}-attack. Several N-activated 2-aryl aziridines were synthesised for the attempted synthesis of {beta}-[{sup 18}F] fluorophenylalanine and {beta}-[{sup 18}F]fluorodopa. Ring-opening with [{sup 18}F]fluoride showed no evidence of {beta}-fluorinated products and it is proposed that attack occurs exclusively at the {alpha}-carbon, giving the corresponding {alpha}-[{sup 18}F]fluoro-{beta}-amino acids. Further evidence for this was the reaction of the {beta}-unsubstituted N-activated aziridine-2-carboxylate with [{sup 18}F]fluoride. This reaction was totally regiospecific and afforded exclusively the {alpha}-substituted product, {alpha}-[{sup 18}F]fluoro-{beta}-alanine. Aziridine precursors were resolved by chiral HPLC. On labelling the chiral aziridines, however, racemic {sup 11}C- and {sup 18}F-labelled amino acids were obtained. This was attributed to racemisation of the initially formed ring-opened products. The use of [{sup 11}C]methyl lithium as a nucleophile for aziridine ring-opening was investigated. Reaction was expected to occur at low temperature, thus potentially avoiding racemisation. No products corresponding to aziridine ring-opening with [{sup 11}C]methyl lithium were, however, observed. A difluorinated analogue of amphetamine was synthesised by fluorination of an azirine (via an aziridine). This racemic compound was resolved as its chiral tartarate salts and subsequently labelled by methylation with [{sup 11}C]methyl iodide, giving the novel compound {beta}, {beta}-difluoro[N-methyl-{sup 11}C]methamphetamine in high

Indirect spectrophotometric determination of BIDA, DISIDA, DTPA and MDP in labelled compounds

International Nuclear Information System (INIS)

Van der Walt, T.N.; Coetzee, P.P.

1989-01-01

N-(4-(n-butyl)acetanilide)iminodiacetic acid (BIDA), N-(2,6-diisopropylacetanilide)iminodiacetic acid (DISDA), diethylenetriaminepentaacetic acid (DTPA) and methylene diphosphonic acid (MDP) are used in labelling kits. The contents of BIDA, DISIDA or MDP of the 99m Tc-labelled compounds can be determined (indirectly) spectrophotometrically with copper, eriochrome cyanine R (ECC) and dodecyl-ethyldimethylammonium bromide (DEDA) in a sodium barbital buffered system at pH 8.5. The calibration curves obey Beer's Law from 0 to 40 μg/25 mL for BIDA and DISIDA, 0 to 60 μg/25 mL for DTPA and 0 to 100 μg/10 mL for MDP. (author)

The physical and chemical characteristics of 175Yb-EDTMP labelled compound

International Nuclear Information System (INIS)

Azmairit Aziz; Marlina; Muhammad Basit Febrian

2010-01-01

Bone pain is a common complication for patient with bone metastases from breasts, prostate and lung cancers. The derivative of phosphonate groups, i.e. diphosphonate as well as poly phosphonate ligands e.g. EDTMP have high affinity in bone matrix. The labeled compound of 175 Yb-EDTMP can be used as an alternative radiopharmaceutical for bone pain palliation. The compound of 175 Yb-EDTMP can be produced by labeling of ethylenediamine tetramethylene phosphonic acid (EDTMP) with itterbium-175 ( 175 YbCl 3 ). Before 175 Yb-EDTMP is used for bone pain palliation in nuclear medicine, the compound have to be characterized to full fill the criteria of the good radiopharmaceutical. The physical and chemical characteristics of 175 Yb-EDTMP had been studied. It consists of: pH, solution clearity, the radiochemical purity that was determined by paper chromatography and paper electrophoresis techniques, electricity charge was determined by paper electrophoresis, stability, lipophilicity of 175 Yb-EDTMP was obtained by determination of octanol-water partition and the plasma binding protein was in-vitro investigated with precipitation method using 5% of trichloroacetic acid solution, and the binding to hydroxyapatite. From the experiment, it was obtained that the 175 Yb-EDTMP solution has the pH of 7, clear, the radiochemical purity of 98.66 ± 0.53%, and the negative electric charge. The compound of 175 Yb-EDTMP has lipophilicity (P) of 0.0135 ± 0.003%, the human plasma binding protein of 8.94 ± 0.66%, and the hydroxyapatite binding of 94.78 ± 2.16%. Stability evaluation indicated that 175 Yb-EDTMP solution was still stable for nine days at room temperature with the radiochemical purity more than 95% (98.62 ± 0.83%). This study expects that 175 Yb-EDTMP compound can fulfill the requirement as radiopharmaceutical for use in palliative treatment of painful bone metastases and supports the development of nuclear medicine in Indonesia. (author)

Possible application of labelled compounds in plant physiology, biochemistry and protection

International Nuclear Information System (INIS)

Hanker, I.

1981-01-01

Compounds labelled with 14 C, 32 P, 35 S, 54 Mn, 45 Ca, 65 Zn and 86 Rb were used for the study of side effects of insecticides, fungicides, herbicides and other substances used for the treatment of crop plants, of the effects of some plant diseases on biochemical processes in plants, and of the reasons of plant resistance to diseases, i.e., of factors responsible for this resistance. (author)

Indirect spectrophotometric determination of BIDA, DISIDA, DTPA and MDP in labelled compounds

Energy Technology Data Exchange (ETDEWEB)

Van der Walt, T.N.; Coetzee, P.P. (Rand Afrikaans Univ., Johannesburg (South Africa). Dept. of Chemistry); Fourie, P.J. (Atomic Energy Corp. of South Africa (Pty) Ltd., Pretoria (South Africa))

1989-01-01

N-(4-(n-butyl)acetanilide)iminodiacetic acid (BIDA), N-(2,6-diisopropylacetanilide)iminodiacetic acid (DISDA), diethylenetriaminepentaacetic acid (DTPA) and methylene diphosphonic acid (MDP) are used in labelling kits. The contents of BIDA, DISIDA or MDP of the {sup 99m}Tc-labelled compounds can be determined (indirectly) spectrophotometrically with copper, eriochrome cyanine R (ECC) and dodecyl-ethyldimethylammonium bromide (DEDA) in a sodium barbital buffered system at pH 8.5. The calibration curves obey Beer's Law from 0 to 40 {mu}g/25 mL for BIDA and DISIDA, 0 to 60 {mu}g/25 mL for DTPA and 0 to 100 {mu}g/10 mL for MDP. (author).

Possible application of labelled compounds in plant physiology, biochemistry and protection

Energy Technology Data Exchange (ETDEWEB)

Hanker, I. (Vyzkumne Ustavy Rostlinne Vyroby, Prague (Czechoslovakia). Ustav Ochrany Rostlin)

1981-06-01

Compounds labelled with /sup 14/C, /sup 32/P, /sup 35/S, /sup 54/Mn, /sup 45/Ca, /sup 65/Zn and /sup 86/Rb were used for the study of side effects of insecticides, fungicides, herbicides and other substances used for the treatment of crop plants, of the effects of some plant diseases on biochemical processes in plants, and of the reasons of plant resistance to diseases, i.e., of factors responsible for this resistance.

Multi-label classifier based on histogram of gradients for predicting the anatomical therapeutic chemical class/classes of a given compound.

Science.gov (United States)

Nanni, Loris; Brahnam, Sheryl

2017-09-15

Given an unknown compound, is it possible to predict its Anatomical Therapeutic Chemical class/classes? This is a challenging yet important problem since such a prediction could be used to deduce not only a compound's possible active ingredients but also its therapeutic, pharmacological and chemical properties, thereby substantially expediting the pace of drug development. The problem is challenging because some drugs and compounds belong to two or more ATC classes, making machine learning extremely difficult. In this article a multi-label classifier system is proposed that incorporates information about a compound's chemical-chemical interaction and its structural and fingerprint similarities to other compounds belonging to the different ATC classes. The proposed system reshapes a 1D feature vector to obtain a 2D matrix representation of the compound. This matrix is then described by a histogram of gradients that is fed into a Multi-Label Learning with Label-Specific Features classifier. Rigorous cross-validations demonstrate the superior prediction quality of this method compared with other state-of-the-art approaches developed for this problem, a superiority that is reflected particularly in the absolute true rate, the most important and harshest metric for assessing multi-label systems. The MATLAB code for replicating the experiments presented in this article is available at https://www.dropbox.com/s/7v1mey48tl9bfgz/ToolPaperATC.rar?dl=0 . loris.nanni@unipd.it. Supplementary data are available at Bioinformatics online. © The Author (2017). Published by Oxford University Press. All rights reserved. For Permissions, please email: journals.permissions@oup.com

Biosynthesis of gallic and ellagic acids with 14C-labeled compounds in Acer and Rhus leaves

International Nuclear Information System (INIS)

Ishikura, Nariyuki; Hayashida, Shunzo; Tazaki, Kiyoshi

1984-01-01

The biosynthetic pathway for gallic and ellagic acids in young, mature and autumn leaves of Acer buergerianum and Rhus succedanea was examined by tracer experiments, and also by isotope competition, with D-shikimic acid- 14 C, L-phenylalanine-U- 14 C, L-phenyllactic acid-U- 14 C, gallic acid-G- 14 C and their unlabeled compounds. In young leaves of both plants, the incorporation rate of labeled shikimic acid into gallic acid was significantly higher than that of labeled phenylalanine, whereas in the mature and autumn leaves the latter was a good precursor rather than the former for the gallic acid biosynthesis. Therefore, two pathways for gallic acid formation, through β-oxidation of phenylpropanoid and through dehydrogenation of shikimic acid, could be operating in Acer and Rhus leaves, and the preferential pathway is altered by leaf age. In both plants, the incorporation rate of labeled phenyllactic acid during a 24 hr metabolic period was almost the same as that of labeled phenylalanine. The incorporation of D-shikimic acid-G- 14 C, L-phenylalanine-U- 14 C and L-phenyllactic acid-U- 14 C into ellagic acid was very similar to the case of the radioactive gallic acid formation. Furthermore, regardless of the presence of unlabeled shikimic acid and/or phenylalanine, incorporation of the radioactivity of labeled gallic acid into ellagic acid occurred at a very high rate, suggesting the reciprocal radical reaction of gallic acid for the ellagic acid formation. The incorporation of labeled compounds into ellagitannins was also examined and their biosynthesis discussed further. (author)

Measurement of loss rates of organic compounds in snow using in situ experiments and isotopically labelled compounds

Directory of Open Access Journals (Sweden)

Erika von Schneidemesser

2012-07-01

Full Text Available Organic molecular marker compounds are widely used to identify emissions from anthropogenic and biogenic air pollution sources in atmospheric samples and in deposition. Specific organic compounds have been detected in polar regions, but their fate after deposition to snow is poorly characterized. Within this context, a series of exposure experiments were carried out to observe the post-depositional processing of organic compounds under real-world conditions in snow on the surface of the Greenland Ice Sheet, at the Summit research station. Snow was prepared from water spiked with isotopically labelled organic compounds, representative of typical molecular marker compounds emitted from anthropogenic activities. Reaction rate constants and reaction order were determined based on a decrease in concentration to a stable, non-zero, threshold concentration. Fluoranthene-d10, docosane-d46, hexadecanoic acid-d31, docosanoic acid-d43 and azelaic acid-d14 were estimated to have first order loss rates within surface snow with reaction rate constants of 0.068, 0.040, 0.070, 0.067 and 0.047 h−1, respectively. No loss of heptadecane-d36 was observed. Overall, these results suggest that organic contaminants are archived in polar snow, although significant post-depositional losses of specific organic compounds occur. This has implications for the environmental fate of organic contaminants, as well as for ice-core studies that seek to use organic molecular markers to infer past atmospheric loadings, and source emissions.

Preparation of 19-iodocholesterol labelled with 125 I

International Nuclear Information System (INIS)

Rodriguez, L.; Rebollo, D. V.; Ruiz, J. M.

1986-01-01

In this paper a new method of synthesis of 19-iodo cholesterol labelled with ''125 I, from commercial cholesterol, is described. Its high chemical (96%) and radiochemical (99.9%) purities high yield and short time of preparation permit us to dispose or a more accessible labelled compound, which results appropriates for clinical investigations and in the diagnosis of disturbances of the suprarenal glands. (Author) 9 refs

Combining position-specific 13C labeling with compound-specific isotope analysis: first steps towards soil fluxomics

Science.gov (United States)

Dippold, Michaela; Kuzyakov, Yakov

2015-04-01

Understanding the soil organic matter (SOM) dynamics is one of the most important challenges in soil science. Transformation of low molecular weight organic substances (LMWOS) is a key step in biogeochemical cycles because 1) all high molecular substances pass this stage during their decomposition and 2) only LMWOS will be taken up by microorganisms. Previous studies on LMWOS were focused on determining net fluxes through the LMWOS pool, but they rarely identified transformations. As LMWOS are the preferred C and energy source for microorganisms, the transformations of LMWOS are dominated by biochemical pathways of the soil microorganisms. Thus, understanding fluxes and transformations in soils requires a detailed knowledge on the biochemical pathways and its controlling factors. Tracing C fate in soil by isotopes became on of the most applied and promising biogeochemistry tools. Up to now, studies on LMWOS were nearly exclusively based on uniformly labeled organic substances i.e. all C atoms in the molecules were labeled with 13C or 14C. However, this classical approach did not allow the differentiation between use of intact initial substances in any process, or whether they were transformed to metabolites. The novel tool of position-specific labeling enables to trace molecule atoms separately and thus to determine the cleavage of molecules - a prerequisite for metabolic tracing. Position-specific labeling of LMWOS and quantification of 13CO2 and 13C in bulk soil enabled following the basic metabolic pathways of soil microorganisms. However, only the combination of position-specific 13C labeling with compound-specific isotope analysis of microbial biomarkers and metabolites allowed 1) tracing specific anabolic pathways in diverse microbial communities in soils and 2) identification of specific pathways of individual functional microbial groups. So, these are the prerequisites for soil fluxomics. Our studies combining position-specific labeled glucose with amino

preparation of some radiopharmaceutical compounds for medical use

International Nuclear Information System (INIS)

El-shaboury, G.H.

1983-01-01

In this thesis investigations were carried out aiming to elaboration of a new improved and short time techniques to prepare some radioiodinated labelled organic compounds having high chemical and radiochemical purity and with high specific activity for clinical use in nuclear medicine as diagnostic aids. The labelled compounds were the following: 1. radioiodinated rose bengal ( tetra-chloro-tetraiodo-fluorescein) for liver function studies. 2. radioiodinated long chain fatty acids. 2.1 16-1-hexadecanoic acid. 2.2 17-1-heptadecanoic acid. for myocardial infarction studies

New radioactively labelled amines, procedure of preparation of the new compounds as well as the diagnostic preparations based on these new compounds

Energy Technology Data Exchange (ETDEWEB)

1979-02-07

This patent describes the composition and preparation of new radioactively labelled amine conpounds for use as radiopharmaceuticals, particularly for the detection and/or localization of thrombi in the body. They are not alien to the body, are used to trace the fibrin network, and lead to favourable ratios between the presence of radioactivity in the blood clot and that in the rest of the body. These new compounds have the general formula Y - (CH/sub 2/)/sub 2/-X-(CH/sub 2/)/sub 2/ - NH/sub 2/ in which X is an oxygen or sulfur atom or a methylene, ethylene or trimethylene group and Y is an organic molecule labelled with radioactive iodine, or in which X is a radioactively labelled selenium or tellurium atom and Y is an organic molecule.

Abstracts of the papers presented at the workshop 'synthesis and application of radioactively labelled organic compounds'

International Nuclear Information System (INIS)

1988-10-01

The abstracts of the 12 papers read at the Rossendorf workshop comprise syntheses and radioactive labelling of organic compounds such as herbicides, steroids, peptides and others and their application as tracers, above all in kinetic studies

Separation-oriented derivatization of native fluorescent compounds through fluorous labeling followed by liquid chromatography with fluorous-phase.

Science.gov (United States)

Sakaguchi, Yohei; Yoshida, Hideyuki; Todoroki, Kenichiro; Nohta, Hitoshi; Yamaguchi, Masatoshi

2009-06-15

We have developed a new and simple method based on "fluorous derivatization" for LC of native fluorescent compounds. This method involves the use of a column with a fluorous stationary phase. Native fluorescent analytes with target functional groups are precolumn derivatized with a nonfluorescent fluorous tag, and the fluorous-labeled analytes are retained in the column, whereas underivatized substances are not. Only the retained fluorescent analytes are detected fluorometrically at appropriate retention times, and retained substrates without fluorophores are not detected. In this study, biologically important carboxylic acids (homovanillic acid, vanillylmandelic acid, and 5-hydroxyindoleacetic acid) and drugs (naproxen, felbinac, flurbiprofen, and etodolac) were used as model native fluorescent compounds. Experimental results indicate that the fluorous-phase column can selectively retain fluorous compounds including fluorous-labeled analytes on the basis of fluorous separation. We believe that separation-oriented derivatization presented here is the first step toward the introduction of fluorous derivatization in quantitative LC analysis.

Sulfur Isotope Exchange between S-35 Labeled Inorganic Sulfur-Compounds in Anoxic Marine-Sediments

DEFF Research Database (Denmark)

FOSSING, H.; THODEANDERSEN, S.; JØRGENSEN, BB

1992-01-01

Isotope exchange reactions between S-35-labeled sulfur compounds were studied in anoxic estuarine sediment slurries at 21-degrees-C and pH 7.4-7.7. Two experiments labeled with radioactive elemental sulfur (S-35-degrees) and one labeled with radioactive sulfate ((SO42-)-S-35) were performed as time......% of the total S-35 was recovered in the SIGMA-HS- pool in less than 1.5 h. With no detectable SIGMA-HS- (less than 1-mu-M) in the slurry, 58% of the total S-35 was observed in the pyrite pool within 1.5 h. The FeS pool received up to 31% of all S-35 added. The rapid S-35 incorporation from S-35-degrees...... into SIGMA-HS- and FeS pools was explained by isotope exchange reactions. In contrast, there was evidence that the radioactivity observed in the 'pyrite pool' was caused by adhesion of the added S-35-degrees to the FeS2 grains. In all S-35-degrees-labeled experiments we also observed oxidation...

Tritium labeling for bio-med research

International Nuclear Information System (INIS)

Lemmon, R.M.

1980-01-01

A very large fraction of what we know about biochemical pathways in the living cell has resulted from the use of radioactively-labeled tracer compounds; the use of tritium-labeled compounds has been particularly important. As research in biochemistry and biology has progressed the need has arisen to label compounds of higher specific activity and of increasing molecular complexity - for example, oligo-nucleotides, polypeptides, hormones, enzymes. Our laboratory has gradually developed special facilities for handling tritium at the kilocurie level. These facilities have already proven extremely valuable in producing labeled compounds that are not available from commercial sources. The principal ways employed for compound labeling are: (1) microwave discharge labeling, (2) catalytic tritio-hydrogenation, (3) catalytic exchange with T 2 O, and (4) replacement of halogen atoms by T. Studies have also been carried out on tritiation by the replacement of halogen atoms with T atoms. These results indicate that carrier-free tritium-labeled products, including biomacromolecules, can be produced in this way

Determination of one-dimensional distribution of 14C-labelled compounds

International Nuclear Information System (INIS)

Rexa, R.; Kron, I.; Kralik, P.; Tykva, R.

1988-01-01

Three methods used for the determination of one-dimensional distribution of 14 C-labelled compounds are compared: measurement with position-sensitive detector (LB 282/511), liquid scintillation counting (LSC), and autoradiography with densitometric quantification. For a mutual comparison of these methods samples of blood serum were used, in which the fractional esterification rate (FER) was determined by means of LCAT Test. The agreement of the methods of FER determination on the basis of the measurement with LB 282/511 or LSC was checked. In the case of autoradiography a correction for non-linearity between the blackening and the number of β-particles striking the area unit was necessary. (author) 5 refs.; 5 figs

Off-label psychopharmacologic prescribing for children: History supports close clinical monitoring

Directory of Open Access Journals (Sweden)

Fegert Joerg M

2008-09-01

Full Text Available Abstract The review presents pediatric adverse drug events from a historical perspective and focuses on selected safety issues associated with off-label use of medications for the psychiatric treatment of youth. Clinical monitoring procedures for major psychotropic drug classes are reviewed. Prior studies suggest that systematic treatment monitoring is warranted so as to both minimize risk of unexpected adverse events and exposures to ineffective treatments. Clinical trials to establish the efficacy and safety of drugs currently being used off-label in the pediatric population are needed. In the meantime, clinicians should consider the existing evidence-base for these drugs and institute close clinical monitoring.

Labelling of some iodinated organic compounds by halogen exchange in organic media

International Nuclear Information System (INIS)

Hallaba, E.; Suhybani, A.Al-; Khowaiter, S.Al-; Abdel-Wahid, M.

1983-01-01

Describes a general method for labelling Rose Bengal in an organic medium. An isotopic exchange technique with interactive iodine as carrier for radioiodine is used. The effect of temperature, carrier, pH of the solvent and solvent are investigated. The optimum conditions for maximum yield of exchange are: .0.2 micro mole carrier inactive iodine per one micro mole of Rose Bengal, reaction mixture is 10ml ethyl alcohol 96% as a solvent for Rose Bengal and 3ml of ether or carbon tetrachloride containing the inactive and radioiodine. In case of ether, the reaction is slow and is completed in two hours with maximum yield of 90% at boiling temperature. Addition of 175 λ of 1 M acetate buffer with carbon tetrachloride gave a yield of 90% in one hour. This method can be applied successfully to label any iodinated organic compound, such as hypuran, thyroxine, tyrosine or aliphatic fatty acids, for application in nuclear medicine. 10 Ref

Direct labeling of doxorubicin with technetium-99m. Its optimization, characterization and quality control

International Nuclear Information System (INIS)

Rizvi, F.A.; Bokhari, T.H.; Roohi, S.; Mushtaq, A.

2012-01-01

Doxorubicin (DOX) is an anthracycline antineoplastic and one of the most potent and widely used drugs in clinical oncology. It is used in the treatment of a wide variety of cancers. The aim of this study was the direct labeling of DOX with 99m Tc; its optimization, characterization and quality control of the radiolabeled DOX. Labeling efficiency was determined by paper chromatography. More than 92% labeling was obtained at pH 6-7, 10-12 μg stannous chloride and 200 μg of DOX. The stability of 99m Tc-DOX was studied up to 5 h. All the experiments were performed at room temperature (25 ± 2 deg C). The characterization of the labeling compound was performed by HPLC and electrophoresis. Electrophoresis indicates that labeled DOX has no charge and HPLC shows single specie of labeled compound. (author)

Clinical application of antibody monoclonal humanized anti-EGFrnimotuzumab labeled

International Nuclear Information System (INIS)

Perera Pintado, Alejandro; Peña Quián, Yamilé; Batista Cuéllar, Juan F.; Prats Capote, Anaís; Torres Aroche, Leonel A.; Casacó Santana, Caridad; Sánchez Mendosa, Elvia L.; Sánchez González, Yolaine; Romero Collado, Susana; Quesada Pozo, Rodobaldo; Valladares Oviedo, Lourdes; Masquida García, Elsa M.; Leyva Montaña, René; Casacó, Angel; Ramos Suzarte, Mayra; Crombet, Tania

2016-01-01

Most malignant tumors are of epithelial origin. These are characterized by overexpression of the receptor of epidermal growth factor (EGFR), which the neoplastic cells escape the regulatory mechanisms are allowed, so its high concentration of membrane is generally associated with a poor prognosis . By binding an antibody specifically to this receptor, preventing binding of EGF latter and activation mechanism tyrosine kinase inhibiting cell mitosis and apoptosis causing tumor cell. For this reason, the EGFr has been considered as an attractive target for anti-tumor therapy. The humanized monoclonal antibody anti-EGFr nimotuzumab was developed by the Center of Molecular Immunology (Havana, Cuba). Numerous clinical trials have been developed in the Department of Clinical Research Center Isotopes (Cuba), in which it has been applied this antibody, both labeled with 99mTc for immuno gammagraphic detection of tumors, as labeled with 188 Re for radioimmunotherapy of gliomas high degree of malignancy. The aim of this paper is to show the experience of the Department of Clinical Research of CENTIS in various clinical trials with marking for both immuno gammagraphics detection of tumors, such as for radioimmunotherapy nimotuzumab. (author)

Indium-111 labelled platelets: experimental and clinical studies

International Nuclear Information System (INIS)

Gjerloeff Schmidt, K.

1985-10-01

The object of the present study became to develop a method of effective and gentle isolation and 111-In labelling of human platelets, as well as to employ these platelets in human clinical studies with the object of elucidating a number of physiological and pathophysiological mechanisms and processes in which platelets take part. 111-In-oxine presents obvious advantages over 51-Cr-sodium chromate; a high labelling efficiency, and more advantageous physical properties (a half life of 68 hours (against the half life of 28 days for 51-Cr) and considerably more effective gamma emission), making external registration by means of a gamma camera possible. Considering the role played by platelets in the development of atherosclerosis and its thromboembolic complications, in the early phases of deep venous thrombosis, and in graft rejection, it is natural that attempts have been made to use 111-In-labelled platelets for scintigraphic and kinetic evaluation of thromboembolic processes. Accumulation of 111-In-labelled platelets at sites of vessel wall injury, on pulmonary emboli (presumably on deep vein thrombi as well), and on catheter material has been demonstrated. Beyond this, the number of publications concerning the use of 111-In-labelled platelets for visualization of atherosclerosis, venous thromboembolism, arterial grafts, intracardiac thrombi, aortic aneurysms, renal allograft rejection, and other situations in which platelet thromboembolism takes place, provides evidence that a tool has finally been found for the study of their nature and response to therapeutic intervention. (eg)

Labelling of some organic compounds with radioactive iodine for medical uses

International Nuclear Information System (INIS)

El-tawoosy, M.E.M.

1997-01-01

Among all radioisotopes, radioiodine(i.e. 122 I, 123 I, 125 I. 131 I) is the most available tagging element when considering new radiopharmaceutical compounds intended for nuclear medicine uses for in -Vitro and in - vivo measurements. The aim of this work is to optimize and developed new methods of radioiodination of some organic molecules for use in nuclear medicine as diagnostic agents. Some trials for labelling of meta - iodo benzyl guanidine (MIBG), antipyrine (AP) and 3,5,3- tri - iodothyronine (T 3 ) will be done. In the present study, we will try to get easier, short time, high yield, high specific activity, high radiochemical purity and economic methods for the preparation of the following radiopharmaceutical compounds: 1- (m- 131 I) meat - iodo benzyl guanidine (m- 131 I) MIBG for adrenal medulla and myocardial measurements. 2-(4- 131 I) iodoantipyrine (4- 131 I) IAP for brain measurements. 3-( 131 I) tetra -iodothyronine ( 131 I) T 4 for thyroid gland function studies. The influence of substrate conc., reaction time, different oxidizing agents and catalyst concentrations will be investigated to elucidate the optimum methods suitable for preparation of these compounds. Chromatographic techniques such as paper chromatography, thin layer chromatography (TLC), column chromatography and high pressure liquid chromatography (HPLC) will be used for the identification, quality control, purification and quality assurance of the final product. 4.2 tabs., 4.5 figs., 204 refs

Real-time imaging of radioisotope labeled compounds in a living plant

International Nuclear Information System (INIS)

Kanno, S.; Ohya, T.; Hayashi, Y.; Tanoi, K.; Nakanishi, T.M.

2007-01-01

We developed a quantitative, real-time imaging system of labeled compounds in a living plant. The system was composed of CsI scintillator to convert β-rays to visible light and an image intensifier unit (composed of GaAsP semiconductor and MCP; micro channel plate) to detect extremely weak light. When the sensitivity and resolution of the image of our system was compared with that of an imaging plate (IP), the sensitivity of our system (with 20 minutes) was higher than that of an IP, with similar quality to that of an IP. Using this system, the translocation of 32 P in a soybean plant tissue was shown in successive images. (author)

Applications of stable isotopes of 2H, 13C and 15N to clinical problems

International Nuclear Information System (INIS)

Klein, P.D.; Szczepanik, P.A.; Hachey, D.L.

1974-01-01

The function of the Argonne Program is to provide synthetic, analytical instrumental capability in a core facility for the clinical investigator who needs to use 2 H, 13 C, or 15 N labelled compounds for metabolic or clinical research on pregnant women, newborn infants, young children, or for mass screening. To carry out such application development, there were six stages which were recurrent steps in every application. Five fundamental strategies should be adopted to establish the use of stable isotopes in clinical work. The instrument required for measurements was a combined gas chromatograph-mass spectrometer, and its use was schematically illustrated. Some of the successful experiences with compounds labelled by stable isotopes, such as deuterium labelled chenodeoxycholic acid, and respective 13 C and 15 N-labelled glycine were described. Deutrium labelled bile acid enabled easy and safe determination of the size of the bile acid pool and the replacement rate, providing clearer diagnoses for cholestatic liver disease and gallstones. 13 C and 15 N labelled compounds were used in clinical studies, of children with genetic disorders of amino acid metabolism, i.e., non ketotic hyperflycinemia, B 12 -responsive methyl malonic acidemia, and Lesch-Nyhan syndrome. 15 N-labelled glycine was also studied in a child with Lesch-Nyhan syndrome. (Mukohata, S.)

/sup 99m/Tc-labelled hepatobiliary radiopharmaceuticals

International Nuclear Information System (INIS)

Galli, G.; Maini, C.L.

1986-01-01

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

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

International Nuclear Information System (INIS)

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

1991-01-01

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

Preparation and preclinical evaluation of 211At-labelled compounds for α-particle radiotherapy

International Nuclear Information System (INIS)

Larsen, R.H.

1994-01-01

The interest for α-particle emitters in internal radiotherapy is increasing due to improved conjugation chemistry. Experimental work has concentrated on 211 At and 212 Bi since these to nuclides have radiochemical and physical properties suitable for medical application. In this report it is demonstrated that biologically active 211 At-labelled compounds can be prepared within a relatively short time allowing utilization of this 7.2 h α-particle. It is further shown that 211 At-TP-3 treatment of human osteosarcoma in vitro gives promising therapeutic ratios. 76 refs., 5 figs., 3 tabs

Experimental and clinical experience with iodine 123-labeled iodophenylpentadecanoic acid in cardiology.

Science.gov (United States)

Reske, S N

1994-01-01

Iodine 123-labeled iodophenylpentadecanoic acid (IPPA) has been synthesized for investigating myocardial free fatty acid (FFA) metabolism. The diagnostic application of labeled FFA in heart disease may be important, because FFA is the preferred substrate of cardiac energy metabolism at rest in the fasting state. In addition, regional myocardial FFA uptake and regional myocardial blood flow are tightly coupled in normal myocardium with beta-oxidation, which is extremely sensitive to oxygen deprivation. This article outlines basic physiologic pathways of cardiac IPPA metabolism in normal, acutely ischemic, and reperfused viable myocardium and summarizes the results of experimental studies in animals, validating the application of IPPA as an 123I-labeled fatty acid analog. In addition, the most important clinical studies indicating the clinical use of IPPA for diagnosis of coronary heart disease and myocardial viability are presented.

Synthesis, evaluation and application of radioiodine labeled compounds in nuclear medicine

International Nuclear Information System (INIS)

Ahmed, M. O. M.

2006-01-01

This study reviews synthesis, evaluation,diagnostic and therapeutic applications of iodine radiopharmaceutical especially with 13I I and 123 I in contemporary nuclear medicine. It is well Known that iodine is used in thyroid diagnostic and therapy with sodium iodide and played an important role in diagnostic procedures using single photon emission tomography (SPECT). The study covers the general chemistry of iodine, physical properties, biological role of iodine, general uses of iodine compounds , production and decay schemes of 131 I, 125 I and 123 I in the first chapter. Preparation of radioiodine labeled compounds, quality control of radiopharmaceuticals and safety of radioiodination are dealt with in detail in two chapters. These were followed by chapters dealing in length with the chemistry, preparation, quality control, pharmacokinetics and radiation dosimetry of some iodine radiopharmaceuticals, and then current trends in diagnostic and therapeutic applications of iodine radiopharmaceuticals particularly 131 / 123 I-MIBG and 123 I-IMP. We found that the iodine radiopharmaceuticals are considered amongst principal indicators in single photon emission tomography (SPECT), and 131 / 123 I-MIBG and 123 I-IMP appear to be appropriate diagnostic and therapeutic agents for variety of diseases.(Author)

SIMulation of Medication Error induced by Clinical Trial drug labeling: the SIMME-CT study.

Science.gov (United States)

Dollinger, Cecile; Schwiertz, Vérane; Sarfati, Laura; Gourc-Berthod, Chloé; Guédat, Marie-Gabrielle; Alloux, Céline; Vantard, Nicolas; Gauthier, Noémie; He, Sophie; Kiouris, Elena; Caffin, Anne-Gaelle; Bernard, Delphine; Ranchon, Florence; Rioufol, Catherine

2016-06-01

To assess the impact of investigational drug labels on the risk of medication error in drug dispensing. A simulation-based learning program focusing on investigational drug dispensing was conducted. The study was undertaken in an Investigational Drugs Dispensing Unit of a University Hospital of Lyon, France. Sixty-three pharmacy workers (pharmacists, residents, technicians or students) were enrolled. Ten risk factors were selected concerning label information or the risk of confusion with another clinical trial. Each risk factor was scored independently out of 5: the higher the score, the greater the risk of error. From 400 labels analyzed, two groups were selected for the dispensing simulation: 27 labels with high risk (score ≥3) and 27 with low risk (score ≤2). Each question in the learning program was displayed as a simulated clinical trial prescription. Medication error was defined as at least one erroneous answer (i.e. error in drug dispensing). For each question, response times were collected. High-risk investigational drug labels correlated with medication error and slower response time. Error rates were significantly 5.5-fold higher for high-risk series. Error frequency was not significantly affected by occupational category or experience in clinical trials. SIMME-CT is the first simulation-based learning tool to focus on investigational drug labels as a risk factor for medication error. SIMME-CT was also used as a training tool for staff involved in clinical research, to develop medication error risk awareness and to validate competence in continuing medical education. © The Author 2016. Published by Oxford University Press in association with the International Society for Quality in Health Care; all rights reserved.

Lyophilized kits of diamino dithiol compounds for labelling with 99m-technetium. Pharmacokinetics studies and distribution compartmental models of the related complexes

International Nuclear Information System (INIS)

Araujo, Elaine Bortoleti de

1995-01-01

The present work reflects the clinical interest for labelling diamino dithiol compounds with technetium-99m. Both chosen compounds, L,L-Ethylene dicysteine (L,L-EC) and L,L-Ethylene dicysteine diethyl esther (L,L-ECD) were obtained with relative good yield and characterized by IR and NMR. The study of labelling conditions with technetium-99m showed the influence of the type and mass of reducing agent as well as the pH on the formation of complexes with desired biological characteristics. Radiochemical purity was determined by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Lyophilised kits of L,L-EC and L,L-ECD for labelling with 99m Tc were obtained, with stability superior to 120 days, when stored under refrigeration, enabling the kits marketing. The ideal formulation of the kits as well as the use of liquid nitrogen in the freezing process, determined the lyophilization success. Distribution biological studies of the 99m Tc complexes were performed on mice by invasive method and on bigger animals by scintigraphic evaluation. Biological distribution studies of the complex 99m Tc-L,L-EC showed fast blood clearance, with the elimination of about 90% of the administered dose after 60 minutes, almost exclusively by the urinary system. The biological distribution results were adjusted to a three compartmental distribution model, as expected for a radiopharmaceutical designed to renal dynamic studies, with tubular elimination. The complex interaction with renal tubular receptors is related with structural characteristics of the compound, more specifically with the presence and location of polar groups. In comparison with 99m Tc-L,L-EC, biological studies of the complex 99m Tc -L,L-ECD showed different distribution aspects, despite some structural similarities. The presence of ethyl groups confers to the complex neutrality and lipophilicity. It cross the intact blood brain barrier and is retained in the brain for enough period

Unlabelled and radioactive labelled derivatives of butylamino propiophenone and their preparation

International Nuclear Information System (INIS)

Findlay, J.W.A.; Butz, R.F.; Welch, R.M.

1986-01-01

This invention relates to new unlabelled and radioactive labelled derivatives of butylamino propiophenone and their preparation. This invention is primarily directed to a radioimmunoassay for clinical or experimental testing for the presence of and quantitation of bupropion, a pharmacologically active antidepressant compound, in biological fluids

Synthesis and pre-clinical evaluation of a new class of high-affinity "1"8F-labeled PSMA ligands for detection of prostate cancer by PET imaging

International Nuclear Information System (INIS)

Kelly, James; Amor-Coarasa, Alejandro; Williams, Clarence; Ponnala, Shashikanth; Nikolopoulou, Anastasia; Kim, Dohyun; Babich, John W.

2017-01-01

Current clinical imaging of PSMA-positive prostate cancer by positron emission tomography (PET) mainly features "6"8Ga-labeled tracers, notably ["6"8Ga]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 ["1"8F]triazoles were isolated following a Cu(I)-catalyzed click reaction between the alkynes and ["1"8F]fluoroethylazide. The "1"8F-labeled compounds were evaluated in nude mice bearing LNCaP tumors and compared to ["6"8Ga]Ga-PSMA-HBED-CC and ["1"8F]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_5_0) 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 ["6"8Ga]Ga-PSMA-HBED-CC and ["1"8F]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 ["6"8Ga]Ga-PSMA-HBED-CC. Six ["1"8F]triazolylphenyl ureas were prepared in good radiochemical yield

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

Modulating effect of new potential antimelanomic agents, spin-labeled triazenes and nitrosoureas on the DOPA-oxidase activity of tyrosinase.

Science.gov (United States)

Gadjeva, V; Zheleva, A; Raikova, E

1999-07-01

The modulating effect of newly synthesized alkylating spin labeled triazene and spin labeled nitrosourea derivatives on the DOPA-oxidase activity of mushroom tyrosinase has been investigated by Bumett's spectrophotometric method (Burnett et al., 1967). All spin labeled triazenes have exhibited activating effect on DOPA-oxidase activity of tyrosinase, whereas clinically used triazene (DTIC), which does not contain nitroxide moiety, have showed inhibiting effect. At the same experimental conditions the spin labeled aminoacid nitrosoureas have showed dual effect - activating, in the beginning of the enzyme reaction and inhibiting later on. It is deduced that the activating effect of the spin labeled compounds is due to the nitroxide moiety and the inhibiting effect of all compounds depends on their half-life time. This study might contribute to make more clear the mechanism of action of the new compounds and on the other hand would come in quite useful as a preliminary prognosis for their antimelanomic activity.

New compounds as potential radio diagnosticians Alzheimer

International Nuclear Information System (INIS)

Rivera Marrero, S.; Sablón Carrazana, M.; Bencomo Martinez, A.; Merceron Martínez, D.; Jimenez Martín, J.; Pérez Perera, R.; Díaz García, O.; Rodríguez Tanty, Ch.; Prats Capote, A.; Perera Pintado, A; Fernández Maza, L.; Balcerzyk, M; Fernández Gómez, I.; Parrado Gallego, Á; León Chaviano, S.; Acosta Medina, E.

2016-01-01

Alzheimer's disease (AD) is the most common cause of dementia in Cuba and all over the World. According to demographic trends it has been called the epidemic of the century. It is characterized by the presence of neuropathological brain deposits: senile plaques, formed by neurofibrillary tangles (NT) and deposits of β-amyloid protein (Aß). Aß plaques could appear even 20 years before the establishment of first clinical symptoms of the disease. The aim of this study was to synthesize new naphthalene derivatives, feasible to be labeled with radionuclides emitters of either gamma radiation or positrons. These labeled compounds should be able to cross blood–brain barrier (BBB) in healthy and AD transgenic animals. As a result of this work, several synthetic precursors were synthesized, which were labeled with iodine-131, carbon-11 and fluorine-18 with a satisfactory radiochemical purity. The corresponding non-radioactive control compounds were also synthesized.In in vitro and in silico studies, obtained compounds showed affinity for the β-amyloid protein. According to SPECT and PET-CT images in healthy laboratory animals, obtained labeled compounds crossed BBB in a bi-directional way without any sign of brain uptake.Furthermore, evaluation of the biodistribution of the [ 18 F] -2- (3-fluoropropyl) -6-methoxynaphthalene ([[ 18 F] Amyloid® was performed in healthy animals.[[ 18 F]Amylovis crossed blood brain barrier. Renal and hepatic pathways were the main excretion routes. On the other hand, in transgenic mice with AD, its uptake and its retention time were higher in comparison with healthy mice. Immunohistochemistry and Congo red staining of control and transgenic mice brain slices were performed to identify β-amyloid plaques.Conclusions: Obtained compounds were able to bi-directionally cross BBB.[[ 18 F]Amylovis® could be a promising PET radiotracer for amyloid plaques visualization. (author)

On-site preparation of technetium-99m labeled human serum albumin for clinical application

International Nuclear Information System (INIS)

Wang Yuhfeng; Chuang Meihua; Cham Thauming; Chung Meiing; Chiu Jainnshiun

2007-01-01

Technetium-99m labeled human serum albumin (Tc-99m HSA) is an important radiopharmaceutical for clinical applications, such as cardiac function tests or protein-losing gastroenteropathy assessment. However, because of transfusion-induced infectious diseases, the safety of serum products is a serious concern. In this context, serum products acquired from patients themselves are the most ideal tracer. However, the development of rapid separation and easy clinical labeling methods is not yet well established. Under such situation, products from the same ethnic group or country are now recommended by the World Health Organization as an alternative preparation. This article describes the on-site preparation of Tc-99m HSA from locally supplied serum products. Different formulations were prepared and the labeling efficiency and stability were examined. Radio-labeling efficiencies were more than 90% in all preparation protocols, except for one that omitted the stannous solution. The most cost-effective protocol contained HSA 0.1 mg, treated with stannous fluoride 0.2 mg, and mixed with Tc-99m pertechnetate 30 mCi. A biodistribution study was performed in rats using a gamma camera immediately after intravenous administration of radiolabeled HSA. Tissue/organ uptake was obtained by measuring the radioactivity in organs after sacrificing the rats at timed intervals. The biologic half-life was about 32 min, determined from sequential venous blood collections. These data indicate that our preparation of Tc-99m HSA is useful and potentially applicable clinically. In addition, this on-site preparation provides the possibility of labeling a patient's own serum for subsequent clinical application. (author)

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)

Respiratory drugs prescribed off-label among children in the outpatient clinics of a hospital in Malaysia.

Science.gov (United States)

Mohamad, Nurul Fadilah; Mhd Ali, Adliah; Mohamed Shah, Noraida

2015-02-01

Prescribing medicines in an unlicensed and off-label manner for children is a widespread practice around the world. To determine the extent and predictors of off-label respiratory drug prescriptions for children in the outpatient clinics of a hospital in Malaysia. Outpatient clinics at the Universiti Kebangsaan Malaysia Medical Centre, a tertiary teaching hospital in Malaysia. The pharmacy-based computer system and medical records of the patients were utilized to collect data from 220 pediatric patients who were prescribed at least one respiratory drug from July 2011 to December 2011. Characteristics of the off-label respiratory drug prescriptions were measured. A total of 134 children (60.9 %) received at least one respiratory drug prescribed in an off-label manner. The most common reasons for the off-label prescribing of drugs were off-label use by indication (31.5 %), followed by higher than the recommended dose (24.9 %) and lower than the recommended frequency (17.1 %). Diphenhydramine was the most common respiratory drug prescribed off-label. The number of medications prescribed was the only significant predictor of off-label prescription of respiratory drugs. Pediatric patients receiving 4-6 medications were 7.8 times more likely to receive at least one off-label respiratory drug compared to pediatric patients that received 1-3 medications (OR 7.8, 95 % CI 1.74-37.44). There was substantial prescribing of respiratory drugs for children in an off-label manner at the outpatient clinics at the Universiti Kebangsaan Malaysia Medical Centre. This highlights the need for more research to be carried out on respiratory drugs in the pediatric population.

Structured prediction models for RNN based sequence labeling in clinical text.

Science.gov (United States)

Jagannatha, Abhyuday N; Yu, Hong

2016-11-01

Sequence labeling is a widely used method for named entity recognition and information extraction from unstructured natural language data. In clinical domain one major application of sequence labeling involves extraction of medical entities such as medication, indication, and side-effects from Electronic Health Record narratives. Sequence labeling in this domain, presents its own set of challenges and objectives. In this work we experimented with various CRF based structured learning models with Recurrent Neural Networks. We extend the previously studied LSTM-CRF models with explicit modeling of pairwise potentials. We also propose an approximate version of skip-chain CRF inference with RNN potentials. We use these methodologies for structured prediction in order to improve the exact phrase detection of various medical entities.

High Throughput, Label-free Screening Small Molecule Compound Libraries for Protein-Ligands using Combination of Small Molecule Microarrays and a Special Ellipsometry-based Optical Scanner.

Science.gov (United States)

Landry, James P; Fei, Yiyan; Zhu, X D

2011-12-01

Small-molecule compounds remain the major source of therapeutic and preventative drugs. Developing new drugs against a protein target often requires screening large collections of compounds with diverse structures for ligands or ligand fragments that exhibit sufficiently affinity and desirable inhibition effect on the target before further optimization and development. Since the number of small molecule compounds is large, high-throughput screening (HTS) methods are needed. Small-molecule microarrays (SMM) on a solid support in combination with a suitable binding assay form a viable HTS platform. We demonstrate that by combining an oblique-incidence reflectivity difference optical scanner with SMM we can screen 10,000 small-molecule compounds on a single glass slide for protein ligands without fluorescence labeling. Furthermore using such a label-free assay platform we can simultaneously acquire binding curves of a solution-phase protein to over 10,000 immobilized compounds, thus enabling full characterization of protein-ligand interactions over a wide range of affinity constants.

The Near-Term Viability and Benefits of eLabels for Patients, Clinical Sites, and Sponsors.

Science.gov (United States)

Smith-Gick, Jodi; Barnes, Nicola; Barone, Rocco; Bedford, Jeff; James, Jason R; Reisner, Stacy Frankovitz; Stephenson, Michael

2018-01-01

Current clinical trial labels are designed primarily to meet regulatory requirements. These labels have low patient and site utility, few are opened, and they have limited space and small fonts. As our world transitions from paper to electronic, an opportunity exists to provide patients with information about their investigational clinical trial product in a way that is more easily accessible, meets Health Authority requirements, and provides valuable additional information for the patient and caregiver. A TransCelerate initiative was launched to understand the current regulatory and technology landscape for the potential use an electronic label (eLabel) for investigational medicinal products (IMPs). Concepts and an example proof of concept were developed intended to show the "art of the possible" for a foundational eLabel and a "universal printed label." In addition, possible patient-centric enhancements were captured in the eLabel proof of concept. These concepts were shared with Health Authorities as well as patient and site advisory groups to gather feedback and subsequently enhance the concepts. Feedback indicated that the concept of an eLabel provides value and concepts should continue to be pursued. While the Health Authorities engaged with did not express issues with the use of an eLabel per se, the reduction in the content on the paper label is not possible in some geographic locations due to existing regulations. There is nothing that prevents transmitting the label electronically in conjunction with current conventional labeling. While there are still some regulatory barriers that need to be addressed for reducing what is on the paper label, advancement toward a more patient-centric approach benefits stakeholders and will enable a fully connected patient-centric experience. The industry must start now to build the foundation.

Bismuth absorption from sup 205 Bi-labelled pharmaceutical bismuth compounds used in the treatment of peptic ulcer disease

Energy Technology Data Exchange (ETDEWEB)

Dresow, B.; Fischer, R.; Gabbe, E.E.; Wendel, J.; Heinrich, H.C. (Eppendorf University Hospital, Hamburg (Germany))

1992-04-01

The absorption of bismuth from five {sup 205}Bi-labelled pharmaceutically used bismuth compounds was studied in man. From single oral doses of all compounds under investigation only <0.1% bismuth was absorbed and excreted with the urine. A significantly higher absorption was observed from the colloidal bismuth subcitrate and the basic bismuth gallate than from the basic bismuth salicylate, nitrate and aluminate. No retention of bismuth in the whole body was found from the single dose experiment. The biologic fast-term half-lives of absorbed bismuth were calculated to be 0.12 and 1.5 days. 14 refs., 2 figs., 1 tab.

Preparation and preclinical evaluation of {sup 211}At-labelled compounds for {alpha}-particle radiotherapy

Energy Technology Data Exchange (ETDEWEB)

Larsen, R H

1994-12-31

The interest for {alpha}-particle emitters in internal radiotherapy is increasing due to improved conjugation chemistry. Experimental work has concentrated on {sup 211}At and {sup 212}Bi since these to nuclides have radiochemical and physical properties suitable for medical application. In this report it is demonstrated that biologically active {sup 211}At-labelled compounds can be prepared within a relatively short time allowing utilization of this 7.2 h {alpha}-particle. It is further shown that {sup 211}At-TP-3 treatment of human osteosarcoma in vitro gives promising therapeutic ratios. 76 refs., 5 figs., 3 tabs.

Leucocyte labeling: Preliminary clinical evaluation of RP517, the 99mTc-Leukotriene B4 receptor antagonist for infection/inflammation

International Nuclear Information System (INIS)

Soroa, V.E.; Velasquez, M.H.; Nicolini, J.; Ughetti, R.; Camin, L.

2002-01-01

99mTc- Leukotriene B4 (LTB4) is a receptor antagonist RP517 that labels predominantly neutrophils, in whole blood. This new radiopharmaceutical has been developed for imaging infection and inflammation. Aim: We conducted this clinical trial to obtain the best protocol imaging and the efficacy of this novel agent in the detection of suspected infected/inflamed patients. Materials and Methods: RP517 was labelled with 15-20 mCi (555-740 MBq) 99mTc for each patient, with a labeling efficiency of 86-95%. Nine patients studied (F 3, M 6) with ages 45-83, suspected of bone, joint and soft tissue infection (8) and one with fever of unknown origin (FUO). Laboratory, anatomical images and one other scintiscan (MDP, Gallium or 99mTc-ciprofloxacin) were used for evaluation. Acquisition protocol: flow, 30 min, 1, 2, 3, 4 - 24h planar or SPECT images if required. Results were compared to histology, cultures, the clinical derivation and follow up. Scans were classified as positive if abnormal uptake persisted through the 24h images or negative when absent pathological uptake or when positivity faded in later images. Results: No adverse reaction encountered. Image protocol modified to a flow, 30 min, 4 and 24h acquisitions. Early bladder excretion and intestinal activity requires previous cleansing enemas and food restrain. Late bone marrow activity is less visible than with in vitro leucocyte labeling. Coincident images were obtained in 3 True Positive, in 5 True Negative except in a hip prosthesis where Gallium and 99mTc-ciprofloxacin showed positivity and RP517 was False negative. Conclusions: A kit should be produced in order to make it available for Nuclear Medicine Departments. Known advantages of RP517 is the lack of in vitro cell labeling manipulation. We do not recommend investigation of FUO or abdominal pathologies. A larger series must be studied in order to be able to obtain statistics on joint bone and soft tissue infection/inflammation where this compound seems to be

Cooperation of CMEA member states in the field of the manufacture and use of stable isotopes and compounds thus labelled

International Nuclear Information System (INIS)

Ertel, G.; Ewald, G.

1977-01-01

The contribution presents a survey of scientific-technical cooperation of CMEA member states in the field of stable isotopes, it deals with the specialization of stable isotope production and compounds thus labelled, and gives the prospects for further development of this cooperation. (HK) [de

Measurement of renal glomerular filtration rate using labelled substances with compartmental analysis

International Nuclear Information System (INIS)

Eberstadt, P.L.

1981-10-01

Using a model for the two-compartmental open system and experiments on animals (rabbits and dogs) as well as on human healthy volunteers, an attempt was made to study the advantages and limitations of different radionuclide methods for glomerular filtration rate determination. Labelled compounds used in different combinations were: 3 H-inulin, sup(113m)In-EDTA, 131 I-iothalamate, sup(99m)Tc-DTPA and 14 C-creatinine. The results of the study lead to some working hypotheses concerning the value of creatinine and other labelled substances in the measurement of glomerular filtration rate in clinical practice. The advantages and disadvantages of individual methods summarized in the final report are generally in agreement with the present views of many research workers. Also the hypothesis can be justified that the different labelled compounds which have been studied might be handled independently by the membranes involved but at the long run produce similar homeostatic balance

Labeling of - N-Isopropil - p - I-Anphetamine (IMP-131I) and its biological distribution in rats

International Nuclear Information System (INIS)

Barboza, M.F. de; Goncalves, R.S.V.; Muramoto, E.

1988-09-01

The described labeling and purification preparation of N-Isopropil-p 131 I-anphetamine ( 131 I-IMP) represents a fast and efficient method to obtains a compound that fullfills all criterions of purity for its application 'IN VIVO'. The labeling yield was 68-78% and the radiochemical purity performed by paper chromatography and electrophorese was 97-99%. As demostrated in animal experiments, the cerebral affinity offers a possibility to study brain diseases in clinical studies when the product will be labelled with 123 I. (author) [pt

Deuterium labeled cannabinoids

International Nuclear Information System (INIS)

Driessen, R.A.

1979-01-01

Complex reactions involving ring opening, ring closure and rearrangements hamper complete understanding of the fragmentation processes in the mass spectrometric fragmentation patterns of cannabinoids. Specifically labelled compounds are very powerful tools for obtaining more insight into fragmentation mechanisms and ion structures and therefore the synthesis of specifically deuterated cannabinoids was undertaken. For this, it was necessary to investigate the preparation of cannabinoids, appropriately functionalized for specific introduction of deuterium atom labels. The results of mass spectrometry with these labelled cannabinoids are described. (Auth.)

What's in a Label? Is Diagnosis the Start or the End of Clinical Reasoning?

Science.gov (United States)

Ilgen, Jonathan S; Eva, Kevin W; Regehr, Glenn

2016-04-01

Diagnostic reasoning has received substantial attention in the literature, yet what we mean by "diagnosis" may vary. Diagnosis can align with assignment of a "label," where a constellation of signs, symptoms, and test results is unified into a solution at a single point in time. This "diagnostic labeling" conceptualization is embodied in our case-based learning curricula, published case reports, and research studies, all of which treat diagnostic accuracy as the primary outcome. However, this conceptualization may oversimplify the richly iterative and evolutionary nature of clinical reasoning in many settings. Diagnosis can also represent a process of guiding one's thoughts by "making meaning" from data that are intrinsically dynamic, experienced idiosyncratically, negotiated among team members, and rich with opportunities for exploration. Thus, there are two complementary constructions of diagnosis: 1) the correct solution resulting from a diagnostic reasoning process, and 2) a dynamic aid to an ongoing clinical reasoning process. This article discusses the importance of recognizing these two conceptualizations of "diagnosis," outlines the unintended consequences of emphasizing diagnostic labeling as the primary goal of clinical reasoning, and suggests how framing diagnosis as an ongoing process of meaning-making might change how we think about teaching and assessing clinical reasoning.

Preparation of 19-iodo cholesterol labelled with 125 I; Preparacion del 19-yodocolesterol marcado con 125 I

Energy Technology Data Exchange (ETDEWEB)

Rodriguez, L; Rebollo, D V; Ruiz, J M

1986-07-01

In this paper a new method of synthesis of 19-iodo cholesterol labelled with ''125 I, from commercial cholesterol, is described. Its high chemical (96%) and radiochemical (99.9%) purities high yield and short time of preparation permit us to dispose or a more accessible labelled compound, which results appropriates for clinical investigations and in the diagnosis of disturbances of the suprarenal glands. (Author) 9 refs.

Synthesis and application of labelled growth regulators

International Nuclear Information System (INIS)

Shyutte, G.R.

1982-01-01

For the investigation of the metabolism both of phytoeffectors like herbicides and plant growth regulators such compounds are needed in radioactive labelled form. The synthesis of radioactive labelled fluorodifen, nitrofen, ethephon, diphenylic acetic acid, 2,4-dichlorophenoxyisobutyric acid, abscisic acid, hydroxybenzoic acids and different conjugates are described. Some examples of these compounds metabolism in plants are discussed [ru

Tritium NMR in the analysis of tritiated compounds

International Nuclear Information System (INIS)

Kaspersen, F.M.; Funke, C.W.; Vader, Jan; Wagenaars, G.N.

1993-01-01

An overview is given of the possibilities of 3 H NMR in the characterisation of 3 H-labelled compounds. This technique gives information on the identity of the tritiated compounds, the position of the tritium, the distribution of the label and even the radiochemical purity of the labelled products. (author)

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

International Nuclear Information System (INIS)

Mani, R.S.

1978-03-01

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

Radio-labelling of long-lasting erythropoietin

International Nuclear Information System (INIS)

Liu Guoxia; Zeng Xianyin; Bao Lun; Xu Xiankun; Chen Zhiyu; Liu Xianyi

2004-01-01

The study is designed to investigate the labelling of LL-EPO, purification of labelled compound, and therefore, to prepare the labelled LL-EPO with high purity and biological activity. LL-EPO was labelled with 125 I by the common used chloramine-T and the modified two-phase chloramine-T method, respectively. The labelled compound was purified by both gel filtration and ultrafiltration method, respectively. The purity of the labelled LL-EPO was determined by both trichloroacetic acid (TCA) and SDS-PAGE method, and the biological activity was determined by the reticulocyte counting method. The results demonstrated that the iodine incorporation and specific radioactivities were 89% and 5.82 x 10 5 Bq·μg -1 for LL-EPO labelled by the modified two-phase chloramine-T method and were 20.65% and 3.62 x 10 5 Bq·μg -1 for LL-EPO labelled by the common used chloramine-T method, respectively. The purity of labelled LL-EPO purified by both gel filtration and ultrafiltration were over 96% with TCA method purification. The labelled LL-EPO showed two bands with Rf of 0.28 and 0.49, respectively, which is identical to that of standard LL-EPO through SDS-PAGE. There was no loss of biological activity of LL-EPO after labelling as determined by reticulocyte counting method

Preparation of 19-iodo cholesterol labelled with 125 I; Preparacion del 19-yodocolesterol marcado con 125 I

Energy Technology Data Exchange (ETDEWEB)

Rodriguez, L.; Rebollo, D. V.; Ruiz, J. M.

1986-07-01

In this paper a new method of synthesis of 19-iodo cholesterol labelled with ''125 I, from commercial cholesterol, is described. Its high chemical (96%) and radiochemical (99.9%) purities high yield and short time of preparation permit us to dispose or a more accessible labelled compound, which results appropriates for clinical investigations and in the diagnosis of disturbances of the suprarenal glands. (Author) 9 refs.

Ethical and social significance of microdose clinical trial. Background of guidance draw-up

International Nuclear Information System (INIS)

Kurihara, Chieko

2008-01-01

Microdose clinical trial (MCT) aims to elucidate only the mass balance (pharmacokinetics, PK) in human of a new drug candidate compound before the first Phase I trial and is going to be approved by the authority MHLW in Japan. In MCT, the compound is administered in human in an extremely small amount (microdose) that is unexpected to exert its pharmacological effect ( 14 C) labeled compound is administered, LC/MS/MS with non-isotopic compound and positron emission tomography (PET) with compound labeled by positron emitter like 11 C, 13 N, etc. Under promotions by support and demand of related scientific societies and corporations in Japan as well as by ICH agreement, MHLW has defined MCT as one of clinical trials linked with GMP standard of drug candidate for clinical trials, with concept for assessment of internal radiation exposure, and with consistency with handling of radioisotopes, because of ethical consideration for volunteers to be enrolled. MCT can expectedly improve the cost- and time-effectiveness of new drug development, which ultimately leads to earlier supply of superior medicines. (R.T.)

Contribution to the study of the biological properties of compounds labeled with radio-chromium 51Cr

International Nuclear Information System (INIS)

Ingrand, J.

1964-07-01

Among the radioisotopes commonly used in biology and medicine which are controlled Individually in the Radioelement Departement of the Saclay Nuclear Research Centre before being sent to the users, the author has chosen chromium 51 incorporated in inorganic salts or in organic substrates for a study of the biological properties of the compounds. In the first part, he has compared the pathways followed by the radioactive sodium chromate and chromic chloride mixed with blood or given to the whole animal, the object being to determine whether a reduction of hexavalent chromium occurs, both in vitro and in vivo. In the second part, the author has tried to show the validity of using, various substrates labeled with chromium 51, red cells, haemoglobin, plasma proteins and cytochrome c. The results obtained have contributed to underline the interest of using such compounds for biological applications. (author) [fr

Isotopically labelled vitamin D derivatives and processes for preparing same

International Nuclear Information System (INIS)

Deluca, H.R.; Schnoes, H.K.; Napoli, J.L.; Fivizzani, M.A.

1981-01-01

This invention relates to 26,27-isotopically labelled vitamin D 3 compounds, including radiolabelled vitamin D 3 compounds of high specific activity, methods for their preparation, and intermediates obtained in their synthesis. The method involves reacting an ester of a 26,27-dinor-vitamin D-25-carboxylic acid with an isotopically labelled methyl Grignard reagent or methyl lithium reagent to obtain a 26,27-isotopically labelled compound in which at least some of the H atoms and/or C atoms are heavy isotopes. (author)

Direct isotope determination of isotopically labelled lipids by field desorption mass spectrometry

International Nuclear Information System (INIS)

Lehmann, W.D.; Kessler, M.

1982-01-01

Lipids labelled with deuterium or carbon-14 have been investigated by field desorption mass spectrometry for determination of their degree of labelling. This application is demonstrated for free fatty acids, cholesterol, cholesteryl esters, triglycerides, and L-α-phosphatidylcholines. Comparison of the molecular ion groups of the non-labelled and of the labelled compounds enables a fast and reliable determination of the degree of labelling. For multiply labelled compounds the label distribution is also obtained from the molecular ion group. In addition, for cholesteryl esters and for phosphatidylcholines structurally significant fragment ions provide information about the position of the label. Several hundred nanograms of the compound are typically required for a single analysis with a relative standard error of 0.5-2% in the value calculated for atom% hydrogen-2 or for the specific carbon-14 activity. (orig.) [de

Studies on the clinical application of MR perfusion image using arterial spin labeling method

International Nuclear Information System (INIS)

Miyasaka, Kenji

1999-01-01

A new technique for imaging brain perfusion, arterial spin labeling method was applied in clinic. Brain perfusion was imaged by FAIR and EPISTAR both of which using arterial spin labeling (ASL) method. Suitable parameters for small contamination were examined using a imaging phantom. Then normal volunteers were examined for imaging timing. Suitable time between labeling pulse and imaging pulse for brain capillary and parenchyma was 1.0 sec. For clinical application study, total 48 patients with brain diseases were examined by FAIR and/or EPISTAR. A lesion/white matter signal intensity ratio was calculated in all clinical cases. Average of signal intensity ratio in infarction, tumor and arteriovenous malformation (AVM) were 0.8, 2.2 and 18.6 at FAIR, and 0.6, 2.2 and 12.8 at EPISTAR, respectively. Low perfusion diseases such as cerebral infarction have low signal intensity ratio and high perfusion diseases such as AVM have high signal intensity ratio in both FAIR and EPISTAR. Brain lesions were imaged similarly in FAIR and EPISTAR, and no remarkable difference was found between FAIR and EPISTAR. As a result of diagnostic trial by signal intensity ratio in operated tumor, hemorrhagic cases could be diagnosed by accuracies of 75% in FAIR and 100% in EPISTAR, respectively. (author)

Radiopharmaceutical potential of I-131 labelled diazepam

International Nuclear Information System (INIS)

Yurt, F.; Unek, P.; Asikoglu, M.; Baggi, S.; Erener, G.; Ozkilic, H.; Uluc, F.; Tuglular, I.

1998-01-01

In this study, diazepam is a derivative of the 1.4 benzodiazepine family that the most widely used drug as anticonvulsant agent has been labeled with I-131, as a new radiopharmaceutical and its radiopharmaceutical potential has been determined. Labeling of diazepam has been performed by iodogen method and optimum labeling conditions have been determined. Optimum reaction conditions are 1 mg for iodogen amount; 1-5 mg for diazepam amount, 15-20 minutes for reaction time and room temperature for reaction temperature. Specific activity of labeled compound was 0,15 Ci/mmol level. N-octanol/water ratio was found 1.9 for 131 IDZ ( 131 I labeled diazepam). In vivo experiments have been carried out to determine radiopharmaceutical potentials of labeled compound. Biodistribution studies on rats showed that 131 IDZ have accumulated in kidneys, liver, lungs and brain tissues. Scintigraphic results taken with gamma camera on rabbits agree with biodistribution results of rats. (author)

Reductive methods for isotopic labeling of antibiotics

International Nuclear Information System (INIS)

Champney, W.S.

1989-01-01

Methods for the reductive methylation of the amino groups of eight different antibiotics using 3 HCOH or H 14 COH are presented. The reductive labeling of an additional seven antibiotics by NaB 3 H 4 is also described. The specific activity of the methyl-labeled drugs was determined by a phosphocellulose paper binding assay. Two quantitative assays for these compounds based on the reactivity of the antibiotic amino groups with fluorescamine and of the aldehyde and ketone groups with 2,4-dinitrophenylhydrazine are also presented. Data on the cellular uptake and ribosome binding of these labeled compounds are also presented

Comparison of Two Kinds of 64Cu Labelled Octreotide Analogues

Directory of Open Access Journals (Sweden)

HAN Zhen-yi1;LIANG Ji-xin1;HU Ji2;LUO Hong-yi1;QING Jing2;CHEN Yu-qing2;LI Guang2;LI Hong-yu1,2

2016-10-01

Full Text Available Octreotide analogues DOTA-TOC and DOTA-TATE were labeled with 64Cu. The influences of the ratio of peptide mass to 64Cu activity, pH value, temperature and reaction time on labeling yield were investigated. The optimum labeling was determined. In vitro stability tests in saline and 10% bovine serum had been carried out. Biodistribution of the two radiolabelled compounds in normal mice and Micro PET imaging in nude mice bearing U87MG tumor had been evaluated. The results showed that the labeling yields of 64Cu-DOTA-TOC and 64Cu-DOTA-TATE were higher than 95%. Two kinds of octreotide analogues labeled with 64Cu were quite stable in saline and decomposed slowly in 10% bovine serum at 37 ℃. Biodistribution results in normal mice showed that two 64Cu labelled tracers had similar profiles. Both of the compounds washed out from the blood quickly. High uptake of radioactivity in liver and kidneys indicated the tracers were excreted via both hepatobiliary system and renal system. At the same time, compared to 64Cu-DOTA-TOC, higher radioactivity accumulation of 64Cu-DOTA-TATE in liver and kidneys was observed. Micro PET images of U87MG tumor-bearing nude mice with 64Cu-DOTA-TOC and 64Cu-DOTA-TATE showed the tumors very clearly. The radioactivity uptake of 64Cu-DOTA-TATE in tumor was higher than that of 64Cu-DOTA-TOC. This work has paved the way for further preclinical and clinical application of 64Cu-DOTA-TOC and 64Cu-DOTA-TATE as PET tumor imaging agents.

(18)F-labeled rhodamines as potential myocardial perfusion agents: comparison of pharmacokinetic properties of several rhodamines.

Science.gov (United States)

Bartholomä, Mark D; Zhang, Shaohui; Akurathi, Vamsidhar; Pacak, Christina A; Dunning, Patricia; Fahey, Frederic H; Cowan, Douglas B; Treves, S Ted; Packard, Alan B

2015-10-01

We recently reported the development of the [(18)F]fluorodiethylene glycol ester of rhodamine B as a potential positron emission tomography (PET) tracer for myocardial perfusion imaging (MPI). This compound was developed by optimizing the ester moiety on the rhodamine B core, and its pharmacokinetic properties were found to be superior to those of the prototype ethyl ester. The goal of the present study was to optimize the rhodamine core while retaining the fluorodiethyleneglycol ester prosthetic group. A series of different rhodamine cores (rhodamine 6G, rhodamine 101, and tetramethylrhodamine) were labeled with (18)F using the corresponding rhodamine lactones as the precursors and [(18)F]fluorodiethylene glycol ester as the prosthetic group. The compounds were purified by semipreparative HPLC, and their biodistribution was measured in rats. Additionally, the uptake of the compounds was evaluated in isolated rat cardiomyocytes. As was the case with the different prosthetic groups, we found that the rhodamine core has a significant effect on the in vitro and in vivo properties of this series of compounds. Of the rhodamines evaluated to date, the pharmacologic properties of the (18)F-labeled diethylene glycol ester of rhodamine 6G are superior to those of the (18)F-labeled diethylene glycol esters of rhodamine B, rhodamine 101, and tetramethylrhodamine. As with (18)F-labeled rhodamine B, [(18)F]rhodamine 6G was observed to localize in the mitochondria of isolated rat cardiomyocytes. Based on these results, the (18)F-labeled diethylene glycol ester of rhodamine 6G is the most promising potential PET MPI radiopharmaceutical of those that have evaluated to date, and we are now preparing to carry out first-in-human clinical studies with this compound. Copyright © 2015 Elsevier Inc. All rights reserved.

18F-labeled rhodamines as potential myocardial perfusion agents: comparison of pharmacokinetic properties of several rhodamines

International Nuclear Information System (INIS)

Bartholomä, Mark D.; Zhang, Shaohui; Akurathi, Vamsidhar; Pacak, Christina A.; Dunning, Patricia; Fahey, Frederic H.; Cowan, Douglas B.; Ted Treves, S.; Packard, Alan B.

2015-01-01

Introduction: We recently reported the development of the [ 18 F]fluorodiethylene glycol ester of rhodamine B as a potential positron emission tomography (PET) tracer for myocardial perfusion imaging (MPI). This compound was developed by optimizing the ester moiety on the rhodamine B core, and its pharmacokinetic properties were found to be superior to those of the prototype ethyl ester. The goal of the present study was to optimize the rhodamine core while retaining the fluorodiethyleneglycol ester prosthetic group. Methods: A series of different rhodamine cores (rhodamine 6G, rhodamine 101, and tetramethylrhodamine) were labeled with 18 F using the corresponding rhodamine lactones as the precursors and [ 18 F]fluorodiethylene glycol ester as the prosthetic group. The compounds were purified by semipreparative HPLC, and their biodistribution was measured in rats. Additionally, the uptake of the compounds was evaluated in isolated rat cardiomyocytes. Results: As was the case with the different prosthetic groups, we found that the rhodamine core has a significant effect on the in vitro and in vivo properties of this series of compounds. Of the rhodamines evaluated to date, the pharmacologic properties of the 18 F-labeled diethylene glycol ester of rhodamine 6G are superior to those of the 18 F-labeled diethylene glycol esters of rhodamine B, rhodamine 101, and tetramethylrhodamine. As with 18 F-labeled rhodamine B, [ 18 F]rhodamine 6G was observed to localize in the mitochondria of isolated rat cardiomyocytes. Conclusions: Based on these results, the 18 F-labeled diethylene glycol ester of rhodamine 6G is the most promising potential PET MPI radiopharmaceutical of those that have evaluated to date, and we are now preparing to carry out first-in-human clinical studies with this compound

18F-labeled Rhodamines as Potential Myocardial Perfusion Agents: Comparison of Pharmacokinetic Properties of Several Rhodamines

Science.gov (United States)

Bartholoma, Mark D.; Zhang, Shaohui; Akurathi, Vamsidhar; Pacak, Christina A.; Dunning, Patricia; Fahey, Frederic H.; Cowan, Douglas B.; Treves, S. Ted; Packard, Alan B.

2015-01-01

Introduction We recently reported the development of the [18F]fluorodiethylene glycol ester of rhodamine B as a potential positron emission tomography (PET) tracer for myocardial perfusion imaging (MPI). This compound was developed by optimizing the ester moiety on the rhodamine B core, and its pharmacokinetic properties were found to be superior to those of the prototype ethyl ester. The goal of the present study was to optimize the rhodamine core while retaining the fluorodiethyleneglycol ester prosthetic group. Methods A series of different rhodamine cores (rhodamine 6G, rhodamine 101, and tetramethylrhodamine) were labeled with 18F using the corresponding rhodamine lactones as the precursors and [18F]fluorodiethylene glycol ester as the prosthetic group. The compounds were purified by semipreparative HPLC, and their biodistribution was measured in rats. Additionally, the uptake of the compounds was evaluated in isolated rat cardiomyocytes. Results As was the case with the different prosthetic groups, we found that the rhodamine core has a significant effect on the in vitro and in vivo properties of this series of compounds. Of the rhodamines evaluated to date, the pharmacologic properties of the 18F-labeled diethylene glycol ester of rhodamine 6G are superior to those of the 18F-labeled diethylene glycol esters of rhodamine B, rhodamine 101, and tetramethylrhodamine. As with 18F-labeled rhodamine B, [18F]rhodamine 6G was observed to localize in the mitochondria of isolated rat cardiomyocytes. Conclusions Based on these results, the 18F-labeled diethylene glycol ester of rhodamine 6G is the most promising potential PET MPI radiopharmaceutical of those that have been evaluated to date, and we are now preparing to carry out first-in-human clinical studies with this compound. PMID:26205075

Studies on the preparation of labelled compounds for γ-scintigraphy use

International Nuclear Information System (INIS)

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

1991-03-01

To develop 99m Tc instant labelling kit of d,1-HMPAO and 131 I labelled IMP for the regional cerebral blood flow scintigraphic use, d,1-HMPAO and IMP were synthesized. The former was prepared from 2,3-butadione monoxim and 2,2-dimethyl-1,3-propanediamine in the presence of cation exchange resin, and then selective reduction of imine bond with sodium borohydride followed by fractional crystallization of diastereometric mixture of HMPAO. The latter was prepared by condensation of p-iodophenylpropanone with isopropylamine, and then reduction of double bond with sodium borohydride. For the preparation of 99m Tc labelled HSA, experiments on incorporation of bifunctional chelating agent of DTPA to HSA, establishment of optimal conditions of 99m Tc labelling, determination of labelling yield and radiochemical purity, and examination of stability were carried out. (Author)

Applications of stable isotopes of /sup 2/H, /sup 13/C and /sup 15/N to clinical problems. Experience of a collaborative program at Argonne National Laboratory

Energy Technology Data Exchange (ETDEWEB)

Klein, P D; Szczepanik, P A; Hachey, D L [Argonne National Lab., Evanston, Ill. (USA)

1974-08-01

The function of the Argonne Program is to provide synthetic, analytical instrumental capability in a core facility for the clinical investigator who needs to use /sup 2/H, /sup 13/C, or /sup 15/N labelled compounds for metabolic or clinical research on pregnant women, newborn infants, young children, or for mass screening. To carry out such application development, there were six stages which were recurrent steps in every application. Five fundamental strategies should be adopted to establish the use of stable isotopes in clinical work. The instrument required for measurements was a combined gas chromatograph-mass spectrometer, and its use was schematically illustrated. Some of the successful experiences with compounds labelled by stable isotopes, such as deuterium labelled chenodeoxycholic acid, and respective /sup 13/C and /sup 15/N-labelled glycine were described. Deutrium labelled bile acid enabled easy and safe determination of the size of the bile acid pool and the replacement rate, providing clearer diagnoses for cholestatic liver disease and gallstones. /sup 13/C and /sup 15/N labelled compounds were used in clinical studies, of children with genetic disorders of amino acid metabolism, i.e., non ketotic hyperflycinemia, B/sub 12/-responsive methyl malonic acidemia, and Lesch-Nyhan syndrome. /sup 15/N-labelled glycine was also studied in a child with Lesch-Nyhan syndrome.

Clinical diagnostic system using a small cyclotron for medical use

International Nuclear Information System (INIS)

Yonekura, Y.; Magata, Y.; Konishi, J.

1990-01-01

Since a small cyclotron and a positron emission tomography (PET) scanner have been installed at the Kyoto University Hospital in 1983, a great deal of effort has been directed to the clinical application of the PET-cyclotron system. This paper outlines the experience with PET in the clinical setting, including the facility, equipments and staff involved, weekly schedule, typical clinical protocols, and some results from the patients. The system consists of small cyclotron for production of the short-lived positron emitting radionuclides, fully automated synthesis system for labeling various compounds, scanning for measurement of radioactivities, and data analysis system for calculating physiological parameters. A resolving cylinder target system with eight smaller cylinders is equipped for production of C-11, N-13, O-15, and F-18. Labeled compounds are quickly delivered to the PET scanner room by two systems--the continuous delivery system for the labeled gas and the rapid delivery system for the liquid compounds by compressed air. A PET scanner devoted for clinical studies is a multislice whole-body PET scanner. Ten PET studies are performed weekly on the average for measuring blood flow and oxygen and glucose metabolism in the brain, blood flow and glucose and fatty acid metabolism in the heart, blood flow and amino acid uptake in the pancreas, lung ventilation, and tumor glucose metabolism. The availability of PET-cyclotron system is still limited in view of cost. The previous clinical studies suggest the contribution of PET to the the understanding of the mechanism of disease pathophysiology. (N.K.)

Design and operations at the National Tritium Labelling Facility

International Nuclear Information System (INIS)

Morimoto, H.; Williams, P.G.

1991-09-01

The National Tritium Labelling Facility (NTLF) is a multipurpose facility engaged in tritium labeling research. It offers to the biomedical research community a fully equipped laboratory for the synthesis and analysis of tritium labeled compounds. The design of the tritiation system, its operations and some labeling techniques are presented

Synthesis of pyridine and isoquinoline labelled with 14C on the nitrogen heterocycle

International Nuclear Information System (INIS)

Robveille, Jacques

1985-01-01

This research thesis addresses the synthesis of derivatives of pyridine and isoquinoline labelled with carbon 14 ( 14 C) in the nitrogenated heterocycle as these compounds are of biological and pharmacological interest. The author aimed at developing rather general synthesis schemes which could be easily applied to the synthesis of radioactive compounds, and could produce, through a given synthesis way, the largest as possible family of differently substituted compounds. Different sources for labelled pyridine and isoquinoline have been used: dioxo-1,5 or their corresponding dioxins, substituted pentadienoic acids, derivatives of acrylic acid, and derivatives of cinnamic acid. Thus, three different synthesis processes have been developed to obtain 14 C labelled pyridine, and one of them is applied to the preparation of 14 C labelled isoquinoline. These synthesis processes can have a very general application, and allow different 14 C labelling positions to be envisaged. The possibility to obtain the same compounds but labelled with tritium can also be envisaged to obtain much higher specific activities [fr

Increase of the radiochemical purity of aqueous solutions of compounds labelled with 131I using a ClAg sterile column

International Nuclear Information System (INIS)

Pliego, O.H.; Mitta, A.E.A.

1980-01-01

The use of a C1Ag sterile column that may be easily assembled at any nuclear medical center is proposed. The column is easy to handle and allows to obtain aqueous solutions of compounds labelled with radioactive iodine, with a radiochemical purity greater than 99%, conserving pH values, activity concentration, apyretogenia and sterility, the controls of toxicity and presence of heavy metals being negative. (C.A.K) [es

A new 99mTc-red blood cell labeling procedure for cardiac blood pool imaging: Clinical results

International Nuclear Information System (INIS)

Kelbaek, H.; Buelow, K.; Aldershvile, J.; Moegelyang, J.; Nielsen, S.L.; Copenhagen Univ.

1989-01-01

The first clinical results of a new 99m Tc-red blood cell labeling procedure avoiding cell centrifugation are presented. One ml heparinized blood samples were incubated with small amounts of a stannous kit. By titration studies, ideal quantities of sodium hypochlorite for oxidation of extracellular tin and of EDTA as stabilizer of the label were found. The Cl - concentration and pH of the labeled blood were acceptable, and EDTA increased labeling yield and stability determined in vitro by a few percent. The new procedure gave a slightly higher labeling yield than a current technique using centrifugation of cells. Labeling efficiency expressed as cell bound/total activity was 96.6%±1.3% in healthy subjects and 95.5%±2.2% in cardiac patients and remained high for 2 h after reinjection. The biological halflife of labeled cells following the new procedure was 11-12 h rendering it suitable for serial determinations of radionuclide cardiography. (orig.)

Radiochemistry, pre-clinical studies and first clinical investigation of 90Y-labeled hydroxyapatite (HA) particles prepared utilizing 90Y produced by (n,γ) route

International Nuclear Information System (INIS)

Vimalnath, K.V.; Chakraborty, Sudipta; Rajeswari, A.; Sarma, H.D.; Nuwad, Jitendra; Pandey, Usha; Kamaleshwaran, K.; Shinto, Ajit; Dash, Ashutosh

2015-01-01

Introduction: The scope of using no carrier added (NCA) 90 Y [T 1/2 = 64.1 h, E β(max) = 2.28 MeV] obtained from 90 Sr/ 90 Y generator in radiation synovectomy (RSV) is widely accepted. In the present study, the prospect of using 90 Y produced by (n,γ) route in a medium flux research reactor for use in RSV was explored. Methods: Yttrium-90 was produced by thermal neutron irradiation of Y 2 O 3 target at a neutron flux of ~ 1 × 10 14 n/cm 2 .s for 14 d. The influence of various experimental parameters were systematically investigated and optimized to arrive at the most favorable conditions for the formulation of 90 Y labeled hydroxyapatite (HA) using HA particles of 1–10 μm size range. An optimized kit formulation strategy was developed for convenient one-step compounding of 90 Y-HA, which is easily adaptable at hospital radiopharmacy. The pre-clinical biological evaluation of 90 Y-HA particles was studied by carrying out biodistribution and bioluminiscence imaging studies in Wistar rats. The first clinical investigation using the radiolabeled preparation was performed on a patient suffering from chronic arthritis in knee joint by administering 185 MBq 90 Y-HA formulated at the hospital radiopharmacy deploying the proposed strategy. Results: Yttrium-90 was produced with a specific activity of 851 ± 111 MBq/mg and radionuclidic purity of 99.95 ± 0.02%. 90 Y-labeled HA particles (185 ± 10 MBq doses) were formulated in high radiochemical purity (> 99%) and excellent in vitro stability. The preparation showed promising results in pre-clinical studies carried out in Wistar rats. The preliminary results of the first clinical investigation of 90 Y-HA preparation in a patient with rheumatoid arthritis in knee joints demonstrated the effectiveness of the formulation prepared using 90 Y produced via (n,γ) route in the management of the disease. Conclusion: The studies revealed that effective utilization of 90 Y produced via (n,γ) route in a medium flux research

Photoaffinity labeling of the oxysterol binding protein

International Nuclear Information System (INIS)

Taylor, F.R.; Kandutsch, A.A.; Anzalone, L.; Spencer, T.A.

1986-01-01

A cytosolic receptor protein for oxygenated sterols, that is thought to be involved in the regulation of HMG-CoA reductase and cholesterol biosynthesis, can be labeled covalently by the photoactivated affinity compound [5,6- 3 H]-7,7'-azocholestane-3β,25-diol (I). Several other compounds were tested including 25-hydroxycholesta-4,6-dien-3-one, 25-azido-27-norcholest-5-en-3β-ol,3β,25-dihydroxycholest-5-en-7-one and 3β-hydroxycholesta-8(14),9(11)-dien-15-one. However, these sterols either did not bind to the receptor with adequate affinity or did not react covalently with the receptor during photolysis. Compound I binds to the receptor with very high affinity (K/sub d/ = 30 nM). After activation with long wavelength UV, two tritium labeled proteins, M/sub r/ approximately 95K and 65K daltons, are found upon SDS gel electrophoresis. No labeling occurs when the binding reaction is carried out in the presence of a large excess of 25-hydroxycholesterol. It is possible that the smaller polypeptide is a degradation product. Under the reaction conditions investigated so far labeling is relatively inefficient (< 1% of bound sterol). These results are generally consistent with previous information suggesting that the M/sub r/ of the receptor subunit is 97,000. Covalent labeling of the receptor should greatly facilitate its further purification and characterization

Concentration of labelled polyphosphates in soft tissue lesions. Application to the study of cerebral and myocardial infarction

International Nuclear Information System (INIS)

Guillemart, Alain.

1975-01-01

The biological behavior and tissue localization of phosphorus compounds used in Nuclear Medicine are reviewed. The mechanism of skeletal localization is emphasized. Labeled pyrophosphate compounds have proved extremely useful for skeletal imaging, however the mechanism of increased accumulation of these agents has been observed also in soft tissues. They localize in the acutely infarcted myocardium and in brain lesions. Clinical results obtained with sup(99m)Tc stannous pyrophosphate in brain and myocardium imaging are reported [fr

Assessment of volatile organic compounds and particulate matter in a dental clinic and health risks to clinic personnel.

Science.gov (United States)

Hong, Yu-Jue; Huang, Yen-Ching; Lee, I-Long; Chiang, Che-Ming; Lin, Chitsan; Jeng, Hueiwang Anna

2015-01-01

This study was conducted to assess (1) levels of volatile organic compounds (VOCs) and particulate matter (PM) in a dental clinic in southern Taiwan and (2) dental care personnel's health risks associated with due to chronic exposure to VOCs. An automatic, continuous sampling system and a multi-gas monitor were employed to quantify the air pollutants, along with environmental comfort factors, including temperature, CO2, and relative humidity at six sampling sites in the clinic over eight days. Specific VOC compounds were identified and their concentrations were quantified. Both non-carcinogenic and carcinogenic VOC compounds were assessed based on the US Environmental Protection Agency's Principles of Health Risk Assessment in terms of whether those indoor air pollutants increased health risks for the full-time dental care professionals at the clinic. Increased levels of VOCs were recorded during business hours and exceeded limits recommended by the Taiwan Environmental Protection Agency. A total of 68 VOC compounds were identified in the study area. Methylene methacrylate (2.8 ppm) and acetone (0.176 ppm) were the only two non-carcinogenic compounds that posed increased risks for human health, yielding hazard indexes of 16.4 and 4.1, respectively. None of the carcinogenic compounds increased cancer risk. All detected PM10 levels ranged from 20 to 150 μg/m(3), which met the Taiwan EPA and international limits. The average PM10 level during business hours was significantly higher than that during non-business hours (P = 0.04). Improved ventilation capacity in the air conditioning system was recommended to reduce VOCs and PM levels.

Labeled estrogens as mammary tumor probes

International Nuclear Information System (INIS)

Feenstra, A.

1981-01-01

In this thesis estrogens labeled with a gamma or positron emitting nuclide, called estrogen-receptor binding radiopharmaceuticals are investigated as mammary tumour probes. The requirements for estrogen-receptor binding radiopharmaceuticals are formulated and the literature on estrogens labeled for this purpose is reviewed. The potential of mercury-197/197m and of carbon-11 as label for estrogen-receptor binding radiopharmaceuticals is investigated. The synthesis of 197 Hg-labeled 4-mercury-estradiol and 2-mercury-estradiol and their properties in vitro and in vivo are described. It appears that though basically carbon-11 labeled compounds are very promising as mammary tumour probes, their achievable specific activity has to be increased. (Auth.)

Development of Tc-99m labeled myocardial imaging agent

International Nuclear Information System (INIS)

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

2006-02-01

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

Design and Synthesis of 11C-Labelled Compound Libraries for the Molecular Imaging of EGFr, VEGFr-2, AT1 and AT2 Receptors: Transition-Metal Mediated Carbonylations Using [11C]Carbon Monoxide

International Nuclear Information System (INIS)

Aaberg, Ola

2009-01-01

This work deals with radiochemistry and new approaches to develop novel PET tracers labelled with the radionuclide 11 C. Two methods for the synthesis of 11 C-labelled acrylamides have been explored. First, [1- 11 C]-acrylic acid was obtained from a palladium(0)-mediated 11 C-carboxylation of acetylene with [ 11 C]carbon monoxide; this could be converted to the corresponding acyl chloride and then combined with benzylamine to form N-benzyl[carbonyl- 11 C]acrylamide. In the second method, the palladium(0)-mediated carbonylation of vinyl halides with [ 11 C]carbon monoxide was explored. This latter method, yielded labelled acrylamides in a single step with retention of configuration at the C=C double bond, and required less amine compared to the acetylene method. The vinyl halide method was used to synthesize a library of 11 C-labelled EGFr-inhibitors in 7-61% decay corrected radiochemical yield via a combinatorial approach. The compounds were designed to target either the active or the inactive form of EGFr, following computational docking studies. The rhodium(I)-mediated carbonylative cross-coupling of an azide and an amine was shown to be a very general reaction and was used to synthesize a library of dual VEGFr-2/PDGFrβ inhibitors that were 11 C-labelled at the urea position in 38-78% dc rcy. The angiotensin II AT 1 receptor antagonist eprosartan was 11 C-labelled at one of the carboxyl groups in one step using a palladium(0)-mediated carboxylation. Autoradiography shows specific binding in rat kidney, lung and adrenal cortex, and organ distribution shows a high accumulation in the intestines, kidneys and liver. Specific binding in frozen sections of human adrenal incidentalomas warrants further investigations of this tracer. Three angiotensin II AT 2 ligands were 11 C-labelled at the amide group in a palladium(0)-mediated aminocarbonylation in 16-36% dc rcy. One of the compounds was evaluated using in vitro using autoradiography, and in vivo using organ

99mTc labeling of carbon nanomaterials

International Nuclear Information System (INIS)

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

2008-01-01

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

15N-labelled pyrazines of triterpenic acids

International Nuclear Information System (INIS)

Vlk, Martin; Micolova, Petra; Sarek, Jan

2016-01-01

Triterpenoid pyrazines from our research group were found selectively cytotoxic on several cancer cell lines with IC 50 in low micromolar range. This sparked our interest in preparing their labeled analogs for metabolic studies. In this work, we prepared a set of non-labeled pyrazines from seven triterpenoid skeletal types along with their 15 N labelled analogs. In this work, we present the synthesis and characterization of the target 15 N labelled pyrazines. Currently, these compounds are being studied in complex metabolic studies. (author)

99Tcsup(m)-HMPAO labelled leucocytes: comparison with 111In-tropolonate labelled granulocytes

International Nuclear Information System (INIS)

Peters, A.M.; Roddie, M.E.; Zacharopoulos, G.P.; George, P.; Stuttle, A.W.J.; Lavender, J.P.; Danpure, H.J.; Osman, S.

1988-01-01

The lipophilic complex, 99 Tcsup(m)-hexamethylpropyleneamine oxime (HMPAO) is an efficient leucocyte label, and labels granulocytes with more stability than mononuclear leucocytes. The recovery of 99 Tcsup(m)-HMPAO granulocytes was similar to 111 In-labelled granulocytes isolated and labelled in plasma using tropolone. The Tsub(1/2) of 99 Tcsup(m)-HMPAO labelled granulocytes in blood was less than that of 111 In-labelled granulocytes. The initial biodistribution of 99 Tcsup(m)-labelled leucocytes was similar to 111 In-labelled granulocytes, with a rapid initial lung transit, prominent splenic activity, bone marrow activity and minimal hepatic activity, although, unlike 111 In, 99 Tcsup(m) activity was also seen in urine, occasionally in the gallbladder, and, from about 4 h, consistently in the colon. Bone marrow activity was particularly prominent with 99 Tcsup(m). About 6% of 99 Tcsup(m) was excreted in the faeces up to 48 h after injection, and about 17% in urine up to 24 h. The time-activity curves of reticuloendothelial activity up to 24 h were broadly similar for the two labelled cell preparations. Clinical information given by the two agents was similar in 27 of 30 patients who received both. We conclude that with respect to granulocyte kinetics and clinical data, 99 Tcsup(m)-HMPAO labelled leucocytes are comparable with 111 In-tropolonate labelled granulocytes. (author)

Labelling strategies for enhanced application of ICPMS in protein analysis

International Nuclear Information System (INIS)

Bettmer, J.; Kutscher, D.J.

2009-01-01

Full text: Quantitative protein analysis is one of today's challenges in analytical chemistry. Herein, mass spectrometric techniques play an important role with the use of both label-free and labelling approaches. In the field of ICPMS, the latter approach is attractive as it can provide highly sensitive detection of proteins after labelling with metal-containing compounds. Following a brief introduction to the different strategies described in the literature, this presentation will be focussed on protein labelling using a mercury compound (p-hydroxymercuribenzoic acid, pHMB). Besides fundamental studies on the derivatization process itself, a strategy will be presented in which absolute protein quantification can be achieved. Finally, the potential, but also limitations of the technique will be highlighted. (author)

Short-lived positron emitter labeled radiotracers - present status

International Nuclear Information System (INIS)

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

1982-01-01

The preparation of labelled compounds is important for the application of positron emission transaxial tomography (PETT) in biomedical sciences. This paper describes problems and progress in the synthesis of short-lived positron emitter ( 11 C, 18 F, 13 N) labelled tracers for PETT. Synthesis of labelled sugars, amino acids, and neurotransmitter receptors (pimozide and spiroperidol tagged with 11 C) is discussed in particular

Labelled chemotherapeutic drugs and neurotransmitter precursors

International Nuclear Information System (INIS)

Diksic, M.

1989-01-01

The authors have synthesized several chemotherapeutic drugs and their analogs labelled with 11 C or 18 F positron emitting radionuclides. The pharmacokinetics of several of these, 1,3-bis-2-chloroethylnitroso [ 11 C] urea [ 11 C-BCNU] and sarcosinamide congenerate of BCNU [SarCNU] were studied in animals and humans. This evaluation permitted them to have a better understanding of the tissue trapping of nitrosoureas and also the opportunity to do biological modelling permitting a better schedule of chemotherapy for these drugs. They have also been working on an analog of tryptophan, α-methyl-L-tryptophan, the compound studied for the past 15 years. An introduction of 11 C-label permitted in vivo evaluation of that compound and in conjunction with biochemical measurements done with 14 C-compound estimates of the rate of the brain serotonin synthesis without any metabolic manipulation

Chemoenzymatic synthesis of carbon-14 labelled antioxidants

International Nuclear Information System (INIS)

Deigner, H.P.; Freyberg, C.; Heck, R.

1993-01-01

The syntheses of [ 14 C] labelled antioxidants are described. We developed an efficient synthetic methodology to prepare a series of labelled amides with antioxidant activity, starting from [ 14 C] KCN and alkyl or aryl halides. By a combination of nucleophilic displacement of halides by [ 14 C] cyanide, mediated by ultrasound and subsequent mild and selective enzymatic hydrolysis of the resulting nitriles, labelled carboxylic acids were obtained. Labelled amines were prepared by reduction of the respective nitriles. Availability of [ 14 C] KCN, efficient introduction of the label by ultrasound mediated reaction and selective and mild hydrolysis by commercially available nitrilase (Rhodococcus sp.), makes possible a wide range of applications of this methodology in the synthesis of functionalized labelled compounds. (Author)

In vivo stability and inertness of various direct labelled and chelate-tagged protein

International Nuclear Information System (INIS)

Janoki, A.; Korosi, L.; Klivenyi, G.; Spett, B.

1987-01-01

There were looking for methods giving precise information about composition and activity distribution of protein components, both in the initial samples and serum samples after intravenous administration. It was tested the applicability of electroimmunoassay, polyacrilamide gel electrophoresis and high performance liquid chromatography for the assessment of in vivo stability and labelled proteins. The model compound was human serum albumin (HSA) labelled with 99m Tc and 125 I, respectively. Bifunctional chelate labelling was done with desferrioxamine, in this case protein was labelled with 67 Ga. Biodistribution of the labelled compounds and their elimination from the blood were studied in rabbits. Experience with various labelling proteins, especially with Tc-Sn-HSA system indicate that in vivo stability of this compounds are generally low. Following intravenous injection of proteins labelled with metal isotopes, due to dilution and to the presence of considerable amount of compatitive protein in the serum, part of the label is being detached from the carrier protein. Distribution of the detached metal is different from the original distribution of the protein. This problem arises also with radiopharmaceuticals based on monoclonal antibodies. (M.E.L.) [es

The radioactive labeling of monocytes

International Nuclear Information System (INIS)

Ensing, G.J.

1985-01-01

With the aim of studying a possible relationship between circulating monocytes and Sternberg-Reed cells investigations were started on the specific labeling of monocytes. In this thesis the literature on the pertinent data has been reviewed and a series of experiments on the monocyte labeling procedure has been described. The principles of cell labeling with radioactive compounds were discussed. 1. Total separation of the particular cell population to be labeled and subsequent labeling with a non-specific radiopharmaceutical. 2. Specific cell labeling in a mixture of cell types based on a well defined affinity of the cell under study for the radiopharmaceutical used. Next the radionuclides that can be used for cell labeling purposes were discussed with special attention for 111 In and its chelates. The principles of radiodosimetry were also discussed shortly. This section was focussed on the radiation dose the labeled cells receive because of the intracellular localized radioactivity. The radiation burden is high in comparison to amounts of radiation known to affect cell viability. A newly developed method for labeling monocytes specifically by phagocytosis of 111 In-Fe-colloid without apparent loss of cells was described in detail. (Auth.)

Evaluation of radiolabeling of annexin A5 with technetium-99m: influence of the labeling methods on physico-chemical and biological properties of the compounds

International Nuclear Information System (INIS)

Santos, Josefina da Silva

2009-01-01

Annexin A5 (ANXA5) is an intracellular human protein of 36 kDa with high affinity for membrane-bound phosphatidylserine that is selectively exposed on the surface of cells undergoing apoptosis. Apoptosis is important in normal physiology and innumerous pathologic states. Clinical applications for ANXA5 imaging are being developed in oncology, organ transplantation and cardiovascular diseases. Many strategies to radiolabel the protein have been described, including direct labeling, derivatization through a bifunctional chelating agent (BFC), production of mutated protein or peptide analogs. Several 99 mTc-labeling techniques have been reported using different cores, including [Tc=O] +3 , [Tc]HYNIC, [Tc≡N]+2 and [Tc(CO 3 )] +1 . In this study, we evaluated the influence of 99 mTc cores on biological behavior and physico-chemical properties of radiolabeled annexin. Radiolabeling procedure using [Tc≡N] +2 core was a two-step procedure including the reaction of 99 mTcO4 - with SDH in the presence of SnCl 2 and PDTA to obtain the intermediate 99 mTcN-SDH, and successive addition of ANXA5. The results obtained were not satisfactory, despite the high efficiency in the production of the intermediate. The [Tc=O] +3 core was produced using the ethylene dicysteine (EC) as BFC. TSTU was employed in the derivatization to produce the corresponding hydroxysuccinimide ester. Different ANXA5:EC ratios were studied and all labeling conditions resulted in high radiochemical yield but with differences in lipophilicity, stability, biological distribution and affinity for apoptotic cells. The HYNIC-ANXA5 also produced the labeled protein with high radiochemical yield. The stability of the radiolabeled ANXA5 was evaluated after storing at room temperature, at 2 - 8 degree C and in human serum at 37 degree C. The analysis of these results showed that the 99 mTc-EC-ANXA5 (ratio 10-2) was the most stable compound in all the studied conditions. Partition coefficient assay resulted in

Synthesis of deuterium labeled perillyl alcohol and dual C-13 and deuterium labeled perillic acid, major metabolites of d-limonene

International Nuclear Information System (INIS)

Chen, Haitao; Chan, K.C.

1997-01-01

Dual C-13 and deuterium labeled perillic acid, [(1,1-dideuterio-1- 13 C-2-methyl)ethenyl]-1-cyclohexene -1-carboxylic acid (6) and deuterated perillyl alcohol, [(2,2-dideuterio-1-methyl)ethenyl]-1-deuteriohydroxymethyl-1-cyclo -hexene (9) were synthesized from commercially available (4S)-(-)-perillaidehyde (1). Compound 1 was first protected with ethylene glycol to yield the ethylene ketal followed by oxidation with OsO 4 /NalO 4 to cleave the terminal double bond to afford the key intermediate ketone, 4-acetyl-1-cyclohexene-1-carboxaldehyde ethylene ketal (3). 3 was then converted to the labeled perillyl aldehyde by Wittig reaction with prepared Ph 3 P 13 CD 3 l or Ph 3 PCD 3 l. Followed by deprotection to give the labeled perillaldehydes, [(2,2-dideuterio-2- 13 C-1-methyl)ethenyl] -1-cyclohexene-1-carboxaldehyde-1-carboxaldehyde (5) or [(2,2-dideuterio-1-methyl)ethenyl] -1-cyclohexene-1-carboxaldehyde (8). 5 was further oxidized by freshly prepared Ag 2 O to give the desired compound 6. 8 was reduced by LiAID 4 to afford the desired compound 9. The same synthetic procedure may be adopted to synthesize the radioactive isotope labeled perillic acid and perilly alcohol. (author)

Biogenic volatile organic compounds (BVOCs) emission of Scots pine under drought stress - a 13CO2 labeling study to determine de novo and pool emissions under different treatments

Science.gov (United States)

Lüpke, M.

2015-12-01

Plants emit biogenic volatile organic compounds (BVOCs) to e.g. communicate and to defend herbivores. Yet BVOCs also impact atmospheric chemistry processes, and lead to e.g. the built up of secondary organic aerosols. Abiotic stresses, such as drought, however highly influence plant physiology and subsequently BVOCs emission rates. In this study, we investigated the effect of drought stress on BVOCs emission rates of Scots pine trees, a de novo and pool emitter, under controlled climate chamber conditions within a dynamic enclosure system consisting of four plant chambers. Isotopic labeling with 13CO2 was used to detect which ratio of emissions of BVOCs derives from actual synthesis and from storage organs under different treatments. Additionally, the synthesis rate of the BVOCs synthesis can be determined. The experiment consisted of two campaigns (July 2015 and August 2015) of two control and two treated trees respectively in four controlled dynamic chambers simultaneously. Each campaign lasted for around 21 days and can be split into five phases: adaptation, control, dry-out, drought- and re-watering phase. The actual drought phase lasted around five days. During the campaigns two samples of BVOCs emissions were sampled per day and night on thermal desorption tubes and analyzed by a gas chromatograph coupled with a mass spectrometer and a flame ionization detector. Additionally, gas exchange of water and CO2, soil moisture, as well as leaf and chamber temperature was monitored continuously. 13CO2 labeling was performed simultaneously in all chambers during the phases control, drought and re-watering for five hours respectively. During the 13CO2 labeling four BVOCs emission samples per chamber were taken to identify the labeling rate on emitted BVOCs. First results show a decrease of BVOCs emissions during the drought phase and a recovery of emission after re-watering, as well as different strength of reduction of single compounds. The degree of labeling with 13

Simultaneous quantitative analysis of nine vitamin D compounds in human blood using LC-MS/MS.

Science.gov (United States)

Abu Kassim, Nur Sofiah; Gomes, Fabio P; Shaw, Paul Nicholas; Hewavitharana, Amitha K

2016-01-01

It has been suggested that each member of the family of vitamin D compounds may have different function(s). Therefore, selective quantification of each compound is important in clinical research. Development and validation attempts of a simultaneous determination method of 12 vitamin D compounds in human blood using precolumn derivatization followed by LC-MS/MS is described. Internal standard calibration with 12 stable isotope labeled analogs was used to correct for matrix effects in MS detector. Nine vitamin D compounds were quantifiable in blood samples with detection limits within femtomole levels. Serum (compared with plasma) was found to be a more suitable sample type, and protein precipitation (compared with saponification) a more effective extraction method for vitamin D assay.

A spin labelling study of immunomodulating peptidoglycan monomer and adamantyltripeptides entrapped into liposomes.

Science.gov (United States)

Frkanec, Ruza; Noethig-Laslo, Vesna; Vranesić, Branka; Mirosavljević, Krunoslav; Tomasić, Jelka

2003-04-01

The interaction of immunostimulating compounds, the peptidoglycan monomer (PGM) and structurally related adamantyltripeptides (AdTP1 and AdTP2), respectively, with phospholipids in liposomal bilayers were investigated by electron paramagnetic resonance spectroscopy. (1). The fatty acids bearing the nitroxide spin label at different positions along the acyl chain were used to investigate the interaction of tested compounds with negatively charged multilamellar liposomes. Electron spin resonance (ESR) spectra were studied at 290 and 310 K. The entrapment of the adamantyltripeptides affected the motional properties of all spin labelled lipids, while the entrapment of PGM had no effect. (2). Spin labelled PGM was prepared and the novel compound bearing the spin label attached via the amino group of diaminopimelic acid was chromatographically purified and chemically characterized. The rotational correlation time of the spin labelled molecule dissolved in buffer at pH 7.4 was studied as a function of temperature. The conformational change was observed above 300 K. The same effect was observed with the spin labelled PGM incorporated into liposomes. Such effect was not observed when the spin labelled PGM was studied at alkaline pH, probably due to the hydrolysis of PGM molecule. The study of possible interaction with liposomal membrane is relevant to the use of tested compounds incorporated into liposomes, as adjuvants in vivo.

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.

Cyclotrons, radionuclides, precursors, and demands for routine versus research compounds

International Nuclear Information System (INIS)

Wolf, A.P.

1984-01-01

Accelerators for producing commonly used short-lived positron emitters for positron emission tomography are addressed in the context of their use for the preparation of labeled compounds for research and routine biomedical applications. Progress and direction in the preparation and use of radiotracers for studies of the brain are discussed. Advancement to complete automation is stressed as an important factor for the eventual use of positron emission tomography as a routine clinical tool in universities and major medical centers

Understanding the mechanism of sweet taste: synthesis of tritium labeled guanidineacetic acids

Energy Technology Data Exchange (ETDEWEB)

Nagarajan, S.; Kellogg, M.S.; DuBois, G.E. (NutraSweet Company, Mt. Prospect, IL (United States)); Williams, D.S. (Amersham International plc, Cardiff (United Kingdom). Cardiff Labs.); Gresk, C.J.; Markos, C.S. (Searle Research and Development, Skokie, IL (United States))

1992-08-01

Syntheses of tritium labeled guanidineacetic acid sweetener and a tritiated photoaffinity labeling reagent via the catalytic hydrogenation of the dibromo intermediates are described. These labeled compounds were required for the investigation of sweet taste mechanism. (author).

Understanding the mechanism of sweet taste: synthesis of tritium labeled guanidineacetic acids

International Nuclear Information System (INIS)

Nagarajan, S.; Kellogg, M.S.; DuBois, G.E.; Williams, D.S.

1992-01-01

Syntheses of tritium labeled guanidineacetic acid sweetener and a tritiated photoaffinity labeling reagent via the catalytic hydrogenation of the dibromo intermediates are described. These labeled compounds were required for the investigation of sweet taste mechanism. (author)

The use of compound topical anesthetics: a review.

Science.gov (United States)

Kravitz, Neal D

2007-10-01

The author reviewed the history of, federal regulations regarding, risks of and adverse drug reactions of five compound topical anesthetics: tetracaine, adrenaline/epinephrine and cocaine (TAC); lidocaine, adrenaline/epinephrine and tetracaine (LET); lidocaine, tetracaine and phenylephrine (TAC 20 percent Alternate); lidocaine, prilocaine and tetracaine (Profound); and lidocaine, prilocaine, tetracaine and phenylephrine with thickeners (Profound PET). The author reviewed clinical trials, case reports, descriptive articles, and U.S. Food and Drug Administration (FDA) regulations and recent public advisory warnings regarding the federal approval of and risks associated with the use of compound topical anesthetics. Compound topical anesthetics are neither FDA-regulated nor -unregulated. Some compounding pharmacies bypass the new FDA drug approval process, which is based on reliable scientific data and ensures that a marketed drug is safe, effective, properly manufactured and accurately labeled. Two deaths have been attributed to the lay use of compound topical anesthetics. In response, the FDA has announced the strengthening of its efforts against unapproved drug products. Compound topical anesthetics may be an effective alternative to local infiltration for some minimally invasive dental procedures; however, legitimate concerns exist in regard to their safety. Until they become federally regulated, compound topical anesthetics remain unapproved drug products whose benefits may not outweigh their risks for dental patients.

Labelled antibiotics as tumour-localizing agents

International Nuclear Information System (INIS)

Taylor, D.M.; McCready, V.R.

1976-01-01

The published results of clinical and experimental studies of labelled bleomycins and tetracyclines are reviewed. None of the labelled antibiotics yet studied show anything approaching absolute tumour specificity. Clinical trials suggest that 57 Co-bleomycin is superior to either 111 In- or 99 Tcsup(m)-bleomycin and that it may possess some advantages over 67 Ga-citrate in respect of lower uptake in the abdomen and, possibly, lower uptakes in benign and inflammatory lesions. Radioiodine-labelled or 99 Tcsup(m)-labelled tetracyclines appear to be of little value in tumour localization. (author)

Efficient method of enzymatic synthesis of nucleosides labelled with 14C and 3H

International Nuclear Information System (INIS)

Nejedly, Z.; Filip, J.

1988-01-01

The method is presented of enzymatic synthesis of nucleosides labelled with 14 C or 3 H either uniformly or specifically in the base or the deoxyribosyl or ribosyl moiety. The method is based on the ribosylation or deoxyribosylation of the nucleic acid bases (non-labelled or labelled with 14 C or 3 H) by the catalytic effect of enzymes occurring in the supernatant fractions of non-purified homogenates of Escherichia coli B. bacteria. The non-labelled and labelled nucleosides are used as donors of ribosyl or deoxyribosyl groups. The HPLC method is used for separating labelled nucleosides. The radiochemical purity of the labelled nucleosides is higher than 98%, molar activity ranges from 9.2 to 18.5 GBq.mmol -1 ( 14 C-labelled compounds) and from 0.6 to 1.9 TBq.mmol -1 (3H-labelled compounds). (author). 4 figs., 8 refs

Studies in the preparation of /sup 32/P labelled compounds from high grade rock phosphate with high fluorine content. [Water soluble P/sub 2/O/sub 5/, acidulation, curing

Energy Technology Data Exchange (ETDEWEB)

Murthy, T S; Cherian, S; Shivarudrappa, V; Subramanian, T K; Achari, P S [Bhabha Atomic Research Centre, Bombay (India). Primary Isotopes Section

1981-01-01

The labelled phosphate to be used for crop evaluation studies should have characteristics exactly similar to the industrial product employed in agriculture. For the preparation of /sup 32/P labelled compound from rock phosphate with high fluorine content, a number of parameters have been studied like particle size of the rock, temperature and amount of acid required, the curing time, etc. Because of the high reaction temperature, the curing time is reduced to experimental limits compared to the commercial product. This paper describes a method for the preparation of such a labelled phosphate and this yields a product with about 95% of the phosphate in the water soluble form.

Clinical Evaluation of 57Co-labelled Bleomycin for Tumor Localization

International Nuclear Information System (INIS)

Ryu, Yong Wun; Kim, Jang Hee; Lee, Jhin Oh

1987-01-01

Investigation with 57 Co-Bleomycin in patients with the various cancers and in tumor bearing animals are described. In the patients, 57 Co-Bleomycin appears to be one of the useful tumor- seeking radiopharmaceuticals, and worth applicable to clinical uses. Labelled yield of 57 Co-Bleo was about 97% by thin layer chromatography. The pyrogen free tests were performed to meet U.S.P. critical ranges. In clinical studies with 57 Co-Bleo, 4 cases out of 5 patients with lung cancer, 2 cases among 3 thyroid cancer patients, and all 3 hepatoma patients showed positive tumor scans. The patients with stomach cancer, and the esophageal cancer showed false negative scintigraphy. A case with pulmonary tuberculosis showed a positive scan while liver abscess showed a negative picture. The merits of 57 Co-Bleomycin scintigraphy seems to be its relatively high affinity to tumors and low radiation hazard in spite of long physical half life.

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

International Nuclear Information System (INIS)

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

1995-01-01

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

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

International Nuclear Information System (INIS)

Jiang Ningyi; Sha Xiaozhen; Zhang Hua

1996-01-01

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

Synthesis of carbon-14 and tritium labeled cis-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzamidehydrochloride, an anticonvulsant agent

International Nuclear Information System (INIS)

Hsi, R.S.P.; Stolle, W.T.; Ayer, D.E.

1992-01-01

The title compound, U-54494A, is an anticonvulsant agent with clinical potential for treating epilepsy and a broad spectrum of seizure disorders. Structurally it is related to kappa opiod agonists and shares their anticonvulsant properties, but appears to be devoid of analgesic, sedative, and diuretic side effects. It also has been shown to inhibit neuronal damage and seizures induced by excitatory amino acids. This report describes the synthesis of the racemic U-54494A labeled with carbon-14 at the carboxamide carbon and with tritium in the pyrrolidine ring at C-3 and C-4. These radioisotope labeled versions of U-54494A were prepared for conducting drug disposition studies of this compound in test animals and human subjects

The tritium labelling of ibuprofen by heterogeneous catalytic exchange

International Nuclear Information System (INIS)

Santamaria, J.; Rebollo, D.V.; Rivera, P.; Estaban, M.

1986-01-01

The tritium labelling of 2-(4-isobutylphenyl) propionic acid (ibuprofen) was performed. The method employed was heterogeneous catalytic exchange between ibuprofen and tritiated water. Prior to labelling, thermic stability of ibuprofen was studied. Purification was accomplished through thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Concentration, purity and specific activity of the labelled compound were determined by ultraviolet, HPLC and liquid scintillation techniques. (author)

101 labeled brain images and a consistent human cortical labeling protocol

Directory of Open Access Journals (Sweden)

Arno eKlein

2012-12-01

Full Text Available We introduce the Mindboggle-101 dataset, the largest and most complete set of free, publicly accessible, manually labeled human brain images. To manually label the macroscopic anatomy in magnetic resonance images of 101 healthy participants, we created a new cortical labeling protocol that relies on robust anatomical landmarks and minimal manual edits after initialization with automated labels. The Desikan-Killiany-Tourville (DKT protocol is intended to improve the ease, consistency, and accuracy of labeling human cortical areas. Given how difficult it is to label brains, the Mindboggle-101 dataset is intended to serve as brain atlases for use in labeling other brains, as a normative dataset to establish morphometric variation in a healthy population for comparison against clinical populations, and contribute to the development, training, testing, and evaluation of automated registration and labeling algorithms. To this end, we also introduce benchmarks for the evaluation of such algorithms by comparing our manual labels with labels automatically generated by probabilistic and multi-atlas registration-based approaches. All data and related software and updated information are available on the http://www.mindboggle.info/data/ website.

101 Labeled Brain Images and a Consistent Human Cortical Labeling Protocol

Science.gov (United States)

Klein, Arno; Tourville, Jason

2012-01-01

We introduce the Mindboggle-101 dataset, the largest and most complete set of free, publicly accessible, manually labeled human brain images. To manually label the macroscopic anatomy in magnetic resonance images of 101 healthy participants, we created a new cortical labeling protocol that relies on robust anatomical landmarks and minimal manual edits after initialization with automated labels. The “Desikan–Killiany–Tourville” (DKT) protocol is intended to improve the ease, consistency, and accuracy of labeling human cortical areas. Given how difficult it is to label brains, the Mindboggle-101 dataset is intended to serve as brain atlases for use in labeling other brains, as a normative dataset to establish morphometric variation in a healthy population for comparison against clinical populations, and contribute to the development, training, testing, and evaluation of automated registration and labeling algorithms. To this end, we also introduce benchmarks for the evaluation of such algorithms by comparing our manual labels with labels automatically generated by probabilistic and multi-atlas registration-based approaches. All data and related software and updated information are available on the http://mindboggle.info/data website. PMID:23227001

Benzylic rearrangement stable isotope labeling for quantitation of guanidino and ureido compounds in thyroid tissues by liquid chromatography-electrospray ionization mass spectrometry

International Nuclear Information System (INIS)

Fan, Ruo-Jing; Guan, Qing; Zhang, Fang; Leng, Jia-Peng; Sun, Tuan-Qi; Guo, Yin-Long

2016-01-01

Benzylic rearrangement stable isotope labeling (BRSIL) was explored to quantify the guanidino and ureido compounds (GCs and UCs). This method employed a common reagent, benzil, to label the guanidino and ureido groups through nucleophilic attacking then benzylic migrating. The use of BRSIL was investigated in the analysis of five GCs (creatine, L-arginine, homoarginine, 4-guanidinobutyric acid, and methylguanidine) and two UCs (urea and citrulline). The labeling was found simple and specific. The introduction of bi-phenyl group and the generation of nitrogen heterocyclic ring in the benzil-d0/d5 labeled GCs and UCs improved the retention behaviors in liquid chromatography (LC) and increased the sensitivity of electrospray ionization mass spectrometry (ESI MS) detection. The fragment ion pairs of m/z 182/187 and m/z 210/215 from the benzil-d0/d5 tags facilitated the discovery of potential GCs and UCs candidates residing in biological matrices. The use of BRSIL combined with LC-ESI MS was applied for simultaneously quantitation of GCs and UCs in thyroid tissues. It was demonstrated that nine GCs and UCs were detected, six of which were further quantified based on corresponding standards. It was concluded that five GCs and UCs (L-arginine, homoarginine, 4-guanidinobutyric acid, methylguanidine, and citrulline) were statistically significantly different (p < 0.05) between the para-carcinoma and carcinoma thyroid tissue samples. - Highlights: • A common reagent, benzil-d0/d5 was employed to label the GCs and UCs through BRSIL. • The benzil-d0/d5 labeling improved the retention behavior in RPLC and increased the sensitivity by ESI MS detection. • BRSIL coupled with LC-ESI MS was applied to the qualitation and quantitation of GCs and UCs in thyroid tissues.

Benzylic rearrangement stable isotope labeling for quantitation of guanidino and ureido compounds in thyroid tissues by liquid chromatography-electrospray ionization mass spectrometry

Energy Technology Data Exchange (ETDEWEB)

Fan, Ruo-Jing [State Key Laboratory of Organmetallic Chemistry and National Center for Organic Mass Spectrometry in Shanghai, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032 (China); Guan, Qing [Department of Head and Neck Surgery, Fudan University Shanghai Cancer Center, Shanghai, 200032 (China); Department of Oncology, Shanghai Medical College, Fudan University, Shanghai, 200032 (China); Zhang, Fang, E-mail: fzhang@sioc.ac.cn [State Key Laboratory of Organmetallic Chemistry and National Center for Organic Mass Spectrometry in Shanghai, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032 (China); Leng, Jia-Peng [State Key Laboratory of Organmetallic Chemistry and National Center for Organic Mass Spectrometry in Shanghai, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032 (China); Sun, Tuan-Qi, E-mail: tuanqisun@163.com [Department of Head and Neck Surgery, Fudan University Shanghai Cancer Center, Shanghai, 200032 (China); Department of Oncology, Shanghai Medical College, Fudan University, Shanghai, 200032 (China); Guo, Yin-Long, E-mail: ylguo@sioc.ac.cn [State Key Laboratory of Organmetallic Chemistry and National Center for Organic Mass Spectrometry in Shanghai, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032 (China)

2016-02-18

Benzylic rearrangement stable isotope labeling (BRSIL) was explored to quantify the guanidino and ureido compounds (GCs and UCs). This method employed a common reagent, benzil, to label the guanidino and ureido groups through nucleophilic attacking then benzylic migrating. The use of BRSIL was investigated in the analysis of five GCs (creatine, L-arginine, homoarginine, 4-guanidinobutyric acid, and methylguanidine) and two UCs (urea and citrulline). The labeling was found simple and specific. The introduction of bi-phenyl group and the generation of nitrogen heterocyclic ring in the benzil-d0/d5 labeled GCs and UCs improved the retention behaviors in liquid chromatography (LC) and increased the sensitivity of electrospray ionization mass spectrometry (ESI MS) detection. The fragment ion pairs of m/z 182/187 and m/z 210/215 from the benzil-d0/d5 tags facilitated the discovery of potential GCs and UCs candidates residing in biological matrices. The use of BRSIL combined with LC-ESI MS was applied for simultaneously quantitation of GCs and UCs in thyroid tissues. It was demonstrated that nine GCs and UCs were detected, six of which were further quantified based on corresponding standards. It was concluded that five GCs and UCs (L-arginine, homoarginine, 4-guanidinobutyric acid, methylguanidine, and citrulline) were statistically significantly different (p < 0.05) between the para-carcinoma and carcinoma thyroid tissue samples. - Highlights: • A common reagent, benzil-d0/d5 was employed to label the GCs and UCs through BRSIL. • The benzil-d0/d5 labeling improved the retention behavior in RPLC and increased the sensitivity by ESI MS detection. • BRSIL coupled with LC-ESI MS was applied to the qualitation and quantitation of GCs and UCs in thyroid tissues.

/sup 99/Tcsup(m)-HMPAO labelled leucocytes: comparison with /sup 111/In-tropolonate labelled granulocytes

Energy Technology Data Exchange (ETDEWEB)

Peters, A.M.; Roddie, M.E.; Zacharopoulos, G.P.; George, P.; Stuttle, A.W.J.; Lavender, J.P.; Danpure, H.J.; Osman, S.

1988-06-01

The lipophilic complex, /sup 99/Tcsup(m)-hexamethylpropyleneamine oxime (HMPAO) is an efficient leucocyte label, and labels granulocytes with more stability than mononuclear leucocytes. The recovery of /sup 99/Tcsup(m)-HMPAO granulocytes was similar to /sup 111/In-labelled granulocytes isolated and labelled in plasma using tropolone. The Tsub(1/2) of /sup 99/Tcsup(m)-HMPAO labelled granulocytes in blood was less than that of /sup 111/In-labelled granulocytes. The initial biodistribution of /sup 99/Tcsup(m)-labelled leucocytes was similar to /sup 111/In-labelled granulocytes, with a rapid initial lung transit, prominent splenic activity, bone marrow activity and minimal hepatic activity, although, unlike /sup 111/In, /sup 99/Tcsup(m) activity was also seen in urine, occasionally in the gallbladder, and, from about 4 h, consistently in the colon. Bone marrow activity was particularly prominent with /sup 99/Tcsup(m). About 6% of /sup 99/Tcsup(m) was excreted in the faeces up to 48 h after injection, and about 17% in urine up to 24 h. The time-activity curves of reticuloendothelial activity up to 24 h were broadly similar for the two labelled cell preparations. Clinical information given by the two agents was similar in 27 of 30 patients who received both. We conclude that with respect to granulocyte kinetics and clinical data, /sup 99/Tcsup(m)-HMPAO labelled leucocytes are comparable with /sup 111/In-tropolonate labelled granulocytes.

A Complex Multiherbal Regimen Based on Ayurveda Medicine for the Management of Hepatic Cirrhosis Complicated by Ascites: Nonrandomized, Uncontrolled, Single Group, Open-Label Observational Clinical Study.

Science.gov (United States)

Patel, Manish V; Patel, Kalapi B; Gupta, Shivenarain; Michalsen, Andreas; Stapelfeldt, Elmar; Kessler, Christian S

2015-01-01

Hepatic cirrhosis is one of the leading causes of death worldwide, especially if complicated by ascites. This chronic condition can be related to the classical disease entity jalodara in Traditional Indian Medicine (Ayurveda). The present paper aims to evaluate the general potential of Ayurvedic therapy for overall clinical outcomes in hepatic cirrhosis complicated by ascites (HCcA). In form of a nonrandomized, uncontrolled, single group, open-label observational clinical study, 56 patients fulfilling standardized diagnostic criteria for HCcA were observed during their treatment at the P. D. Patel Ayurveda Hospital, Nadiad, India. Based on Ayurvedic tradition, a standardized treatment protocol was developed and implemented, consisting of oral administration of single and compound herbal preparations combined with purificatory measures as well as dietary and lifestyle regimens. The outcomes were assessed by measuring liver functions through specific clinical features and laboratory parameters and by evaluating the Child-Pugh prognostic grade score. After 6 weeks of treatment and a follow-up period of 18 weeks, the outcomes showed statistically significant and clinically relevant improvements. Further larger and randomized trials on effectiveness, safety, and quality of the Ayurvedic approach in the treatment of HCcA are warranted to support these preliminary findings.

Radiochemical study on preparation and quality control of 1-125/1-131 labelled some organic compounds for medical uses

International Nuclear Information System (INIS)

El-azoney, K.M.S.E.

1997-01-01

The main objective of this thesis is to investigate the optimum condition for the radioiodination of some organic compounds which find wide applications in nuclear medicine. Iodine-131 (T 1 /2= 8.04 d) which is of great importance in the field, are used for this purpose. long chain fatty acids such as 16-Bromo-hexadecanoic (16-brHDA) and -phenyl -fatty acids such as 15-p-iodophenyl pentadecanoic acid (p-IPPA) will be used as model substrates. 1- Labelling of 16-Br-HDA with Na 131 I. Labelling of 16-BrHDA will be investigated via the non-isotopic exchange between 16-Br HDA and Na 131 I to give 16- 131 IHDA. In order to obtain a high radiochemical yield with high radiochemical purity for the product 16- 131 IHDA, simple and fast methods will be followed. The influence of reagents concentrations, time, temperature, solvents and four quaternary ammonium salts as phase transfer catalysts with only one crown ether will be studied. The determination of reaction velocities and activation energies of catalysed systems was effected and compared with results on the dry state system. 2- Labelling of p-Ipa with Na 131 I. Radioiodination of 15-p-iodophenyl pentadecanoic acid is investigated by the nucleophilic substitution reaction via the isotopic exchange between p-Ipa and Na 131 I. As with 16-BrHDA, factors affecting the labelling yield such as reagent concentrations, solvents, reaction time, temperature and catalyst, is examine. The effect of different temperatures on the radiochemical yield of P- 131 Ipa is studied to determine the activation energy of the exchange reaction. Because of the necessity to separate the iodinated products from the starting materials, high performance liquid chromatographic techniques were applied for this purpose. 3.15 figs., 3.2 tabs., 179 refs

Frustrated Lewis pairs-assisted reduction of carbonyl compounds

Czech Academy of Sciences Publication Activity Database

Marek, Aleš; Pedersen, M. H. F.

2015-01-01

Roč. 71, č. 6 (2015), s. 917-921 ISSN 0040-4020 Institutional support: RVO:61388963 Keywords : frustrated Lewis pairs * hydrogen activation * benzyl alcohol * tritium labeling * labeled compounds Subject RIV: CC - Organic Chemistry Impact factor: 2.645, year: 2015

Chemical compound-based direct reprogramming for future clinical applications

Science.gov (United States)

Takeda, Yukimasa; Harada, Yoshinori; Yoshikawa, Toshikazu; Dai, Ping

2018-01-01

Recent studies have revealed that a combination of chemical compounds enables direct reprogramming from one somatic cell type into another without the use of transgenes by regulating cellular signaling pathways and epigenetic modifications. The generation of induced pluripotent stem (iPS) cells generally requires virus vector-mediated expression of multiple transcription factors, which might disrupt genomic integrity and proper cell functions. The direct reprogramming is a promising alternative to rapidly prepare different cell types by bypassing the pluripotent state. Because the strategy also depends on forced expression of exogenous lineage-specific transcription factors, the direct reprogramming in a chemical compound-based manner is an ideal approach to further reduce the risk for tumorigenesis. So far, a number of reported research efforts have revealed that combinations of chemical compounds and cell-type specific medium transdifferentiate somatic cells into desired cell types including neuronal cells, glial cells, neural stem cells, brown adipocytes, cardiomyocytes, somatic progenitor cells, and pluripotent stem cells. These desired cells rapidly converted from patient-derived autologous fibroblasts can be applied for their own transplantation therapy to avoid immune rejection. However, complete chemical compound-induced conversions remain challenging particularly in adult human-derived fibroblasts compared with mouse embryonic fibroblasts (MEFs). This review summarizes up-to-date progress in each specific cell type and discusses prospects for future clinical application toward cell transplantation therapy. PMID:29739872

Studies on the preparation of labelled compounds for γ-scintigraphy use

International Nuclear Information System (INIS)

Park, Kyung Bae; Kim, Jae Rok; Awh, Ok Doo; Sin, Byung Cheul; Park, Woong Woo; Han, Kwang Hee

1992-03-01

1. Development of 165 Dy-HMA for the treatment of rheumatoid arthritis 1) Irradiation of twelve mg of 164 Dy 2 O 3 showing specific activity of 2x10 13 n/cm 2 sec for four hours gave 165 Dy 2 O 3 showing specific activity(∼480 mCi/mg Dy 2 O 3 ) and radionuclidic purity(>99.9%). 2) 165 Dy-HMA was prepared in yield of 80 - 85% from the 165 DyCl 3 solution which was made by dissolving 165 Dy 2 O 3 with hydrochloric acid and adjusting pH to 3.0, and then followed by the treatment with aqueous sodium hydroxide solution. 3) Serial filtration using polycarbonate filter (1 - 10μm) of 165 Dy-HMA suspension in saline after treatment with sonificator exhibited that the majority of particles are in the 3 - 8μm range. 4) Even though the 165 Dy-HMA suspension in saline was left to stand for 24 hours at room temperature, there was no significant change in particle size resulting in high stability of 165 Dy-HMA. 2. Study on the 99mTc labelling of bioactive material 1) The labelling of antibody [F(ab') 2 ] coupled to DTPA with Na99mTcO 4 in the presence of sodium dithionite(μg) gave labelling yield of 40% determined by ITLC-SG. 2) The labelling of 500μl of antibody solution in phosphate buffer(0.2M, pH 7.4, 1.5mg antibody/ml) with Na 131 I(3 - 5mCi) in the presence of chloramine-T(0.14mg) for 30minutes at room temperature exibited labelling yield of 60 - 70%, radiochemical purity of 97%, specific activity of 1.2 - 3.5 mCi/mg, respectively, determined by ITLC-SG. 3) The results obtained from the animal experiment in rabbit to study the specificity and sensitivity of 131 I labelled antibody exhibited hot uptake until 72 hours in the case of tuberculous infection, with the highest target/background ratio(2.52) at 24 hours after injection of 131 I-F(ab') 2 4) In the case of rabbit infected with syphilitic orchitis, it exhibited the highest target/background ratio(3.51) at 2 hours after injection and showed fast decrease after 24 hours. (Author)

State of the science of blood cell labeling

International Nuclear Information System (INIS)

Srivastava, S.C.; Straub, R.F.

1989-01-01

Blood cell labeling can be considered a science in as far as it is based on precise knowledge and can be readily reproduced. This benchmark criterion is applied to all current cell labeling modalities and their relative merits and deficiencies are discussed. Mechanisms are given where they are known as well as labeling yields, label stability, and cell functionality. The focus is on the methodology and its suitability to the clinical setting rather than on clinical applications per se. Clinical results are cited only as proof of efficacy of the various methods. The emphasis is on technetium as the cell label, although comparisons are made between technetium and indium, and all blood cells are covered. 52 refs., 6 figs., 7 tabs

Tritium labelling of two new analgesic drugs

International Nuclear Information System (INIS)

Santamaria, J.; Rebollo, D.V.; Rivera, P.; Esteban, M.

1986-01-01

The labelling with tritium of two arylpropionic esters was studied. The synthesis between 3 H-Ibuprofen and the two unlabelled alcoholic moieties (Cl-Alkanol and CF 3 -Alkanol) was performed. Assuming that we got ready the acidic moiety, 3 H-Ibuprofen, in our Laboratory, we attempted to label with tritium the alcoholic moiety and then go on to its esterification. Prior to labelling, thermic stability of 2-(4-(3-chlorophenyl)-1-piperazinyl) ethanol (Cl-Alkanol) was studied. As result of this study we had to change the labelling method, so that the Cl-Alkanol was unstable at 70 0 C. Purification was accomplished through thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Concentration, purity and specific activities of the two labelled compounds were determined by ultraviolet, HPLC and liquid scintillation techniques. (author)

Study of the behaviour of P-oxides produced in the combustion of phosphorus-bearing organic compounds and their absorption on suitable substances by means of compounds labelled with 32P. I

International Nuclear Information System (INIS)

Binkowski, J.; Gizinski, S.; Kaminski, R.; Reimschuessel, W.

1976-01-01

During the pyrolytic reaction of phosphorus-bearing compounds in an atmosphere of oxygen, there are produced P-oxides, which interfere in the determination of carbon and hydrogen. The behaviour of these P-oxides was studied intensively in the empty combustion tube in dependence on temperature, velocity of the carrier gas, the nature of the combustion and the positioning of the tube. The P-oxides were determined by the employment of 32 P-labelled aniline phosphate and by activation measurement of the 32 P directly through the tube walls as well as in the finely divided material. In conventional combustions the P-oxides separate abundantly on the walls of the tube provided that the gas velocity is low, especially in those zones of the tube where there is marked temperature lowering, or where very high temperature prevail. Deposited P-oxides are swept out of the tube only in the course of a very long time. Consequently a tube in which the P-bearing compounds have been burned will interfere because of the eluted P-oxides and hence will interfere also if P-free compounds are burned in this same tube

Perfusion magnetic resonance imaging with continuous arterial spin labeling: methods and clinical applications in the central nervous system

Energy Technology Data Exchange (ETDEWEB)

Detre, John A. E-mail: detre@mail.med.upenn.edu; Alsop, David C

1999-05-01

Several methods are now available for measuring cerebral perfusion and related hemodynamic parameters using magnetic resonance imaging (MRI). One class of techniques utilizes electromagnetically labeled arterial blood water as a noninvasive diffusible tracer for blood flow measurements. The electromagnetically labeled tracer has a decay rate of T1, which is sufficiently long to allow perfusion of the tissue and microvasculature to be detected. Alternatively, electromagnetic arterial spin labeling (ASL) may be used to obtain qualitative perfusion contrast for detecting changes in blood flow, similar to the use of susceptibility contrast in blood oxygenation level dependent functional MRI (BOLD fMRI) to detect functional activation in the brain. The ability to obtain blood flow maps using a non-invasive and widely available modality such as MRI should greatly enhance the utility of blood flow measurement as a means of gaining further insight into the broad range of hemodynamically related physiology and pathophysiology. This article describes the biophysical considerations pertaining to the generation of quantitative blood flow maps using a particular form of ASL in which arterial blood water is continuously labeled, termed continuous arterial spin labeling (CASL). Technical advances permit multislice perfusion imaging using CASL with reduced sensitivity to motion and transit time effects. Interpretable cerebral perfusion images can now be reliably obtained in a variety of clinical settings including acute stroke, chronic cerebrovascular disease, degenerative diseases and epilepsy. Over the past several years, the technical and theoretical foundations of CASL perfusion MRI techniques have evolved from feasibility studies into practical usage. Currently existing methodologies are sufficient to make reliable and clinically relevant observations which complement structural assessment using MRI. Future technical improvements should further reduce the acquisition times

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

International Nuclear Information System (INIS)

Sajid, K.M.; Mahmood, R.

2012-01-01

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

synthesis and labelling of some nitrogenous heterocyclic compounds

International Nuclear Information System (INIS)

Mahmoud, A.A.L.

2002-01-01

the imidazole nucleus has wide range of pharmaceutical activities . also , radioiodinated compounds are used in nuclear medicine. this thesis deals with the synthesis of 2-(iodophenyl)-4-oxazoline-5-ons e, which are used as starting materials in the synthesis of the corresponding imidazolinone derivatives. also, it deals with radioiodination f the synthesized compounds to evaluate their application in nuclear medicine. interaction of o- iodo hippuric acid (I) with aromatic aldehydes (i.e., benzaldehyde, p- methoxybenzaldehyde and p- nitrobenzaldehyde) in acetic anhydride and in the presence of fused sodium acetate effected cyclization to afford the corresponding 2-(2-iodophenyl)-4-arylidene- 2-oxazoline-5-ones(l l a-c )

Imaging of Enzymes in the Steroid Biosynthetic Pathway: Synthesis of 18F-Labelled Tracers

International Nuclear Information System (INIS)

Erlandsson, Maria

2009-01-01

This thesis deals with the synthesis and development of 18 F-labelled alkyl etomidate and vorozole analogues, and their use as positron emission tomography (PET) tracers for the imaging of the steroid enzymes 11β-hydroxylase and aromatase. Two synthetic 18 F-labelling approaches to the etomidate and vorozole analogues were developed, and the analogues were evaluated in some biological assays. The two-step labelling method was used to synthesise many compounds for biological evaluation. In the first step, a 18 F-labelled intermediate based on a ditosylate or a halogenated diethyl ether was synthesised and used directly in the next alkylation step. The decay-corrected (d.c.) radiochemical yield was higher compared to other known two-step labelling methods. Once an appropriate candidate has been chosen for clinical evaluation, a one-step labelling method will be more suitable. We therefore developed a method based on precursors that had leaving groups at the end of their alkyl chains, and used these directly in the 18 F-labelling synthesis. The one-step 18 F-labelling synthesis required less reaction time and produced higher specific radioactivity and d.c. radiochemical yield than our two-step synthesis. With microwave heating, the reaction time was reduced to seconds and the d.c. radiochemical yield was better than that obtained with conventional heating. The one-step synthesis simplified the technical handling by allowing the tracer syntheses to be automated on the TRACERLab FX FN

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

International Nuclear Information System (INIS)

Jacobson, Orit; Laky, Desideriu; Carlson, Kathryn E.; Elgavish, Sharona; Gozin, Michael; Even-Sapir, Einat; Leibovitc, Ilan; Gutman, Mordechai; Chisin, Roland; Katzenellenbogen, John A.; Mishani, Eyal

2006-01-01

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/μmol 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

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

International Nuclear Information System (INIS)

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

1992-01-01

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

The fluorodediazonation - a method for n.c.a.-18F-labelling of aromatic substrates

International Nuclear Information System (INIS)

Zwernemann, O.

1991-06-01

For the positron emission tomography (PET) applications, radiopharmaceuticals are required that are labelled with short-lived positron emitters. Fluorine-18 has become the leading radionuclide used for PET, due to its favourable physical properties. However, the labelling of aromatic substances with fluorine-18 with the methods available presents problems not encountered with aliphatic compounds. The decomposition of aromatic diazonium salts opens up feasible ways of preparing a broad range of labelled compounds. The dissertation investigated the possibilities of labelling with fluorine-18 by way of dediazonation on the standard substrate p-Toluidyl diazonium ion. The results reported show that the method of fluorodediazonation is an interesting further method for F-18 labelling of aromatic substrates in addition to the hitherto applied techniques. It allows carrier-free labelling of a large group of substances which cannot be fluorinated via direct nucleophilicity. (BBR) [de

Clinical Evaluation of {sup 57}Co-labelled Bleomycin for Tumor Localization

Energy Technology Data Exchange (ETDEWEB)

Ryu, Yong Wun; Kim, Jang Hee; Lee, Jhin Oh [Korea Cancer Center Hospital, Seoul (Korea, Republic of)

1987-03-15

Investigation with {sup 57}Co-Bleomycin in patients with the various cancers and in tumor bearing animals are described. In the patients, {sup 57}Co-Bleomycin appears to be one of the useful tumor- seeking radiopharmaceuticals, and worth applicable to clinical uses. Labelled yield of {sup 57}Co-Bleo was about 97% by thin layer chromatography. The pyrogen free tests were performed to meet U.S.P. critical ranges. In clinical studies with {sup 57}Co-Bleo, 4 cases out of 5 patients with lung cancer, 2 cases among 3 thyroid cancer patients, and all 3 hepatoma patients showed positive tumor scans. The patients with stomach cancer, and the esophageal cancer showed false negative scintigraphy. A case with pulmonary tuberculosis showed a positive scan while liver abscess showed a negative picture. The merits of {sup 57}Co-Bleomycin scintigraphy seems to be its relatively high affinity to tumors and low radiation hazard in spite of long physical half life.

The tritium labelling of organic molecules by heterogeneous catalytic exchange

International Nuclear Information System (INIS)

Angoso, M.; Kaiser, F.

1977-01-01

The influence of the temperature at 65degC and 120degC on the labelling of three organic molecules with tritium was studied. The compounds were: benzoic acid, diphenyl glioxal and 2,3-tetramethylene-4-phenylthien-7-oxodiacetin. The method employed was the heterogeneous catalytic exchange between tritiaded water and the organic compound. The purification was made by thin-layer chromatography and the concentration, purity and specific activity of the products were determined by counting and ultraviolet techniques. The thermal stability and the radiolitic effects on labelled benzoic acid were also considered. (author) [es

Comparative studies of antibody anti-CD20 labeled with 188Re

International Nuclear Information System (INIS)

Dias, Carla Roberta de Barros Rodrigues

2010-01-01

. The formulation of 99 mTc(I)-RTX red was faster than 188 Re(I)-RTX red , that on the other hand showed better stability in human plasma and no transquelation in the cysteine or histidine challenge studies. Both compounds showed good binding affinity and a biodistribution in mice bearing tumor compatible with the normal mAb distribution and a reasonable tumor uptake proving the efficiency of the labeling and the potential clinical use. (author)

Correlation of 111In-labeled leukocyte scintigraphy with clinical and laboratory findings

International Nuclear Information System (INIS)

Uchida, Yoshitaka; Kitakata, Yuusuke; Uno, Kimiichi; Minoshima, Satoshi; Arimizu, Noboru.

1993-01-01

This study evaluated the relationship between 111 In-labeled leukocyte scintigraphy and clinical information and laboratory findings in 24 patients with bone infection and 35 patients with abdominal infection. Fifty-nine scintigrams were retrospectively reviewed and classified into positive or negative results. As the laboratory findings, C-reactive protein (CRP) level, erythrocyte sedimentation rate (ESR) at 60 minutes, and peripheral blood leukocyte counts (WBCC) were evaluated. Clinical information such as presence of fever and administration of antibiotics was also compared. No significant relationship between the scintigraphic results and clinical as well as laboratory findings was observed in bone infection patients. CRP levels in positive scintigraphic patients were significantly higher than those in negative scintigraphic patients in the abdominal infection group, otherwise the other indices were not correlated with the scintigraphic results. A few patients with slightly increased CRP (mostly chronic cases) did not show positive scintigrams, suggesting an increased false negative rate of leukocyte scintigraphy in such circumstances. These results suggest that it is inappropriate to determine the application of leukocyte scintigraphy depending on clinical as well as laboratory findings, and leukocyte scintigraphy would yield additional information different from other indices when evaluating inflammatory foci. (author)

15N liver function tests - concept, validity, clinical use

International Nuclear Information System (INIS)

Faust, H.; Jung, K.; Krumbiegel, P.; Hirschberg, K.; Reinhardt, R.; Junghans, P.

1987-01-01

Several liver function tests using the oral application of a nitrogen compound labelled with 15 N and the subsequent determination of 15 N in a certain fraction of urine by emission spectrometry are described. Because of the key position of the liver in the metabolism of nitrogen compounds the results of these tests allow conclusions concerning disturbances of special liver functions. Instructions for the clinical use of the '[ 15 N]Ammonium Test', '[ 15 N]Hippurate Test' the '[ 15 N]Methacetin Test', and the '[ 15 N]Glycine Test' are given. (author)

Radioactive labelling of alkaloids with morphine skeleton

International Nuclear Information System (INIS)

Toth, Geza; Sirokman, Ferenc

1985-01-01

Results achieved by the sup(14)C, sup(125)I and sup(3)H labelling of alkaloids with morphine skeleton for kinetic, receptor, metabolims and pharmacological investigations are summarized and evaluated. The methods for the preparation of sup(3)H labelled dihydromorphine, dihydroethylmorphine, dihydrocodeine, naloxone and naloxazone are described. The compounds have higher specific molar activity than those referred to in literature which makes them suitable for a number of investigations. (author)

Absorption, Translocation and Metabolism of {sup 14}C-Labelled Dichlobenil

Energy Technology Data Exchange (ETDEWEB)

Pate, D. A.; Funderburk, Jr., H. H. [Auburn University Agricultural Experiment Station, Auburn, AL (United States)

1966-05-15

Autoradiographs of bean (Phaseolus vulgaris L.) and alligatorweed (Alternanthera philoxeroides (Mart.) Griseb.) indicated that {sup 14}C-nitrile-labelled dichlobenil (2,6-dichlorobenzonitrile) was slightly absorbed by the leaf and some translocation occurred following foliar application. Plants with roots submersed in radioactive aqueous solution absorbed and translocated the {sup 14}C throughout the plant. An investigation of some of the chemical and physical properties of {sup 14}C-nitrile-labelled dichlobenil was conducted. Loss because of volatilization from counting planchets was considerably reduced by application of acrylic plastic immediately after the solution dried. The plastic coating also eliminated contamination of counting chambers and windows. Two higher plants (bean and alligatorweed ) and four fungi (Fusarium sp., Geotrichum sp., Penicillium sp., Trichoderma sp.) were selected for metabolism studies. Dichlobenil- {sup 14}C was added to Hoagland and Arnon's nutrient solution containing beans or alligatorweed and to liquid cultures containing the other organisms for 12 to 120 h. Extracts from the plants or fungi were chromatographed on silica gel thin-layers. Autoradiographs of the thin-layer chromatographed aqueous extracts revealed a {sup C}-labelled compound of Rf 0.25 that differed from that of dichlobenil, which was 0.6. After esterification of the extracts, a {sup 14}C-labelled compound was observed at Rf 0.95 on thin-layer chromatograms. Chromatography of the unaltered extracts with 2,6- dichlorobenzoic acid revealed identical Rf-values. The esterified aqueous extracts chromatographed precisely with methyl-2,6-dichlorobenzoate. Gas chromatography of the {sup 14}C-labelled compound with an Rf of 0.95 exhibited a retention time identical to that of methyl-2,6-dichlorobenzoate. The quantity of {sup 14}C-labelled compound that chromatographed as 2,6-dichlorobenzoate increased with time of exposure of the various test organisms to dichlobenil {sup

Simple, rapid method for the preparation of isotopically labeled formaldehyde

Science.gov (United States)

Hooker, Jacob Matthew [Port Jefferson, NY; Schonberger, Matthias [Mains, DE; Schieferstein, Hanno [Aabergen, DE; Fowler, Joanna S [Bellport, NY

2011-10-04

Isotopically labeled formaldehyde (*C.sup..sctn.H.sub.2O) is prepared from labeled methyl iodide (*C.sup..sctn.H.sub.3I) by reaction with an oxygen nucleophile having a pendant leaving group. The mild and efficient reaction conditions result in good yields of *C.sup..sctn.H.sub.2O with little or no *C isotopic dilution. The simple, efficient production of .sup.11CH.sub.2O is described. The use of the .sup.11CH.sub.2O for the formation of positron emission tomography tracer compounds is described. The reaction can be incorporated into automated equipment available to radiochemistry laboratories. The isotopically labeled formaldehyde can be used in a variety of reactions to provide radiotracer compounds for imaging studies as well as for scintillation counting and autoradiography.

Carbon-14 labelling of biomolecules induced by 14CO ionized gas

International Nuclear Information System (INIS)

Lier, J.E. van; Sanche, L.

1979-01-01

Ionized 14 CO gas provides a rapid method for producing 14 C-labelled biomolecules. The apparatus consists of a high vacuum system in which a small amount of 14 CO is ionized by electron impact. The resulting species drift towards a target where they interact with the molecule of interest to produce 14 C-labelled compounds. Since the reaction time is only 2 minutes, the method is particularly promising for producing tracer biomolecules with short-lived 11 C at high specific activities. The applicability of the method to various classes of compounds of biological importance, including steroids, alkaloids, prostaglandins, nucleosides, amino acids and proteins has been studied. All compounds treated gave rise to 14 C addition and degradation products. Furthermore, for some compounds, chromatographic analysis in multiple systems followed by derivatization and crystallization to constant specific activity, indicated that carbon exchange may occur to produce the labelled, but otherwise unaltered substrate in yields of the order of 10-100 mCi/mol. More conclusive proof of radiochemical identity must await production of larger quantities of material and rigorous purification including at least two different chromatographic techniques. (author)

Self-decomposition components generated from [sup 35]S-labeled amino acids

Energy Technology Data Exchange (ETDEWEB)

Kato, Takahisa; Saito, Kazumi; Kurihara, Norio (Kyoto Univ. (Japan). Radioisotope Research Center)

1994-06-01

We examined the fragment molecules in the gaseous components generated from [sup 35]S-amino acids with high specific radioactivity. The self-decomposition mode of a molecule labeled with a [beta]-emitter was similar to the fragmentation mode of organic compounds impacted by accelerated electrons as in organic mass spectrometry. Degradation products of unlabeled amino acids irradiated by [sup 60]Co [gamma]-ray indicated that the degradation mode induced by external [gamma]-rays irradiation was different from the self-decomposition mode of labeled compounds. (Author).

[Impact of microdose clinical trials in the preclinical stage].

Science.gov (United States)

Kim, Soonih

2014-01-01

A microdose clinical trial may be useful as a safe early-phase exploratory study using doses as low as 100 μg or less for determination of the disposition of a candidate compound in humans in a short period of time. This may increase confidence in candidate compounds, especially those for which it is difficult to predict disposition based on the results of in vitro or preclinical studies. In this study, we examined microdose trials performed in the preclinical stage for two first-in-class compounds with a new mechanism of action. These compounds showed species difference in first pass metabolism in the digestive tract and liver, causing uncertainty in prediction of disposition in humans. For this reason, first-in-human microdose clinical trials were performed. The results showed that the two compounds had effective blood concentrations after oral administration at a dose of 100 mg qd. Administration of an extremely small dose of one (14)C-labeled compound permitted identification of major metabolites. No toxic metabolites were detected. The preclinical toxic dose was determined based on prediction of blood exposure at the estimated maximum clinical dose. For the other candidate compound, the findings of the microdose trial indicated a high bioavailability after oral administration and low hepatic clearance after intravenous administration. These results suggested only a small risk of a change in disposition in patients with hepatic disorder. The data obtained for the two compounds suggest that microdose clinical trials can be useful for improving the process of candidate selection in the preclinical stage.

Development of new methods for the radioactive labelling of compounds useful in biology. Application to the study of digestive tract hormones and their analogues (gastrine, pentagastrine, cholecystokinine, pancreozymine, caeruleine, somatostatine)

International Nuclear Information System (INIS)

Girma, J.-P.

1976-01-01

To establish the kinetics of fixation on receptor sites, tissular distribution and metabolism of hormones, it is necessary to obtain high specific activity labelled hormones possessing biological activities identical with those of the originals. In this context two aims were pursued: hormonal peptide labelling at high specific radioactivity; research on the biological fate of the intermediate compounds involved in the preparations. This research was centred chiefly on gastrine, caeruleine, cholecystokinine and pentagastrine, structural analogues representing one of the two groups of digestive tract hormones (the gastrine family). After a brief review of present knowledge on the gastro-intestinal system; the hormones selected are situated in their biological context. Part two is devoted mainly to the study of iodine and tritium labelling of peptides and includes the adaptation of an existing method to the problem of gastrine labelling and the development of two new tritium-labelling methods, one specific to tryptophanyl residues and the other to tyrosyl residues. Finally the separation of modified hormones during the preparations offered the occasion to develop a study of the biological behavior of these analogues [fr

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.

Fluorine-18 labeled tracers for PET studies in the neurosciences

International Nuclear Information System (INIS)

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

1995-01-01

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

Synthesis of labelled ecdysone precursors

International Nuclear Information System (INIS)

Haag, T.; Hetru, C.; Nakatani, Y.; Luu, B.; Meister, M.; Pichat, L.; Audinot, M.

1985-01-01

High specific activity tritiated 3β,14α-dihydroxy-5β-cholest-7-en-6-one, has been prepared using a precursor which permits rapid and easy labelling. This compound is converted to ecdysone under in vitro conditions by insect prothoracic glands, a well known site of ecdysone biosynthesis. (author)

Isotopic labelling with carbon-14 and tritium

International Nuclear Information System (INIS)

Evans, E.A.

1980-01-01

In this paper general methods of isotopic labelling with 14 C and with 3 H are briefly reviewed with special attention to examples of compounds likely to be of wide interest in biological research. (author)

'Serial review on clinical PET tracers'. Manufacturing and quality control of positron emitting radiopharmaceuticals produced by in-house cyclotron

International Nuclear Information System (INIS)

Saji, Hideo

2009-01-01

In order to establish PET diagnosis as a routine clinical tool, manufacture's compliance with regulations under the Good Manufacturing Practice (GMP) principle for PET radiopharmaceuticals is necessary. For this purpose, the Sub-committee on Medical Application of Positron Emitting Radionuclides, Medical Science and Pharmaceutical Committee of Japan Radioisotopes Association has proposed 'Standards for Compounds Labeled with Emitting Radionuclides Approved as Established Techniques for Medical Use'. This guideline includes the general notices, general rules for preparations, general tests for the quality control, quality of each PET agents, guideline for manufacturing environment and manufacturing process at manufacturing facilities of PET agents. Each facility should have a committee and establish an internal system to account for manufacturing compounds labeled with positron emitting radionuclides produced in the facility, and compile standards by referring to the 'Established Standard Techniques of Labeling Compounds with Emitting Radionuclides for use as Radiopharmaceuticals: approved by the Subcommittee on Medical Application of Cyclotron-Produced Radionuclides (revised in 2009)', in order to maintain the quality of radiopharmaceuticals. (author)

Use of Vitex agnus-castus in migrainous women with premenstrual syndrome: an open-label clinical observation.

Science.gov (United States)

Ambrosini, Anna; Di Lorenzo, Cherubino; Coppola, Gianluca; Pierelli, Francesco

2013-03-01

Premenstrual syndrome (PMS) affects most women during their reproductive life. Headache is regarded as a typical symptom of PMS and, close to menses, migrainous women could experience their worst migraine attacks. Vitex agnus-castus (VAC) is a phytopharmaceutical compound, considered worldwide to be a valid tool to treat PMS. Aim of this study is to explore if headache is ameliorate in migrainous women treated with VAC for PMS by an open-label clinical observation. Migrainous women with PMS were enrolled in the study and advised to assume a treatment with VAC (40 mg/day) for PMS for a 3-month period. Effects both on PMS and headache were assessed. Out of 107 women, 100 completed the 3-month treatment for PMS. Out of them, 66 women reported a dramatic reduction of PMS symptoms, 26 a mild reduction, and 8 no effect. Concerning migraine, 42 % of patients experienced a reduction higher than 50 % in frequency of monthly attacks, and 57 % of patients experienced a reduction higher than 50 % in monthly days with headache. No patients reported remarkable side effects. Pending a placebo-controlled trial to confirm our results, we observed that the use of VAC in migrainous women affected by PMS resulted to be safe and well tolerated, and may positively influence the frequency and duration of migraine attacks.

Clinical evaluation of a 51Cr-labeled red blood cell survival test for in vivo blood compatibility testing

International Nuclear Information System (INIS)

Pineda, A.A.; Dharkar, D.D.; Wahner, H.W.

1984-01-01

Modified red blood cell survival studies with use of 51Cr were performed in three groups of subjects. Group 1 consisted of normal subjects who were given labeled autologous blood, group 2 were subjects in need of blood transfusions and given labeled ABO and Rh crossmatch-compatible blood, and group 3 were patients in need of blood transfusion but in whom problems arose in finding compatible blood. The results of the studies suggest that for patients with blood compatibility problems, normal red blood cell survival values at 1 hour do not exclude the possibility of severe hemolysis 24 hours later. Thus, if a 1-hour test result is normal, the procedure should be extended routinely to 24 hours. Moreover, the test can be used to evaluate the clinical importance of antibodies. We showed that anti-Yka and anti-Lan were clinically significant, but high-titer, low-avidity antibodies, anti-Kna, anti-I, and anti-HI were clinically insignificant in the cases studied. This finding emphasizes the importance of an in vivo test for the final compatibility evaluation in complicated blood replacement problems

Synthesis of isotopically labelled angiotensin II receptor antagonist GR138950X

International Nuclear Information System (INIS)

Carr, R.M.; Cable, K.M.; Newman, J.J.; Sutherland, D.R.

1996-01-01

Syntheses of [ 13 C] and [ 14 C]-labelled versions of angiotensin II receptor antagonist GR138950X, labelled in the imidazole carboxamide residue, are described. These involved preparation of an iodoimidazole substrate by a novel iododecarboxylation procedure, followed by cyanation with a mixture of carbon-labelled potassium cyanide and copper (l) iodide in DMF at high temperature. The preparation of a mass-labelled (M+5) version of GR138950X is also described. This involved the synthesis of an [ 13 C 3 , 15 N 2 ]-labelled imidazole from a 1,2,3-tricarbonyl compound, [ 13 C 3 ]propionaldehyde and [ 15 N]ammonia. The labelled imidazole was further elaborated into multiply-labelled GR138950X. (Author)

The tritium labelling of organic molecules by heterogeneous catalytic exchange

International Nuclear Information System (INIS)

Angoso Marina, M.; Kaiser Ruiz del Olmo, F.

1977-01-01

The influence of the temperature at 65 degree centigree and 120 degree centigree on the labelling of three organic molecules with tritium was studied. The compounds were: benzoic acid, de phenyl glyoxal and 2,3-tetramethylene-4-pantothenyl-7-oxo diacetin.The method employed was the heterogeneous catalytic exchange between tritiated water and the organic compound. The purification was made by thin-layer chromatography and the concentration, purity and specific activity of the products were determined by counting and ultraviolet techniques. The thermal stability and the radiolytic effects on labelled benzoic acid were also considered. (Author) 9 refs

Syntheses with isotopically labelled carbon. Methyl iodide, formaldehyde and cyanide

International Nuclear Information System (INIS)

Finn, R.D.; Boothe, T.E.; Vora, M.M.; Hildner, J.C.; Emran, A.M.; Kothari, P.J.

1984-01-01

Many of the uniquely labelled synthetic precursors currently employed in the design of sophisticated radiolabelled compounds have their origins in the field of hot atom chemistry. Particularly, the development during the past few years of automated, on-line synthetic procedures which combine the nuclear reaction, hot atom and classical chemistry, and rapid purification methods has allowed the incorporation of useful radionuclides into suitable compounds of chemical and biochemical interest. The application of isotopically labelled methyl iodide, formaldehyde, and cyanide anion as synthetic intermediates in research involving human physiology and nuclear medicine, as well as their contributions to other scientific methodology, is reviewed. (author)

Analysis of fluorescently labeled glycosphingolipid-derived oligosaccharides following ceramide glycanase digestion and anthranilic acid labeling.

Science.gov (United States)

Neville, David C A; Coquard, Virginie; Priestman, David A; te Vruchte, Danielle J M; Sillence, Daniel J; Dwek, Raymond A; Platt, Frances M; Butters, Terry D

2004-08-15

Interest in cellular glycosphingolipid (GSL) function has necessitated the development of a rapid and sensitive method to both analyze and characterize the full complement of structures present in various cells and tissues. An optimized method to characterize oligosaccharides released from glycosphingolipids following ceramide glycanase digestion has been developed. The procedure uses the fluorescent compound anthranilic acid (2-aminobenzoic acid; 2-AA) to label oligosaccharides prior to analysis using normal-phase high-performance liquid chromatography. The labeling procedure is rapid, selective, and easy to perform and is based on the published method of Anumula and Dhume [Glycobiology 8 (1998) 685], originally used to analyze N-linked oligosaccharides. It is less time consuming than a previously published 2-aminobenzamide labeling method [Anal. Biochem. 298 (2001) 207] for analyzing GSL-derived oligosaccharides, as the fluorescent labeling is performed on the enzyme reaction mixture. The purification of 2-AA-labeled products has been improved to ensure recovery of oligosaccharides containing one to four monosaccharide units, which was not previously possible using the Anumula and Dhume post-derivatization purification procedure. This new approach may also be used to analyze both N- and O-linked oligosaccharides.

Investigations on the production of labelled organic compounds by recoil labelling with gamma,n-produced 11-C-atoms

International Nuclear Information System (INIS)

Wagenbach, U.

1981-01-01

''Hot'' 11 C atoms are produced from 12 C(γ,n) 11 C nuclear reactions by bremsstrahlung at the 65 MeV electron linear accelerator in Giessen. The relative retention in various C-atoms of the amino acid, methionine, is determined by splitting of the terminal C-atoms of the molecule and by independent determination of the content of 11 C in the isolated and derived fragments. The terminal groups (thiomethyl or carboxyl groups) each carry approx. 25% of the total retained radioactivity, the remaining 50% being spread over the three inner carbon atoms. The activation of alkylamines, crystallised as hydrochlorides, hydrofluorides, oxalates and sulphates, leads to similar yields of direct labelling from 5 to 15%. Amines activated in the liquid state show a retention of less than 5%. The yields for labelled synthetic products are between 10 and 15% for amino acids and are often higher for crystallised amines. Amines activated in the liquid state produced greater yields of synthesis products but at the same time an increase in the product range. The labelled synthesis products can be separated faster by suitable methods such as preparative HPLC and are then available for carrier-free studies in the life sciences. (orig./EF) [de

Imaging with 123I labelled fatty acids

International Nuclear Information System (INIS)

Dudczak, R.

1985-01-01

This report describes the clinical results obtained with radioiodinated aromatic and aliphatic fatty acids. The radiopharmaceuticals were 123 I labelled p-phenylpentadecanoic (p-IPPA) and 123 I labelled heptadecanoic acid (HDA). The possibility to evaluate the myocardial metabolic function in man noninvasively add a complementary diagnostic tool in the clinical follow-up of patients with heart disease. (Auth.)

The preparation of 32P labelled phosphorous acid

International Nuclear Information System (INIS)

Henderson, D.; Jenkinson, A.; Sorby, P.

1986-11-01

Phosphorous acid labelled with 32 P has been prepared, on a small scale, starting from neutron-irradiated phosphorus. The compound is intended for tracer studies in the development of novel fungicides

Clinical applications of indium-111-acetylacetone-labelled blood cells

International Nuclear Information System (INIS)

Georgi, P.; Sinn, H.; Wellman, H.; Clorius, J.H.; Becker, W.

1981-01-01

A method permitting red-cell labelling with 111 In-acetylacetone was reported in 1974 for evaluating intestinal blood loss, the liver-spleen ratio and the red-cell volume. White blood cells can be tagged similarly. In white-cell labelling, simultaneous red-cell or platelet tagging is avoided. Several procedures (dextran separation and gradient centrifugations) have been combined, to develop a highly selective cell separation. In osteomyelitis it may not be as advantageous to use 67 Ga-citrate, as in inflammatory soft tissue processes. The detection of inflammatory processes with labelled leukocytes could be of great importance for the scintigraphic diagnosis of osteomyelitidies. A group of 97 patients with suspected osteomyelitis have been examined using 111 In-acetylacetone-labelled leukocytes ( 111 In-AAL) immediately following positive routine skeletal scintigraphy. Images obtained 24 h post injection usually were the most satisfactory. In the followup group of 70 patients 21 true positives, 43 true negatives, 21 false negatives and 3 false positives were observed. These findings result in a specificity of 92%, sensitivity of 50% and accuracy of 70% with 111 In-AAL for osteomyelitis. Preliminary investigations using 111 In-acetylacetone-labelled thrombocytes ( 111 In-AAT) were carried out to detect rejection of transplanted kidneys. The platelets were separated by means of additional special density gradient centrifugations but no dextran from 15-20 ml of autologous whole blood. Scans have been obtained 15 min, 2.5 h and 24 h post injection in an initial group of 10 patients. In acute rejection, a high transplant uptake has been detected, whereas patients without acute rejection showed no or only a minimum activity accumulation. Patients with chronic rejection have intermediate uptakes

[MR implant labelling and its use in clinical MRI practice].

Science.gov (United States)

Mühlenweg, M; Schaefers, G

2015-08-01

Before a magnetic resonance imaging (MRI) examination, implants in patients must be cleared for MR safety in order to exclude the risk of possible severe injuries and implant malfunction in an MR environment. The general contraindication for measurements of patients with implants still applies; however, in the recent past a way has been found to legally circumvent this contraindication. For this purpose special conditions are required: explicit implant identification and the original manufacturer's labelling are necessary, the required conditions for conditionally MR safe implants must be assured and a risk-benefit analysis with appropriate explanation to the patient has to be performed. This process can be very complex as the implants are often poorly documented and detailed information on the implant MR labelling is also often outdated or not easy to interpret. This article provides information about legal and normative principles of MR measurement of patients with implants. The possible physical interactions with implants will be briefly dealt with as well as possible strategies for better identification and investigation of implants and MR labelling. General approaches for minimizing the risk will be discussed using some examples. The second part deals with the content of MR implant labelling and the current test standards. Furthermore, the additional information from the operating instructions of the MR scanner that are necessary for the interpretation of the MR implant labelling, will be explained. The article concludes with an explanation of the current pattern for MR labelling of implants from the U.S. Food and Drug Administration (FDA) and an exemplary application.

MR implant labelling and its use in clinical MRI practice

International Nuclear Information System (INIS)

Muehlenweg, M.; Schaefers, G.

2015-01-01

Before a magnetic resonance imaging (MRI) examination, implants in patients must be cleared for MR safety in order to exclude the risk of possible severe injuries and implant malfunction in an MR environment. The general contraindication for measurements of patients with implants still applies; however, in the recent past a way has been found to legally circumvent this contraindication. For this purpose special conditions are required: explicit implant identification and the original manufacturer's labelling are necessary, the required conditions for conditionally MR safe implants must be assured and a risk-benefit analysis with appropriate explanation to the patient has to be performed. This process can be very complex as the implants are often poorly documented and detailed information on the implant MR labelling is also often outdated or not easy to interpret. This article provides information about legal and normative principles of MR measurement of patients with implants. The possible physical interactions with implants will be briefly dealt with as well as possible strategies for better identification and investigation of implants and MR labelling. General approaches for minimizing the risk will be discussed using some examples. The second part deals with the content of MR implant labelling and the current test standards. Furthermore, the additional information from the operating instructions of the MR scanner that are necessary for the interpretation of the MR implant labelling, will be explained. The article concludes with an explanation of the current pattern for MR labelling of implants from the U.S. Food and Drug Administration (FDA) and an exemplary application. (orig.) [de

Nomenclature and spelling rules of chemistry in Hungary Pt. 1 Nomenclature of elements and inorganic compounds

International Nuclear Information System (INIS)

Fodorne Csanyi, P.

1982-01-01

The part of the updated edition of 'Nomenclature and spelling rules of chemistry in Hungary' (Budapest, 1972), referring to the isotopically modified inorganic compounds is presented. The rules are based on the proposals of IUPAC (1981). Spelling rules concerning the isotopically substituted, isotopically labelled, specifically labelled, selectively and non-selectively labelled compounds, and the positional and numbering rules of nuclides are treated. (Sz.J.)

Profiling of volatile organic compounds produced by clinical Aspergillus isolates using gas chromatography-mass spectrometry

NARCIS (Netherlands)

Gerritsen, M G; Brinkman, P; Escobar Salazar, Natalia; Bos, L D; de Heer, K; Meijer, M; Janssen, H-G; de Cock, H; Wösten, H A B; Visser, C.E.; van Oers, M H J; Sterk, P J

Volatile organic compounds (VOCs) in exhaled breath may identify the presence of invasive pulmonary aspergillosis. We aimed to detect VOC profiles emitted by in vitro cultured, clinical Aspergillus isolates using gas chromatography-mass spectrometry (GC-MS). Three clinical Aspergillus isolates and a

Profiling of volatile organic compounds produced by clinical Aspergillus isolates using gas chromatography-mass spectrometry

NARCIS (Netherlands)

Gerritsen, M. G.; Brinkman, P.; Escobar, N.; Bos, L. D.; de Heer, K.; Meijer, M.; Janssen, H.-G.; de Cock, H.; Wösten, H. A. B.; Visser, C. E.; van Oers, M. H. J.; Sterk, P. J.

2018-01-01

Volatile organic compounds (VOCs) in exhaled breath may identify the presence of invasive pulmonary aspergillosis. We aimed to detect VOC profiles emitted by in vitro cultured, clinical Aspergillus isolates using gas chromatography-mass spectrometry (GC-MS). Three clinical Aspergillus isolates and a

Hydrogen sulfide deactivates common nitrobenzofurazan-based fluorescent thiol labeling reagents.

Science.gov (United States)

Montoya, Leticia A; Pluth, Michael D

2014-06-17

Sulfhydryl-containing compounds, including thiols and hydrogen sulfide (H2S), play important but differential roles in biological structure and function. One major challenge in separating the biological roles of thiols and H2S is developing tools to effectively separate the reactivity of these sulfhydryl-containing compounds. To address this challenge, we report the differential responses of common electrophilic fluorescent thiol labeling reagents, including nitrobenzofurazan-based scaffolds, maleimides, alkylating agents, and electrophilic aldehydes, toward cysteine and H2S. Although H2S reacted with all of the investigated scaffolds, the photophysical response to each scaffold was significantly different. Maleimide-based, alkylating, and aldehydic thiol labeling reagents provided a diminished fluorescence response when treated with H2S. By contrast, nitrobenzofurazan-based labeling reagents were deactivated by H2S addition. Furthermore, the addition of H2S to thiol-activated nitrobenzofurazan-based reagents reduced the fluorescence signal, thus establishing the incompatibility of nitrobenzofurazan-based thiol labeling reagents in the presence of H2S. Taken together, these studies highlight the differential reactivity of thiols and H2S toward common thiol-labeling reagents and suggest that sufficient care must be taken when labeling or measuring thiols in cellular environments that produce H2S due to the potential for both false-positive and eroded responses.

Quantitative chromatography in the analysis of labelled compounds 1. Quantitative paper chromotography of amino acids by A spot comparison technique

International Nuclear Information System (INIS)

Barakat, M.F.; Farag, A.N.; El-Gharbawy, A.A.

1974-01-01

For the determination of the specific activity of labelled compounds separated by paper sheet chromatography, it was found essential to perfect the quantitative aspect of the paper chromatographic technique. Actually, so far paper chromatography has been used as a separation tool mainly and its use in quantification of the separated materials is by far less studied. In the present work, the quantitative analysis of amino acids by paper sheet chromatography has been carried out by methods, depending on the use of the relative spot area values for correcting the experimental data obtained. The results obtained were good and reproducible. The main advantage of the proposed technique is its extreme simplicity. No complicated equipment of procedures are necessary

Minicyclotron-based technology for the production of positron-emitting labelled radiopharmaceuticals

International Nuclear Information System (INIS)

Barrio, J.R.; Bida, G.; Satyamurthy, N.; Padgett, H.C.; MacDonald, N.S.; Phelps, M.E.

1983-01-01

The use of short-lived positron emitters such as carbon 11, fluorine 18, nitrogen 13, and oxygen 15, together with positron-emission tomography (PET) for probing the dynamics of physiological and biochemical processes in the normal and diseased states in man is presently an active area of research. One of the pivotal elements for the continued growth and success of PET is the routine delivery of the desired positron emitting labelled compounds. To date, the cyclotron remains the accelerator of choice for production of medically useful radionuclides. The development of the technology to bring the use of cyclotrons to a clinical setting is discussed

Minicyclotron-based technology for the production of positron-emitting labelled radiopharmaceuticals

Energy Technology Data Exchange (ETDEWEB)

Barrio, J.R.; Bida, G.; Satyamurthy, N.; Padgett, H.C.; MacDonald, N.S.; Phelps, M.E.

1983-01-01

The use of short-lived positron emitters such as carbon 11, fluorine 18, nitrogen 13, and oxygen 15, together with positron-emission tomography (PET) for probing the dynamics of physiological and biochemical processes in the normal and diseased states in man is presently an active area of research. One of the pivotal elements for the continued growth and success of PET is the routine delivery of the desired positron emitting labelled compounds. To date, the cyclotron remains the accelerator of choice for production of medically useful radionuclides. The development of the technology to bring the use of cyclotrons to a clinical setting is discussed. (ACR)

Labelling aflatoxine-B1 by radioactive iodine

International Nuclear Information System (INIS)

Kim, Y.S.; Park, K.B.; Sung, H.K.; Ryu, Y.W.

1977-01-01

Labelling aflatoxines, the potential carcinogenic compounds, by radioactive iodine has been studied. The auflatoxine-B 1 , which is known to be the most abundant components of auflatoxines in the nature, was labelled by radioactive iodine-125 through an acid catalyst chloroamine-T procedure. The radiochemical yield was amounted to 63.6%. The chemical structure of the labelled product was proved to be 6-iodo 5-methoxy coumarine structure of auflatoxine-B 1 molecule by means of I.R. and N.M.R. spectroscopy. The labelled product was orally administered in a test animal (rat) and examined the accumulation of radioactivity in the body at the definite time interval. The accumulation of the radioactivity was pronounced at the blood and the liver. There was no indication of the decomposition of auflatoxine-B 1 - 125 I in the organs of the test animal. (author)

Some chemical synthesis of 14C labelled compounds of pharmaceutical or biological interest

International Nuclear Information System (INIS)

Pichat, I.; Baret, C.; Audinot, M.; Herbert, M.; Lambin, J.

1955-01-01

The recent discovery of the tuberculostatic properties of the hydrazide of isonicotinic acid (so-called 'Isoniazide', 'Rimifon') has raised considerably its interest, as for metabolic studies which it is more interesting to have it labelled with 14 C. We describe in this report the chemical synthesis of 14 C carboxyl labelled isoniazide which were done in the pyridine ring to highlight his metabolic function on the Koch's bacillus. (M.B.)

Study of the transport of mercurial compounds by seric proteins

International Nuclear Information System (INIS)

Jullien-Saint Guily, Nicole

1970-01-01

A bond between the seric proteins and various mercurial compounds labeled with the radioisotopes 203 Hg and 197 Hg was demonstrated by means of research methods specific to radioactivity combined with protein separation techniques. In the course of this study it was shown how strongly the composition of the buffer during electrophoretic migration influences the transport of certain organo-mercurial compounds by the seric proteins. By means of a thioloprive: N - ethyl - maleimide, labeled with 14 C, it was proved that the bonding sites between the proteins and the mercurial compounds were the thiol groups of the proteins but that other bonding sites, in particular the amino groups, could also be involved. (author) [fr

44Sc for labeling of DOTA- and NODAGA-functionalized peptides: preclinical in vitro and in vivo investigations.

Science.gov (United States)

Domnanich, Katharina A; Müller, Cristina; Farkas, Renata; Schmid, Raffaella M; Ponsard, Bernard; Schibli, Roger; Türler, Andreas; van der Meulen, Nicholas P

2017-01-01

Sc, the data presented in this work indicate the possibility of using NODAGA in combination with 44 Sc. In view of a clinical study, thorough investigations will be necessary regarding the labeling conditions and storage solutions in order to guarantee sufficient stability of 44 Sc-labeled NODAGA compounds.

Labelling of TTHA coupled IgG and MCAb with rare earth radionuclides

International Nuclear Information System (INIS)

Wu Younghui; Zhang Yulei; Wu Chuanchu; Wang Xiangyun; Liu Yuanfang

1988-07-01

This article expands a process of labelling G-immunoglobulin (IgG) and monoclonal antibody (MCAb) with rare earth radionuclides. In this labelling process, cycloanhydride (CTTHAA) of Tri-ethyl Tetra-amine Hexa-acetic Acid (TTHA) is employed as a bifunctional chelating conjugate, the metal chelation takes place after CTTHAA has first been linked to IgG, followed by chemical reaction with rare earth radionuclides. Detailed investigations have been carried out to examine the influencing parameters of labelling globulins with rare earth, such as metal to CTTHAA mole-ratio, pH value and labelling time. The immunoreactivity of the labelled compound (RE-TTHA-IgG) has been retained throughout the whole labelling process

The clinical meaningfulness of ADAS-Cog changes in Alzheimer's disease patients treated with donepezil in an open-label trial.

Science.gov (United States)

Rockwood, Kenneth; Fay, Sherri; Gorman, Mary; Carver, Daniel; Graham, Janice E

2007-08-30

In 6-month anti-dementia drug trials, a 4-point change in the Alzheimer's Disease Assessment Scale-Cognitive Subscale (ADAS-Cog) is held to be clinically important. We examined how this change compared with measures of clinical meaningfulness. This is a secondary analysis of a 12 month open-label study of 100 patients (71 women) diagnosed with mild to moderate AD treated with 5-10 mg of donepezil daily. We studied the observed case, 6-month change from baseline on the ADAS-Cog, the Clinician's Interview Based Impression of Change-Plus Caregiver Input (CIBIC-Plus), patient-Goal Attainment Scaling (PGAS) and clinician-GAS (CGAS). At 6 months, donepezil-treated patients (n = 95) were more likely to show no change (+/- 3 points) on the ADAS-Cog (56%) than to improve (20%) or decline (24%) by 4-points. ADAS-Cog change scores were little correlated with other measures: from -0.09 for PGAS to 0.27 for the CIBIC-Plus. While patients who improved on the ADAS-Cog were less likely to decline on the clinical measures (26%), 43% of patients who declined on the ADAS-Cog improved on at least two of the clinical measures. The ADAS-Cog did not capture all clinically important effects. In general, ADAS-Cog improvement indicates clinical improvement, whereas many people with ADAS-Cog decline do not show clinical decline. The open-label design of this study does not allow us to know whether this is a treatment effect, which requires further investigation.

/sup 99m/Tc-labeled solid-phase meal: a quantitative clinical measurement of human gastric emptying

Energy Technology Data Exchange (ETDEWEB)

Martin, J.L.; Beck, W.J.; McDonald, A.P.; Carlson, G.M.; Mathias, J.R.

1983-08-01

A solid-phase meal labeled with /sup 99m/Tc-sulfur colloid provides an improved clinical test for the quantitative evaluation of human gastric emptying. We studied 12 healthy male controls and five male patients with known gastric stasis secondary to a vagotomy and drainage procedure. All subjects were fasted for 8 hours before the study, and each consumed an unbuttered biscuit and a poached egg white containing 1 mCi of /sup 99m/Tc-sulfur colloid. For 2 hours, 60-second counts were measured every 10 minutes by a Pho Gamma III scintillation camera. The t/sup 1///sup 2/ for control subjects was 60 minutes, at which time patients with gastric stasis had retained 98% of the test meal. At 120 minutes, control subjects and patients with gastric stasis had 4.7% and 89%, respectively, of the meal remaining in the stomach. The solid-phase test meal labeled with /sup 99m/Tc-sulfur colloid is easy to perform and can be used clinically to quantitatively measure gastric emptying in humans. This test can discriminate between control subjects and patients with known gastric stasis.

/sup 99m/Tc-labeled solid-phase meal: a quantitative clinical measurement of human gastric emptying

International Nuclear Information System (INIS)

Martin, J.L.; Beck, W.J.; McDonald, A.P.; Carlson, G.M.; Mathias, J.R.

1983-01-01

A solid-phase meal labeled with /sup 99m/Tc-sulfur colloid provides an improved clinical test for the quantitative evaluation of human gastric emptying. We studied 12 healthy male controls and five male patients with known gastric stasis secondary to a vagotomy and drainage procedure. All subjects were fasted for 8 hours before the study, and each consumed an unbuttered biscuit and a poached egg white containing 1 mCi of /sup 99m/Tc-sulfur colloid. For 2 hours, 60-second counts were measured every 10 minutes by a Pho Gamma III scintillation camera. The t 1 / 2 for control subjects was 60 minutes, at which time patients with gastric stasis had retained 98% of the test meal. At 120 minutes, control subjects and patients with gastric stasis had 4.7% and 89%, respectively, of the meal remaining in the stomach. The solid-phase test meal labeled with /sup 99m/Tc-sulfur colloid is easy to perform and can be used clinically to quantitatively measure gastric emptying in humans. This test can discriminate between control subjects and patients with known gastric stasis

Geodesic atlas-based labeling of anatomical trees

DEFF Research Database (Denmark)

Feragen, Aasa; Petersen, Jens; Owen, Megan

2015-01-01

We present a fast and robust atlas-based algorithm for labeling airway trees, using geodesic distances in a geometric tree-space. Possible branch label configurations for an unlabeled airway tree are evaluated using distances to a training set of labeled airway trees. In tree-space, airway tree t...... equally complete airway trees, and comparable in performance to that of experts in pulmonary medicine, emphasizing the suitability of the labeling algorithm for clinical use....

Photolytic inhibition and labeling of proteins with aryl diazonium compounds

International Nuclear Information System (INIS)

Tometsko, A.M.; Turula, J.; Comstock, J.

1978-01-01

In the course of preparing aryl azide derivatives for use as photoprobes, we have observed significant light sensitivity in the precursor aryl diazonium compounds. The photosensitive properties of this class of compounds are of interest since they will seek out cationic binding sites in biological targets, and can be employed to inhibit complementary targets at acid pH. The relationship between photolytic change in the structure of diazonium compounds and the corresponding change in function of a biological target are presented. Experiments are described in which the dark and light sensitive properties of a model diazonium compound, diazobenzene sulfonate (DBS), were determined. The ultraviolet spectra were used to evaluate the dark stability and light sensitivity og DBS. Chymotrypsin and trypsin served as functioning targets for further evaluation of the photochemical properties. Both enzymes are stable to the probe in the dark at acid pH. A rapid loss of enzyme activity was observed following flash photolysis of DBS-enzyme solutions. Photolytic incorporation of radioactive DBS into chymotrypsin was observed. Aryl diazonium salts can be employed to probe the availability of complementary sites in biological targets at different acid pH values. (Author)

Scintigraphy with In-111 labeled leukocytes

International Nuclear Information System (INIS)

Itoh, Kazuo; Tsukamoto, Eriko; Furudate, Masayori; Saito, Chihoko.

1987-01-01

With increasing necessity for In-111 labeled leukocyte scintigraphy (ILLS) as a routine examination, a problem of complicated labeling of leukocytes has arisen. In this study, simplified labeling of leukocytes was examined with respect to its ability to detect abscesses. Simplified labeling method yielded significantly satisfactory results for recovery and labeling rates of leukocytes, as compared with conventional recommended method. Therefore, ILLS by simplified technique was clinically applied in 58 patients with suppurative or non-suppurative diseases who gave informed consent. In an analysis of ILLS for detecting suppurative region, the sensitivity, specificity, and corrected specificity were found to be 81 %, 75 %, and 82 %, respectively. (Namekawa, K.)

Synthesis of molecules of biological interest labelled with high specific activity tritium

International Nuclear Information System (INIS)

Petillot, Yves

1975-01-01

Labelled molecules are artificial organic compounds possessing one or several radioactive or steady isotopic atoms. Using tritium to label molecules presents several benefits: a raw material easy to obtain with a high purity and at reasonable cost; synthesised labelled molecules displaying high specific activities very interesting in molecular biology; high resolution of radiographies; relatively simple and quick introduction of tritium atoms in complex molecules. Thus, this report for graduation in organic chemistry addresses the synthesis and study of new labelled molecules which belong to families of organic compounds which have fundamental activities in biology: uridine 3 H-5,6 and thymidine 3 H-methyl which are nucleotides which intervene under the form of phosphates in the synthesis of nucleic acids, oestradiol 3 H-2,4,6,7 which is a powerful estrogenic hormone which naturally secreted by the ovary; and noradrenaline 3 H-1,1' and dopamine 3 H-1,2 which are usually secreted by adrenal medulla and have multiple actions on the nervous system

Study on Chinese herbal medicine active ingredients labelled with tritium

International Nuclear Information System (INIS)

Dong Mo; Bao Guangliang

2008-01-01

Chinese medicinal herb active ingredients was labeled with triteium by using exchange of new synthesized tritiated water or exchange of low-pressure gas-liquid. The active ingredients was Genipin, acetylalkannin and chlorogenic acid .The radiochemical purity of the three labeled compounds were more than 95% after TLC and HPLC purification. The specific activities of tritium labeled-genipin, acetylalkannin and chlorogenic acid were 5.97, 3.24 and 470 GBq/g, respectively. The results indicated that the unstable Chinese medicinal herb active ingredients could be labeled with tritium by the methods of exchange of new synthesized tritiated water and exchange of low-pressure gas-liquid. (authors)

Preparation of sup(113m)In-labelled compounds of radiopharmaceutical interest. Part of a coordinated programme on radiopharmaceuticals

International Nuclear Information System (INIS)

Servian, J.; Robles, A.

1975-06-01

Techniques for the preparation and control of already known and new sup(113m)In-radiopharmaceuticals were investigated. New rapid procedures for the control and preparation of a number of radiopharmaceuticals were developed and standardized. After biological distribution studies and clinical tests, new techniques for the preparation of the following indium-113 radiopharmaceuticals were adopted: a) Indium - labelled colloids of: S, Al(OH) 3 , Fe(OH) 3 and AlPO 4 for liver and spleen scintigraphy. b) Indium labelled chelates using the ligands EDTA, DTPA, TTHA (Triethylene-tetramine-hexaacetic acid) and DHPTA (Diamino-hydroxy-propane-tetraacetic acid) for brain scintigraphy. c) Indium labelled Fe(OH) 3 macroaggregates and microspheres for lung scintigraphy. d) Several complexes of sup(113m)In with different ligands (fluoride, tartrate, pyrophosphate, tripolyphosphate, trimetaphosphate, EHDP (or ethane-1-hydroxy-1, 1-diphosphonate), ethylendiamine-pyrophosphate were synthesized and its potential use as bone-scanning agents were evaluated. It was found that the complexes with tartrate, tripolyphosphate and EHDP show appreciable skeletal uptake (bone/muscle ratio are 9.0, 5.5, and 4.7 respectively), although they are inferior to the sup(99m)Tc bone-scanning agents. e) A new simple technique is proposed for the preparation of highly concentrated sup(113m)In solutions. The technique is based on the precipitation of In(OH) 3 , millipore filtration and redissolution in a small volume of 0.05 N HCl

Synthesis of a Fluorescently Labeled 68Ga-DOTA-TOC Analog for Somatostatin Receptor Targeting.

Science.gov (United States)

Ghosh, Sukhen C; Hernandez Vargas, Servando; Rodriguez, Melissa; Kossatz, Susanne; Voss, Julie; Carmon, Kendra S; Reiner, Thomas; Schonbrunn, Agnes; Azhdarinia, Ali

2017-07-13

Fluorescently labeled imaging agents can identify surgical margins in real-time to help achieve complete resections and minimize the likelihood of local recurrence. However, photon attenuation limits fluorescence-based imaging to superficial lesions or lesions that are a few millimeters beneath the tissue surface. Contrast agents that are dual-labeled with a radionuclide and fluorescent dye can overcome this limitation and combine quantitative, whole-body nuclear imaging with intraoperative fluorescence imaging. Using a multimodality chelation (MMC) scaffold, IRDye 800CW was conjugated to the clinically used somatostatin analog, 68 Ga-DOTA-TOC, to produce the dual-labeled analog, 68 Ga-MMC(IRDye 800CW)-TOC, with high yield and specific activity. In vitro pharmacological assays demonstrated retention of receptor-targeting properties for the dual-labeled compound with robust internalization that was somatostatin receptor (SSTR) 2-mediated. Biodistribution studies in mice identified the kidneys as the primary excretion route for 68 Ga-MMC(IRDye 800CW)-TOC, along with clearance via the reticuloendothelial system. Higher uptake was observed in most tissues compared to 68 Ga-DOTA-TOC but decreased as a function of time. The combination of excellent specificity for SSTR2-expressing cells and suitable biodistribution indicate potential application of 68 Ga-MMC(IRDye 800CW)-TOC for intraoperative detection of SSTR2-expressing tumors.

Fate of 14C-labelled compounds in marine environment

International Nuclear Information System (INIS)

Kale, S.P.; Raghu, K.; Sherkhane, P.D.; Murthy, N.B.K.

1999-01-01

Model ecosystems have played an important role in predicting environmental behavior of agrochemicals. The microcosms used in these studies generally include soil units containing usual biotic components common for that ecosystem. In present studies, scope of two such ecosystems has been extended to study the fate of 14 C-labelled pesticides in marine environment. 14 C-labelled pesticides used in these studies were chlorpyrifos, DDT and HCH. Two systems were developed in laboratory simulating marine environment to study the fate of these pesticides. The first system was developed in an all glass aquarium tank with marine sediments, seawater, clams and algae and is referred to as marine ecosystem. The second system was developed to permit the total 14 C-mass balance studies. It contained marine sediments under moist (60% water holding capacity) or flooded conditions and it is referred to as continuous flow system. Fate of 14 C-DDT was studied in marine ecosystem while degradation of 14 C-chlorpyrifos and 14 C-HCH was studied in continuous flow system. 14 C-DDT did not bioaccumulate in clams while at the end of 60 days 50% of the applied 14 C-activity was present in sediment fraction of marine ecosystem. 14 C-HCH degradation showed about 22-26% mineralization while 45-55% of the applied activity was recovered as organic volatiles. No significant bound residues were formed. 14 C-chorpyrifos underwent considerable degradation in marine environment. TCP was the major degradation product. (author)

Stability of compounded trilostane suspension in cod liver oil.

Science.gov (United States)

Crosby, Jesse; Brown, Stacy

2017-10-01

Trilostane is a synthetic steroid analog used to treat canine hyperadrenocorticism. For small dogs, the dose found in commercially available dosage forms of trilostane is sometimes too high. Compounding trilostane in a liquid diluent provides an option for more precise dosing and adjustments, and can be easier to administer, versus a tablet or capsule. Trilostane suspends well in cod liver oil, which is generally palatable to dogs. The stability of a compounded trilostane suspension in cod liver oil stored at room temperature was investigated for 90 days. Compounded trilostane retained stability, defined as maintaining 90-105% labeled value, for 60 days when stored in amber glass bottles. However, drug potency fell >10% below the labeled value when stored in amber plastic bottles after 7 days. Copyright © 2017 Elsevier Ltd. All rights reserved.

New bisphosphonate labeled with Iodine-131 for the palliative therapy for bone metastases pain

International Nuclear Information System (INIS)

Prats Capote, Anaís; Perera Pintado, Alejandro; León, Mariela; Hernández González, Ignacio; Leyva Montaña, René; Mocelo Castell, Raúl; O'Reilly, Beatriz; Calderón, Osmar; Griffith Pérez, Yoel; García Batle, Marisé; Rodríguez Tanty, Chryslaine

2016-01-01

The aim of this work was to obtain new bisphosphonate marked with 131I suitable for palliative treatment of bone metastases pain characteristics. Materials and Methods: It started with aromatic amino acids and the synthesis consisted of three stages: 1) Protection of amino groups by acetylation; 2) phosphonation protected amino acids with a mixture of phosphorous acid and phosphorus pentachloride; 3) Lack of protection of the amino groups by basic hydrolysis. The compounds obtained were characterized by IR, 1H NMR, RMN13-C mass. Los spectrometry bisphosphonic acids obtained were labeled with 131I using chloramine T and iodogen as oxidants. Stability of labeled compounds in aqueous solution was studied serum. 3 mg of 2-amino-3- (4-hydroxyphenyl) -1-hydroxypropyl-1,1-bisphosphonic acid labeled of 131I were administered to male wistar rats (170-190 g) through a lateral tail vein. The scintigraphic study was conducted at 2, 6 and 12 hours. Results: The yield of the reactions of the amino group protection four compounds ranged from 75 to 80%, while the phosphonation was between 50 and 60%. The radiochemical purity of 2-amino-3- (4-hydroxyphenyl) -1-hydroxypropyl-1,1- bisphosphonic acid labeled with 131I was (91.5 ± 1.4)% and its stability was satisfactory for 72h. Scintigraphic images suggest excretion by the kidneys of the compound and from 12 h post-administration begin to visualize bone structures of the animal, suggesting that the compound exhibits affinity for these tissues. Conclusions: A novel synthesis method with modifications that yielded the sodium salts of bisphosphonic acids starting from the respective aromatic amino acids was developed. 2-amino-3- (4-hydroxyphenyl) -1-hydroxypropyl-1,1-bisphosphonic acid 131I labeled was stable up to 72h and showed affinity for bone tissue. (author)

Subcellular SIMS imaging of isotopically labeled amino acids in cryogenically prepared cells

International Nuclear Information System (INIS)

Chandra, Subhash

2004-01-01

Ion microscopy is a potentially powerful technique for localization of isotopically labeled molecules. In this study, L-arginine and phenylalanine amino acids labeled with stable isotopes 13 C and 15 N were localized in cultured cells with the ion microscope at 500 nm spatial resolution. Cells were exposed to the labeled amino acids and cryogenically prepared. SIMS analyses were made in fractured freeze-dried cells. A dynamic distribution was observed from labeled arginine-treated LLC-PK 1 kidney cells at mass 28 ( 13 C 15 N) in negative secondaries, revealing cell-to-cell heterogeneity and preferential accumulation of the amino acid (or its metabolite) in the nucleus and nucleolus of some cells. The smaller nucleolus inside the nucleus was clearly resolved in SIMS images and confirmed by correlative light microscopy. The distribution of labeled phenylalanine contrasted with arginine as it was rather homogeneously distributed in T98G human glioblastoma cells. Images of 39 K, 23 Na and 40 Ca were also recorded to confirm the reliability of sample preparation and authenticity of the observed amino acid distributions. These observations indicate that SIMS techniques can provide a valuable technology for subcellular localization of nitrogen-containing molecules in proteomics since nitrogen does not have a radionuclide tracer isotope. Amino acids labeled with stable isotopes can be used as tracers for studying their transport and metabolism in distinct subcellular compartments with SIMS. Further studies of phenylalanine uptake in human glioblastoma cells may have special significance in boron neutron capture therapy (BNCT) as a boron analogue of phenylalanine, boronophenylalanine is a clinically approved compound for the treatment of brain tumors

Subcellular SIMS imaging of isotopically labeled amino acids in cryogenically prepared cells

Energy Technology Data Exchange (ETDEWEB)

Chandra, Subhash

2004-06-15

Ion microscopy is a potentially powerful technique for localization of isotopically labeled molecules. In this study, L-arginine and phenylalanine amino acids labeled with stable isotopes {sup 13}C and {sup 15}N were localized in cultured cells with the ion microscope at 500 nm spatial resolution. Cells were exposed to the labeled amino acids and cryogenically prepared. SIMS analyses were made in fractured freeze-dried cells. A dynamic distribution was observed from labeled arginine-treated LLC-PK{sub 1} kidney cells at mass 28 ({sup 13}C{sup 15}N) in negative secondaries, revealing cell-to-cell heterogeneity and preferential accumulation of the amino acid (or its metabolite) in the nucleus and nucleolus of some cells. The smaller nucleolus inside the nucleus was clearly resolved in SIMS images and confirmed by correlative light microscopy. The distribution of labeled phenylalanine contrasted with arginine as it was rather homogeneously distributed in T98G human glioblastoma cells. Images of {sup 39}K, {sup 23}Na and {sup 40}Ca were also recorded to confirm the reliability of sample preparation and authenticity of the observed amino acid distributions. These observations indicate that SIMS techniques can provide a valuable technology for subcellular localization of nitrogen-containing molecules in proteomics since nitrogen does not have a radionuclide tracer isotope. Amino acids labeled with stable isotopes can be used as tracers for studying their transport and metabolism in distinct subcellular compartments with SIMS. Further studies of phenylalanine uptake in human glioblastoma cells may have special significance in boron neutron capture therapy (BNCT) as a boron analogue of phenylalanine, boronophenylalanine is a clinically approved compound for the treatment of brain tumors.

Synthesis of {sup 13}C- and {sup 14}C-labeled 1192U90, an ortho-amino benzamide with a preclinical atypical antipsychotic profile

Energy Technology Data Exchange (ETDEWEB)

Norman, M.H.; Gabriel, S.D. [Glaxo Wellcome Inc., Research Triangle Park, NC (United States)

1996-03-01

Three isotopic forms of potential antipsychotic agent 1192U90 (2-amino-N-(4-(4-(1,2-benzisthiazol-3-yl)-piperazinyl)butyl)benzam ide) were synthesized: one containing {sup 13}C-isotopes and two containing {sup 14}C-isotopes. The compound in which the ortho-amino benzamide ring is completely {sup 13}C-labeled was prepared in a four-step sequence starting from [{sup 13}C{sub 6}]aniline. The {sup 14}C-labeled compounds were prepared by methods analogous to those previously described for the unlabeled material. The key step involved the condensation of 3-(4-(4aminobutyl)-1-piperazinyl)-1,2-benzisothiazole with isatoic anhydride. The first {sup 14}C-labeled compound (3) was prepared from {sup 14}C-labeled 3-(4-(4-aminobutyl)-1-piperazinyl)-1,2-benzisothiazole, while the second compound (4) derived its isotopic label from [{sup 14}C]isatoic anhydride. Compound 3 had a specific activity of 26.55 mCi/mmol, a radiochemical purity of 99.3%, and a radiochemical yield of 3.4%. Compound 4 had a specific activity of 22.67 mCi/mmol and a radiochemical purity of 99.2%. (author).

Ferrocene, ruthenocene or rhodocene analogues of Haloperidol. Synthesis and organ distribution after labelling with 103Ru or 103mRh

International Nuclear Information System (INIS)

Wenzel, M.; Wu, Y.

1988-01-01

Ferrocene-Haloperidol was synthesized by N-alkylation of 4-(4'-chlorophenyl)-4-hydroxypiperidine with 1-ferrocenyl-4-chlor-butan-1-on. By heating the ferrocene-haloperidol with 103 RuCl 3 the 103 Ru-labelled ruthenocene-haloperidol was obtained. This compound showed a high affinity for lung but not for brain in rats and mice. The decay of the 103 Ru labelled compound results in the formation of the 103m Rh labelled rhodocene-haloperidol, which is rapidly oxidized by air to the corresponding rhodocinium-haloperidol. This compound can be separated by extraction and TLC. (author)

Astatine-211 labelled proteins and their stability in vivo

International Nuclear Information System (INIS)

Yi Changhou; Jin Jannan; Zhang Shuyuan; Wang Ketai; Zhang Dayuan; Zhou Maolun

1989-01-01

211 At or 131 I labelled proteins, e.g. 211 At-IgG or 211 At-BSA (bovine serum albumin) were prepared by 211 At reaction with the diazo-compound of para-aminobenzoic acid, which is then conjugated with IgG or BSA via an acylation reaction. The 211 At-carbon bond was found metabolically stable under in vivo conditions. For the labelling of proteins with 211 At or 131 I, other methods of direct oxidation are also described. The results show that for the labelling of proteins with 211 At, high rate of incorporation can be obtained with hydrogen peroxide as oxidant, but the labelling of proteins with 131 I is more favourable with the strong oxidant Chloramine-T. (author) 12 refs.; 6 figs

A system for oxygen-15 labeled blood for medical applications

International Nuclear Information System (INIS)

Subramanyam, R.; Bucelewicz, W.M.; Hoop, B. Jr.; Jones, S.C.

1977-01-01

Oxygen-15 labeled compounds in blood have been used successfully for cerebral circulation and cerebral oxygen metabolism measurements. The present paper describes a system for the rapid sequential production of 15 O-HgB, C 15 O-Hgb and H 2 15 O in blood under sterile and pyrogen-free conditions. A tonometer has been adopted for labeling blood without hemolysis and foam production. (author)

Tetrazine-Containing Amino Acid for Peptide Modification and Live Cell Labeling.

Directory of Open Access Journals (Sweden)

Zhongqiu Ni

Full Text Available A novel amino acid derivative 3-(4-(1, 2, 4, 5-tetrazine-3-yl phenyl-2-aminopropanoic acid was synthesized in this study. The compound possessed better water-solubility and was synthesized more easily compared with the well-known and commercially available 3-(p-benzylamino-1, 2, 4, 5-tetrazine. Tetrazine-containing amino acid showed excellent stability in biological media and might be used for cancer cell labeling. Moreover, the compound remained relatively stable in 50% TFA/DCM with little decomposition after prolonged exposure at room temperature. The compound could be utilized as phenylalanine or tyrosine analogue in peptide modification, and the tetrazine-containing peptide demonstrated more significant biological activity than that of the parent peptide. The combination of tetrazine group and amino acid offered broad development prospects of the bioorthogonal labeling and peptide synthesis.

Applying label-free dynamic mass redistribution assay for studying endogenous FPR1 receptor signalling in human neutrophils

DEFF Research Database (Denmark)

Christensen, Hanna B; Gloriam, David E; Pedersen, Daniel Sejer

2017-01-01

INTRODUCTION: The label-free dynamic mass redistribution-based assay (DMR) is a powerful method for studying signalling pathways of G protein-coupled receptors (GPCRs). Herein we present the label-free DMR assay as a robust readout for pharmacological characterization of formyl peptide receptors...... (FPRs) in human neutrophils. METHODS: Neutrophils were isolated from fresh human blood and their responses to FPR1 and FPR2 agonists, i.e. compound 43, fMLF and WKYMVm were measured in a label-free DMR assay using Epic Benchtop System from Corning®. Obtained DMR traces were used to calculate agonist...... potencies. RESULTS: The potencies (pEC50) of fMLF, WKYMVm and compound 43, determined on human neutrophils using the label-free DMR assay were 8.63, 7.76 and 5.92, respectively. The DMR response to fMLF, but not WKYMVm and compound 43 could be blocked by the FPR1-specific antagonist cyclosporin H...

Accelerated stem cell labeling with ferucarbotran and protamine

Energy Technology Data Exchange (ETDEWEB)

Golovko, Daniel M.; Henning, Tobias; Bauer, Jan S. [Department of Radiology and Biomedical Imaging, University of California San Francisco, San Francisco, CA (United States); Settles, Marcus; Rummeny, Ernst J. [Technical University Munich, Department of Radiology, Munich (Germany); Frenzel, Thomas [Bayer Schering Pharma AG, Berlin (Germany); Mayerhofer, Artur [Ludwig-Maximilians-Universitaet, Institute of Cell Biology, Munich (Germany); Daldrup-Link, Heike E. [Department of Radiology and Biomedical Imaging, University of California San Francisco, San Francisco, CA (United States); UCSF Medical Center, Contrast Agent Research Group, Department of Radiology, San Francisco, CA (United States)

2010-03-15

To develop and characterize a clinically applicable, fast and efficient method for stem cell labeling with ferucarbotran and protamine for depiction with clinical MRI. The hydrodynamic diameter, zeta potential and relaxivities of ferucarbotran and varying concentrations of protamine were measured. Once the optimized ratio was found, human mesenchymal stem cells (MSCs) were labeled at varying incubation times (1-24 h). Viability was assessed via Trypan blue exclusion testing. 150,000 labeled cells in Ficoll solution were imaged with T1-, T2- and T2*-weighted sequences at 3 T, and relaxation rates were calculated. Varying the concentrations of protamine allows for easy modification of the physicochemical properties. Simple incubation with ferucarbotran alone resulted in efficient labeling after 24 h of incubation while assisted labeling with protamine resulted in similar results after only 1 h. Cell viability remained unaffected. R2 and R2* relaxation rates were drastically increased. Electron microscopy confirmed intracellular iron oxide uptake in lysosomes. Relaxation times correlated with results from ICP-AES. Our results show internalization of ferucarbotran can be accelerated in MSCs with protamine, an approved heparin antagonist and potentially clinically applicable uptake-enhancing agent. (orig.)

Clinical advance in radionuclide imaging of pulmonary cancer

International Nuclear Information System (INIS)

Deng Zhiyong; Yang Lichun

2008-01-01

Radionuclide imaging of pulmonary cancer develops very rapidly in recent years. Its important value on the diagnosis, staging, monitoring recur and metastasis after treatment, and judging the curative effect and prognosis has been demonstrated. Clinicians pay more attention to it than before. This present article introduces the imaging principle, clinical use, good and bad points, progress situation of 67 Ga, 201 Tl, 99 Tc m , 18 F and their labelled compounds, which are more commonly used in clinical. And introduces the clinical progress of radionuclide imaging of pulmonary neoplasm concerning 99 Tc m -sestamibi ( 99 Tc m -MIBI), 99 Tc m -HL91 and 18 F-fluorodeoxyglucose ( 18 F-FDG) with emphasis. (authors)

Preoperative clinical radioimmunodetection of pancreatic cancer by 111In-labeled chimeric monoclonal antibody Nd2

International Nuclear Information System (INIS)

Sawada, Tetsuji; Nishihara, Tamahiro; Yamamoto, Atsushi

1999-01-01

The present study was carried out with the purpose of evaluating the clinical usefulness of radioimmunodetection (RAID) with 111 In-labeled murine/human chimeric monoclonal antibody, Nd2 (c-Nd2) in patients with pancreatic cancer. Nineteen patients suspected to have pancreatic cancer were administered intravenously 74 MBq/2 mg 111 In-labeled c-Nd2 in 100 ml of saline containing 2% albumin over 30 min. A scintigram was obtained on the 3rd day after infusion by using single photon emission computed tomography (SPECT) imaging. Of the 14 patients finally diagnosed as having pancreatic cancer on the basis of surgical specimens or progress of disease, specific focal uptake at the site of the tumor was detected in 12 (true positive cases), representing a sensitivity of 85.7% (12/14), and liver metastasis was found in one case with metastasis. Of the 5 patients diagnosed with tumor-forming pancreatitis (TFP), 4 patients demonstrated true negative imaging, but one patient whose tumor demonstrated interesting findings in histology and immunostaining, showed false positive imaging. Of patients investigated for human anti-chimeric antibody (HACA) response, none showed HACA response, and no allergic reaction was seen in any of the patients administered c-Nd2. These results suggest that RAID with 111 In-labeled c-Nd2 is useful for differential preoperative diagnosis between invasive pancreatic cancer and TFP. (author)

Clinical significance of abdominal scintigraphy using {sup 99m}Tc-HMPAO-labelled leucocytes in patients with seronegative spondyloarthropathies

Energy Technology Data Exchange (ETDEWEB)

Alonso Farto, J.C.; Almoguera Arias, I.; Ortega Valle, A.; Perez Vazquez, J.M. [Department of Nuclear Medicine, Univ. Complutense, Madrid (Spain); Lopez Longo, F.J.; Gonzalez Fernandez, C.M.; Monteagudo Saez, I.; Bascones, M.; Carreno Perez, L. [Department of Rheumatology, ' ' Hospital Universitario Gregorio Maranon' ' , Universidad Complutense, Madrid (Spain)

2000-12-01

Abdominal scintigraphy shows silent gut inflammation in patients with spondyloarthropathies (Sp) without clinical evidence of gut inflammation. Abdominal scintigraphy images are different than those obtained in patients with ulcerative colitis or Crohn's disease and are not related to the anti-inflammatory drugs administered. The aim of this study was to examine the clinical associations of findings on abdominal scintigraphy in patients with Sp. A total of 204 Sp patients (European Spondylarthropathy Study Group 1991 criteria) and 54 non-Sp controls receiving non-steroidal anti-inflammatory drugs were studied. Abdominal scintigraphy images were obtained at 30 and 120 min after injection of technetium-99m hexamethylpropylene amine oxime ({sup 99m}Tc-HMPAO)-labelled leucocytes. {sup 99m}Tc-HMPAO-labelled leucocyte scans were positive in 104 Sp patients (50.9%) and in six non-Sp controls (2.9%) (P<0.001; OR=8.32; 95% CI=3.23-22.67). Silent gut inflammation was not associated with any of the following: age of onset, duration of evolution, sex, family history of Sp or psoriasis, articular manifestations, extra-articular manifestations, radiological findings or HLA-B27 positivity. Positive abdominal scintigraphy was associated with active disease (P<0.0001; OR=52.7; 95% CI=19-145.6) and an increase in the C-reactive protein (P<0.005; OR=3.4; 95% CI=1.5-7.4). It is concluded that (a) abdominal scintigraphy using {sup 99m}Tc-HMPAO-labelled leucocytes is of value in detecting the silent gut inflammation in Sp patients, and (b) silent gut inflammation is related to the clinical activity, but is not associated with any particular type of illness or with HLA-B27. (orig.)

40 CFR 59.103 - Container labeling requirements.

Science.gov (United States)

2010-07-01

... 40 Protection of Environment 5 2010-07-01 2010-07-01 false Container labeling requirements. 59.103... National Volatile Organic Compound Emission Standards for Automobile Refinish Coatings § 59.103 Container... automobile refinish coating or coating component container or package, the day, month, and year on which the...

40 CFR 59.405 - Container labeling requirements.

Science.gov (United States)

2010-07-01

... 40 Protection of Environment 5 2010-07-01 2010-07-01 false Container labeling requirements. 59.405... National Volatile Organic Compound Emission Standards for Architectural Coatings § 59.405 Container... section on the coating container in which the coating is sold or distributed. (1) The date the coating was...

Inter-labeler and intra-labeler variability of condition severity classification models using active and passive learning methods.

Science.gov (United States)

Nissim, Nir; Shahar, Yuval; Elovici, Yuval; Hripcsak, George; Moskovitch, Robert

2017-09-01

Labeling instances by domain experts for classification is often time consuming and expensive. To reduce such labeling efforts, we had proposed the application of active learning (AL) methods, introduced our CAESAR-ALE framework for classifying the severity of clinical conditions, and shown its significant reduction of labeling efforts. The use of any of three AL methods (one well known [SVM-Margin], and two that we introduced [Exploitation and Combination_XA]) significantly reduced (by 48% to 64%) condition labeling efforts, compared to standard passive (random instance-selection) SVM learning. Furthermore, our new AL methods achieved maximal accuracy using 12% fewer labeled cases than the SVM-Margin AL method. However, because labelers have varying levels of expertise, a major issue associated with learning methods, and AL methods in particular, is how to best to use the labeling provided by a committee of labelers. First, we wanted to know, based on the labelers' learning curves, whether using AL methods (versus standard passive learning methods) has an effect on the Intra-labeler variability (within the learning curve of each labeler) and inter-labeler variability (among the learning curves of different labelers). Then, we wanted to examine the effect of learning (either passively or actively) from the labels created by the majority consensus of a group of labelers. We used our CAESAR-ALE framework for classifying the severity of clinical conditions, the three AL methods and the passive learning method, as mentioned above, to induce the classifications models. We used a dataset of 516 clinical conditions and their severity labeling, represented by features aggregated from the medical records of 1.9 million patients treated at Columbia University Medical Center. We analyzed the variance of the classification performance within (intra-labeler), and especially among (inter-labeler) the classification models that were induced by using the labels provided by seven

Labelling by deuteration and nitroxide radicals of mono-, oligo- and polysaccharides (cellulose and amylose)

Energy Technology Data Exchange (ETDEWEB)

Odier, L

1975-01-01

The application of NMR and deuteration labelling to the investigation of polysaccharides has led to considerable progress in recent years in the knowledge of these compounds. Although far more recent, the introduction of spin labelling techniques in the investigation of polymers, has given rise to interesting EPR studies of synthetic and natural macromolecules, but nothing appears to have been accomplished in the area of spin labelling of polysaccharides. This work was aimed at applying these two techniques to the study of glucose derivatives and of some of its oligomers (low molecular weight polymers): cellobiose, maltose and cyclodextrins; and its polymers: cellulose and amylose. Irrespective of the technique employed, the complexity of the polymers and problems connected with handling them always require the same procedure: an initial study of a model compound generally prepared from the monomer or an oligomer (dimer), followed by the oligomers, and finally the polymer. Part 1 is devoted to the deuteration labelling of mono- and oligosaccharides. Part 2 concerns spin labelling of cellulose acetate. In part 3, an attempt is made to apply the spin labelling technique to the determination of conformations of two disaccharides of different glycosidic configurations: cellobiose and maltose. Part 4 is devoted to spin and deuteration labelling of ..cap alpha.. and ..beta.. cyclodextrins.

Fate of 15N and 14C from labelled plant material

DEFF Research Database (Denmark)

Rasmussen, Jim; Gjettermann, Birgitte; Eriksen, Jørgen

2008-01-01

strength of labelled plant residues in dissolved inorganic N (DIN) and dissolved organic N (DON) in pore water from the plough layer, and (ii) the plant uptake of organically bound N. Litterbags containing 14C- and 15N-labelled ryegrass or clover roots or leaves were inserted into the sward of a ryegrass......–clover mixture in early spring. The fate of the released 14C and 15N was monitored in harvested biomass, roots, soil, and pore water percolating from the plough layer. No evidence of plant uptake of dual-labelled organic compounds from the dual-labelled residues could be observed. N in pore water from the plough...

Labeling pharmaceuticals with radioactive isotopes. Technical progress report, December 1, 1975--November 30, 1976

International Nuclear Information System (INIS)

Blau, M.; Bender, M.A.

1976-01-01

The purpose of this research is to prepare iodo- and bromo-aliphatic amino acid analogs labeled with γ-emitting isotopes ( 131 I, 123 I and 77 Br) for possible use as pancreas localizing agents. Studies on the halogen exchange reaction (I- for Cl-) for the synthesis of β-iodo-α-aminobutyric acid (a valine analog) have suggested that the iodo compound was formed initially. However, the desired compound cannot be isolated because of its chemical instability. Distribution studies in rats with the crude halogen exchange reaction mixture confirmed this finding. Studies on the addition of hydrogen iodine to allylglycine under various conditions for the synthesis of γ-iodo-α-aminopentanoic acid (a leucine analog) suffered the same obstacle; the chemical instability of the desired iodo compound precludes isolation and characterization. Convinced that the iodo analogs were too unstable for use as practical localizing agents, we turned to the possible use of Br for CH 3 substituted amino acids. The 14 C labeled β-bromo-α-aminobutyric acid methyl ester was synthesized. This methyl ester will be hydrolyzed and the distribution of free amino acid will be studied. Labeled with 77 Br this compound might be useful for pancreas localization

Synthesis of 14C- and 3H-labelled 4-(4-nitrophenyl)aminophenylisothiocyanate (Go 9333/CGP 4540; amoscanate)

International Nuclear Information System (INIS)

Anjaneyulu, B.; Maller, R.K.; Nagarajan, K.

1985-01-01

Amoscanate, a broad spectrum anthelmintic, labelled with carbon-14 on the isothiocyanate carbon atom was prepared in an overall yield of 13% at a specific activity of 4.13 μCi/mg from potassium [ 14 C]thiocyanate. The 4-nitro[U- 14 C]phenyl ring labelled compound was synthesized in 20.4% overall yield from [U- 14 C]aniline at a specific activity of 12.2 μCi/mg. The corresponding tritiated compound was prepared from 4-amino[2- 3 H]acetanilide at 112 μCi/mg. Labelling with tritium in the aromatic ring bearing the isothiocyanate group was achieved by catalysed halogen-tritium replacement. However, for pharmacokinetic and metabolism studies in experimental animals, the 14 C- and 3 H-labels associated with the phenylisothiocyanate moiety subsequently proved disadvantageous because of the instability of the labels in vivo. (author)

Inter-Labeler and Intra-Labeler Variability of Condition Severity Classification Models Using Active and Passive Learning Methods

Science.gov (United States)

Nissim, Nir; Shahar, Yuval; Boland, Mary Regina; Tatonetti, Nicholas P; Elovici, Yuval; Hripcsak, George; Moskovitch, Robert

2018-01-01

Background and Objectives Labeling instances by domain experts for classification is often time consuming and expensive. To reduce such labeling efforts, we had proposed the application of active learning (AL) methods, introduced our CAESAR-ALE framework for classifying the severity of clinical conditions, and shown its significant reduction of labeling efforts. The use of any of three AL methods (one well known [SVM-Margin], and two that we introduced [Exploitation and Combination_XA]) significantly reduced (by 48% to 64%) condition labeling efforts, compared to standard passive (random instance-selection) SVM learning. Furthermore, our new AL methods achieved maximal accuracy using 12% fewer labeled cases than the SVM-Margin AL method. However, because labelers have varying levels of expertise, a major issue associated with learning methods, and AL methods in particular, is how to best to use the labeling provided by a committee of labelers. First, we wanted to know, based on the labelers’ learning curves, whether using AL methods (versus standard passive learning methods) has an effect on the Intra-labeler variability (within the learning curve of each labeler) and inter-labeler variability (among the learning curves of different labelers). Then, we wanted to examine the effect of learning (either passively or actively) from the labels created by the majority consensus of a group of labelers. Methods We used our CAESAR-ALE framework for classifying the severity of clinical conditions, the three AL methods and the passive learning method, as mentioned above, to induce the classifications models. We used a dataset of 516 clinical conditions and their severity labeling, represented by features aggregated from the medical records of 1.9 million patients treated at Columbia University Medical Center. We analyzed the variance of the classification performance within (intra-labeler), and especially among (inter-labeler) the classification models that were induced by

131I labeling of tamoxifen and biodistribution studies in rats

International Nuclear Information System (INIS)

Biber Muftuler, F.Z.; Unak, P.; Teksoz, S.; Acar, C.; Yolcular, S.; Yuerekli, Y.

2008-01-01

Tamoxifen [TAM ([Z]-2-[4-(1,2-diphenyl-1-di-butenyl)-phenoxy]-N,N-dimethylethanamine)] has been used as an antiestrogen drug for treatment and prevention of human breast cancer. Tamoxifen was labeled with 131 I using iodogen as an oxidizing agent. Mass spectroscopy of the cold standard showed that the labeling occurs in ortho position to the phenyl ether position of TAM as expected. Quality control, radiochemical yield and stability were established using the radioelectrophoresis method. The radiolabeled compound maintained its stability throughout working period of 24 h. Scintigraphic imaging was performed and tissue distribution was determined in Albino Wistar rats. According to biodistribution and imaging experiments the radiolabeled compound presented estrogen receptor (ER) specificity and it was uptaken by endometrium as well as breast tissue

Synthesis of labelled compound of ferulic acid and caffeic acid with tritium

International Nuclear Information System (INIS)

Yi Mingguang; Wang Caiyun

1986-01-01

Effective components of Chinese traditional herbs consist of many compounds, but some of the compounds usually contain unsaturated carbon-carbon double bonds. The unsaturated organic compounds 3 H-Ferulic acid and 3 H-Caffeic acid are prepared with their tritiated intermediates made by electric-dischange exposure method, which ensures the compounds contaning double bonds not hydrogenated. The 3 H-Ferulic acid is composed of 3 H-vanillin and Malonic acid. The 3 H-Caffeic acid is composed of 3 H-protocatechuyl aldehyde and Malonic acid and the specific activity of the products is 0.2 mCi/mg. The radiochemicaly purity is greater than 90%

Some chemical synthesis of {sup 14}C labelled compounds of pharmaceutical or biological interest

Energy Technology Data Exchange (ETDEWEB)

Pichat, I; Baret, C; Audinot, M; Herbert, M; Lambin, J [Commissariat a l' Energie Atomique, Lab. du Fort de Chatillon, Fontenay-aux-Roses (France). Centre d' Etudes Nucleaires

1955-07-01

The recent discovery of the tuberculostatic properties of the hydrazide of isonicotinic acid (so-called 'Isoniazide', 'Rimifon') has raised considerably its interest, as for metabolic studies which it is more interesting to have it labelled with {sup 14}C. We describe in this report the chemical synthesis of {sup 14}C carboxyl labelled isoniazide which were done in the pyridine ring to highlight his metabolic function on the Koch's bacillus. (M.B.)

[13N]ammonia in organic solvents; a potent synthetic precursor for 13N-labeling

International Nuclear Information System (INIS)

Tominaga, Toshiyoshi; Hirobe, Masaaki

1987-01-01

13 NH 3 in an organic solvent was prepared and its utility as a labeling precursor was studied. [ 13 N]adenine ([ 13 N]ADN), [ 13 N]nicotinamide ([ 13 N]NAM), [ 13 N]p-nitrophenyl carbamate ([ 13 N]NPC), and [ 13 N]L-glutamine ([ 13 N]Gln) were labeled utilizing this precursor. [ 13 N]ADN and [ 13 N]NAM were labeled in much better yields than from an aqueous solution of 13 NH 3 . [ 13 N]NPC and [ 13 N]Gln, which could not be labeled in an aqueous solution, were labeled in high radiochemical yields. Thus, the advantages of this precursor are the improvement of the labeling yield and the feasibility of labeling compounds unstable in aqueous conditions. (author)

Method for determining the composition of the sugar moiety of a sugar containing compound

DEFF Research Database (Denmark)

2016-01-01

The present invention relates to methods of labeling sugar moieties of sugar containing compounds including glycopeptides. The compounds presented in the present invention facilitate reliable detection of sugar moieties of sugar containing compounds by a combination of spectroscopy methods...

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.

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

International Nuclear Information System (INIS)

Serianni, A.S.

1994-01-01

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

Labeling Lanreotide with 125I and 188Re

International Nuclear Information System (INIS)

Bai Hongsheng

2000-01-01

Lanreotide is a new somatostatin analogue. It can bind to human somatostatin receptor (hSSTR) subtype 2 through 5 with high affinity and to hSSTR subtype I with low affinity. We investigate labeling condition, quality control and stability in vitro of 125 I-Lanreotide and 188 Re-lanreotide respectively. (A) Lanreotide is labeled with 125 I using Chloramine T. The effect of reaction condition (such as reaction time, pH value, Lanreotide amount, quantity of Chloramine T and reaction volume) on labeling yield is investigated in detail. (B) The labeling yield and radiochemical purity (RP) is measured with paper chromatography (PC) and Sep-Pak C 18 Cartridge. (C) The stability of 125 I-Lanreotide in vitro is investigated by labeling compound incubating for 48 hours at 37 deg C in the 0.9% sodium chloride solution and RP is tested by PC at specific time intervals. (D) Lanreotide is labeled directly with 188 Re via the mixture of citrate and tartate using stannous chloride as reduced agent. The influence of reaction conditions such as pH, temperature, amount of stannous chloride, amount of Lanreotide and reaction time on labeling yield is investigated in detail. At the time, the stability in vitro quality control and animal test are evaluated

Synthesis and evaluation of 18f-labeled benzylideneaniline derivatives as new biomarkers for β-amyloid imaging in Alzheimer's disease

International Nuclear Information System (INIS)

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

2005-01-01

Noninvasive early detection of the Aβ plaques in Alzheimer's disease (AD) brain may be useful tool for the treatment of AD patients. We herein describe the synthesis of 18 F-labeled benzylideneaniline derivatives utilizing a novel labeling approach for imaging Aβ plaques in AD patients. Condensation of [ 18 F] 4-fluorobenzaldehyde with various aromatic amines afforded 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 Aβ (1-40) were determined using [ 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 Aβ (1-40) aggregates (Ki 149-304 nM). The 18 F-labeled benzylideneaniline derivatives displayed high brain uptake ratio in normal mice (2.9-24.93). The study suggests that these 18 F-labeled compounds may be suitable for Aβ plaque imaging in AD patients

Development of a general methodology for labelling peptide-morpholino oligonucleotide conjugates using alkyne-azide click chemistry.

Science.gov (United States)

Shabanpoor, Fazel; Gait, Michael J

2013-11-11

We describe a general methodology for fluorescent labelling of peptide conjugates of phosphorodiamidate morpholino oligonucleotides (PMOs) by alkyne functionalization of peptides, subsequent conjugation to PMOs and labelling with a fluorescent compound (Cy5-azide). Two peptide-PMO (PPMO) examples are shown. No detrimental effect of such labelled PMOs was seen in a biological assay.

Synthesis of canrenone and related steroids labelled with tritium, carbon-14, and sulfur-35

International Nuclear Information System (INIS)

Markos, C.S.; Dorn, C.R.; Zitzwitz, D.J.

1988-01-01

The syntheses of [1- 3 H]canrenone, [1- 3 H]spironolactone, [1- 3 H] potassium canrenoate, [22- 14 C]canrenone, [22- 14 C]spironolactone, [22- 14 C]potassium canrenoate, and [ 35 S]spironolactone are reported. Tritium labelled compounds were obtained by catalytic reduction of a 3-keto-1, 4-diene precursor followed by exchange of enolizable label. Carbon-14 compounds were obtained by reaction of a 17-ethynyl steroid with 14 CO 2 . Sulfur-35 spironolactone was synthesized by the in-situ generation of [ 35 S]thiolacetic acid from [ 35 S]sodium sulfide. (author)

Ferrocene, ruthenocene or rhodocene analogues of Haloperidol. Synthesis and organ distribution after labelling with /sup 103/Ru or /sup 103m/Rh

Energy Technology Data Exchange (ETDEWEB)

Wenzel, M; Wu, Y

1988-01-01

Ferrocene-Haloperidol was synthesized by N-alkylation of 4-(4'-chlorophenyl)-4-hydroxypiperidine with 1-ferrocenyl-4-chlor-butan-1-on. By heating the ferrocene-haloperidol with /sup 103/RuCl/sub 3/ the /sup 103/Ru-labelled ruthenocene-haloperidol was obtained. This compound showed a high affinity for lung but not for brain in rats and mice. The decay of the /sup 103/Ru labelled compound results in the formation of the /sup 103m/Rh labelled rhodocene-haloperidol, which is rapidly oxidized by air to the corresponding rhodocinium-haloperidol. This compound can be separated by extraction and TLC.

Purification, labelling and clinical applicability of radioactive asialo-orosomucoid

International Nuclear Information System (INIS)

Rijk, P.P. van

1977-01-01

It is shown that purified and modified orosomucoid is rapidly taken up by the liver. For experiments with rats the pharmacon was labelled with 131 I. The distribution of the radioactivity was determined in samples of tissues after decapitation of the rats. After this study the method of preparation of the pharmacon was changed in order to meet the requirements for human use, e.g. th neuraminidase (Vibrio Cholerae) was removed. The pharmacon, still 131 I-labelled, was tested in a group of patients and controls, however with little success. Therefore a labelling-method was developed which would give better information or even a radiopharmacon which is released via the bile tree. Two methods were developed viz. labelling the pharmacon with sup(99m)Tc and 203 Hg. Tissue distribution studies in the rat showed that both radiopharmaceuticals were taken up rapidly by the liver. The release of the radioactivity however was too slow to be of practical use, although autoradiography showed that the radiopharmacon was taken up by the parenchymal cells. In the course of this study 123 I became commercially available and was also used. The physical characteristics of this radionuclide are more appropriate for dynamic in vivo studies. A mathematical model was developed which assumes three steps viz. an uptake, a delay-time due to catabolism, and release, and it was used for computer simulation studies. Finally, it was concluded that (1) the liver curve obtained from radioactive asialo-orosomucoid studies does not yield enough information, although a correlation exists between delay-time and release rate constant, (2) the functional images show regional defects in which areas with abnormal uptake and abnormal release are not always superimposable

Tests of intestinal absorption using carbon-14-labeled isotopes

International Nuclear Information System (INIS)

Fromm, H.; Sarva, R.P.

1983-01-01

Beta radiation-emitting isotopes are being used increasingly in diagnostic gastroenterology for the study of absorption. The major reason for the popularity of radioisotopes is that their use is convenient for patient and physician alike. They often obviate naso- or orointestinal intubation and the collection, storage, and analysis of stool. The radioactivity used for the studies of digestive and absorptive processes is small and is not hazardous. In spite of the safety of the radiolabeled compounds, their use is restricted in children and pregnant women. Therefore, for most tests, promising alternative methods that make use of the stable isotope of carbon, /sup 13/C, instead of the radioactive /sup 14/C have been developed. The analysis of stable isotopes requires more sophisticated technology than that of radioactive compounds, however. Only a few centers presently are equipped and staffed to analyze stable isotopes on a routine basis. In contrast, the analysis of radioactive isotopes has become a routine procedure in almost ever major laboratory. The last decade has brought the development of several radioactive absorption tests. The clinically most useful tests relate to the study of bile acid, fat, lactose, and xylose absorption. All of these tests utilize the excretion rate of /sup 14/CO/sub 2/ in breath after ingestion of a /sup 14/C-labeled compound as a measure of the rate of its absorption or malabsorption

Synthesis and study of biological behavior of radiopharmaceutical preparations on the base of specific to receptors compounds

International Nuclear Information System (INIS)

Bruskin, A.B.; Klement'eva, O.E.; Kodina, G.E.; Korsunskij, V.N.; Korshunov, V.B.; Slobodnyak, I.I.

2005-01-01

Aim of the present work is study of conditions radionuclide administration in modified biomolecules and study of its conjugation with tumor cells in vivo and in vitro. Octreotide labelling by the 111 In reactions in different buffer systems with yield ≥95 % were carried out. Demands making to quality of initial solution 111 In chloride for providing of radiochemical purity of the labelled compound were determined. Time of maximal accumulation of peptide by tumor cells has been defined. It is shown, that accumulation of control preparation 111 In-DTPA - in dependence on selected cell culture and experiment conditions - in 5-10 time lower, than accumulation of labeled peptide. Lyophilized forms of reagents providing one-stage opportunity of the preparation production at clinic conditions were obtained. The product is stable in laboratory animals blood serum. By the data of biological distribution the differential accumulation coefficients making up: tumor/blood -5-30; tumor-muscle - 2-10. The scintigraphic image of mouse malice's tumor was get

Influence of bone affinity on the skeletal distribution of fluorescently labeled bisphosphonates in vivo.

Science.gov (United States)

Roelofs, Anke J; Stewart, Charlotte A; Sun, Shuting; Błażewska, Katarzyna M; Kashemirov, Boris A; McKenna, Charles E; Russell, R Graham G; Rogers, Michael J; Lundy, Mark W; Ebetino, Frank H; Coxon, Fraser P

2012-04-01

Bisphosphonates are widely used antiresorptive drugs that bind to calcium. It has become evident that these drugs have differing affinities for bone mineral; however, it is unclear whether such differences affect their distribution on mineral surfaces. In this study, fluorescent conjugates of risedronate, and its lower-affinity analogues deoxy-risedronate and 3-PEHPC, were used to compare the localization of compounds with differing mineral affinities in vivo. Binding to dentine in vitro confirmed differences in mineral binding between compounds, which was influenced predominantly by the characteristics of the parent compound but also by the choice of fluorescent tag. In growing rats, all compounds preferentially bound to forming endocortical as opposed to resorbing periosteal surfaces in cortical bone, 1 day after administration. At resorbing surfaces, lower-affinity compounds showed preferential binding to resorption lacunae, whereas the highest-affinity compound showed more uniform labeling. At forming surfaces, penetration into the mineralizing osteoid was found to inversely correlate with mineral affinity. These differences in distribution at resorbing and forming surfaces were not observed at quiescent surfaces. Lower-affinity compounds also showed a relatively higher degree of labeling of osteocyte lacunar walls and labeled lacunae deeper within cortical bone, indicating increased penetration of the osteocyte canalicular network. Similar differences in mineralizing surface and osteocyte network penetration between high- and low-affinity compounds were evident 7 days after administration, with fluorescent conjugates at forming surfaces buried under a new layer of bone. Fluorescent compounds were incorporated into these areas of newly formed bone, indicating that "recycling" had occurred, albeit at very low levels. Taken together, these findings indicate that the bone mineral affinity of bisphosphonates is likely to influence their distribution within the

Clinical utility of labeled cells for detection of allograft rejection and myocardial infarction

International Nuclear Information System (INIS)

Fawwaz, R.A.

1984-01-01

The choice of a specific radiolabeled blood component for use in detection of allograft rejection depends on several factors including the immunosuppressive agents used, the type of organ allografted, and particularly the length of time the allograft resides in the host and the duration of rejection. To date, only the use of 111In-labeled platelets in renal allograft recipients immunosuppressed with azathioprine and corticosteroids has shown clinical promise in the detection of early allograft rejection. Radiolabeled blood components are unlikely to play a significant role in detection of myocardial infarction. The use of these agents for monitoring therapeutic interventions or as indicators of prognosis in patients with myocardial infarction continues to be investigated

Labeled extra virgin olive oil as food supplement; phenolic compounds in oils from some autochthonous Croatian olives

Directory of Open Access Journals (Sweden)

Jakobušić Brala, C.

2015-12-01

Full Text Available Within the framework of an incentive to provide labeled extra virgin olive oils as a food supplement in pharmacies, the phenolic profile analysis of extra virgin olive oils obtained from Croatian olive cultivars has been reported. With the aim of increasing the consumption of EVOO-s in northern Croatia, the varieties Bjelica, Buža and Italian Leccino have been studied involving two different agroclimatic locations, over two harvest years differing significantly in the amount of rainfall. The Croatian cultivars Plominka, Žižolera, Oblica and Lastovka, were also examined. Correlation tests and the insight from PCA reveal that the cultivars are highly individualized in character with regard to relationships among phenolic compounds. Some elements of an innovative labeling aimed to better present the authenticity, quality, excellence and uniqueness of the EVOO-s were suggested.En el marco de los incentivos que se han considerado para proporcionar el etiquetado de aceites de oliva virgen extra como suplemento alimenticio en farmacias, se reporta el análisis del perfil fenólico de aceites de oliva vírgenes extra obtenidos a partir de variedades croatas. Para ampliar el consumo de AOVE-s en el norte de Croacia, se han estudiado las variedades Bjelica, Buža y Leccino italiana procedentes de dos lugares agroclimáticos diferentes que difieren significativamente en la cantidad de lluvia y obtenidos en dos cosechas. Tambien fueron examinados los cultivares croatas Plominka, Žižolera, Oblica y Lastovka. Los test de correlación y los resultados de PCA revelan que las variedades están altamente individualizados en su carácter en lo que respecta a las relaciones entre los compuestos fenólicos. Se sugirieron algunos elementos innovadores para un etiquetado dirigido a presentar mejor la autenticidad, la calidad, la excelencia y la singularidad de los AOVE-s.

Clinical Research on Traditional Chinese Medicine compounds and their preparations for Amyotrophic Lateral Sclerosis.

Science.gov (United States)

Zhu, Jiayi; Shen, Lan; Lin, Xiao; Hong, Yanlong; Feng, Yi

2017-12-01

Amyotrophic lateral sclerosis (ALS) is a chronic, fatal neurodegenerative disease which leads to progressive muscle atrophy and paralysis. In order to summarize the characteristics of Traditional Chinese Medicine compounds and their preparations in the prevention and treatment of ALS through analyzing the mechanism, action site, and symptoms according to effective clinical research. We searched ALS, motor neuron disease, chemical drugs, herbal medicine, Chinese medicine, Traditional Chinese Medicine (TCM), and various combinations of these terms in databases including the PudMed, Springer, Ovid, Google, China National Knowledge Infrastructure, and Wanfang databases. It was found that the chemical drugs almost had not sufficient evidence to show their effectiveness in the treatment of ALS, except RILUZOLE. According to the characteristics of clinical symptoms of ALS, Chinese medicine practitioners believe that this disease belongs to the category of "atrophic disease". In clinical research, many Chinese herbal formulas had good clinical efficacies in the treatment of ALS with multiple targets, multiple links, and few side effects. And four kinds of dialectical treatment had been developed based on Clinical data analysis and the use of dialectical therapy: Benefiting the kidney; Declaring the lungs; Enhancing the Qi; and Dredging the meridian. In this review, we provide an overview of chemical drugs and Traditional Chinese Medicine compound and its preparations in therapy of ALS as well as how they may contribute to the ALS pathogenesis, thereby offering some clues for further studies. Copyright © 2017. Published by Elsevier Masson SAS.

In vivo labelling of acetyl-aspartyl peptides in mouse brain from intracranially and intracranially and intraperitoneally administered acetyl-L-[U-14C]aspartate

International Nuclear Information System (INIS)

Sinichkin, A.; Sterri, S.; Edminson, P.D.; Reichelt, K.L.; Kvamme, E.

1977-01-01

Following intracranial and intraperitoneal injection of acetyl-L-[U- 14 C]aspartate into mice about 5% and 0.7% of the radioactivity, respectively, was recovered from the brain after 30 min. On chromatographic separation of the cationic and anionic compounds on a Dowex 50 column, the former fraction contained about 60% of the radioactivity, predominantly as labelled asparate and glutamate. The anionic compounds, containing 20% of the labelled compounds, were fractionated in several chromatographic systems and resolved into a great variety of labelled peptidic compounds of which five acetyl-[U 14 ]aspartyl peptides, containing two to four amino acids, were purified. One of these, acetyl-aspartyl glutamine, has not previously been found in brain. (author)

Mineralization of 14C-labeled agrochemicals in soil

International Nuclear Information System (INIS)

Xu Bujin; Huang Xiaohua; Hu Xiuqing; Zhang Yongxi

2001-01-01

14 C-labeled compounds were used to study the mineralization of methamidophos, 2,4-D and metsulfuron in soil. Mineralization rate was influenced by the type of soil, concentration of chemical in the soil, the initial soil microbial population and the nature of the chemical. (author)

Biodistribution of Ru-97-labeled DTPA, DMSA and transferrin

International Nuclear Information System (INIS)

Som, P.; Oster, Z.H.; Fairchild, R.G.; Atkins, H.L.; Brill, A.B.; Gil, M.C.; Srivastava, S.C.; Meinken, G.E.; Goldman, A.G.; Richards, P.

1980-01-01

Ruthenium-97 is being produced at the Brookhaven Linac Isotope Producer (BLIP). The favorable physical properties of Ru-97 and chemical reactivity of ruthenium offer a potential for using this isotope to label compounds useful for delayed scanning. Diethylenetriamine pentaacetic acid (DTPA), 2,3-Dimercaptosuccinic acid (DMSA), and Transferrin (TF) were labeled with Ru-97-chloride. Ru-97-DTPA and In-111-DTPA, injected intravenously, showed similar organ distribution, kinetics, and more than 80% excretion by 0.5 h. Ru-97-DTPA and In-111-DTPA injected into the cisterna magna of dogs showed similar kinetics in brain, blood, and urinary bladder. The energy deposited by 1 mCi In-111-DTPA is twice that from 1 mCi Ru-97-DTPA. High quality camera images of the CSF space in the dog were obtained with both isotopes. Ru-97-DMSA was prepared with and without the addition of SnCl 2 .2H 2 O. Tin-free DMSA was rapidly excreted via the kidneys, whereas for maximum cortical deposition, the tin-containing preparation was superior. This compound is suitable for delayed imaging of both normal and impaired kidneys. Tissue distribution studies were performed in abscess-bearing rats with Ru-97-transferrin. Although blood levels were higher than with Ga-67-citrate, the abscess had twice as much Ru-97-TF as Ga-67-citrate and the Ru-97 muscle activity was one-third that of Ga-67. Imaging of abscess-bearing rabbits with Ru-97-TF visualized the abscesses as early as 1/2 hr after injection. Since the initial images visualize the abscess so clearly and since the TF portion of the compound binds to the abscess, Tc-99m-TF is being studied for the same purpose. Ru-97-labeled compounds are a promising replacement for In-111 and possibly also for Ga-67 compounds with the advantages of lower radiation dose and high quality image

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

International Nuclear Information System (INIS)

Nascimento, Rosemeire Fagundes

2007-01-01

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

Application of isotope-labelled compounds in the study of the chemical stability of pesticides

International Nuclear Information System (INIS)

Roesseler, M.; Luther, D.; Abendroth, H.C.; Koch, H.

1980-01-01

The user of pesticides requires specific biological modes of action from the corresponding commercial products. Impurities and degradation products may cause uncontrollable toxicological reactions. Profound knowledge of the chemical stability of the effective substance in question and its formulations under storage conditions as well as under those of analytical sample preparation and detection is required. Radioisotope labelled effective substances dimethoate and 1-butyl-amino-cyclohexane-phosphonic acid dibutyl ester are used to study storage stability of the pure effective substance and its formulations; effects of selected impurities, such as technical by-products, moisture or water content, binding or carrier materials, organic solvents, chemical stabilizers and other formulation components on storage properties; temperature dependence of storage stability; selection of suitable analytical techniques for quantitative determination of the effective substance without interference effects from any by-product; reduction of the necessary analytical expense; disclosure of sources of error in the application of usual analytical techniques; improvement of possibilities of an immediate and clearer discrimination between types and amounts of compounds in a chemical system consisting of one pesticide and its degradation or reaction products at the beginning and at the end of an experimental or reaction period. Radiochemical analytical techniques, such as radio thin-layer chromatography (also combined with liquid scintillation counting), radio gas chromatography, autoradiography and isotope dilution analysis were used. Results are discussed, especially of experiments on dimethoate and its technical by-products

Oxygen-15 labelled water production for positron emission tomography

International Nuclear Information System (INIS)

Janus, A.; Sachinidis, J.I.; Chan, J.G.; Tochon-Danguy, H.J.

1998-01-01

Full text: Functional imaging using positron emission tomography (PET) and 15 O-labelled compounds is both scientifically and clinically challenging. The short half-life of oxygen-15 (t 1/2 = 2 min) allows for multiple administration to a patient without exceeding acceptable levels of absorbed radiation dose and without excessive delay between administrations. The clinical usefulness of [ 15 O]-labelled water for cerebral blood flow measurements has been well established. Here we report the development and construction of a [ 15 O]water generator based on an earlier design from Hammersmith Hospital, London. The cyclotron produces a continuous flow of [ 15 O]O 2 gas by the irradiation of a natural nitrogen target (1% O 2 in N 2 ) with a 5 MeV deuteron beam, via the nuclear reaction ( 14 N(d,n) 15 O). The radioactive gas is then mixed with 5% hydrogen in nitrogen and piped to the water generator located in the scanner room. The O 2 /N 2 gas mixture is reacted over a palladium catalyst at 1500 deg C to produce [ 15 O]H 2 O vapour. The vapour passes through an exchanger where it diffuses across a semi-permeable membrane (cellulose acetate) into saline solution. At the optimum gas flow- rate of 500 mL/min, more than 95% of the radioactive oxygen is converted to radioactive water. Waste radioactive gas is piped back to the cyclotron vault to decay before release into the atmosphere. The saline solution (0.9% NaCl) is pumped continuously through the system at 6 mL/min with an infusion pump (3M AVI470). The present system has been in operation for more than a year and has been used for clinical evaluation of stroke patients and for brain activation research studies

Preparation of [In-111]-labeled-DTPA-bombesin conjugates at high specific activity and stability: Evaluation of labeling parameters and potential stabilizers

Energy Technology Data Exchange (ETDEWEB)

Pujatti, P.B., E-mail: pujatti.pb@gmail.com [Directory of Radiopharmacy, Nuclear and Energy Research Institute (IPEN/CNEN), Av. Prof. Lineu Prestes, 2242 - Cidade Universitaria da USP - Butanta, Sao Paulo - SP - Brazil - CEP: 05508-000 (Brazil); Massicano, A.V.F.; Mengatti, J.; Araujo, E.B. de [Directory of Radiopharmacy, Nuclear and Energy Research Institute (IPEN/CNEN), Av. Prof. Lineu Prestes, 2242 - Cidade Universitaria da USP - Butanta, Sao Paulo - SP - Brazil - CEP: 05508-000 (Brazil)

2012-05-15

The aim of the present work was to obtain stabilized high specific activity (HSA) {sup 111}In-labeled bombesin conjugates for preclinical evaluations. Parameters influencing the kinetics of labeling were investigated and the effect of stabilizers on HSA radiopeptides stability at room temperature were systematically categorized applying chromatography techniques. A SA of 174 GBq/{mu}mol was achieved with high radiochemical purity, but the labeled compounds exhibited low stability. The addition of stabilizers avoided their radiolysis and significantly increased their stability. - Highlights: Black-Right-Pointing-Pointer We aimed to obtain stabilized high specific activity (SA) {sup 111}In-labeled bombesin conjugates. Black-Right-Pointing-Pointer The effect of stabilizers on high SA radiopeptides stability were investigated. Black-Right-Pointing-Pointer A maximum specific activity of 174 GBq/{mu}mol was achieved. Black-Right-Pointing-Pointer The studied stabilizers significantly increased the stability of high SA radiopeptides. Black-Right-Pointing-Pointer These stabilized bombesin conjugates will be applied in preclinical studies.

Preparation and preclinical evaluation of 211At-labelled compounds for α-particle radiotherapy

International Nuclear Information System (INIS)

Larsen, R.H.

1994-01-01

The present work demonstrate that significant therapeutic gain can be achieved with 211 At-labelled MoAbs on single tumour cells and microscopic disease. Β-emitters are less effective on microscopic disease because of radiation dispersion, while longer halflives (e.g., 90 Y and 131 I) allow favourable therapeutic ratios to be reached in larger tumors. 211 At-labelled MoAbs may therefore possibly be used in combination with β-emitting RIC in systemically delivered radioimunnotherapy. Larger tumor nodules are then irradiated effectively due to cross-fire of the longer ranged β-particles while the fraction of tumour cells distributed as single cells and micrometastases may be more effectively radiated with 211 At-RIC. 76 refs

Clinical evaluation of the effect of a herbal compound made for treatment of discolorations caused by dental fluorosis

Directory of Open Access Journals (Sweden)

Mahshid Mohammdi Basir

2013-08-01

Full Text Available   Background and Aims: The purpose of this study was research on a new herbal compound (Seidlitzia Rosmarinus made by Traditional Medicine Research Group, University of shahed to find a safer alternative to HCL-Pumice compound technique.   Materials and Methods: In this randomized clinical trial seventy two anterior teeth from 9 patients were divided in to three groups according to fluorosis severity: mild (34 teeth, moderate (14 teeth, and sever (24 teeth. In each patient, half of the teeth were treated with “Shahed” compound and other half treated with HCL-Pumice compound. Before and after treatment, photographs were taken in both groups. HCL-Pumice treatment compound was applied for 30 seconds periods and continued for 10 minutes if necessary. In case of herbal Shahed compound the time was determined by clinical symptoms or when labial contour was dismissed, If the result was not esthetistically acceptabale for the patient, HCL-Pumice compound was applied on teeth. NaF was applied after mouth washing. The photographs of the teeth before and after treatment were reviewed by two experienced observer unaware of the treatment modality. The results were analyzed using willcoxon’s, kruskal-wallis and scheffe test.   Results: There was over 81.3% acceptance between two observers and no significant differences in intraobservers evaluation (P>0.05. Improvement in beauty indexes were observed in all degrees of dental fluorosis by 18% with HCL-Pumice compound application, but “Shahed” herbal compound induced significant reduction in the amount of white spots in mild fluorosis and stain intensity of moderate fluorosis (P<0.05 , while the reduction in the severity of discoloration in group 2, these two techniques were statistically equivalent but in the remainder, HCL-Pumice compound was more significantly effective (P<0.05 .   Conclusion: HCL-Pumice compound reduces the severity of the discoloration of the teeth. Shahed herbal compound

Development of new and improved labelling procedures for introducing isotopic hydrogen and carbon-11 into organic compounds

International Nuclear Information System (INIS)

Al-Qahtani, M.H.S.

1999-10-01

New and improved methods for introducing radioisotopic hydrogen (tritium) and carbon (positron-emitting short-lived carbon-11, t 1/ 2 = 20.4 min) into organic molecules for application in biological research have been explored. In Chapter 1 the applications of radioactive isotopes in biological and clinical research is surveyed, with particular emphasis on the value of β-emitting tritium and positron-emitting carbon-11. In Chapter 2 we report the use of the non-radioactive hydrogen isotope, deuterium, as a surrogate for tritium in the development of microwave-enhanced labelling procedures, based on catalytic hydrogen transfer to olefins (e.g. styrene, styrene derivatives, cinnamic acid and its derivatives). Hydrogen or deuterium donors (e.g. formate salts) were used alone or in combination with other sources (e.g. D 2 O). The method was found to give fully hydrogenated products using very short microwave irradiation times (∼ 2 min) and was highly reproducible. Importantly, the method is environmentally clean, as when extended to tritiated formates little or no radioactive waste is produced. In Chapter 3 we explored the labelling of CGP 62349 {3-[1-(R)-[3-(4-methoxybenzyl)phosphinyl-2-(S)-hydroxy-propyl- amino]ethyl]benzoic acid}, a γ-aminobutyric acid type B (GABA B ) receptor antagonist, with carbon-11 in order to provide a prospective radioligand for medical imaging with positron emission tomography (PET). Labelling agents, [ 11 C]iodomethane and [ 11 C]methyl triflate, prepared by improved methods, were used in the rapid methylation of desmethyl-CGP 62349. Substantially higher radiochemical yields (78%) of [ 11 C]CGP 62349 were achieved by the new methods compared to that produced in a previously published procedure (9%). In addition, the use of [ 11 C]methyl triflate rather than [ 11 C]iodomethane has the advantage of giving a high radiochemical yield and a lower amount of carrier. In Chapter 4 we report on the use of [ 11 C]carbon monoxide as a labelling

A comparative study on the iodine-labeled methods of protein and polypeptide

International Nuclear Information System (INIS)

Li Huaifen; Niu Huisheng; Yuan Mingyue; Yu Jinghua

1994-01-01

There are three methods: chloramine-T, Iodogen and lactoperoxidase(LPO). 125 I-ACTH, 125 I-insulin and 125 I-HSA are prepared by these techniques. The results show that lactoperoxidase is isolated and purified from fresh milk, meanwhile, the enzyme is used in experiments of 125 I-labeled protein, peptide hormone and mono-clone antibody, etc. LPO is a very successful method for it's mild, complete reaction, controllable, high labelling yield, higher purity of iodine-labeled compound and so on. It remains biological activation and stable character more than other two techniques

Supercritical fluid synthesis inthe preparation of β+-emitting labelled compounds

International Nuclear Information System (INIS)

Jacobson, G.; Markides, K.E.; Laangstroem, B.

1994-01-01

A system for synthesis in supercritical fluids has been developed for the microscale synthesis of pharmaceuticals labelled with 11 C. Supercritical ammonia was selected as the reaction medium and the following variables were studied in detail: trapping efficiency, cell design, substrate concentration, operation design, and temperature and pressure conditions. Alkylation of phenol by [ 11 C]methyl iodide to yield [methyl- 11 C]anisole was used as a model reaction for evaluation of the system. The results show an increased radiochemical yield in the highly compressible near-critical region. (au) (40 refs.)

Radioimmunoassay in basic and clinical pharmacology

International Nuclear Information System (INIS)

Patrono, C.; Peskar, B.A.

1987-01-01

The subject of the book is the development, validation and application of radioimmunoassay (RIA) techniques for the measurement of a variety of substances in animal and human body fluids. The book discusses methodological and conceptual issues related to the main classes of mediators of drug action and to drugs themselves, as assayed by this particular analytical technique. A number of introductory chapters provide basic information concerning production and characterization of antibodies, labeling techniques, statistical aspects and validation criteria, insight into problems related to the development and validation of RIA for the newly discovered mediator(s). In the following chapters, the emphasis is placed on the technical details relevant to each class of compounds and on specific aspects of their applications to basic and/or clinical pharmacological studies. New developments in this area, such as monoclonal antibodies and non-radioactive labeling techniques, are also covered

Sulfonyl fluoride-based prosthetic compounds as potential 18F labelling agents.

Science.gov (United States)

Inkster, James A H; Liu, Kate; Ait-Mohand, Samia; Schaffer, Paul; Guérin, Brigitte; Ruth, Thomas J; Storr, Tim

2012-08-27

Nucleophilic incorporation of [(18)F]F(-) under aqueous conditions holds several advantages in radiopharmaceutical development, especially with the advent of complex biological pharmacophores. Sulfonyl fluorides can be prepared in water at room temperature, yet they have not been assayed as a potential means to (18)F-labelled biomarkers for PET chemistry. We developed a general route to prepare bifunctional 4-formyl-, 3-formyl-, 4-maleimido- and 4-oxylalkynl-arylsulfonyl [(18)F]fluorides from their sulfonyl chloride analogues in 1:1 mixtures of acetonitrile, THF, or tBuOH and Cs[(18)F]F/Cs(2)CO(3(aq.)) in a reaction time of 15 min at room temperature. With the exception of 4-N-maleimide-benzenesulfonyl fluoride (3), pyridine could be used to simplify radiotracer purification by selectively degrading the precursor without significantly affecting observed yields. The addition of pyridine at the start of [(18)F]fluorination (1:1:0.8 tBuOH/Cs(2)CO(3(aq.))/pyridine) did not negatively affect yields of 3-formyl-2,4,6-trimethylbenzenesulfonyl [(18)F]fluoride (2) and dramatically improved the yields of 4-(prop-2-ynyloxy)benzenesulfonyl [(18)F]fluoride (4). The N-arylsulfonyl-4-dimethylaminopyridinium derivative of 4 (14) can be prepared and incorporates (18)F efficiently in solutions of 100 % aqueous Cs(2)CO(3) (10 mg mL(-1)). As proof-of-principle, [(18)F]2 was synthesised in a preparative fashion [88(±8) % decay corrected (n=6) from start-of-synthesis] and used to radioactively label an oxyamino-modified bombesin(6-14) analogue [35(±6) % decay corrected (n=4) from start-of-synthesis]. Total preparation time was 105-109 min from start-of-synthesis. Although the (18)F-peptide exhibited evidence of proteolytic defluorination and modification, our study is the first step in developing an aqueous, room temperature (18)F labelling strategy. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

One-carbon 13C-labeled synthetic intermediates. Comparison and evaluation of preparative methods

International Nuclear Information System (INIS)

Ott, D.G.

1978-01-01

Frequently the biggest stumbling block to the synthesis of a structurally complex labeled compound is obtaining the required low molecular weight, structurally simple, isotopic intermediates. Selection of a particular scheme from various alternatives depends on the available capabilities and quantity of product desired, as well as on anticipated future requirements and need for related compounds. Many of the newer reagents for organic synthesis can be applied effectively to isotopic preparations with improvements of yields and simplification of procedures compared to established classical methods. New routes developed for higher molecular weight compounds are sometimes not directly adaptable to the one-carbon analogs, either because of isolation difficulties occasioned by physical properties or by chemical reactivities peculiar to their being first members of homologous series. Various routes for preparation of carbon-13 labeled methanol, formaldehyde, and cyanide are compared

High-level production of C-11-carboxyl-labeled amino acids

International Nuclear Information System (INIS)

Washburn, L.C.; Sun, T.T.; Byrd, B.L.; Hayes, R.L.; Butler, T.A.; Callahan, A.P.

1979-01-01

Carbon-11-labeled amino acids have significant potential as agents for positron tomographic functional imaging. We have developed a rapid, high-temperature, high-pressure modification of the Buecherer--Strecker amino acid synthesis and found it to be quite general for the production of C-11-carboxyl-labeled neutral amino acids. Production of C-11-carboxyl-labeled DL-tryptophan requires certain modifications in the procedure. Twelve different amino acids have been produced to date by this technique. Synthesis and chromatographic purification require approximately 40 min, and C-11-carboxyl-labeled amino acids have been produced in yields of up to 425 mCi. Two C-11-carboxyl-labeled amino acids are being investigated clinically for tumor scanning and two others for pancreatic imaging. Over 120 batches of the various agents have been produced for clinical use over a three-year period

Labeling of monoclonal antibody conjugates with 90Y

International Nuclear Information System (INIS)

Motta-Hennessy, Cecilia; Sharkey, R.M.; Goldenberg, D.M.

1991-01-01

An anti-carcinoembryonic antigen (CEA) antibody, NP-4, was labeled with 90 Y using p-isothiocyanatobenzyl DTPA (SCN-Bz-DTPA) and its derivatives 1-(p-isothiocyanatobenzyl)-3-methyl-DTPA (1B3M), 2-(p-isothiocyanatobenzyl)-4-methyl-DTPA (1M3B), 1-(2)-methyl-4-isothiocyanatobenzyl-DTPA (MX-DTPA) as the chelating agents. The 90 Y conjugates were purified from unbound 90 Y by two different methods, HPLC or acrylamide size exclusion gel chromatography, in order to evaluate the best purification method. Labeling efficiency, reaction kinetics and immunoreactivity were compared to the same antibodies labeled with [ 111 In]citrate. Labeling efficiency, as determined by either HPLC or ITLC (instant thin layer chromatography), was consistently higher by ITLC than HPLC for 90 Y-labeled MAb, but equal for 111 In-labeled MAbs. Discrepancies between the 2 methods were linked to impurities in the 90 Y that remained at the origin of ITLC plates. After purification by acrylamide gel filtration, recovery was 50-60% of loaded 90 Y activity, but was more than 87% for the 111 In compounds. Using HPLC, the recovery measured 85% for 90 Y-labeled MAb and more than 93% for 111 In-labeled conjugates. Immunoreactivity of the [ 90 Y]MAb was comparable to the 111 In-labeled conjugates. These studies indicate that HPLC purification of the [ 90 Y] MAbs improves recovery of activity, and suggests that impurities found in the 90 Y and metal-binding properties of acrylamide may have contributed to the poor recoveries from acrylamide gels. (author)

Compounding and Extralabel Use of Drugs in Exotic Animal Medicine.

Science.gov (United States)

Powers, Lauren V; Davidson, Gigi

2018-05-01

Extralabel drug use is the use of a Food and Drug Administration (FDA)-approved drug in a manner different from what is stipulated on the approved label. Compounding is the process of preparing a medication in a manner not indicated on the label to create a formulation specifically tailored to the needs of an individual patient. Extralabel drug use and compounding are vital aspects of safe and effective drug delivery to patients in exotic animal practice. There are few FDA-approved drugs for exotic animal species, and many approved drugs for other species are not available in suitable formulations for use in exotic animals. Copyright © 2018 Elsevier Inc. All rights reserved.

Food and Drug Labeling and the Adult Reader.

Science.gov (United States)

McKenna, Michael C.; Aker, Richard

1978-01-01

Full disclosure of ingredients on food, drugs, and cosmetic labels is really non-disclosure where the chemical formulation has no common name or where one generic name covers a variety of formations. The Food and Drug Administration offers suggestions for adult education programs in consumer awareness, understanding compound nomenclature, and…

Synthesis of puric bases labelled with carbon 14 and nitrogen 15

International Nuclear Information System (INIS)

Lamorre, Yves

1975-01-01

In this report for graduation in organic chemistry engineering, the author reports the synthesis of adenine 14 C-2 et 14 C-6 by two different chemical ways from two derivatives of imidazole. He has used adenine 14 C-6 to obtain hypoxanthine 14 C-6, and then, by enzymatic processing, uric acid 14 C-6. He reports the study of the production of guanine 14 C-2 by cyclization of silylated derivative of imidazole with the carbon 14 C sulphur. However, a method of complete synthesis of this same compound revealed to be more practical. This complete synthesis way allowed the labelling of guanine in positions 1, 2 and 3 by the 96 per cent isotopic nitrogen. Nitrogen in positions 7 and 9 could have been labelled by the same way from the ethyl cyanoacetate 15 N and from the sodium nitrite 15 N. The study of the mass spectrum of these compounds labelled with nitrogen 15 N allowed most of fragments obtained during this analysis to be identified [fr

A Study on Labelling of Linolenic Acid as A Model of Isolated Benalu Teh for Cancer Diagnosis with Iodine-131

International Nuclear Information System (INIS)

Isti Daruwati; Eva Maria Widyasari; Nanny Kartini Oekar

2009-01-01

A study on active fraction of benalu teh has been carried out at Center for Application of Isotope and Radiation Technology - BATAN. This benalu teh active fraction has inhibition capability about 99% to the cancer cell. The isolated fraction is octadeca-8,10,12-triyonic acid compound which have long chain unsaturated fatty acid compound with three triple bonds. The Benalu teh active fraction has similar structure with linolenic acid which is a long chain unsaturated fatty acid with three triple bonds. Based on this similarity, the study of labelling of linolenic acid with iodine-131 has been conducted. The research was focused on optimum conditions for labelling of linolenic acid using Iodine-131 radionuclide. Labelling with iodine-131 was conducted using KIO 3 as an oxidizing agent, which can additionated linolenic acid and sodium metabisulfite for ending the reaction. Labelling efficiency determination was conducted using paper chromatography technique. The result showed that the optimum condition achieved by using KIO 3 as an oxidizing agent that gave radiochemical purity of 99,44% in virgin coconut oil, and labelling efficiency of about 69,9%. The labelled compound has high radiochemical purity i.e 96,85% in chloroform and 98,33% virgin coconut oil that was stable until 10 days in refrigerator. (author)

Microfluidic Radiometal Labeling Systems for Biomolecules

Energy Technology Data Exchange (ETDEWEB)

Reichert, D E; Kenis, P J. A.

2011-12-29

In a typical labeling procedure with radiometals, such as Cu-64 and Ga-68; a very large (~ 100-fold) excess of the non-radioactive reactant (precursor) is used to promote rapid and efficient incorporation of the radioisotope into the PET imaging agent. In order to achieve high specific activities, careful control of reaction conditions and extensive chromatographic purifications are required in order to separate the labeled compounds from the cold precursors. Here we propose a microfluidic approach to overcome these problems, and achieve high specific activities in a more convenient, semi-automated fashion and faster time frame. Microfluidic reactors, consisting of a network of micron-sized channels (typical dimensions in the range 10 - 300¼m), filters, separation columns, electrodes and reaction loops/chambers etched onto a solid substrate, are now emerging as an extremely useful technology for the intensification and miniaturization of chemical processes. The ability to manipulate, process and analyze reagent concentrations and reaction interfaces in both space and time within the channel network of a microreactor provides the fine level of reaction control that is desirable in PET radiochemistry practice. These factors can bring radiometal labeling, specifically the preparation of radio-labeled biomolecules such as antibodies, much closer to their theoretical maximum specific activities.

Synthesis of /sup 14/C- and /sup 3/H-labelled 4-(4-nitrophenyl)aminophenylisothiocyanate (Go 9333/CGP 4540; amoscanate)

Energy Technology Data Exchange (ETDEWEB)

Anjaneyulu, B.; Maller, R.K.; Nagarajan, K. (Hindustan Ciba-Geigy Ltd., Bombay (India). Isotope Lab.); Kueng, W.; Wirz, B. (Ciba-Geigy A.G., Basel (Switzerland))

1985-04-01

Amoscanate, a broad spectrum anthelmintic, labelled with carbon-14 on the isothiocyanate carbon atom was prepared in an overall yield of 13% at a specific activity of 4.13 ..mu..Ci/mg from potassium (/sup 14/C)thiocyanate. The 4-nitro(U-/sup 14/C)phenyl ring labelled compound was synthesized in 20.4% overall yield from (U-/sup 14/C)aniline at a specific activity of 12.2 ..mu..Ci/mg. The corresponding tritiated compound was prepared from 4-amino(2-/sup 3/H)acetanilide at 112 ..mu..Ci/mg. Labelling with tritium in the aromatic ring bearing the isothiocyanate group was achieved by catalysed halogen-tritium replacement. However, for pharmacokinetic and metabolism studies in experimental animals, the /sup 14/C- and /sup 3/H-labels associated with the phenylisothiocyanate moiety subsequently proved disadvantageous because of the instability of the labels in vivo.

Profiling structured product labeling with NDF-RT and RxNorm

Science.gov (United States)

2012-01-01

Background Structured Product Labeling (SPL) is a document markup standard approved by Health Level Seven (HL7) and adopted by United States Food and Drug Administration (FDA) as a mechanism for exchanging drug product information. The SPL drug labels contain rich information about FDA approved clinical drugs. However, the lack of linkage to standard drug ontologies hinders their meaningful use. NDF-RT (National Drug File Reference Terminology) and NLM RxNorm as standard drug ontology were used to standardize and profile the product labels. Methods In this paper, we present a framework that intends to map SPL drug labels with existing drug ontologies: NDF-RT and RxNorm. We also applied existing categorical annotations from the drug ontologies to classify SPL drug labels into corresponding classes. We established the classification and relevant linkage for SPL drug labels using the following three approaches. First, we retrieved NDF-RT categorical information from the External Pharmacologic Class (EPC) indexing SPLs. Second, we used the RxNorm and NDF-RT mappings to classify and link SPLs with NDF-RT categories. Third, we profiled SPLs using RxNorm term type information. In the implementation process, we employed a Semantic Web technology framework, in which we stored the data sets from NDF-RT and SPLs into a RDF triple store, and executed SPARQL queries to retrieve data from customized SPARQL endpoints. Meanwhile, we imported RxNorm data into MySQL relational database. Results In total, 96.0% SPL drug labels were mapped with NDF-RT categories whereas 97.0% SPL drug labels are linked to RxNorm codes. We found that the majority of SPL drug labels are mapped to chemical ingredient concepts in both drug ontologies whereas a relatively small portion of SPL drug labels are mapped to clinical drug concepts. Conclusions The profiling outcomes produced by this study would provide useful insights on meaningful use of FDA SPL drug labels in clinical applications through

Profiling structured product labeling with NDF-RT and RxNorm

Directory of Open Access Journals (Sweden)

Zhu Qian

2012-12-01

Full Text Available Abstract Background Structured Product Labeling (SPL is a document markup standard approved by Health Level Seven (HL7 and adopted by United States Food and Drug Administration (FDA as a mechanism for exchanging drug product information. The SPL drug labels contain rich information about FDA approved clinical drugs. However, the lack of linkage to standard drug ontologies hinders their meaningful use. NDF-RT (National Drug File Reference Terminology and NLM RxNorm as standard drug ontology were used to standardize and profile the product labels. Methods In this paper, we present a framework that intends to map SPL drug labels with existing drug ontologies: NDF-RT and RxNorm. We also applied existing categorical annotations from the drug ontologies to classify SPL drug labels into corresponding classes. We established the classification and relevant linkage for SPL drug labels using the following three approaches. First, we retrieved NDF-RT categorical information from the External Pharmacologic Class (EPC indexing SPLs. Second, we used the RxNorm and NDF-RT mappings to classify and link SPLs with NDF-RT categories. Third, we profiled SPLs using RxNorm term type information. In the implementation process, we employed a Semantic Web technology framework, in which we stored the data sets from NDF-RT and SPLs into a RDF triple store, and executed SPARQL queries to retrieve data from customized SPARQL endpoints. Meanwhile, we imported RxNorm data into MySQL relational database. Results In total, 96.0% SPL drug labels were mapped with NDF-RT categories whereas 97.0% SPL drug labels are linked to RxNorm codes. We found that the majority of SPL drug labels are mapped to chemical ingredient concepts in both drug ontologies whereas a relatively small portion of SPL drug labels are mapped to clinical drug concepts. Conclusions The profiling outcomes produced by this study would provide useful insights on meaningful use of FDA SPL drug labels in clinical

Profiling structured product labeling with NDF-RT and RxNorm.

Science.gov (United States)

Zhu, Qian; Jiang, Guoqian; Chute, Christopher G

2012-12-20

Structured Product Labeling (SPL) is a document markup standard approved by Health Level Seven (HL7) and adopted by United States Food and Drug Administration (FDA) as a mechanism for exchanging drug product information. The SPL drug labels contain rich information about FDA approved clinical drugs. However, the lack of linkage to standard drug ontologies hinders their meaningful use. NDF-RT (National Drug File Reference Terminology) and NLM RxNorm as standard drug ontology were used to standardize and profile the product labels. In this paper, we present a framework that intends to map SPL drug labels with existing drug ontologies: NDF-RT and RxNorm. We also applied existing categorical annotations from the drug ontologies to classify SPL drug labels into corresponding classes. We established the classification and relevant linkage for SPL drug labels using the following three approaches. First, we retrieved NDF-RT categorical information from the External Pharmacologic Class (EPC) indexing SPLs. Second, we used the RxNorm and NDF-RT mappings to classify and link SPLs with NDF-RT categories. Third, we profiled SPLs using RxNorm term type information. In the implementation process, we employed a Semantic Web technology framework, in which we stored the data sets from NDF-RT and SPLs into a RDF triple store, and executed SPARQL queries to retrieve data from customized SPARQL endpoints. Meanwhile, we imported RxNorm data into MySQL relational database. In total, 96.0% SPL drug labels were mapped with NDF-RT categories whereas 97.0% SPL drug labels are linked to RxNorm codes. We found that the majority of SPL drug labels are mapped to chemical ingredient concepts in both drug ontologies whereas a relatively small portion of SPL drug labels are mapped to clinical drug concepts. The profiling outcomes produced by this study would provide useful insights on meaningful use of FDA SPL drug labels in clinical applications through standard drug ontologies such as NDF-RT and

The method of obtaining of sodium orthoiodohippurate labelled with iodine-131

International Nuclear Information System (INIS)

Aripov, D.; Abdukayumov, M.; Shukurov, A.Sh.

1994-01-01

The method of labelling of sodium orthoiodohippurate was elaborated with the purpose of increasing the preparation quality. Method includes the reaction of isotopic exchange between orthoiodhippur acid and sodium iodide solution labelled with iodine-131 with volume activity 150-200 mCu/mL and pH=6,5-7,0. Reaction occurs at temperature 120-130 C during 1,1-1,3 hours and the compound obtained is dissolved in 1% sodium bicarbonate solution. (author)

Gadolinium labeled pharmaceuticals as potential MRI contrast agents for liver and biliary tract

International Nuclear Information System (INIS)

Najafi, A.; Amparo, E.G.; Johnson, R.F. Jr.

1987-01-01

Three gadolinium-labeled compounds, potential nuclear magnetic resonance (NMR) imaging contrast agents for liver and biliary tract, were studied: 1) Gd-DISIDA, 2) Gd-DTPA-Liposomes, and 3) Gd-DTPA dihexadecylamide (Gd-diamide). In each case, ''Carrier Added'' Gd-153 with specific activity of about 5uCi/mg was used. Each labeled compound was evaluated in experimental animals. Gd-DISIDA proved unsatisfactory because of in vivo instability. Gd-DTPA-Liposomes demonstrated strong toxic effects probably due to pulmonary embolism when large amounts of this compound was administered intravenously. Gd-diamide showed good uptake in the hepatocytes with subsequent excretion into the biliary tract. Several rabbits were imaged in a 0.6T NMR imaging system before and after injection of Gd-diamide. Pulse sequences were chosen that would yield T1-weighted images and permit calculation of T1 relaxation times. This compound produced significant shortening of the T1 relaxation times of the liver and observable increase in intensity on the T1-weighted images. Gd-diamide shows promise as potential NMR contrast agent for liver and biliary tract imaging. (author)

A comparative study on the iodine-labeled methods of protein and polypeptide

Energy Technology Data Exchange (ETDEWEB)

Huaifen, Li; Huisheng, Niu; Mingyue, Yuan; Jinghua, Yu [Chinese Academy of Medical Sciences, Tianjin (China). Inst. of Radiation Medicine

1994-02-01

There are three methods: chloramine-T, Iodogen and lactoperoxidase(LPO). [sup 125]I-ACTH, [sup 125]I-insulin and [sup 125]I-HSA are prepared by these techniques. The results show that lactoperoxidase is isolated and purified from fresh milk, meanwhile, the enzyme is used in experiments of [sup 125]I-labeled protein, peptide hormone and mono-clone antibody, etc. LPO is a very successful method for it's mild, complete reaction, controllable, high labelling yield, higher purity of iodine-labeled compound and so on. It remains biological activation and stable character more than other two techniques.

Human Aortic Endothelial Cell Labeling with Positive Contrast Gadolinium Oxide Nanoparticles for Cellular Magnetic Resonance Imaging at 7 Tesla

Directory of Open Access Journals (Sweden)

Yasir Loai

2012-03-01

Full Text Available Positive T1 contrast using gadolinium (Gd contrast agents can potentially improve detection of labeled cells on magnetic resonance imaging (MRI. Recently, gadolinium oxide (Gd2O3 nanoparticles have shown promise as a sensitive T1 agent for cell labeling at clinical field strengths compared to conventional Gd chelates. The objective of this study was to investigate Gado CELLTrack, a commercially available Gd2O3 nanoparticle, for cell labeling and MRI at 7 T. Relaxivity measurements yielded r1 = 4.7 s−1 mM−1 and r2/r1 = 6.2. Human aortic endothelial cells were labeled with Gd2O3 at various concentrations and underwent MRI from 1 to 7 days postlabeling. The magnetic resonance relaxation times T1 and T2 of labeled cell pellets were measured. Cellular contrast agent uptake was quantified by inductively coupled plasma–atomic emission spectroscopy, which showed very high uptake compared to conventional Gd compounds. MRI demonstrated significant positive T1 contrast and stable labeling on cells. Enhancement was optimal at low Gd concentrations, attained in the 0.02 to 0.1 mM incubation concentration range (corresponding cell uptake was 7.26 to 34.1 pg Gd/cell. Cell viability and proliferation were unaffected at the concentrations tested and up to at least 3 days postlabeling. Gd2O3 is a promising sensitive and stable positive contrast agent for cellular MRI at 7 T.

Lyophilized kits of diamino dithiol compounds for labelling with {sup 99m}-technetium. Pharmacokinetics studies and distribution compartmental models of the related complexes; Conjuntos de reativos liofilizados de compostos diaminoditiolicos para marcacao com tecnecio-99m. Estudo farmacocinetico e elaboracao de modelos compartimentalizados dos respectivos complexos

Energy Technology Data Exchange (ETDEWEB)

Araujo, Elaine Bortoleti de

1995-07-01

The present work reflects the clinical interest for labelling diamino dithiol compounds with technetium-99m. Both chosen compounds, L,L-Ethylene dicysteine (L,L-EC) and L,L-Ethylene dicysteine diethyl esther (L,L-ECD) were obtained with relative good yield and characterized by IR and NMR. The study of labelling conditions with technetium-99m showed the influence of the type and mass of reducing agent as well as the pH on the formation of complexes with desired biological characteristics. Radiochemical purity was determined by thin layer chromatography (TLC) and high performance liquid chromatography (HPLC). Lyophilised kits of L,L-EC and L,L-ECD for labelling with {sup 99m}Tc were obtained, with stability superior to 120 days, when stored under refrigeration, enabling the kits marketing. The ideal formulation of the kits as well as the use of liquid nitrogen in the freezing process, determined the lyophilization success. Distribution biological studies of the {sup 99m}Tc complexes were performed on mice by invasive method and on bigger animals by scintigraphic evaluation. Biological distribution studies of the complex {sup 99m}Tc-L,L-EC showed fast blood clearance, with the elimination of about 90% of the administered dose after 60 minutes, almost exclusively by the urinary system. The biological distribution results were adjusted to a three compartmental distribution model, as expected for a radiopharmaceutical designed to renal dynamic studies, with tubular elimination. The complex interaction with renal tubular receptors is related with structural characteristics of the compound, more specifically with the presence and location of polar groups. In comparison with {sup 99m}Tc-L,L-EC, biological studies of the complex {sup 99m}Tc -L,L-ECD showed different distribution aspects, despite some structural similarities. The presence of ethyl groups confers to the complex neutrality and lipophilicity. It cross the intact blood brain barrier and is retained in the brain

Plant-Derived Anti-Inflammatory Compounds: Hopes and Disappointments regarding the Translation of Preclinical Knowledge into Clinical Progress

Directory of Open Access Journals (Sweden)

Robert Fürst

2014-01-01

Full Text Available Many diseases have been described to be associated with inflammatory processes. The currently available anti-inflammatory drug therapy is often not successful or causes intolerable side effects. Thus, new anti-inflammatory substances are still urgently needed. Plants were the first source of remedies in the history of mankind. Since their chemical characterization in the 19th century, herbal bioactive compounds have fueled drug development. Also, nowadays, new plant-derived agents continuously enrich our drug arsenal (e.g., vincristine, galantamine, and artemisinin. The number of new, pharmacologically active herbal ingredients, in particular that of anti-inflammatory compounds, rises continuously. The major obstacle in this field is the translation of preclinical knowledge into evidence-based clinical progress. Human trials of good quality are often missing or, when available, are frequently not suitable to really prove a therapeutical value. This minireview will summarize the current situation of 6 very prominent plant-derived anti-inflammatory compounds: curcumin, colchicine, resveratrol, capsaicin, epigallocatechin-3-gallate (EGCG, and quercetin. We will highlight their clinical potential and/or pinpoint an overestimation. Moreover, we will sum up the planned trials in order to provide insights into the inflammatory disorders that are hypothesized to be beneficially influenced by the compound.

Direct determination of N-methyl-2-pyrrolidone metabolites in urine by HPLC-electrospray ionization-MS/MS using deuterium-labeled compounds as internal standard.

Science.gov (United States)

Suzuki, Yoshihiro; Endo, Yoko; Ogawa, Masanori; Yamamoto, Shinobu; Takeuchi, Akito; Nakagawa, Tomoo; Onda, Nobuhiko

2009-11-01

N-methyl-2-pyrrolidone (NMP) has been used in many industries and biological monitoring of NMP exposure is preferred to atmospheric monitoring in occupational health. We developed an analytical method that did not include solid phase extraction (SPE) but utilized deuterium-labeled compounds as internal standard for high-performance liquid chromatography-electrospray ionization-mass spectrometry using a C30 column. Urinary concentrations of NMP and its known metabolites 5-hydoxy-N-methyl-2-pyrrolidone (5-HNMP), N-methyl-succinimide (MSI), and 2-hydroxy-N-methylsuccinimide (2-HMSI) were determined in a single run. The method provided baseline separation of these compounds. Their limits of detection in 10-fold diluted urine were 0.0001, 0.006, 0.008, and 0.03 mg/L, respectively. Linear calibration covered a biological exposure index (BEI) for urinary concentration. The within-run and total precisions (CV, %) were 5.6% and 9.2% for NMP, 3.4% and 4.2% for 5-HNMP, 3.7% and 6.0% for MSI, and 6.5% and 6.9% for 2-HMSI. The method was evaluated using international external quality assessment samples, and urine samples from workers exposed to NMP in an occupational area.

The effect of catalytic reaction conditions on the incorporation of tritium in unsaturated compounds

Energy Technology Data Exchange (ETDEWEB)

Shevchenko, V P; Nagayev, I Yu; Myasoedov, N F [AN SSSR, Moscow (USSR). Inst. Molekulyarnoj Genetiki

1989-10-01

We have obtained multiple-tritium-labelled 5-{alpha}-androstan-3-one, dihydropicrotoxin, dimethyl-propyl-3-chloro-butyl-ammonium chloride, 2,2-di(trifluoromethyl)-3,3-dicyanobicyclohept(2,2,1)ane, dihydroalprenolol, undecanoic acid, dihydro-m,m'-di-tert.-butyl-p-coumaric acid and dihydrofusicoccin. By varying the conditions for the hydrogenation of terminal double bonds, one can considerably increase the molar radioactivity of such compounds through isotopic exchange. We discuss some tentative explanations of the effect of the labelling reaction conditions upon the synthesis of compounds with desired properties. (author).

The effect of catalytic reaction conditions on the incorporation of tritium in unsaturated compounds

International Nuclear Information System (INIS)

Shevchenko, V.P.; Nagayev, I.Yu.; Myasoedov, N.F.

1989-01-01

We have obtained multiple-tritium-labelled 5-α-androstan-3-one, dihydropicrotoxin, dimethyl-propyl-3-chloro-butyl-ammonium chloride, 2,2-di(trifluoromethyl)-3,3-dicyanobicyclohept[2,2,1]ane, dihydroalprenolol, undecanoic acid, dihydro-m,m'-di-tert.-butyl-p-coumaric acid and dihydrofusicoccin. By varying the conditions for the hydrogenation of terminal double bonds, one can considerably increase the molar radioactivity of such compounds through isotopic exchange. We discuss some tentative explanations of the effect of the labelling reaction conditions upon the synthesis of compounds with desired properties. (author)

Learning classification models with soft-label information.

Science.gov (United States)

Nguyen, Quang; Valizadegan, Hamed; Hauskrecht, Milos

2014-01-01

Learning of classification models in medicine often relies on data labeled by a human expert. Since labeling of clinical data may be time-consuming, finding ways of alleviating the labeling costs is critical for our ability to automatically learn such models. In this paper we propose a new machine learning approach that is able to learn improved binary classification models more efficiently by refining the binary class information in the training phase with soft labels that reflect how strongly the human expert feels about the original class labels. Two types of methods that can learn improved binary classification models from soft labels are proposed. The first relies on probabilistic/numeric labels, the other on ordinal categorical labels. We study and demonstrate the benefits of these methods for learning an alerting model for heparin induced thrombocytopenia. The experiments are conducted on the data of 377 patient instances labeled by three different human experts. The methods are compared using the area under the receiver operating characteristic curve (AUC) score. Our AUC results show that the new approach is capable of learning classification models more efficiently compared to traditional learning methods. The improvement in AUC is most remarkable when the number of examples we learn from is small. A new classification learning framework that lets us learn from auxiliary soft-label information provided by a human expert is a promising new direction for learning classification models from expert labels, reducing the time and cost needed to label data.

Development of [103Pd]-labeled-bis(N4-methylthiosemicarbazone) complexes as possible therapeutic agents

International Nuclear Information System (INIS)

Jalilian, A.R.; Sadeghi, M.; Kamrani, Y.Y.

2006-01-01

Due to interesting tumor seeking properties of bis-thiosemicarbazones, two radio palladium-bis-thiosemicarbazone complexes, i.e., [ 103 Pd]-pyruvaldehyde-bis(N 4 -methylthiosemicarbazone) ([ 103 Pd] PTSM) and [ 103 Pd]-diacetyl-bis(N 4 -methylthiosemicarbazone) ([ 103 Pd]ATSM) were prepared according to the analogy of radio copper homologs. Palladium-103 (t 1/2 = 16.96 d) was produced via the 103 Rh(p, n) 103 Pd nuclear reaction with proton energy 18 MeV. The final activity was eluted in form of Pd(NH 3 ) 2 Cl 2 in order to react with bis-thiosemicarbazones to yield [ 103 Pd]-labeled compounds. Chemical purity of the product was confirmed to be below the accepted limits by polarography. [ 103 Pd]-labeled bis-thiosemicarbazones were prepared with a radiochemical yield of more than 80% at room temperature after 60-90 min by vortexing a mixture of thiosemicarbazones and Pd activity in ethanol. The purification of the labeled compounds performed by reverse phase column chromatography using C 18 plus Sep-Pak. Radiochemical purity of more than 99% specific activity of about 12500-13 000 Ci/mol was obtained. The stability of the complexes was checked in final product and presence of human serum at 37 C up to 48 h. The partition co-efficients of the final complexes were determined. The initial physico-chemical properties of the labeled compounds were compared to those of their copper homologues. (orig.)

Iodine-131 labelled octreotide: not an option for somatostatin receptor therapy

International Nuclear Information System (INIS)

Bakker, W.H.; Breeman, W.A.P.; Pluijm, M.E. van der; Jong, M. de; Visser, T.J.; Krenning, E.P.

1996-01-01

This study deals with the radioiodination of very small amounts of peptide on a therapeutic scale, the required purification procedures after radioiodination, and the influence of high beta fluxes from 131 I on a peptide during radioiodination and purification. Based on the regularly used therapeutic doses of 131 I in cancer treatment and out previous experience with [ 111 In-DTPA-D-Phe 1 ]-octreotide, it was assumed that a minimal effective therapeutic dose of 3.7 GBq 131 I has to be coupled to a maximum of ∼100 μg peptide, representing only a slight excess of peptide over 131 I. This contrasts with non-peptide radiopharmaceuticals in which high compound to radionuclide ratios are usually used. Labelling at low peptide to radionuclide ratios (low labelling yields) results in the formation of di-iodinated compounds, whereas at high peptide to radionuclide ratios mono-iodinated products of low specific activity are formed. Thus, after radioiodination the desired mono-iodinated peptide has to be separated form unreacted iodide, and from di-iodinated and unreacted peptide, as both compounds compete for the receptors. Possible radiolysis of the peptide during labelling and separation steps were investigated by irradiating 30 μg unlabelled peptide with 370 MBq 131 I in a small volume. The peptide composition of the incubation mixtures was investigated by high-performance liquid chromatography after irradiation for 30 min to 24 h. The results showed that the peptide was degraded with a half-life of less than 1 h. During the preparation of a real therapeutic dose (at much higher β-flux) the peptide will be degraded even faster during the various steps required. In conclusion, intact mono-iodinated 131 I-labelled somatostatin analogues for peptide receptor therapy will be difficult to obtain. (orig./VHE)

Use of tritium-labeled PCBs for investigation of PCBs biodegradation by soil bacteria

International Nuclear Information System (INIS)

Kim, A.A.; Djuraeva, G.T.; Takhtobiri, K.S.; Yadgarov, H.T.; Zinovev, P. V.; Abdukarimov, A.A.

2002-01-01

The method for tritium labelling of polychlorinated biphenyls (PCBs) was developed. The strains of soil bacteria - destructors of chloro organic compounds was studied with the help of test-system based on the using of tritium-labeled PCBs. The strains of bacteria were grown on the agar synthetic medium and then were introduced into the synthetic medium containing tritium-labeled mixture of PCBs (commercial mark - SOVOL) as alone source of carbon. The samples were analysed after one and two months period of incubation. PCBs were extracted by hexane from fraction of bacteria and fraction of cultural medium and radioactivity was measured. The samples were analyzed by thin layer chromatography (TLC) with following radioautography. Additionally samples were analyzed by gas chromatography. It was found that all selected strains survived in the medium with PCBs as alone source of carbon and bacteria accumulated PCBs from cultural medium. Accumulation of PCBs by strains of bacteria was different. The TLC analysis detected additional compounds labeled by tritium, that prove the degradation of PCBs in presence of bacteria. The gas chromatography analysis of cultural medium and bacteria detected redistribution in the system and qualitative changes of PCBs in bacteria. The strains of bacteria also were grown in model condition on the soil with tritium labeled PCBs. We found that some strains effectively destroy PCBs with decreasing level of tritium label in the soil. The using of tritium labeled PCBs' allows to introduce precise quantitative characteristics for study of accumulation and biodegradation PCBs by soil bacteria strains. Developed test-system is very useful tool for selection of new strains of soil bacteria - destructors of PCBs

[(64) Cu]-labelled trastuzumab: optimisation of labelling by DOTA and NODAGA conjugation and initial evaluation in mice.

Science.gov (United States)

Schjoeth-Eskesen, Christina; Nielsen, Carsten Haagen; Heissel, Søren; Højrup, Peter; Hansen, Paul Robert; Gillings, Nic; Kjaer, Andreas

2015-05-30

The human epidermal growth factor receptor-2 (HER2) is overexpressed in 20-30% of all breast cancer cases, leading to increased cell proliferation, growth and migration. The monoclonal antibody, trastuzumab, binds to HER2 and is used for treatment of HER2-positive breast cancer. Trastuzumab has previously been labelled with copper-64 by conjugation of a 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator. The aim of this study was to optimise the (64) Cu-labelling of DOTA-trastuzumab and as the first to produce and compare with its 1,4,7-triazacyclononane, 1-glutaric acid-5,7 acetic acid (NODAGA) analogue in a preliminary HER2 tumour mouse model. The chelators were conjugated to trastuzumab using the activated esters DOTA mono-N-hydroxysuccinimide (NHS) and NODAGA-NHS. (64) Cu-labelling of DOTA-trastuzumab was studied by varying the amount of DOTA-trastuzumab used, reaction temperature and time. Full (64) Cu incorporation could be achieved using a minimum of 10-µg DOTA-trastuzumab, but the fastest labelling was obtained after 15 min at room temperature using 25 µg of DOTA-trastuzumab. In comparison, 80% incorporation was achieved for (64) Cu-labelling of NODAGA-trastuzumab. Both [(64) Cu]DOTA-trastuzumab and [(64) Cu]NODAGA-trastuzumab were produced after purification with radiochemical purities of >97%. The tracers were injected into mice with HER2 expressing tumours. The mice were imaged by positron emission tomography and showed high tumour uptake of 3-9% ID/g for both tracers. © 2015 The Authors Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd.

Detection of 2-alkylcyclobutanones by labelling with fluorophene

International Nuclear Information System (INIS)

Moersel, J.T.; Schmiedl, D.

1993-01-01

Radiolysis of triglycerides results in radiolytic formation of 2-alkylcyclobutanone. Identification of such radiolysis products is attractive for both the detection of irradiation treatment of food and for quality assurance of irradiated foods. The authors demonstrated the model compound 2-dodecylcyclobutanone by the key compound 1-bromo-1-ethoxycyclopropane. Detection was effected by labelling the cyclobutanone with suitable fluorescent dies and by tracing them analytically by fluorescence detection using HPLC. 1-Pyrene-butyryl acid hydrazide (P-101) and 7-diethylaminecumarine-3-carbonylazide (D-1446) were used as fluorophores. Suitable model matrices resulted in a sensitive detection of dodecylcyclobutanone. (orig./UHE) [de

Synthetic routes to some isotopically labelled intermediates for diterpenoid biosynthesis

International Nuclear Information System (INIS)

Dawson, R.M.; Godfrey, I.M.; Hogg, R.W.; Knox, J.R.

1989-01-01

The exo-15-hydrogen of ent-kaurene can be exchanged through a reversible ene reaction in a convenient and efficient procedure which has the potential for giving high specific activity 3 H-labelling. Copalol, the (Z)-double bond stereoisomer, and the allylic alcohol isomers ent-manool and ent-epimanool have been obtained through divergent synthetic pathways involving a 15,16-bisnor ketone intermediate. These pathways have also allowed the four compounds to be obtained with 14 C-labelling. A method, involving a Wittig reaction to form a vinyl bromide intermediate, has been developed for obtaining copalol, as the trityl ether derivative, with stereospecific isotopic labelling of one or the other of the hydrogens of the exocyclic methylene group. 27 refs., figs

N-13 labeled amino acids: biodistribution, metabolism and dosimetric considerations

International Nuclear Information System (INIS)

Rosenspire, K.C.; Gelbard, A.S.

1986-01-01

With the growing interest in metabolic imaging and with the increasing number of cyclotron/PET facilities, more studies are being performed in animal and humans using short-lived positron-emitting radionuclides. Amino acids labeled either with N-13 or C-11 are one group of compounds being used to study in vivo regional organ (i.e., brain and heart) or tumor metabolism. Of the studies previously reported using C-11 or N-13 labeled amino acids (methionine, alanine, valine, glutamate, glutamine and tryptophan), imaging was restricted mainly to the organ or tissue of interest with little information obtained about the whole-bode distribution of the label. Such data are important for studying interorgan transport of amino acids and for determining accurate dosimetric measurements after intravenous injection of labeled amino acids. The goals of the authors study were to compare the distribution of several N-13 L-amino acids and N-13 ammonia in tumor-bearing mice and to determine the metabolic fate of the label in vivo. The following amino acids were enzymatically labeled using N-13 ammonia: glutamine, glutamate, methionine, α-aminobutyric acid, valine and leucine. 30 references, 2 figures, 14 tables

Labelling and optimization of PHOTOFRIN registered with 99mTc

International Nuclear Information System (INIS)

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

2010-01-01

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

What Drives Adoption of National Labels as Global Reference Labels? A Case Study With the JPI.

Science.gov (United States)

Yoshida, Shimon; Matsui, Rie; Kikuchi, Chikara

2018-01-01

Pharmaceutical labeling describes the safe and effective use of an approved product. Such information may be provided to consumers and/or health care physicians, and available online or in the pack in a variety of different formats according to local or regional regulations. Depending on the Health Authority (HA), content within a nationally approved label is generally reliant on two primary sources, a Company Core Data Sheet (CCDS), and the text approved by the Health Authority. Content in the nationally approved label may differ from the CCDS for a variety of reasons. In some countries, HAs require the Marketing Authorization Holder (MAH) to base their national label on an already approved label in a "major market" economy, only approving changes to the label when there is evidence that the major market has already approved. In this paper, we examine recent steps taken by the Ministry of Health, Labour and Welfare (MHLW) and Pharmaceuticals and Medical Devices Agency (PMDA) to change labeling regulation in Japan in the context of the recently communicated national strategy, and assess whether this may impact on uptake of the J-PI as a reference label. Decreases in approval times by PMDA for new products, development of basic principles on multiregional clinical trials, greater transparency of content on the PMDA website, and increasing outreach to other Asian Agencies in recent years are highlighted. Labeling harmonization across regions, particularly of safety-related information, represents a key factor in promoting patient safety and risk communication, and is a worthy topic for future ICH consideration.

The synthesis of Org 3770 labelled with 3H, 13C and 14C

International Nuclear Information System (INIS)

Kaspersen, F.M.; Rooij, F.A.M. van; Sperling, E.G.M.; Wieringa, J.H.

1989-01-01

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 3 H (and 2 H), 13 C and 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 3 H 2 . 13 C-labelled material was obtained in a seven-step synthesis starting from 13 C-labelled benzene whereas 14 C-Org 3770 was prepared in a three-step synthesis starting with 14 CO 2 . All labelled compounds were analyzed by TLC, HPLC, MS and NMR. (author)

Abdominal scintigraphy using 99mTc-HMPAO-labelled leucocytes in patients with seronegative spondylarthropathies without clinical evidence of inflammatory bowel disease

International Nuclear Information System (INIS)

Alonso, J.C.; Lopez-Longo, F.J.; Lampreave, J.L.; Gonzalez, C.M.; Vegazo, O.; Carreno, L.; Almoguera, I.

1996-01-01

Abdominal scintigraphy with technetium-99m hexamethylpropylene amine oxime ( 99m Tc-HMPAO)-labelled leucocytes is an excellent tool for evaluating disease extent and activity of intestinal lesions in patients with inflammatory bowel disease (IBD). In some cases of seronegative spondylarthropathies (SSp), IBD may remain subclinical. The aim of this study was to evaluate the presence of positive abdominal scintigraphy in patients with SSp and without clinical symptoms or signs of IBD. To this end we studied 32 patients with active SSp (European Spondylarthropathy Study Group 1991 criteria) without clinical evidence of IBD (eight had ankylosing spondylitis, four psoriatic arthritis, three reactive arthritis an 17 undifferentiated SSp) and 11 controls without SSp. All SSp and control patients received similar doses of non-steroidal anti-inflammatory drugs (NSAIDs). Abdominal scintigraphic images were obtained at 30 and 120 min after re-injection of 99m Tc-HMPAO-labelled leucocytes. The 99m Tc-HMPAO-labelled leucocyte scan was positive in 17 patients with SSp (53.1%) (six with ankylosing spondylitis, three with psoriatic arthritis, two with reactive arthritis and six with undifferentiated SSp). Fourteen patients scored from 2 to 4 on the intensity of uptake scale. The colon and terminal ileum were predominantly involved. Axial involvement was more frequent in patients with a positive scan than in patients with negative results (P 99m Tc-HMPAO-labelled leucocyte scan shows increased uptake among patients with SSp without evidence of IBD. These findings provide new evidence linking SSp with intestinal inflammation and suggest that in some cases a bowel-related process could contribute to the development of SSp. Long-term follow-up studies with more patients are necessary to evaluate the diagnostic and therapeutic implications of these results. (orig.). With 3 figs., 3 tabs

Labeling of creatinine with technetium-99m

Energy Technology Data Exchange (ETDEWEB)

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

2004-07-01

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

The method for production of high purity carrier free ortophosphoric acid labeled with isotopes Phosphorus-32 and Phosphorus-33

International Nuclear Information System (INIS)

Abdukayumov, M.N.; Abdusalyamov, A.N.; Chistyakov, P.G.; Yuldashev, B.S.

2001-01-01

Extensive application for various radioactive isotopes was found in an extremity of the 20-Th century in a science and production. Labeled compounds are used with growing effectiveness in a molecular biology, gene engineering, medicine and other areas. Phosphorus-32 and Phosphorus-33 isotopes as a different labeled compounds that are used mainly in molecular biology are produced at the Radiopreparat enterprise of the Institute of Nuclear Physics of Academy of Sciences of Uzbekistan Republic. The quality of labeled preparations is very high. The specifications for above mentioned preparations corresponds to demands most of customers in different countries. P-32 or P-33 labeled orthophosphoric acid has high radiochemical purity (more than 99 %) and specific radioactivity close to theoretical. Orthophosphoric acid prepared by the described above method has radiochemical purity about 95 % and output of the target product 99%

Carbon transfer in soil - plant system. Molecular labelling utilization for determining rhizosphere compounds

International Nuclear Information System (INIS)

Leguay, J.J.

2000-01-01

The growing up of the bacteria developing in the rhizosphere of plants is dependent on the compounds exudation by plant roots. Even the bacterial genetics use has permitted to identify diverse functions involved in the process of the rhizosphere colonisation ( mobility, heterotrophic bacteria, growing rate, antibiotics production), there is a big delay in vegetal partners. To decrease this delay we tried to characterize the interactions between a plant model, Arabidopsis thaliana and the rhizosphere bacteria. An experimental device has been conceived for measuring the transfer of carbon issued from the photosynthesis to roots and soil. The exudation by roots has been studied. The analysis of rhizospheric compounds in situ pose some methodological problems, especially, the rhizospheric compounds must be extracted from the soil matrix. we suggest an analysis method of rhizospheric compound and of their dynamics. (F.M.)

Effect of comorbid tics on a clinically meaningful response to 8-week open-label trial of fluoxetine in obsessive compulsive disorder.

Science.gov (United States)

Husted, David S; Shapira, Nathan A; Murphy, Tanya K; Mann, Giselle D; Ward, Herbert E; Goodman, Wayne K

2007-01-01

Currently, there are limited published data evaluating the effects of tics on serotonin reuptake inhibitor (SRI) monotherapy responses in treating obsessive-compulsive disorder (OCD). One retrospective case-controlled analysis of OCD patients treated with SRI monotherapy showed lesser improvement in OCD symptoms in patients with tics than those without. However, more recently there were preliminary reports of OCD subjects treated with SRI monotherapy which did not demonstrate poorer response in subjects with tics or Tourette's Syndrome (TS). The specific aim of this study was to investigate whether the presence of comorbid chronic tics affected "clinically meaningful improvement" [McDougle, C.J., Goodman, W.K., Leckman, J.F., Barr, L.C., Heninger, G.R., Price, L.H., 1993. The efficacy of fluvoxamine in obsessive-compulsive disorder: effects of comorbid chronic tic disorder. Journal of Clinical Psychopharmacology 13, 354-358] of OCD in an 8-week open-label trial of fluoxetine monotherapy. Seventy-four adult subjects (13 patients with comorbid chronic tics and 61 patients without tics) with a primary DSM-IV OCD diagnosis were treated with up to 40mg fluoxetine for 8 weeks and had at least one post-baseline evaluation. The results indicate that there was a significant response by time in both fluoxetine-with-tic subjects and fluoxetine-without-tic subjects. Additionally, there were 3 (23.0%) OCD subjects with tics who had clinically meaningful improvement versus 16 (26.2%) OCD subjects without tics that demonstrated similar levels of improvement. These findings indicate that OCD patients with or without chronic tic disorders did not have a differential response to an 8-week open-label trial of fluoxetine. Limitations include the relatively low number of tic subjects and the open-label nature of the study. Additional data are needed on how comorbid tics may affect SRI treatment response in OCD.

Rapid radiochemical methods for preparation of sup(99m)Tc labelled compounds

International Nuclear Information System (INIS)

Narasimhan, D.V.S.; Banodkar, S.M.; Kothari, K.; Mani, R.S.

1981-01-01

Several inorganic and organic compounds incorporating sup( 99 m)Tc are being extensively used for imaging various body organs. The preparation of these sup( 99 m)Tc compounds with the necessary purity requirements is carried out by controlled reduction of sup( 99 m)Tc-pertechnetate using Sn(II) ions as the reducing agent followed by complexation with various active ingredients. The authors here present procedures developed at Radiopharmaceuticals Section of BARC for preparing sup( 99 m)Tc-diphosphonate, sup( 99 m)Tc-glucoheptonate, sup( 99 m)Tc-albumin microspheres and sup( 99 m)Tc-phytate with high radiochemical purity. The paper also describes procedures for the preparation of freeze-dried kits for single step preparation of these compounds. The paper also describes the authors' experience with various analytical procedures for the determination of radiochemical purity of these preparations. (author)

15N-labelled glycine synthesis

International Nuclear Information System (INIS)

Tavares, Claudineia R.O.; Bendassolli, Jose A.; Sant'Ana Filho, Carlos R.; Prestes, Clelber V.; Coelho, Fernando

2006-01-01

This work describes a method for 15 N-isotope-labeled glycine synthesis, as well as details about a recovery line for nitrogen residues. To that effect, amination of α-haloacids was performed, using carboxylic chloroacetic acid and labeled aqueous ammonia ( 15 NH 3 ). Special care was taken to avoid possible 15 NH 3 losses, since its production cost is high. In that respect, although the purchase cost of the 13 N-labeled compound (radioactive) is lower, the stable tracer produced constitutes an important tool for N cycling studies in living organisms, also minimizing labor and environmental hazards, as well as time limitation problems in field studies. The tests were carried out with three replications, and variable 15 NH 3(aq) volumes in the reaction were used (50, 100, and 150 mL), in order to calibrate the best operational condition; glycine masses obtained were 1.7, 2, and 3.2 g, respectively. With the development of a system for 15 NH 3 recovery, it was possible to recover 71, 83, and 87% of the ammonia initially used in the synthesis. With the required adaptations, the same system was used to recover methanol, and 75% of the methanol initially used in the amino acid purification process were recovered. (author)

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

International Nuclear Information System (INIS)

Zhou Xirui; Chen Shaoliang; Chen Guohui; Xu Qinfeng

1993-01-01

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

(/sup 13/N)ammonia in organic solvents; a potent synthetic precursor for /sup 13/N-labeling

Energy Technology Data Exchange (ETDEWEB)

Tominaga, Toshiyoshi; Hirobe, Masaaki; Suzuki, Kazutoshi; Inoue, Osamu; Irie, Toshiaki; Yamasaki, Toshio

1987-01-01

/sup 13/NH/sub 3/ in an organic solvent was prepared and its utility as a labeling precursor was studied. (/sup 13/N)adenine ((/sup 13/N)ADN), (/sup 13/N)nicotinamide ((/sup 13/N)NAM), (/sup 13/N)p-nitrophenyl carbamate ((/sup 13/N)NPC), and (/sup 13/N)L-glutamine ((/sup 13/N)Gln) were labeled utilizing this precursor. (/sup 13/N)ADN and (/sup 13/N)NAM were labeled in much better yields than from an aqueous solution of /sup 13/NH/sub 3/. (/sup 13/N)NPC and (/sup 13/N)Gln, which could not be labeled in an aqueous solution, were labeled in high radiochemical yields. Thus, the advantages of this precursor are the improvement of the labeling yield and the feasibility of labeling compounds unstable in aqueous conditions.

Synthesis of tritium-labelled isopenicillin N, penicillin N and 6-aminopenicillanic acid

International Nuclear Information System (INIS)

Usher, J.J.; Loder, B.; Abraham, E.P.

1975-01-01

1. Phenoxymethylpenicillin sulphoxide 4-methoxybenzyl ester was labelled with 3 H in its 2-β-methyl group. Its specific radioactivity was 362mCi/mmol. 2. Removal of the side chain of this compound yielded the corresponding ester of 6-aminopenicillanic acid sulphoxide and coupling of the latter with the appropriate protected α-aminoadipic acid gave 4-methoxybenzyloxycarbonylisopenicillin N sulphoxide di-4-methoxybenzyl ester or the corresponding derivative of penicillin N. 3. Removal of the protective groups by hydrogenolysis and reduction of the sulphoxide group yielded 3 H-labelled isopenicillin N or penicillin N. 4. 3 H-labelled phenoxymethylpenicillin sulphoxide was obtained by hydrogenolysis from its 4-methoxybenzyl ester. Reducton of its sulphoxide group and subsequent removal of the side chain gave 3 H-labelled 6-aminopenicillanic acid. (author)

Novel inhibitors of HIV discovered among existing classes of pharmaceutical compounds indicated for unrelated clinical indications.

Science.gov (United States)

Kucherov, I I; Rytik, P G; Podol'skaya, I A; Mistryukova, L O; Korjev, M O

2009-01-01

In vitro screening of 307 drugs with various clinical indications (cardiotropic, neurotropic, antibacterial, etc.) has revealed 6 compounds which displayed remarkable antiretroviral activity. Three of these drugs had a tendency to have undesirable side effects and were thus excluded from further consideration. Remaining three, i.e., Xantinol Nicotinate, Tardiferon, and Trental may become valid candidates for inclusion into antiviral regimens such as HAART. In vitro tests have shown that xantinol and trental display synergistic effect with azidothymidine, inhibit the replication AZT-resistant strains of HIV, and have no competing undesirable activities. These compounds should be evaluated in safety studies to determine optimal doses for patients with HIV. If these studies confirm in vitro results these compounds may become valid candidates as safe and affordable means to be added into the arsenal of antiretroviral drugs.

Obtaining of labelled 'Co-101' preparation and study of its pharmacological kinetics

International Nuclear Information System (INIS)

Khujaev, S.; Sultanov, A.; Ganiev, D.A.; Tashmetov, M.; Shermatova, L.; Aliev, Kh.U.; Nazarov, E.A.

2004-01-01

Full text: One of the most actual problems for the last years is the problem of studying physiological role of microelements in animate nature and their use in biological and medical practice. For some time coordination compounds of microelements are used more bots as less toxic and biologically active medical products. Among numerous microelements favorably influencing a number of physiological processes in an organism, special place takes Cobalt. This element differs from others in that it is part of vitamin B 12 (4,5%). Microorganisms for biosynthesis of B 12 in an organism use Cobalt. At lack of vitamin B 12 in an organism, preparations and concentrates of the vitamin B 12 may be used. One of such preparations is the new preparation 'Co-101', synthesized in Tashkent Pharmaceutical Institute. The given preparation is coordination compound of Cobalt with Inozin. In research of the new preparation Co-101', the most modern method - radio indication (a method of labeled compounds) is used. For labeling of the preparation 57 Co and 58 Co radioisotopes are used. Radioisotopes are obtaining in a nuclear reactor ( 58 Co) and on cyclotron ( 57 Co). From the point of radioactive safety, the more favorable appeared to be 57 Co. Two variants of introduction of radioactive Cobalt in chemical structure of a preparation are of considered: 1-by exchange of an isotope, 2- by introduce of radioisotopes Cobalt into asparagine Cobalt at stage of it synthesis, which is an intermediate product during synthesis of preparation 'Co-101'. The second method had been yield with output compound of up 80% and higher. Received labeling preparation has been used for investigation of his own pharmacological kinetics

labelling of some pharmaceutical compounds with radioiodine

International Nuclear Information System (INIS)

Ahmed, N.F.M.

2001-01-01

electrophilic radioiodination of three of medically important compounds namely, pindolol (Pin) , benzamide (s(-)BZM) and lysuride (LIS) was carried out by using several oxidizing agents such as chloramine- T, iodogen, iodine monochloride at room temperature and hydrogen peroxide at 100 0 C. the factors affecting the percent radiochemical yield such as substrate concentration, Ph, oxidizing agent concentration , reaction time and the concentration of K1 carrier were studied. the conditions, which gave high radiochemical yield, were summarized in one reaction to give the optimum radiochemical yield . optimization of the radiochemical yield resulted in 90% for radioiodobenzamide ( * IBZM) when the reaction was carried out in 0.1 M phosphate buffer (Ph-3) or in ammonium acetate buffer (ph=4) for 5 minutes reaction time . A radiochemical yield of 50% of * IPIN was obtained when the reaction was carried out in 0.1 M phosphate buffer (Ph=7) for 30 min. a radiochemical yield of 70% of * ILIS was obtained when the reaction was affected in 0.1 M phosphate buffer (Ph=7) within 30 min reaction time

Evaluation of radiolabeled ruthenium compounds as tumor-localizing agents

International Nuclear Information System (INIS)

Srivastava, S.C.; Richards, P.; Meinken, G.E.; Som, P.; Atkins, H.L.; Larson, S.M.; Grunbaum, Z.; Rasey, J.S.; Clarke, M.H.; Dowling, M.

1979-01-01

This work introduces a new class of radiopharmaceuticals based on ruthenium-97. The excellent physical properties of Ru-97, the high chemical reactivity of Ru, the potential antitumor activity of several Ru coordination compounds, and BLIP production of Ru-97, provide a unique combination for the application of this isotope in nuclear oncology. A systematic study was undertaken on the synthesis, characterization, and evaluation of a number of ruthenium-labeled compounds. In a variety of animal tumor models, several compounds show considerable promise as tumor-localizing agents when compared to gallium-67 citrate. The compounds studied (with Ru in different oxidation states) include ionic Ru, a number of hydrophilic and lipophilic chelates, and various ammine derivatives

Fatty acids labelled in the. omega. -position with iodine isotopes

Energy Technology Data Exchange (ETDEWEB)

Mathieu, J.P.; Busquet, G.; Comet, M. (Universite Scientifique et Medicale de Grenoble, 38 - La Tronche (France)); Riche, F.; Vidal, M. (Laboratoire d' Etudes Dynamiques et Structurales de la Selectivite, 38 - Grenoble (France)); Coornaert, S.; Bardy, A. (CEA, Centre de Saclay, 91 - Gif-sur-Yvette (France)); Godart, J. (Institut des Sciences Nucleaires, 38 - Grenoble (France))

1982-01-01

The synthesis of saturated acetylenic and olefinic (Z or E) ..omega..-iodinated fatty acids has been carried out and their labelling with iodine-131 or 123 by exchange I/sup -/, *I/sup -/ has been studied. The influence of several parameters -water and fatty acid concentrations, specific activity, labelling solution acidity, iodine carrier presence- on this exchange reaction has been noted, enabling experimental conditions to be defined that produce labelling yields of greater than 95%. These results should lead to widespread clinical use of iodine labelled fatty acids.

Chemical method of labelling proteins with the radionuclides of technetium at physiological condition

International Nuclear Information System (INIS)

Wong, D.W.

1983-01-01

A novel rapid chemical method of labeling plasma proteins, other compounds and/or substances containing protein with radionuclides of technetium such as sup(95m)Tc, sup(99m)Tc or sup(99)Tc at physiologic pH 7.4 condition, producing a sterile non-pyrogenic radioactive tracer material suitable for biological and medical uses. These radiolabeled protein substances are not denatured by the labeling process but retain their natural physiological and immunological properties. This novel labeling technique provides a simple and rapid means of labeling plasma proteins such as human serum albumin, fibrinogen, antibodies, hormones and enzymes with sup(95m)Tc or sup(99m)Tc for scintigraphic imaging which may allow visualization of thrombi, emboli, myocardial infarcts, infectious lesions or tumors

Forensic nurses' perceptions of labels of mental illness and personality disorder: clinical versus management issues.

Science.gov (United States)

Mason, T; Hall, R; Caulfied, M; Melling, K

2010-03-01

Anecdotally, forensic psychiatric nurses generally have a more negative perception of people diagnosed with a personality disorder and this negativity is focused more towards managing the behaviours rather than on treatment efficacy and clinical outcomes. This study reports on research carried out across the High, Medium and Low secure psychiatric services in the UK. One thousand two hundred questionnaires were distributed with a response rate of 34.6%. The results indicated a statistically significant difference across High (z = 9.69; P < or = 0.01), Medium (z = 11.06; P < or = 0.01) and Low (z= 9.57; P= 0.01) security with a focus on the management of people with a personality disorder using the Wilcoxon paired samples test. There was also a statistically significant difference in relation to a more clinical/treatment focus for those with a diagnosis of mental illness in Medium (z = 9.69; P < or = 0.01) and Low (z = 9.57; P < or = 0.01) security but not in the High security services. Finally, the results showed significant differences between High, Medium and Low security on each of the four scales of Personality Disorder Clinical-Personality Disorder Management and Mental Illness Clinical-Mental Illness Management. This raises issues of stigma, prejudice and discrimination and suggests a refocus on skills development, acquisition and application for those with a label of personality disorder.

Labeling of monoclonal antibody conjugates with sup 90 Y

Energy Technology Data Exchange (ETDEWEB)

Motta-Hennessy, Cecilia; Sharkey, R.M.; Goldenberg, D.M. (Center for Molecular Medicine and Immunology, Newark, NJ (USA))

1991-01-01

An anti-carcinoembryonic antigen (CEA) antibody, NP-4, was labeled with {sup 90}Y using p-isothiocyanatobenzyl DTPA (SCN-Bz-DTPA) and its derivatives 1-(p-isothiocyanatobenzyl)-3-methyl-DTPA (1B3M), 2-(p-isothiocyanatobenzyl)-4-methyl-DTPA (1M3B), 1-(2)-methyl-4-isothiocyanatobenzyl-DTPA (MX-DTPA) as the chelating agents. The {sup 90}Y conjugates were purified from unbound {sup 90}Y by two different methods, HPLC or acrylamide size exclusion gel chromatography, in order to evaluate the best purification method. Labeling efficiency, reaction kinetics and immunoreactivity were compared to the same antibodies labeled with ({sup 111}In)citrate. Labeling efficiency, as determined by either HPLC or ITLC (instant thin layer chromatography), was consistently higher by ITLC than HPLC for {sup 90}Y-labeled MAb, but equal for {sup 111}In-labeled MAbs. Discrepancies between the 2 methods were linked to impurities in the {sup 90}Y that remained at the origin of ITLC plates. After purification by acrylamide gel filtration, recovery was 50-60% of loaded {sup 90}Y activity, but was more than 87% for the {sup 111}In compounds. Using HPLC, the recovery measured 85% for {sup 90}Y-labeled MAb and more than 93% for {sup 111}In-labeled conjugates. Immunoreactivity of the ({sup 90}Y)MAb was comparable to the {sup 111}In-labeled conjugates. These studies indicate that HPLC purification of the ({sup 90}Y) MAbs improves recovery of activity, and suggests that impurities found in the {sup 90}Y and metal-binding properties of acrylamide may have contributed to the poor recoveries from acrylamide gels. (author).

Diagnostic Labels, Stigma, and Participation in Research Related to Dementia and Mild Cognitive Impairment

Science.gov (United States)

Garand, Linda; Lingler, Jennifer H.; Conner, Kyaien O.; Dew, Mary Amanda

2010-01-01

Health care professionals use diagnostic labels to classify individuals for both treatment and research purposes. Despite their clear benefits, diagnostic labels also serve as cues that activate stigma and stereotypes. Stigma associated with the diagnostic labels of dementia and mild cognitive impairment (MCI) can have a significant and negative impact on interpersonal relationships, interactions with the health care community, attitudes about service utilization, and participation in clinical research. The impact of stigma also extends to the family caregivers of individuals bearing such labels. In this article, we use examples from our investigations of individuals with dementia or MCI and their family caregivers to examine the impact of labeling and stigma on clinical research participation. We also discuss how stigma can affect numerous aspects of the nursing research process. Strategies are presented for addressing stigma-related barriers to participation in clinical research on dementia and MCI. PMID:20077972

Study of the biogenesis of flavones and cinnamic acids by using molecules labelled with carbon 14

International Nuclear Information System (INIS)

Chabannes, Bernard

1970-01-01

This research thesis reports the study of flavones, flavonoid compounds and cinnamic acids which are very common as natural pigments in plant species. The author first reports the study of the synthesis of shikimic acid labelled with carbon 14 (biological methods of preparation, synthesis), and then the synthesis of prunin labelled with carbon 14. The next part reports the study of the transformation of prunin labelled with carbon 14 into cosmosiine in flowers with white cosmos. The author finally compares the introduction of cinnamic acid and of shikimic acid (both labelled with carbon 14) into the sinapic acid of red cabbage leaves

14C-labeled diesel exhaust particles: chemical characteristics and bioavailability studies

International Nuclear Information System (INIS)

Sun, J.D.; Wolff, R.K.; Dutcher, J.S.; Brooks, A.L.

1981-01-01

Little is known about the deposition, retention and biological fate of the organic compounds associated with diesel exhaust particles. In the studies reported here, a one-cylinder diesel engine was operated on diesel fuel spiked with 14 C-benzene, 14 C-hexadecane or 14 C-dotriacontane to generate 14 C-labeled diesel exhaust. Approximately 1% of the exhaust radioactivity was associated with the particulate phase of diesel exhaust. Chemical fractionation of the particle extract showed the 14 C to be present in each of the various chemical class fractions collected. Serum removed approx. 60% of the dichloromethane extractable radioactivity from these diesel particles while saline removed only approx. 6%. This suggested that the organic compounds may be removed from diesel particles in vivo. Future inhalation exposures of rodents to 14 C-labeled diesel exhausts are planned to gain additional information on the health risk of human exposure to diesel exhaust

Method for evaluating the potential of 14C labeled plant polyphenols to cross the blood-brain barrier using accelerator mass spectrometry

International Nuclear Information System (INIS)

Janle, Elsa M.; Lila, Mary Ann; Grannan, Michael; Wood, Lauren; Higgins, Aine; Yousef, Gad G.; Rogers, Randy B.; Kim, Helen; Jackson, George S.; Weaver, Connie M.

2010-01-01

Bioactive compounds in botanicals may be beneficial in preventing age-related neurodegenerative diseases, but for many compounds conventional methods may be inadequate to detect if these compounds cross the blood-brain barrier or to track the pharmacokinetics in the brain. By combining a number of unique technologies it has been possible to utilize the power of AMS to study the pharmacokinetics of bioactive compounds in the brain at very low concentrations. 14 C labeled compounds can be biosynthesized by plant cell suspension cultures co-incubated with radioisotopically-labeled sucrose and isolated and separated into a series of bioactive fractions. To study the pharmacokinetics and tissue distribution of 14 C labeled plant polyphenols, rats were implanted with jugular catheters, subcutaneous ultrafiltration probes and brain microdialysis probes. Labeled fractions were dosed orally. Interstitial fluid (ISF) and brain microdialysate samples were taken in tandem with blood samples. It was often possible to determine 14 C in blood and ISF with a β-counter. However, brain microdialysate samples 14 C levels on the order of 10 7 atoms/sample required AMS technology. The Brain Microdialysate AUC /Serum AUC ranged from .021- to .029, with the higher values for the glycoside fractions. By using AMS in combination with traditional methods, it is possible to study uptake by blood, distribution to ISF and determine the amount of a dose which can reach the brain and follow the pharmacokinetics in the brain.

Use of mixed labelling in kinetic studies of phosphorus metabolism in plants

International Nuclear Information System (INIS)

Hanker, I.

1984-01-01

A modified method of mixed labelling with radionuclides 33 P and 32 P (a modification of ''pulse chase-labelling'') is briefly described. After separation of the different fractions of phosphorus or individual Psub(i)-metabolites and after measurement of their activities, the ratios 32 P/ 33 P (i.e., their relative specific activities, RSA) were determined. The RSA values obtained under suitable experimental conditions yield information on the metabolic turnover of the P-compound or P-fraction under investigation. (author)

Investigation into reaction of heterogenous isotopic exchange with gaseoUs tritium in solution for preparation labelled lipid compounds

International Nuclear Information System (INIS)

Shevchenko, V.P.; Myasoedov, N.F.

1983-01-01

The applicability of the method of heterogeneous catalytic isotopic exchange with gaseous tritium in the solution for the production of labelled lipide preparations is studied. Labelled saturated and unsaturated aliphatic acids, prostaglandins, phospholipides and sphingolipides are prepared

Lymphocyte labelling technique for the exploration of kidney transplants

International Nuclear Information System (INIS)

Guey, A.; Touraine, J.L.; Collard, M.; Claveyrolas, P.; Bouteiller, O. de; Traeger, J.

The labelling technique is developed with a precise clinical exploration in view and has to take into account the following rules or conditions: - the blood sample must be smaller than 20 ml; - the manipulation must not last more than 3 hours; - the immunological properties of the labelled lymphocytes must be kept intact; - the solution reinjected into the patient must contain no aggregates, be absolutely sterile and possess a radioactivity above 1mCi. The technique of extraction and labelling from a sample of about 15ml is described. The main factors responsible for the quality of the labelling are analysed, together with the labelling and irradiation dose effects on certain properties of the lymphocytes (viability, rosette E formation, proliferative response to mitogens) [fr

Carbon dioxide absorbents containing potassium hydroxide produce much larger concentrations of compound A from sevoflurane in clinical practice.

Science.gov (United States)

Yamakage, M; Yamada, S; Chen, X; Iwasaki, S; Tsujiguchi, N; Namiki, A

2000-07-01

We investigated the concentrations of degraded sevoflurane Compound A during low-flow anesthesia with four carbon dioxide (CO(2)) absorbents. The concentrations of Compound A, obtained from the inspiratory limb of the circle system, were measured by using a gas chromatograph. In the groups administered 2 L/min fresh gas flow with 1% sevoflurane, when the conventional CO(2) absorbents, Wakolime(TM) (Wako, Tokyo, Japan) and Drägersorb(TM) (Dräger, Lübeck, Germany), were used, the concentrations of Compound A increased steadily from a baseline to 14.3 ppm (mean) and 13.2 ppm, respectively, at 2 h after exposure to sevoflurane. In contrast, when the other novel types of absorbents containing decreased or no potassium hydroxide/sodium hydroxide, Medisorb(TM) (Datex-Ohmeda, Louisville, CO) and Amsorb(TM) (Armstrong, Coleraine, Northern Ireland), were used, Compound A remained at baseline (potassium hydroxide/sodium hydroxide produce much larger concentrations of Compound A from sevoflurane in clinical practice. An absorbent containing neither potassium hydroxide nor sodium hydroxide produces the smallest concentrations of Compound A.

Comparative Studies on the Radiolabeling and Chromatographic Purification of Some Medically Important Compounds

International Nuclear Information System (INIS)

El-Gizawy, M.A.E.

2013-01-01

The present thesis comprises five basic chapters: The first chapter includes the main idea of our study and its problems, also includes the aim of the work of our study. The second chapter includes the theoretical consideration of the subject. It deals with the general methods of labeling, factors that influence the integrity of labeled compounds, radionuclides used for diagnostic nuclear medicine, production methods and radioactive properties of 123 I, 125 I and 131 I. It includes also the techniques used for the preparation of the radioiodinated compounds especially the electrophilic radioiodination technique. This chapter deals also with the medical imaging, techniques of diagnostic nuclear medicine and the purification of radioiodinated compounds using different chromatographic techniques. Since these radioiodinated compounds are used for diagnosis and therapeutic treatment of human diseases, quality control tests such as determination of chemical purity, radionuclidic purity, radiochemical purity, sterility, pyrogenicity and biodistribution are performed to ensure the purity, the safety and efficiency of these products for the intended nuclear medicine application. The third chapter describes the experimental section; comprising chemicals, reagents, the radionuclides, the equipments and the counting systems used in the study. It describes the electrophilic radioiodination using chloramine-T (CAT), iodogen and lactoperoxidase oxidizing agents and the factors affecting the radiochemical yield of the radioiodination of histamine and L-tyrosine methyl ester such as substrate concentration, ph of the medium, reaction time, temperature and stability of the labeled product. This chapter also includes the techniques used in the Purification of radioiodinated compounds, including paper electrophoresis, thin layer chromatography (TLC), Poly acrylamide-acrylic acid resin [P(AAm-AA) resin] and high performance liquid chromatography (HPLC), in addition, the quality control

Preparation of labelled lipids by the use of plant cell cultures

International Nuclear Information System (INIS)

Mangold, H.K.

1978-01-01

The preparation of some radioacitvely labelled lipids by the use of plant cell cultures is discussed and further applications of the new method are suggested. Cell suspension cultures of rape (Brassica napus) and soya (Glycine max) have been used for the preparation of lipids labelled with radioisotopes. Radioactive acetic acid as well as various long-chain fatty acids are readily incorporated into the neutral and ionic lipids of plant cell cultures. In addition, 14 C-labelled glycerol, ethanolamine and choline are well utilized by the cells. Randomly labelled lipids have been obtained by incubating cell suspension cultures of rape and soya with [1- 14 C] acetic acid, and uniformly labelled lipids have been isolated from cultures that had been incubated with a mixture of [1- 14 C] acetic acid plus [2- 14 C] acetic acid. The use of techniques of plant cell cultures for the preparation of lipds labelled with stable or radioactive isotopesappears particularly rewarding because the uptake of precursors by the cells and their incorporation into various lipid compounds proceeds rapidly and often quanitatively.This new approach should be useful also for the biosynthesis of lipids whose acyl moieties contain a spn radical, a fluorescent group, or a light-sensitive label. Thus, plant cell cultures constitute valuable new tools for the biosynthetic preparation of a great variety of labelled lipids. (A.G.)

Mechanisms and Clinical Application of Tetramethylpyrazine (an Interesting Natural Compound Isolated from Ligusticum Wallichii): Current Status and Perspective.

Science.gov (United States)

Zhao, Yingke; Liu, Yue; Chen, Keji

Tetramethylpyrazine, a natural compound from Ligusticum wallichii ( Chuan Xiong ), has been extensively used in China for cardiovascular and cerebrovascular diseases for about 40 years. Because of its effectiveness in multisystems, especially in cardiovascular, its pharmacological action, clinical application, and the structural modification have attracted broad attention. In this paper its mechanisms of action, the clinical status, and synthetic derivatives will be reviewed briefly.

Photosynthetic carbon metabolism in seagrasses C-labeling evidence for the c(3) pathway.

Science.gov (United States)

Andrews, T J; Abel, K M

1979-04-01

The delta(13)C values of several seagrasses were considerably less negative than those of terrestrial C(3) plants and tended toward those of terrestrial C(4) plants. However, for Thalassia hemprichii (Ehrenb.) Aschers and Halophila spinulosa (R. Br.) Aschers, phosphoglycerate and other C(3) cycle intermediates predominated among the early labeled products of photosynthesis in (14)C-labeled seawater (more than 90% at the earliest times) and the labeling pattern at longer times was brought about by the operation of the C(3) pathway. Malate and aspartate together accounted for only a minor fraction of the total fixed label at all times and the kinetic data of this labeling were not at all consistent with these compounds being early intermediates in seagrass photosynthesis. Pulse-chase (14)C-labeling studies further substantiated these conclusions. Significant labeling of photorespiratory intermediates was observed in all experiments. The kinetics of total fixation of label during some steady-state and pulse-chase experiments suggested that there may be an intermediate pool of inorganic carbon of variable size closely associated with the leaves, either externally or internally. Such a pool may be one cause for the C(4)-like carbon isotope ratios of seagrasses.

Biogenic volatile organic compound and respiratory CO2 emissions after 13C-labeling: online tracing of C translocation dynamics in poplar plants.

Science.gov (United States)

Ghirardo, Andrea; Gutknecht, Jessica; Zimmer, Ina; Brüggemann, Nicolas; Schnitzler, Jörg-Peter

2011-02-28

Globally plants are the primary sink of atmospheric CO(2), but are also the major contributor of a large spectrum of atmospheric reactive hydrocarbons such as terpenes (e.g. isoprene) and other biogenic volatile organic compounds (BVOC). The prediction of plant carbon (C) uptake and atmospheric oxidation capacity are crucial to define the trajectory and consequences of global environmental changes. To achieve this, the biosynthesis of BVOC and the dynamics of C allocation and translocation in both plants and ecosystems are important. We combined tunable diode laser absorption spectrometry (TDLAS) and proton transfer reaction mass spectrometry (PTR-MS) for studying isoprene biosynthesis and following C fluxes within grey poplar (Populus x canescens) saplings. This was achieved by feeding either (13)CO(2) to leaves or (13)C-glucose to shoots via xylem uptake. The translocation of (13)CO(2) from the source to other plant parts could be traced by (13)C-labeled isoprene and respiratory (13)CO(2) emission. In intact plants, assimilated (13)CO(2) was rapidly translocated via the phloem to the roots within 1 hour, with an average phloem transport velocity of 20.3±2.5 cm h(-1). (13)C label was stored in the roots and partially reallocated to the plants' apical part one day after labeling, particularly in the absence of photosynthesis. The daily C loss as BVOC ranged between 1.6% in mature leaves and 7.0% in young leaves. Non-isoprene BVOC accounted under light conditions for half of the BVOC C loss in young leaves and one-third in mature leaves. The C loss as isoprene originated mainly (76-78%) from recently fixed CO(2), to a minor extent from xylem-transported sugars (7-11%) and from photosynthetic intermediates with slower turnover rates (8-11%). We quantified the plants' C loss as respiratory CO(2) and BVOC emissions, allowing in tandem with metabolic analysis to deepen our understanding of ecosystem C flux.

Pyrolysis of Cigarette Ingredients Labelled with Stable Isotopes

Directory of Open Access Journals (Sweden)

Stotesbury S

2014-12-01

mass spectra from the labelled compounds and their natural counterparts, the major degradation products from the labelled compounds could be readily identified in the chromatograms of the corresponding smoke extracts. Evidence of some degradation at above the transfer temperature was indicated for both additives. The amount of degradation was found to be less than 1% for p-anisaldehyde and only 0.1% for vanillin. This low level of degradation was acceptably consistent with the intact transfer values of 97% and 100%, respectively, obtained by pyrolysis.

Clinical evaluation of {sup 99m}Tc-HMPAO labeled leukocyte imaging in ulcerative colitis

Energy Technology Data Exchange (ETDEWEB)

Saitoh, Yasuhiro; Aburano, Tamio; Takashio, Tetsuya; Shuke, Noriyuki; Ayabe, Tokiyoshi; Nomura, Masashi; Kohgo, Yutaka; Ishikawa, Yukio; Satoh, Junichi [Asahikawa Medical Coll., Hokkaido (Japan)

1996-07-01

Inflammatory imaging using {sup 99m}Tc-HMPAO-labeled mixed leukocytes was assessed for use in treating 11 cases diagnosed as ulcerative colitis: 10 cases with total colitis and 1 with left-sided colitis. They consisted of 8 patients with relapse-remitting type and 3 with chronic continuous type. Radionuclide abdominal images were obtained at 1 hr, 4 hr and 24 hr after intravenous injection of 200 MBq prepared {sup 99m}Tc leukocytes. Obvious colonic activity noted at 4 hr served as the basis for positive comparative criterion in the present study. The diagnostic efficacy of radionuclide imaging was compared with endoscopic findings (based on Matts` classification) and the clinical manifestations as reference. The sensitivity and specificity of this imaging were 83.3% and 85.7%, respectively, these values being consistent with endoscopic findings and clinical manifestations at sites of disease activity. All of positive images changed to negative after treatment by leukocyte apheresis or glucocorticoid. Based on these results, {sup 99m}Tc leukocyte imaging can be used to accurately evaluate severity and treatment response in ulcerative colitis. Leukocytes may be closely related to the pathogenesis of ulcerative colitis. (author)

Optimised labeling, preclinical and initial clinical aspects of CCK-2 receptor-targeting with 3 radiolabeled peptides

Energy Technology Data Exchange (ETDEWEB)

Breeman, Wouter A.P. [Department of Nuclear Medicine, Erasmus MC Rotterdam' s 3015 CE Rotterdam (Netherlands)], E-mail: w.a.p.breeman@erasmusmc.nl; Froeberg, A.C.; Blois, E. de; Gameren, A. van; Melis, M.; Jong, M. de [Department of Nuclear Medicine, Erasmus MC Rotterdam' s 3015 CE Rotterdam (Netherlands); Maina, T.; Nock, B.A. [Molecular Radiopharmacy Section, I/R-RP, NCSR ' Demokritos' , Athens (Greece); Erion, J.L. [BioSynthema Inc., St. Louis, MO (United States); Maecke, H.R. [Radiological Chemistry, University Hospital Basel (Switzerland); Krenning, E.P. [Department of Nuclear Medicine, Erasmus MC Rotterdam' s 3015 CE Rotterdam (Netherlands); Department of Internal Medicine, Erasmus MC, Rotterdam (Netherlands)

2008-11-15

Medullary thyroid carcinoma (MTC) expresses CCK-2 receptors. {sup 111}In-labeled DOTA-DGlu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH{sub 2} (DOTA-MG11), DOTA-DAsp-Tyr-Nle-Gly-Trp-Nle-Asp-Phe-NH{sub 2} (DOTA-CCK), and {sup 99m}Tc-labeled N{sub 4}-Gly-DGlu-(Glu){sub 5}-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH{sub 2} ({sup 99m}Tc-Demogastrin 2) are analogs developed for CCK-2 receptor-targeted scintigraphy. All 3 radiolabeled analogs were selected on the basis of their high CCK-2 receptor affinity and their good in vitro serum stability, with in vitro serum t{sub 1/2} values of several hours. Radiolabeling of DOTA-peptides with {sup 111}In requires a heating procedure, typically in the range of 80 deg. - 100 deg. C up to 30 min. Following this procedure with DOTA-MG11 resulted in a >98 % incorporation of {sup 111}In, however, with a radiochemical purity (RCP) of <50 %. The decrease in RCP was found to be due to oxidation of the methionine residue in the molecule. Moreover, this oxidized compound lost its CCK-2 receptor affinity. Therefore, conditions during radiolabeling were optimised: labeling of DOTA-MG11 and DOTA-CCK with {sup 111}In involved 5 min heating at 80 deg. C and led to an incorporation of {sup 111}In of >98 %. In addition, all analogs were radiolabeled in the presence of quenchers to prevent radiolysis and oxidation resulting in a RCP of >90 %. All 3 radiolabeled analogs were i.v. administered to 6 MTC patients: radioactivity cleared rapidly by the kidneys, with no significant differences in the excretion pattern of the 3 radiotracers. All 3 radiolabeled analogs exhibited a low in vivo stability in patients, as revealed during analysis of blood samples, with the respective t{sub 1/2} found in the order of minutes. In patient blood, the rank of radiopeptide in vivo stability was: {sup 99m}Tc-Demogastrin 2 (t{sub 1/2} 10-15 min)>{sup 111}In-DOTA-CCK (t{sub 1/2}{approx}5-10 min)>{sup 111}In-DOTA-MG11 (t{sub 1/2}<5 min)

Cyclotron production of molecules labelled with short-lived radioisotopes β+ emitters (15O, 13N, 11C) and their clinical uses

International Nuclear Information System (INIS)

Bougharouat, B.

1981-01-01

Clinical use of three short-lived radioisotopes: 15 O, 13 N and 11 C is studied on two complementary aspects. A production and purification system is realized; detection instruments in medical use are studied. The production of labelled molecules with the three radiotracers 15 O, 13 N, 11 C from the target bombardment with charged and accelerated particles was studied [fr

A new technique of ion beam tritium labelling

International Nuclear Information System (INIS)

Zhang Nianbao; Sheng Shugang; Yao Fuzeng

1990-01-01

In this paper a new technique is reported for tritium labelling of proteins, peptides and other nonvolatile organic compounds. A tritium ion beam is accelerated to bombard solid sample target for producing tritium exchange with hydrogen. The tritium labelling method has been applied to tritiated soybean trypsin inhibitor, ribonuclease A, elastin, pachyman and others totalled 11. After purifying by dialysis, ion exchange chromatography and gel filtration, the tritiated proteins and polysaccharide were obtained with specific activity over 37 GBq/mmol, without decomposition and with biological activity well preserved. By amino acid analysis of tritiated protein it was shown that the relative specific radioactivities for His., Tyr. and Phe. residues were higher while those for Val., Ile. and Ser. residues were lower

Unpacking Noun-Noun Compounds

DEFF Research Database (Denmark)

Smith, Viktor; Barratt, Daniel; Zlatev, Jordan

2014-01-01

In two complementary experiments we took an integrated approach to a set of tightly interwoven, yet rarely combined questions concerning the spontaneous interpretation of novel (unfamiliar) noun-noun compounds (NNCs) when encountered in isolation, and possible (re)interpretations of novel as well...... concerning the relations between semantics and pragmatics, as well as system and usage, and psycholinguistic issues concerning the processing of NNCs. New insights and methodological tools are also provided for supporting future best practices in the field of food naming and labelling...

The labeling of kanamycin using radionuclide of technetium as an agent for early detection of infectious deseases

International Nuclear Information System (INIS)

Widyasari, E.; Zainuddin, M.N.; Nuraeni, W.

2013-01-01

Infectious diseases are still the leading cause of death in the world. Early detection and determination of the exact location of infection and accurate imaging through the use of nuclear techniques can facilitate treatment. Antibiotics radioactive labeled compound otherwise be able to be a solution to distinguish between infective and non-infective inflammatory. Kanamycin is an antibiotic used for the treatment of infections where other drugs such as penicillin and several other drugs that are less potent infection can not be used. This study aims to determine the optimum labeling conditions of 99m Tc-kanamycin in order to obtain high labeling efficiency. Kanamycin has successfully labeled with technetium-99m through indirect labeling method using pyrophosphate as a co-ligand. Labeling efficiency and determination of radiochemical purity of these compounds simultaneously determined by ascending paper chromatography using Whatman paper 3 as the stationary phase, and acetone as the mobile phase to separate the radiochemical impurities in the form of 99m Tc-pertechnetate; while impurities in the form of reduced 99m Tc-separated by using the stationary phase ITLC-SG and 0.5 N NaOH as mobile phase. The result showed that the optimal labeling conditions was obtained on the use of 6 mg kanamycin, 300 mg SnCl2, 1.5 mg of Na-pyrophosphate, and pH = 6. The incubation time of 0-30 min at room temperature, provide labeling efficiency of 96.54 ± 0.36%. The successful of kanamycin labeling with high efficiency makes 99m Tc-kanamycin potentially to be used as a radiopharmaceutical for the early detection of infectious diseases. (author)

A novel facile method of labeling octreotide with (18)F-fluorine.

Science.gov (United States)

Laverman, Peter; McBride, William J; Sharkey, Robert M; Eek, Annemarie; Joosten, Lieke; Oyen, Wim J G; Goldenberg, David M; Boerman, Otto C

2010-03-01

-IMP466 was stable in vivo, because bone uptake was only 0.4 +/- 0.2 %ID/g, whereas free Al(18)F accumulated rapidly in the bone (36.9 +/- 5.0 %ID/g at 2 h after injection). Small-animal PET/CT scans showed excellent tumor delineation and high preferential accumulation in the tumor. NOTA-octreotide could be labeled rapidly and efficiently with (18)F using a 2-step, 1-pot method. The compound was stable in vivo and showed rapid accretion in somatostatin receptor subtype 2-expressing AR42J tumors in nude mice. This method can be used to label other NOTA-conjugated compounds with (18)F.

A facile method for steroid labeling by heavy isotopes of hydrogen

Czech Academy of Sciences Publication Activity Database

Marek, Aleš; Klepetářová, Blanka; Elbert, Tomáš

2015-01-01

Roč. 71, č. 29 (2015), s. 4874-4882 ISSN 0040-4020 R&D Projects: GA AV ČR IAA400550801 Institutional support: RVO:61388963 Keywords : brassinosteroids * alpha-hydroxy ketones * reductive dehalogenation * tritium * labeled compounds Subject RIV: CC - Organic Chemistry Impact factor: 2.645, year: 2015

Analysis of S-35 labeled WR-2721 and its metabolites in biological fluids

International Nuclear Information System (INIS)

Anderson, K.W.; Krohn, K.A.; Grunbaum, Z.; Phillips, R.B.; Mahler, P.A.; Menard, T.W.; Spence, A.M.; Rasey, J.S.

1984-01-01

Studies with WR-2721 and related compounds have been hindered by the lack of a suitable assay for the drug and its major metabolites. A chromatographic method which requires no derivation for the separation and detection of WR-2721, the free thiol, its symmetrical disulfide and other mixed disulfides has been developed. The procedure involves ion-pairing for separation of ionizable compounds by causing polar molecules to become more lipophilic and hence separable using reverse phase HPLC. Detection is based upon liquid scintillation counting of S-35 incorporated during the synthesis of the parent compound. This method requires no pre-column preparation of samples and, by detecting the S-35 label, eliminates the chance that a coeluting species could interfere with detection, as might occur with post-column derivatization. This analytical technique employing radiotracers can be used to study radioprotective mechanisms by time dependent measurements of the tissue distribution and chemical form of labeled drug. Such chemical information can then be correlated with biological measures of radiation protection

Laboratory of radioisotopes of IOCB ASCR - recent results of labeling by 3H and 125I

Czech Academy of Sciences Publication Activity Database

Elbert, Tomáš; Veselá, Iva

2009-01-01

Roč. 52, 7/8 (2009), s. 253-254 ISSN 0362-4803. [15th Workshop of the International Isotope Society - Central European Division: The synthesis and applications of isotopes and isotopically labelled compounds. 12.06.2009-13.06.2008, Bad Soden] Institutional research plan: CEZ:AV0Z40550506 Keywords : tritium * 125-I labeled peptides Subject RIV: CC - Organic Chemistry

Abcess detection using radiocolloid-labelled-leukocytes

International Nuclear Information System (INIS)

Simon, J.; Auvergnat, J.C.; Armengaud, M.; Guiraud, R.; Le Net, R.; Auvergnat, R.

1975-01-01

The early detection of infections centres using labelled polynuclear neutrophile (LPN) as vector was investigated. The method was based on one of the physiological properties of this substance, its phagocytotic power towards colloidal sulphur particles labelled with pertechnetate-Tc 99m. The preliminary results of experiments on dogs are reported and confirm that centres of infection can be determined in experimental animals by the use of polynuclear neutrophiles labelled by phagocytosis. It seems that these results are really due to the presence of LPN in situ and not to simple inflammatory hyperhaemia or to an excess of free pertechnetate. The nature of the vector, tracer and lebelling agent, the quality of the results obtained and the harmlessness of the method warrant its clinical application in human beings [fr

Technique of leukocyte harvesting and labeling: problems and perspectives

International Nuclear Information System (INIS)

McAfee, J.G.; Subramanian, G.; Gagne, G.

1984-01-01

Mixed leukocyte suspensions obtained after gravity sedimentation of red cells and labeled with 111 In lipophilic chelates are now widely used clinically for abscess localization at many medical centers. So far, labeling with 111 In-oxine or tropolone has been more successful than any 99 mTc method. More sophisticated approaches are available for isolation and labeling of specific leukocyte cell types, to study their migration in vivo. The most significant advances in cell harvesting include newer density gradients for isopyknic centrifugation, centrifugal elutriation, and flow cytometry. Unlike current radioactive agents which label many cell types indiscriminately, more selective ligands are being developed which bind to specific cell surface receptors. These will label certain leukocyte populations or subtypes while not reacting with others, thereby avoiding laborious separation techniques. Monoclonal antibodies against leukocyte cell-surface antigens appear particularly promising as agents for selective cell labeling

Identification of novel candidate compounds targeting TrkB to induce apoptosis in neuroblastoma

International Nuclear Information System (INIS)

Nakamura, Yohko; Suganami, Akiko; Fukuda, Mayu; Hasan, Md Kamrul; Yokochi, Tomoki; Takatori, Atsushi; Satoh, Shunpei; Hoshino, Tyuji; Tamura, Yutaka; Nakagawara, Akira

2014-01-01

Neuroblastoma (NB) is one of the most frequent solid tumors in children and its prognosis is still poor. The neurotrophin receptor TrkB and its ligand brain-derived neurotrophic factor (BDNF) are expressed at high levels in high-risk NBs and are involved in defining the poor prognosis of the patients. However, the TrkB targeting therapy has never been realized in the clinic. We performed an in silico screening procedure utilizing an AutoDock/grid computing technology in order to identify novel small chemical compounds targeting the BDNF-binding domain of TrkB. For the first screening, a library of three million synthetic compounds was screened in silico and was ranked according to the Docking energy. The top-ranked 37 compounds were further functionally screened for cytotoxicity by using NB cell lines. We have finally identified seven compounds that kill NB cells with the IC 50 values of 0.07–4.6 μmol/L. The terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay showed that these molecules induce apoptosis accompanied by p53 activation in NB cell lines. The candidate compounds and BDNF demonstrated an antagonistic effect on cell growth, invasion, and colony formation, possibly suggesting competition at the BDNF-binding site of TrkB. The candidate compounds had tumor-suppressive activity in xenograft and in vivo toxicity tests (oral and intravenous administrations) using mice, and did not show any abnormal signs. Using in silico Docking screening we have found new candidate TrkB inhibitors against high-risk NBs, which could lead to new anti-cancer drugs

Dissipation kinetics of asparagine in soil measured by compound-specific analysis with metabolite tracking

DEFF Research Database (Denmark)

Czaban, Weronika; Rasmussen, Jim; Nicolaisen, Mogens

2016-01-01

labeled glutamic acid were detected in soil. This highlights the fast turnover of amino acid in soil and that the estimation of concentration of the formed compounds is important when evaluating plant available organic N. Efficiency of the compound-specific analysis showed to be a powerful technique......Estimating the potential for direct plant acquisition of organic N, in particular amino acids, requires assessment of their turnover times in soil. It is well known from 14C studies that mineralization of amino acids occurs within hours, but mineralization to 14CO2 does not indicate the rate...... of disappearance of the intact amino acid or the possible formation of metabolites during amino acid dissipation. We here used compound-specific isotope analysis with metabolite tracking to investigate the dissipation rate of universally labeled intact 13C15N-asparagine at two concentrations and the subsequent...

No-carrier-added labeling of the neuroprotective Ebselen with selenium-73 and selenium-75.

Science.gov (United States)

Helfer, Andreas; Ermert, Johannes; Humpert, Sven; Coenen, Heinz H

2015-03-01

Selenium-73 is a positron emitting non-standard radionuclide, which is suitable for positron emission tomography. A copper-catalyzed reaction allowed no-carrier-added labeling of the anti-inflammatory seleno-organic compound Ebselen with (73) Se and (75) Se under addition of sulfur carrier in a one-step reaction. The new authentically labeled radioselenium molecule is thus available for preclinical evaluation and positron emission tomography studies. Copyright © 2015 John Wiley & Sons, Ltd.

Development and labeling of EP-00652218 analogues, NK1 receptors antagonist, for PET and SPECT imaging

International Nuclear Information System (INIS)

Bagot-Gueret, C.

2001-12-01

The aim of this work was the synthesis and radiosynthesis of compounds labelled either with a positron emitter (fluorine-18, t 1/2 = 109 minutes) or with a gamma emitter (iodine-123, t 1/2 = 16.2 hours), for Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) studies. EP-00652218 is a novel potent antagonist, with a sub-nano-molar affinity towards the NK 1 receptors. In order to develop ligands that could be used either in PET or SPECT, we undertook the synthesis of poly-halogenated analogues of EP-00652218. Compound 17 was synthesized through two different synthetic pathways. A series of original compounds has been obtained from compound 17 by halogen exchanges on the naphthyridone or the benzene ring. These molecules were tested to determine their in vitro affinity towards NK 1 receptors. Compound 21 was labelled with fluorine-18 in 135 minutes and with a 20% radiochemical yield. Compound 26 was radioiodinated following reaction with Na 125 I (t 1/2 = 60.14 days) in a 18% radiochemical yield. Despite expectation, these analogues of EP-00652218 exhibited an insufficient affinity for NK 1 receptors (IC 50 = 10 -7 M) and thus unlikely usable for in vivo studies with PET and SPECT. (author)

Synthesis of 14C-labelled butoxyethoxyethanol

International Nuclear Information System (INIS)

Thijssen, J.B.A.; Janssen, C.G.M.; Verluyten, W.L.M.; Heykants, J.J.P.

1986-01-01

Butoxyethoxyethanol, an organic solvent used as carrier in the levamisole pour-on formulation, was synthesized via a Makosza etherification of 1- 14 C-labelled bromobutane with mono tetrahydropyranyl (T.H.P.) protected diethylene glycol and subsequent removal of the T.H.P. protecting group. The compounds' synthetic yield was 88.8%; it had a specific activity of 32.5 mCi/mmol. The reaction product was radiochemically pure (99.6%) according to high-performance liquid chromatography and thin-layer chromatography in three solvent systems. (author)

Potential Negative Effects of Antimicrobial Allergy Labelling on Patient Care: A Systematic Review.

Science.gov (United States)

Wu, Julie Hui-Chih; Langford, Bradley J; Schwartz, Kevin L; Zvonar, Rosemary; Raybardhan, Sumit; Leung, Valerie; Garber, Gary

2018-01-01

Antimicrobial allergy labels, either self-reported or placed in a patient's medical record, are common, but in many cases they are not associated with a true immunoglobulin E-mediated allergic response. To assess the impact of antimicrobial allergy labels on antimicrobial prescribing, resource utilization, and clinical outcomes. The MEDLINE, Embase, CINAHL, and Scopus electronic databases were searched for the period 1990 to January 2016. Controlled studies with the objective of assessing antimicrobial prescribing, resource utilization, and/or clinical outcomes associated with antimicrobial allergy labels were included. The search identified 560 unique citations, of which 7 articles met the inclusion criteria. One additional article identified by an expert in the field was also included. Four of the identified papers were limited to penicillin or other β-lactam allergies. Six studies noted differences in antibiotic selection between patients with allergy labels and those without such labels. Broader-spectrum or second-line agents (e.g., vancomycin, clindamycin, and fluoroquinolones) were more commonly prescribed for patients with penicillin allergy labels. Antibiotic therapy costs were significantly higher for patients with allergy labels than for those without. The impact of allergy labels on clinical outcomes was mixed. One study indicated a longer length of hospital stay, 2 studies reported higher readmission rates, and 1 study reported a higher rate of antibiotic-resistant organisms for patients with allergy labels. Most of the available literature is limited to penicillin or β-lactam allergy. The growing body of knowledge supports the concept that β-lactam allergy labels are not benign and that labelling in the absence of a true allergy has a negative effect on patient care. Allergy labelling appears to be associated with suboptimal antibiotic selection, greater treatment costs, prolonged length of stay, greater readmission rates, and higher prevalence of

Chemical Composition and Labeling of Substances Marketed as Selective Androgen Receptor Modulators and Sold via the Internet.

Science.gov (United States)

Van Wagoner, Ryan M; Eichner, Amy; Bhasin, Shalender; Deuster, Patricia A; Eichner, Daniel

2017-11-28

Recent reports have described the increasing use of nonsteroidal selective androgen receptor modulators, which have not been approved by the US Food and Drug Administration (FDA), to enhance appearance and performance. The composition and purity of such products is not known. To determine the chemical identity and the amounts of ingredients in dietary supplements and products marketed and sold through the internet as selective androgen receptor modulators and compare the analyzed contents with product labels. Web-based searches were performed from February 18, 2016, to March 25, 2016, using the Google search engine on the Chrome and Internet Explorer web browsers to identify suppliers selling selective androgen receptor modulators. The products were purchased and the identities of the compounds and their amounts were determined from April to August 2016 using chain-of-custody and World Anti-Doping Association-approved analytical procedures. Analytical findings were compared against the label information. Products marketed and sold as selective androgen receptor modulators. Chemical identities and the amount of ingredients in each product marketed and sold as selective androgen receptor modulators. Among 44 products marketed and sold as selective androgen receptor modulators, only 23 (52%) contained 1 or more selective androgen receptor modulators (Ostarine, LGD-4033, or Andarine). An additional 17 products (39%) contained another unapproved drug, including the growth hormone secretagogue ibutamoren, the peroxisome proliferator-activated receptor-δ agonist GW501516, and the Rev-ErbA agonist SR9009. Of the 44 tested products, no active compound was detected in 4 (9%) and substances not listed on the label were contained in 11 (25%). In only 18 of the 44 products (41%), the amount of active compound in the product matched that listed on the label. The amount of the compounds listed on the label differed substantially from that found by analysis in 26 of 44 products

Synthesis of Novel C-2- or C-15-Labeled BODIPY—Estrone Conjugates

Directory of Open Access Journals (Sweden)

Ildikó Bacsa

2018-04-01

Full Text Available Novel BODIPY–estrone conjugates were synthesized via Cu(I-catalyzed azide–alkyne cycloaddition (CuAAC. Estrone-alkynes or an estrone-azide as starting compounds were synthesized via Michael addition or Sonogashira reaction as key steps. Fluorescent dyes based on BODIPY-core were provided by azide or alkyne functional groups. Fluorescent labeling of estrone was efficiently achieved at the C-2 or C-15 position. The newly-elaborated coupling procedures might have a broad applicability in the synthesis of fluorescent-labeled estrone conjugates suitable for biological assays.

Synthesis of carbon-14-labeled sodium palmoxirate and its coenzyme A ester

Energy Technology Data Exchange (ETDEWEB)

Weaner, L.E.; Hoerr, D.C.

1986-04-01

Synthetic procedures for the preparation of carbon-14-labeled sodium palmoxirate (TDGA), labeled either in the carboxyl position or in the tetradecyl hydrocarbon chain, are described. In addition, the synthesis of the coenzyme A ester of TDGA-14C with a specific activity of 51 mCi/mmol is reported. The coenzyme A ester was prepared by formation of the acyl chloride with oxalyl chloride followed by reaction with coenzyme A (CoA) in a borate-buffered tetrahydrofuran solution. Purification methods and analytical and stability data are reported for the compounds.

Recent progress in fluorine-18 labelled peptide radiopharmaceuticals

Energy Technology Data Exchange (ETDEWEB)

Okarvi, S.M. [Cyclotron and Radiopharmaceuticals Department, King Faisal Specialist Hospital and Research Centre, Riyadh (Saudi Arabia)

2001-07-01

The application of biologically active peptides labelled with positron-emitting nuclides has emerged as a useful and interesting field in nuclear medicine. Small synthetic receptor-binding peptides are currently the preferred agents over proteins and antibodies for diagnostic imaging of various tumours. Due to the smaller size of peptides, both higher target-to-background ratios and rapid blood clearance can often be achieved with radiolabelled peptides. Hence, short-lived positron emission tomography (PET) isotopes are potential candidates for labelling peptides. Among a number of positron-emitting nuclides, fluorine-18 appears to be the best candidate for labelling bioactive peptides by virtue of its favourable physical and nuclear characteristics. The major disadvantage of labelling peptides with {sup 18}F is the laborious and time-consuming preparation of the {sup 18}F labelling agents. In recent years, various techniques have been developed which allow efficient labelling of peptides with {sup 18}F without affecting their receptor-binding properties. Moreover, the development of a variety of prosthetic groups has facilitated the efficient and site-specific labelling of peptides with {sup 18}F. The {sup 18}F-labelled peptides hold enormous clinical potential owing to their ability to quantitatively detect and characterise a wide variety of human diseases when using PET. Recently, a number of {sup 18}F-labelled bioactive peptides have shown great promise as diagnostic imaging agents. This review presents the recent developments in {sup 18}F-labelled biologically active peptides used in PET. (orig.)

Recent progress in fluorine-18 labelled peptide radiopharmaceuticals

International Nuclear Information System (INIS)

Okarvi, S.M.

2001-01-01

The application of biologically active peptides labelled with positron-emitting nuclides has emerged as a useful and interesting field in nuclear medicine. Small synthetic receptor-binding peptides are currently the preferred agents over proteins and antibodies for diagnostic imaging of various tumours. Due to the smaller size of peptides, both higher target-to-background ratios and rapid blood clearance can often be achieved with radiolabelled peptides. Hence, short-lived positron emission tomography (PET) isotopes are potential candidates for labelling peptides. Among a number of positron-emitting nuclides, fluorine-18 appears to be the best candidate for labelling bioactive peptides by virtue of its favourable physical and nuclear characteristics. The major disadvantage of labelling peptides with 18 F is the laborious and time-consuming preparation of the 18 F labelling agents. In recent years, various techniques have been developed which allow efficient labelling of peptides with 18 F without affecting their receptor-binding properties. Moreover, the development of a variety of prosthetic groups has facilitated the efficient and site-specific labelling of peptides with 18 F. The 18 F-labelled peptides hold enormous clinical potential owing to their ability to quantitatively detect and characterise a wide variety of human diseases when using PET. Recently, a number of 18 F-labelled bioactive peptides have shown great promise as diagnostic imaging agents. This review presents the recent developments in 18 F-labelled biologically active peptides used in PET. (orig.)

Off-Label Uses of Omalizumab.

Science.gov (United States)

El-Qutob, David

2016-02-01

The off-label use of medicines is a common and extensive clinical practice. Omalizumab has been licensed for use in severe allergic asthma and chronic urticaria. Omalizumab dosing was based on body weight and baseline serum IgE concentration. All patients are required to have a baseline IgE between 30 and 700 IU/ml and body weight not more than 150 kg. The use of off-label drugs may lead to several problems including adverse effects and an increased risk/benefit balance. In this article, there are summarized off-label uses of omalizumab in the last recent years in diseases in which IgE maybe or certainly has a corner role such as allergic rhinitis, allergic bronchopulmonary aspergillosis, anaphylaxis, keratoconjunctivitis, food allergy, drug allergy, urticaria, angioedema, non-atopic asthma, atopic dermatitis, nasal polyps, Churg-Strauss syndrome, eosinophilic otitis media, chronic rhinosinusitis, bullous pemphigoid, contact dermatitis, and others. Use in pregnancy asthmatic women and pre-co-administration with specific immunotherapy will also be revised.

Metabolic and improved organ scan studies. II. Nitrogen-13 labeled compounds used as in-vivo probes for enzyme therapy and as tumor localizing and organ imaging agents

International Nuclear Information System (INIS)

Anon.

1976-01-01

A number of 13 N-labeled compounds have been enzymatically synthesized and are being evaluated as tumor and/or organ localizing agents. 13 N-Ammonia, produced after cyclotron generation of 13 N-nitrate and subsequent reduction was used to enzymatically aminate the appropriate substrate to yield 13 N-L-glutamic acid, L-glutamine, L-asparagine, L-valine, L-leucine and L-alanine. The use of 13 N-asparagine as a myocardial scanning agent and as a tumor localizing agent in asparaginase-sensitive tumors is discussed. Two imaging devices were used to study the effectiveness of the compounds as localizing agents. For static whole body distribution studies, a dual-detector high energy gamma ray (HEG) rectilinear scanner, equipped with constant response collimators was employed. The uniformity of response of this system permits quantitative determination of the amount of 13 N activity present in the organ or tumor of interest. The total organ kinetic imaging monitor (TOKIM) gamma camera system was used for dynamic studies covering smaller areas of the subject's body

Co-Labeling for Multi-View Weakly Labeled Learning.

Science.gov (United States)

Xu, Xinxing; Li, Wen; Xu, Dong; Tsang, Ivor W

2016-06-01

It is often expensive and time consuming to collect labeled training samples in many real-world applications. To reduce human effort on annotating training samples, many machine learning techniques (e.g., semi-supervised learning (SSL), multi-instance learning (MIL), etc.) have been studied to exploit weakly labeled training samples. Meanwhile, when the training data is represented with multiple types of features, many multi-view learning methods have shown that classifiers trained on different views can help each other to better utilize the unlabeled training samples for the SSL task. In this paper, we study a new learning problem called multi-view weakly labeled learning, in which we aim to develop a unified approach to learn robust classifiers by effectively utilizing different types of weakly labeled multi-view data from a broad range of tasks including SSL, MIL and relative outlier detection (ROD). We propose an effective approach called co-labeling to solve the multi-view weakly labeled learning problem. Specifically, we model the learning problem on each view as a weakly labeled learning problem, which aims to learn an optimal classifier from a set of pseudo-label vectors generated by using the classifiers trained from other views. Unlike traditional co-training approaches using a single pseudo-label vector for training each classifier, our co-labeling approach explores different strategies to utilize the predictions from different views, biases and iterations for generating the pseudo-label vectors, making our approach more robust for real-world applications. Moreover, to further improve the weakly labeled learning on each view, we also exploit the inherent group structure in the pseudo-label vectors generated from different strategies, which leads to a new multi-layer multiple kernel learning problem. Promising results for text-based image retrieval on the NUS-WIDE dataset as well as news classification and text categorization on several real-world multi

Identification of Agents Active against Methicillin-Resistant Staphylococcus aureus USA300 from a Clinical Compound Library

Directory of Open Access Journals (Sweden)

Hongxia Niu

2017-09-01

Full Text Available Methicillin-resistant Staphylococcus aureus (MRSA poses a significant threat for effective treatment of several difficult-to-treat infections in humans. To identify potential new treatment options for MRSA infections, we screened a clinical compound library consisting of 1524 compounds using a growth inhibition assay in 96-well plates. We identified 34 agents which are either bacteriostatic or bactericidal against log-phase clinical MRSA strain USA300. Among them, 9 candidates (thonzonium, cetylpyridinium, trilocarban, benzododecinium, bithionol, brilliant green, chlorquinaldol, methylbenzethonium and green violet are known antiseptics, 11 candidates are known antibiotics currently recommended for the treatment of MRSA. We identified 9 new drug candidates, 5 of which (thiostrepton, carbomycin, spiramycin, clofazimine and chloroxine are antibiotics used for treating other infections than S. aureus infections; 4 of which (quinaldine blue, closantel, dithiazanine iodide and pyrvinium pamoate are drugs used for treating parasitic diseases or cancer. We ranked these new drug candidates according to their MICs against the MRSA strain USA300. Our findings may have implications for more effective treatment of MRSA infections.

Metabolism of tritium- and carbon-14-labeled tiamulin in dogs, rats, and pigs.

Science.gov (United States)

Dreyfuss, J; Singhvi, S M; Shaw, J M; Egli, P; Ross, J J; Czok, R; Nefzger-Biessels, M; Battig, F; Schuster, I; Schmook, F

1979-05-01

The metabolism of tiamulin hydrogen fumarate, labeled with 3H, 14C, or both, was studied in dogs, rats, and weanling pigs. After a dose of radiolabeled tiamulin, all three species excreted more radioactivity in feces (via bile) than in urine. Dogs absorbed 86% of a single oral dose of tiamulin-3H, and the disposition of the compound was similar after a single or multiple dosage regimen. The ratio of antimicrobial activity to total radioactivity in dog plasma was only about 0.25, and was still less in dog urine. After dosing with tiamulin-14C, rats and pigs excreted at least 1% of the dose as 14CO2 in expired air. In dual-labeled studies, pigs excreted less total 14C than 3H and had greater residues of 14C than 3H in edible tissues, blood, and plasma. After the administration of tiamulin-14C to pigs, radioactivity was incorporated into liver glycogen, indicating metabolic cleavage of the side chain of tiamulin. Tiamulin-3H is the isotopically-labeled compound of choice for studying metabolism and tissue residues in animals.

DMAP-BODIPY alkynes: a convenient tool for labeling biomolecules for bimodal PET-optical imaging.

Science.gov (United States)

Brizet, Bertrand; Goncalves, Victor; Bernhard, Claire; Harvey, Pierre D; Denat, Franck; Goze, Christine

2014-09-26

Several new boron dipyrromethene/N,N-dimethylaminopyridine (BODIPY-DMAP) assemblies were synthesized as precursors for bimodal imaging probes (optical imaging, OI/positron emission tomography, PET). The photophysical properties of the new compounds were also studied. The first proof-of-concept was obtained with the preparation of several new BODIPY-labeled bombesins and evaluation of the affinity for bombesin receptors by using a competition binding assay. Fluorination reactions were investigated on DMAP-BODIPY precursors as well as on DMAP-BODIPY-labeled bombesins. Chemical modifications on the BODIPY core were also performed to obtain luminescent dyes emitting in the therapeutic window (650-900 nm), suitable for in vivo imaging, making these compounds promising precursors for PET/optical dual-modality imaging agents. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Isolation of 14C labelled amino acids by biosynthesis in maize plants (Zea mais L.)

International Nuclear Information System (INIS)

Carreras, N.; Mazon, M.P.

1983-01-01

A method of obtaining 14 C labelled amino acids by biosynthesis in maize plants which had assimilated 14CO 2 , has been assayed. The plants were labelled for 60 minutes with 14 C O2 produced from Ba 14 C O3 (specific activity of 148 KBq/μmol). An extract of the soluble compounds was obtained with 80% ethanol and the amino acids were separated from the rest of the soluble compounds by ion exchange chromatography on column of Dowex 50-X8 resin. Finally, seventeen amino acids were isolated and identified from the purified extract. The acid amino acids were separated in anionic column (Dowex 1-X8) and the neutral and basic amino acids in cationic column (Dowex 50-X4). (Author) 56 refs

Isolation of carbon 14 labelled amino acids by biosynthesis in maize plants (zea mais L.)

International Nuclear Information System (INIS)

Carreras, N.; Mazon, M.P.

1983-01-01

A method of obtaining 14 C labelled amino acids by biosynthesis in maize plants which had assimilated 14 CO 2 , has been assayed. The plants were labelled for 60 minutes with 14 CO 2 produced from Ba 14 CO 3 (specific activity of 148 KBq/μmol). An extract of the soluble compounds was obtained with 80% ethanol and the amino acids were separated from the rest of the soluble compounds by ion exchange chromatography on column of Dowex 50-X8 resin. Finally, seventeen amino acids were isolated and identified from the purified extract. The acid amino acids were separated in anionic column (Dowex 1-X8) and the neutral and basic amino acids in cationic columns (Dowex 50-X4). (author)

Clinical efficacy of puerarin combined with compound ammonium glycyrrhetate S in treatment of alcoholic hepatitis

Directory of Open Access Journals (Sweden)

JI Huichun

2014-10-01

Full Text Available ObjectiveTo investigate the clinical efficacy of puerarin combined with compound ammonium glycyrrhetate S in the treatment of alcoholic hepatitis. MethodsA total of 92 patients with alcoholic hepatitis who were admitted to our hospital from February 2011 to February 2014 were recruited in this study and randomly divided into two groups. The control group (n=46 was treated with conventional therapy combined with compound ammonium glycyrrhetate S. The test group (n=46 was treated with puerarin in addition to the regimen used in the control group. After 20 days of treatment, the levels of total bilirubin (TBil, alanine aminotransferase (ALT, aspartate aminotransferase (AST, glutamyl transpeptidase (GGT, albumin (Alb, Glasgow alcoholic hepatitis score (GAHS, and abdominal ultrasound were measured and compared with the results before the treatment in both groups. The clinical efficacy and adverse reactions in the two groups were also compared. ResultsAfter the treatment, the GAHSs and levels of TBil, ALT, AST, and GGT in the two groups were all significantly lower than those before the treatment (all P＜0.05. In the test group after the treatment, the levels of TBil (20.96±6.85 μmol/L, ALT (33.72±14.18 U/L, and AST (38.69±6.38 U/L were all significantly lower than those in the control group (all P＜0.05. The marked response rate, overall response rate, and rate of improvement in abdominal ultrasound in the test group were 63.04%, 93.48%, and 44.44%, respectively, all significantly higher than those in the control group (all P＜0.05. There was no significant difference in adverse reactions between the two groups (P＞0.05. ConclusionFor patients with alcoholic hepatitis, the combined therapy with puerarin and compound ammonium glycyrrhetate S can improve the treatment outcome and protect the liver function, and it has high safety and holds promise for clinical application.

Selenium-75-labeled sucralfate: comparison with other radiolabels and initial clinical studies

International Nuclear Information System (INIS)

Knight, L.C.; Maurer, A.H.; Kollmann, M.; Ammar, I.A.; Fisher, R.S.; Malmud, L.S.

1988-01-01

Sucralfate was synthesized to include a 75 Se label, then compared with 111 In-sucralfate and /sup 99m/Tc-Human serum albumin (HSA)-sucralfate in vitro and in an animal ulcer model. The 75 Se label was the only one of the three that was stable in both human gastric juice and simulated intestinal fluid in vitro. In rats with gastric ulcers, ulcer:nonulcer ratios of bound radioactivity averaged 15.4, 6.3, and 5.6 for 75 Se, 111 In, and /sup 99m/Tc-HSA labels, respectively. Biodistribution studies of 75 Se-sucralfate indicated that little is absorbed from the gastrointestinal tract, and the distribution is similar to that of 14 C-sucralfate. Selective binding of 75 Se sucralfate was successfully imaged in patients with esophagitis (esophageal mean T1/2 binding = 65 +/- 32 min), gastritis (gastric mean T 1/2 binding = 118 +/- 34 min), and gastric ulcers (ulcer mean T 1/2 binding = 135 +/- 59 min). Duodenal ulcers were not successfully imaged. Normal subjects showed no abnormal localization of sucralfate, and esophageal and gastric clearances were rapid

Pharmacotherapy of alcoholism - an update on approved and off-label medications.

Science.gov (United States)

Soyka, Michael; Müller, Christian A

2017-08-01

Only a few medications are available for the treatment of alcohol use disorders (AUDs). Areas covered: This paper discusses approved AUD medications, including the opioid antagonists naltrexone and nalmefene (the latter is licensed for reduction of alcohol consumption only), the putative glutamate receptor antagonist acamprosate and the aldehyde dehydrogenase inhibitor disulfiram. It also covers off-label medications of interest, including topiramate, gabapentin, ondansetron, varenicline, baclofen, sodium oxybate and antidepressants. Clinical implications, benefits and risks of treatment are discussed. Expert opinion: Acamprosate, naltrexone, nalmefene and disulfiram are the only approved 'alcohol-specific' drugs. Acamprosate and naltrexone have been evaluated in numerous clinical trials and represent evidence-based treatments in AUDs. Nalmefene use, however, is controversial. Supervised disulfiram is a second-line treatment approach. Compounds developed and licensed for different neuropsychiatric disorders are potential alternatives. Encouraging results have been reported for topiramate, gabapentin and also varenicline, which might be useful in patients with comorbid nicotine dependence. The GABA (γ-aminobutyric acid)-B receptor agonist baclofen has shown mixed results; it is currently licensed for the treatment of AUDs in France only. Gabapentin may be close to approval in the USA. Further studies of these novel treatment approaches in AUDs are needed.

Labeling of antibiotics for infection diagnosis

International Nuclear Information System (INIS)

Benitez, A.; Roca, M.; Martin-Comin, J.

2006-01-01

The high impact of infection on daily clinical practice has promoted research into better and more accurate diagnostic and therapeutic methods. Localizing inflammation/infection with nuclear medicine techniques began over 40 years ago. Today, 6 7G a-scintigraphy, 9 9mT c-nanocolloid, 1 11I n and 9 9mT c in vitro labeled leukocytes, and monoclonal anti granulocyte antibodies are widely available for this purpose. While these methods are useful for localizing inflammation, they cannot always differentiate septic from aseptic processes. The ideal properties of an agent for diagnosing infection include: high specificity, early diagnosis, rapid blood clearance, ease of preparation, low toxicity, biodistribution appropriate for the disease under study, absence of immunologic response and low cost. A novel approach to infection diagnosis is the use of radiolabelled antibiotics. Antibiotics localize in the infectious focus, where they are frequently taken up and metabolized by microorganisms. The majority of the various antibiotics studied so far are those of the quinolones group (ciprofloxacin, sparfloxacin, enrofloxacin, levofloxacin, norfloxacin and ofloxacin). More recently, the labeling of ceftizoxime, a semisynthetic third generation cephalosporin, has been reported. The relevant features of labeled antibiotics in research and/or clinical infection diagnosis are the focus of this article

Maximum likelihood pixel labeling using a spatially variant finite mixture model

International Nuclear Information System (INIS)

Gopal, S.S.; Hebert, T.J.

1996-01-01

We propose a spatially-variant mixture model for pixel labeling. Based on this spatially-variant mixture model we derive an expectation maximization algorithm for maximum likelihood estimation of the pixel labels. While most algorithms using mixture models entail the subsequent use of a Bayes classifier for pixel labeling, the proposed algorithm yields maximum likelihood estimates of the labels themselves and results in unambiguous pixel labels. The proposed algorithm is fast, robust, easy to implement, flexible in that it can be applied to any arbitrary image data where the number of classes is known and, most importantly, obviates the need for an explicit labeling rule. The algorithm is evaluated both quantitatively and qualitatively on simulated data and on clinical magnetic resonance images of the human brain

Synthesis of selectively 13C-labelled benzoic acid for nuclear magnetic resonance spectroscopic measurement of glycine conjugation activity

International Nuclear Information System (INIS)

Akira, Kazuki; Hasegawa, Hiroshi; Baba, Shigeo

1995-01-01

The synthesis of [4- 13 C]benzoic acid (BA) labelled in a single protonated carbon, for use as a probe to measure glycine conjugation activity by nuclear magnetic resonance (NMR) spectroscopy, has been reported. The labelled compound was prepared by a seven-step synthetic scheme on a relatively small scale using [2- 13 C] acetone as the source of label in overall yield of 16%. The usefulness of [4- 13 C]BA was demonstrated by the NMR spectroscopic monitoring of urinary excretion of [4- 13 C]hippuric acid in the rat administered with the labelled BA. (Author)

32P-labeling test for DNA damage

International Nuclear Information System (INIS)

Randerath, K.; Reddy, M.V.; Gupta, R.C.

1981-01-01

Covalent adducts formed by the reaction of DNA with chemical carcinogens and mutagens may be detected by a 32 P-labeling test. DNA preparations exposed to chemicals known to bind covalently to DNA [N-methyl-N-nitrosourea, dimethyl sulfate, formaldehyde, β-propiolactone, propylene oxide, streptozotocin, nitrogen mustard, and 1,3-bis(2-chloroethyl)-1-nitrosourea] were digested to a mixture of deoxynucleoside 3'-monophosphates by incubation with micrococcal endonuclease (EC 3.1.31.1) and spleen exonuclease (EC 3.1.16.1). The digests were treated with [γ- 32 P]ATP and T4 polynucleotide kinase (ATP:5'-dephosphopolynucleotide 5'-phosphotransferase, EC 2.7.1.78) to convert the monophosphates to 5'- 32 P-labeled deoxynucleoside 3',5'-bis-phosphates. These compounds were then separated on polyethyl-eneimine-cellulose thin layers in ammonium formate and ammonium sulfate solutions. Autoradiograms of the chromatograms obtained by this high-resolution procedure showed the presence of nucleotides derived from chemically altered, as well as normal, DNA constituents. Maps from DNA exposed to any of the chemicals used exhibited a spot pattern typical for the particular chemical. This method detected a single adduct in 10 5 DNA nucleotides without requiring that the compound under investigation be radioactive and thus provides a useful test to screen chemicals for their capacity to damage DNA by covalent binding

Determination of the isotope distribution in 14C-labelled hydrocarbons by thermal fragmentation

International Nuclear Information System (INIS)

Kopinke, F.D.; Dermietzel, J.; Jockisch, W.; Raeuber, G.

1986-01-01

The gas chromatographic analysis of pyrolysis products of properly labelled hydrocarbons allows a definite and quantitative determination of the 14 C-distribution in those compounds. For this purpose a simple, fast, and versatilely applicable method has been developed and described

Studies on 14C labelled chlorpyrifos in model marine ecosystem

International Nuclear Information System (INIS)

Pandit, G.G.; Mohan Rao, A.M.; Kale, S.P.; Murthy, N.B.K.; Raghu, K.

1997-01-01

Chlorpyrifos is one of the widely used organophosphorus insecticides in tropical countries. Experiments were conducted with 14 C labelled chlorpyrifos to study the distribution of this compound in model marine ecosystem. Less than 50 per cent of the applied activity remained in water in 24 h. Major portion of the applied chlorpyrifos (about 4.2 % residue per g) accumulated into the clams with sediment containing a maximum of 5 to 6 per cent of applied compound. No degradation of chlorpyrifos was observed in water or sediment samples. However, metabolic products were formed in clams. (author). 4 refs., 3 tabs

A new technique for ion beam tritium labelling

International Nuclear Information System (INIS)

Zhang Nianbao; Sheng Shugang; Yao Fuzeng

1990-06-01

An advanced technique, the ion beam tritium labelling method (IBTL), used for labelling proteins, peptides and other nonvolatile organic compounds is introduced. In this method the excited tritium ion beam is accelerated and then bombs a solid sample target in which tritium exchanging for hydrogen is taken place. The IBTL has been used for preparation of tritiated soybean trypsin inhibitor, ribonuclease A, elastin and pachyman etc. After purifing by dialysis, ion exchange chromatography and gel filtration, the tritiated proteins and polysaccharide were obtained with the specific activity over 37 GBq/mmol, the function of tritiated decomposition products was not found. The product was shown to have native biological activity. Amino acid analysis of tritiated protein showed that the relative specific radioactivities were higher for His., Tyr. and Phe. but lower for Val., Ile. and Ser

Tritium labelling of testosteron by selective hydrogenation of dihydrotestosteron

International Nuclear Information System (INIS)

Postolache, Cristian; Matei, Lidia; Simion, Elena; Barna, Catalina; Condac, Eduard

2002-01-01

Elemental tritium is obtained during the decontamination process of the moderator from Cernavoda Nuclear Power Plant. It might be stocked for use in controlled fusion, in a relatively far future, or, it might be immediately used as raw material in the synthesis of labelled compounds with important economic value. Labelling of testosteron with tritium was necessary for the carrying out of radiometric and molecular biology studies concerning androgen dependent diseases. Testosteron was labelled by selective hydrogenation of 1,2 dihydrotestosteron acetate. The forerunner was synthesized in two steps: 1) esterification of testosteron using acetic anhydride, and 2) selective dehydrogenation with 2,6-dichloro-3,5-dicyan-1,4 quinone (DDQ) of the ester formed in the first step. Testosteron acetate was synthesized and purified with yields of 73%, and 80%, respectively. The dehydrogenation process was characterized by yields of 82% for synthesis and 33% for purification. The tritium labelled hormone was obtained in two steps: 1) selective hydrogenation of Δ 1 - testosteron acetate in the presence of T 2 gas, at low pressure, and 2) hydrolysis of the ester at basic pH. The raw product obtained was purified by preparative thin layer chromatography. The physical and chemical characterization of labelled testosteron reveals a radiochemical purity higher than 98% and a specific activity of 53.4 Ci/mmol. (authors)

β-CIT labelled with 131I and its preliminary clinical practice

International Nuclear Information System (INIS)

Ye Bin; Kuang Anren; Ding Hao; Zheng Hongbo; Yuan Qiang; He Li

2002-01-01

β-CIT is labelled with 131 I by the peracetic acid method. 4 normal controls, 8 patients with PD and 3 patients with PS are studied by 131 I-β-CIT SPECT imaging. Striatal specific uptake of 131 I-β-CIT is calculated by the radioactivity ratio of striatal to cerebellar. The results shows that the radiochemical purity of 131 I-β-CIT is (97.6 +- 0.3)%. 131 I-β-CIT remains stable for at least 4 h after incubated with waters and serum respectively. The striatal specific uptake of 131 I-β-CIT in normal controls, PD and PS patients are (4.39 +- 0.14)%, (2.95 +- 0.68)% and (3.96 +- 0.52)% at 4h and (6.60 +- 0.06)%, (3.85 +- 0.71)% and (6.14 +- 0.08)% at 20 h after administration. There is a significant reduction of striatal tracer uptake in PD patients compared to the controls and PS patients. Striatal specific uptake in contralateral to the clinical symptom side is more pronounced reduced than the ipsilateral side in PD patients. 131 I-β-CIT uptake in PD patients is correlated with disease severity. These results suggest that 131 I-β-CIT can be used for the diagnosis of Parkinsion's disease

Distribution of nitrogen-13 from labeled nitrate (13NO3-) in humans and rats

International Nuclear Information System (INIS)

Witter, J.P.; Gatley, S.J.; Balish, E.

1979-01-01

The body distribution of gavaged or intravenously administered nitrate labeled with nitrogen-13 was studied in humans and rats with the following results: (1) the labeled compound is not quickly absorbed from the stomach; (2) the concentration of the label increases inside the lower intestinal tract (cecum and large intestine) when ingested or intravenously injected; and (3) humans and rats have the capacity to store a portion of the label in their bodies. These observations indicate that depletion of body stores, the passage of nitrate down the gut, or the secretion of nitrate into the intestinal lumen may be a better explanation of the urinary, ileal, and fecal concentrations of nitrate and nitrate recently measured in humans than a bacterial nitrification reaction in the intestines, as suggested by Tannenbaum, et al

Spin labelled nitrosoureas and triazenes and their non-labelled clinically used analogues--a comparative study on their physicochemical properties and antimelanomic effects.

Science.gov (United States)

Zheleva, A M; Gadjeva, V G

2001-01-16

Physicochemical properties, such as half life time (tau0.5), alkylating and carbamoylating activity and in vivo antimelanomic effects against B16 melanoma of spin labeled (containing nitroxyl free radical moiety) amino acid nitrosoureas, synthesized in our laboratory, have been studied and compared to those of the antitumor drug N'-cyclohexyl-N-(2-chloroethyl)-N-nitrosourea (lomustine, CCNU). We have shown that the introduction of amino acid moieties and the replacement of cyclohexylamine with nitroxyl moiety leads to a faster decomposition, higher alkylating, lower carbamoylating activity, better antimelanomic activity and lower general toxicity, when compared to those of CCNU. It was also established that spin labeled triazenes, previously synthesized by us, were more stable in phosphate saline than their nonlabeled analogue, 5-(3,3-dimethyltriazene-1-yl)-imidazole-4-carboxamide (dacarbazine, DTIC). A higher cytotoxicity to B16 melanoma cells than to YAC-1 and lymphocytes was demonstrated for all spin labeled triazenes, in comparison with DTIC. An assumption has been made to explain the lower general toxicity of the spin labeled nitrosoureas compared to that of CCNU. Based on the results presented, we accept that a new trend for synthesis of more selective and less toxic nitrosourea and triazene derivatives as potential antimelanomic drugs might be developed.

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

Energy Technology Data Exchange (ETDEWEB)

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

1986-10-25

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

Off-label drug in the newborn

Directory of Open Access Journals (Sweden)

Laura Cuzzolin

2014-06-01

Full Text Available The lack of specific drugs and labelling recommendations for the neonatal population is a long-standing problem throughout the world. With the introduction of the Paediatric Regulation in 2007, in Europe tangible steps have been made to increase clinical research in children, but only a limited number of clinical trials included neonates that remain therapeutic orphans. This leads to a widespread use of medicines outside the terms indicated in the product license (off-label as regards dose, route of administration, indication, age group or in an unlicensed manner (formulations modified, extemporaneous preparations, imported medicines, chemicals used as drugs. This use, often made on the basis of a consolidated clinical experience in absence of other authorized options, does not imply that a drug is contraindicated or disapproved, but simply means that insufficient data are available to grant approval status and the risks and benefits of using a drug in a particular situation have not been examined. Given the importance that neonatal population not be denied of drugs that are clearly beneficial, an updated overview of the worldwide situation of off-label and unlicensed drug use in the newborn will be presented, by analyzing also the impact of recent legislative initiatives and the well recognized problems (increased risk of ineffective or toxic treatments, adverse drug reactions and medication errors. Proceedings of the 10th International Workshop on Neonatology · Cagliari (Italy · October 22nd-25th, 2014 · The last ten years, the next ten years in Neonatology Guest Editors: Vassilios Fanos, Michele Mussap, Gavino Faa, Apostolos Papageorgiou

Development of a kit for RBC labelling with 99mTc and its clinic evaluation

International Nuclear Information System (INIS)

Marafuschi, A.M.; Nowotny, G.A.; Palcos, M.C.; Rotta, M. del C.

1980-01-01

A kit for labelling red blood cells (RBC) with 99m Tc based on a Tin Pyrophosphate mixture freeze-dried and a saline solution saturated with nitrogen has been prepared for spleen and placenta scanning, circulatory studies and blood volume determinations. The stannous tin is intended to reduce the 99m Tc pertechnetate, obtained either from generators or from solvent extraction, to the appropriate valence state suitable for labelling. The technique is as follows: Add to the heparinized blood sample the Tin-Pyrophosphate mixture dissolved in the saline solution. After five minutes incubation time at room temperature the plasma is discarded by centrifugation. Following the addition of the tracer activity to the separated RBC, the supernatant is discarded after a second centrifugation. Depending on the test to be performed, the RBC are either resuspended in saline solution for blood pool or circulation studies or denaturalized at 49.5 deg C for spleen scanning. The labelling yield (95-88%) and its stability has been checked by in vitro measurements, up to four hours after labelling. The biological distribution and spleen uptake have been determined in rats and rabbits. The developed method proved to be adequate for labelling RBC with good labelling retention. An interesting application is shown in babies with congenital cardiac defects and suspected absence of the spleen, where the scan gave a good image of the existing spleen. (author) [es

Iodine-123-labeled pH shift brain-imaging agents

International Nuclear Information System (INIS)

Blau, M.; Kung, H.F.

1985-01-01

HIPDM is an 123 I-labeled agent with a distribution in brain reflecting regional perfusion. This compound is neutral and lipid soluble at blood pH and freely crosses the blood-brain barrier. At the lower pH in brain, it picks up a hydrogen ion and becomes positively charged. In this form the molecule is not lipid soluble and it is trapped in brain

Alpha radioisotopes Ac-225 and Bi-213: a production and labelling of antibodies and peptides for clinical use

Energy Technology Data Exchange (ETDEWEB)

Bruchertseifer, Frank, E-mail: frank.bruchertseifer@ec.europa.eu [European Commission, Joint Research Centre, Karlsruhe (Germany)

2017-07-01

Full text: In various preclinical and clinical works the potential of the alpha emitters {sup 225}Ac and {sup 213}Bi as therapeutic radionuclides for application in targeted alpha therapy of cancer and infectious diseases was demonstrated. Both alpha emitters are available with high specific activity from established radionuclide generators. Their favorable chemical and physical properties have led to the conduction of a large number of preclinical studies and several clinical trials, demonstrating the feasibility, safety and therapeutic efficacy of targeted alpha therapy with {sup 225}Ac and {sup 213}Bi. This presentation will give an overview about the methods for the production of {sup 225}Ac and {sup 213}Bi, the {sup 225}Ac/{sup 213}Bi radionuclide generator systems, labelling of peptides and antibodies with {sup 225}Ac and {sup 213}Bi and relevant in vivo and in vitro works. (author)

A semi-supervised approach using label propagation to support citation screening.

Science.gov (United States)

Kontonatsios, Georgios; Brockmeier, Austin J; Przybyła, Piotr; McNaught, John; Mu, Tingting; Goulermas, John Y; Ananiadou, Sophia

2017-08-01

Citation screening, an integral process within systematic reviews that identifies citations relevant to the underlying research question, is a time-consuming and resource-intensive task. During the screening task, analysts manually assign a label to each citation, to designate whether a citation is eligible for inclusion in the review. Recently, several studies have explored the use of active learning in text classification to reduce the human workload involved in the screening task. However, existing approaches require a significant amount of manually labelled citations for the text classification to achieve a robust performance. In this paper, we propose a semi-supervised method that identifies relevant citations as early as possible in the screening process by exploiting the pairwise similarities between labelled and unlabelled citations to improve the classification performance without additional manual labelling effort. Our approach is based on the hypothesis that similar citations share the same label (e.g., if one citation should be included, then other similar citations should be included also). To calculate the similarity between labelled and unlabelled citations we investigate two different feature spaces, namely a bag-of-words and a spectral embedding based on the bag-of-words. The semi-supervised method propagates the classification codes of manually labelled citations to neighbouring unlabelled citations in the feature space. The automatically labelled citations are combined with the manually labelled citations to form an augmented training set. For evaluation purposes, we apply our method to reviews from clinical and public health. The results show that our semi-supervised method with label propagation achieves statistically significant improvements over two state-of-the-art active learning approaches across both clinical and public health reviews. Copyright © 2017 The Authors. Published by Elsevier Inc. All rights reserved.

Label Review Training: Module 1: Label Basics, Page 21

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. Learn about types of labels.

Stability of rhenium-188 labeled antibody

International Nuclear Information System (INIS)

Lim, B. K.; Jung, J. M.; Jung, J. K.; Lee, D. S.; Lee, M. C.

1999-01-01

For clinical application of beta-emitter labeled antibody, high specific activity is important. Carrier-free Re-188 from W-188/Re-188 generator is an ideal radionuclide for this purpose. However, low stability of Re-188 labeled antibody, especially in high specific activity, due to radiolytic decomposition by high energy (2.1 MeV) beta ray was problem. We studied the stability of Re-188 labeled antibody, and stabilizing effect of several nontoxic radical-quenching agents. Pre-reduced monoclonal antibody (CEA79.4) was labeled with Re-188 by incubating with generator-eluted Re-188-perrhenate in the presence of stannous tartrate for 2 hr at room temperature. Radiochemical purity of each preparation was determined by chromatography (ITLC-SG/acetone, ITLC-SG/Umezawa, Whatman No.1/saline). Human serum albumin was added to the labeled antibodies(2%). Stability of Re-188-CEA79.4 was investigated in the presence of vitamin C, ethanol, or Tween 80 as radical-quenching agents. Specific activities of 4.29∼5.11 MBq/μg were obtained. Labeling efficiencies were 88±4%(n=12). Very low stability after removal of stannous tartrate from the preparation was observed. If stored after purging with N 2 , all the preparations were stable for 10 hr. However, if contacted with air, stability decreased. Perrhenate and Re-188-tartrate was major impurity in declined preparation (12∼47 and 9∼38% each, after 10 hr). Colloid-formation was not a significant problem in all cases. Addition of vitamin C stabilized the labeled antibodies either under N 2 or under air by reducing the formation of perrhenate. High specific activity Re-188 labeled antibody is unstable, especially, in the presence of oxygen. Addition of vitamin C increased the stability

Label Review Training: Module 1: Label Basics, Page 22

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. Learn about what labels require review.

Label Review Training: Module 1: Label Basics, Page 19

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. This section covers supplemental distributor labeling.

Liver and kidney imaging with Ga-68-labeled dihydroxyanthraquinones

International Nuclear Information System (INIS)

Schuhmacher, J.; Maier-Borst, W.; Wellman, H.N.

1980-01-01

This paper describes the preparation of alizarin (1,2-dihydroxyanthraquinone) and alizarin red S (sodium 1,2-dihydroxyanthraquinone-3-sulfonate) labeled with Ga-68, which is obtained from a new high-yield Ge-68 → Ga-68 generator. The uptake of Ga-68 alizarin by liver and spleen RES was studied in rats, dogs, and humans, and amounted to 80 to 85% of the administered dose within 5 min after i.v. injection. Gallium-68 alizarin red S was preferentially accumulated in the renal parenchyma to an extent of 70% within 2 hr after i.v. administration. Complete labeling of 1 mCi Ga-68 was achieved by 100 μg of each compound, amounts that are without any known measurable harm to humans

Comparative analysis of four active compounds of Baikal skullcap and its classical TCM prescriptions according to different clinical curative effects

Directory of Open Access Journals (Sweden)

Guang-Wei Zhu

2017-05-01

Full Text Available Objective: A sensitive HPLC-DAD detection method was established for the comparative analysis of the four active compounds (including baicalin, baicalein, wogonoside and wogonin of Baikal Skullcap and its classical TCM prescriptions according to different clinical curative effects. And analyze the relationship between compatibility of medicines, content and clinical curative effect.

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.

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

International Nuclear Information System (INIS)

Lee, J. H.; Ji, D. Y.; Moon, B. S.; Lee, T. S.; Lee, D. H.; Lee, K. C.; Ahn, G. I.; Yang, S. D.; Choi, C. W.; Jun, K. S.

2005-01-01

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 μL, 100-200 mCi), in the presence of peracetic acid (40 μL) 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

Label Review Training: Module 1: Label Basics, Page 15

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. Learn about the consequences of improper labeling.

Label Review Training: Module 1: Label Basics, Page 14

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. Learn about positive effects from proper labeling.

Label Review Training: Module 1: Label Basics, Page 18

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. This section discusses the types of labels.

Label Review Training: Module 1: Label Basics, Page 26

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. Learn about mandatory and advisory label statements.

Studies of 99mTc-BnAO (HL-91): a non-nitroaromatic compound for hypoxic cell detection

International Nuclear Information System (INIS)

Zhang, X.; Melo, T.; Ballinger, J.R.; Rauth, A.M.

1998-01-01

Purpose: Solid tumours of similar type and stage can vary widely in their hypoxic cell fraction. Such cells may be prognostic for aggressive, metastatic, and radiation-resistant disease. A 99m technetium ( 99m Tc)-labelled non-nitroaromatic agent, butyleneamine oxime ( 99m Tc-BnAO) or HL-91 (Amersham International, Inc., Amersham, UK) has been evaluated both in vitro and in vivo for its possible efficacy as a noninvasive marker for the clinical detection of hypoxic cells in solid tumours. Materials and Methods: Suspension cultures of Chinese hamster ovary (CHO) cells under controlled levels of oxygen were used to measure the oxygen dependency of 99m Tc-BnAO accumulation. V79 cells grown as multilayers on a semipermeable membrane served as an in vitro model for drug penetration through the extravascular space of the tumour. C3H mice bearing KHT-C leg tumours were the in vivo models for selective drug accumulation as a function of time after i.v. administration of 99m Tc-BnAO. Results: 99m Tc accumulated selectively in hypoxic vs. aerobic cells, resulting in a 9 ± 2-fold differential in radioactivity per cell at 4 h. The k m for this selective accumulation was 20 ppm of oxygen. The labelled drug was equally effective in penetrating the cellular multilayer under aerobic or hypoxic conditions. In vivo measurements indicated favourable labelling of solid tumours containing hypoxic cells with 1% of the total activity per g of tumour, a tumour-to-blood ratio of 1.2, and a tumour-to-muscle ratio of 4.6 at 4 to 6 h after drug administration. In contrast to more lipophilic 99m Tc- labelled compounds, excretion was primarily via the urinary tract. Nitro-L-arginine selectively increased solid tumour labelling over normal tissue. Conclusions: 99m Tc-BnAO or HL-91 is a promising agent for clinical studies of tumour hypoxia, although the mechanism of its selective hypoxic cell accumulation remains unexplained

Synthesis and labelling of organo-metallic prosthetic groups used for indirect radioiodination of peptides and proteins

International Nuclear Information System (INIS)

Pozzi, Oscar R.; Castiglia, Silvia G.

1999-01-01

In the framework of an IAEA co-ordinated research programme the prosthetic compound ATE [N-succidinimil 3-(tri-n-butylstannyl) benzoate] has been synthesized and it has been labelled with 131 I and 125 I. Its structure has been confirmed by NMR and mass spectrometry. The labelled ATE has been conjugated with human immunoglobulin G with a yield of 41%-57%. Indirect radioiodination of peptides is currently prepared. (author)

Label Review Training: Module 1: Label Basics, Page 24

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. This page is about which labels require review.

Label Review Training: Module 1: Label Basics, Page 27

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. See examples of mandatory and advisory label statements.

Label Review Training: Module 1: Label Basics, Page 17

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. See an overview of the importance of labels.

Label Review Training: Module 1: Label Basics, Page 23

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. Lists types of labels that do not require review.

Selenium-75-labeled sucralfate: comparison with other radiolabels and initial clinical studies

Energy Technology Data Exchange (ETDEWEB)

Knight, L.C.; Maurer, A.H.; Kollmann, M.; Ammar, I.A.; Fisher, R.S.; Malmud, L.S.

1988-01-01

Sucralfate was synthesized to include a /sup 75/Se label, then compared with /sup 111/In-sucralfate and /sup 99m/Tc-Human serum albumin (HSA)-sucralfate in vitro and in an animal ulcer model. The /sup 75/Se label was the only one of the three that was stable in both human gastric juice and simulated intestinal fluid in vitro. In rats with gastric ulcers, ulcer:nonulcer ratios of bound radioactivity averaged 15.4, 6.3, and 5.6 for /sup 75/Se, /sup 111/In, and /sup 99m/Tc-HSA labels, respectively. Biodistribution studies of /sup 75/Se-sucralfate indicated that little is absorbed from the gastrointestinal tract, and the distribution is similar to that of /sup 14/C-sucralfate. Selective binding of /sup 75/Se sucralfate was successfully imaged in patients with esophagitis (esophageal mean T1/2 binding = 65 +/- 32 min), gastritis (gastric mean T 1/2 binding = 118 +/- 34 min), and gastric ulcers (ulcer mean T 1/2 binding = 135 +/- 59 min). Duodenal ulcers were not successfully imaged. Normal subjects showed no abnormal localization of sucralfate, and esophageal and gastric clearances were rapid.

Metabolic flux analysis of the phenylpropanoid pathway in wound-healing potato tuber tissue using stable isotope-labeled tracer and LC-MS spectroscopy

Energy Technology Data Exchange (ETDEWEB)

Matsuda, Fumio; Morino, Keiko; Miyashita, Masahiro; Miyagawa, Hisashi [Kyoto Univ. (Japan). Department of Agriculture

2003-05-01

The metabolic flux of two phenylpropanoid metabolites, N-p-coumaroyloctopamine (p-CO) and chlorogenic acid (CGA), in the wound-healing potato tuber tissue was quantitatively analyzed by a newly developed method based upon the tracer experiment using stable isotope-labeled compounds and LC-MS. Tuber disks were treated with aqueous solution of L-phenyl-d{sub 5}-alanine, and the change in the ratio of stable isotope-labeled compound to non-labeled (isotope abundance) was monitored for p-CO and CGA in the tissue extract by LC-MS. The time-dependent change in the isotope abundance of each metabolite was fitted to an equation that was derived from the formation and conversion kinetics of each compound. Good correlations were obtained between the observed and calculated isotope abundances for both p-CO and CGA. The rates of p-CO formation and conversion (i.e. fluxes) were 1.15 and 0.96 nmol (g FW){sup -1}h{sup -1}, respectively, and for CGA, the rates 4.63 and 0.42 nmol (g FW){sup -1}h{sup -1}, respectively. This analysis enabled a direct comparison of the biosynthetic activity between these two compounds. (author)

Label Review Training: Module 1: Label Basics, Page 16

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This module of the pesticide label review training provides basic information about pesticides, their labeling and regulation, and the core principles of pesticide label review. Learn about the importance of labels and the role in enforcement.

Attomole detection of isotope-labeled compounds in chemical defense research

Energy Technology Data Exchange (ETDEWEB)

Vogel, J.S.; Buchholz, B.A.; Pawley, N.H.; Mauthe, R.E.; Dingley, K.; Turteltaub, K.

1996-11-01

AMS detects 14C at zeptomole to femtomole sensitivities. We detected the effect of ChE-blocking pyridostigmine bromide on the CNS uptake of a pyrethroid insecticide at scaled human-equivalent exposures in rats. Significant blood to brain protection from permethrin dosed at 5mg/kg is seen in the CNS of rats receiving pyridostigmine bromide pretreatments in chow at 2mg/kg/day. The synergy of these compounds was suggested as a precursor to some symptoms of `Gulf War Syndrome`.

Synthesis of analogues of purine nucleotides selectively labeled by tritium on the C-8 of the purine ring and evaluation of the stability of tritium label

Czech Academy of Sciences Publication Activity Database

Elbert, Tomáš

2010-01-01

Roč. 53, č. 3 (2010), s. 156-157 ISSN 0362-4803. [Workshop of the International Isotope Society - Central European Division. The Synthesis and applications of Isotopes and Isotopically Labelled Compounds /16./. 01.10.2009-02.10.2009, Bad Soden] Institutional research plan: CEZ:AV0Z40550506 Keywords : acyclic nucleotide analogues * tritium Subject RIV: CC - Organic Chemistry

Efficient Multi-Label Feature Selection Using Entropy-Based Label Selection

Directory of Open Access Journals (Sweden)

Jaesung Lee

2016-11-01

Full Text Available Multi-label feature selection is designed to select a subset of features according to their importance to multiple labels. This task can be achieved by ranking the dependencies of features and selecting the features with the highest rankings. In a multi-label feature selection problem, the algorithm may be faced with a dataset containing a large number of labels. Because the computational cost of multi-label feature selection increases according to the number of labels, the algorithm may suffer from a degradation in performance when processing very large datasets. In this study, we propose an efficient multi-label feature selection method based on an information-theoretic label selection strategy. By identifying a subset of labels that significantly influence the importance of features, the proposed method efficiently outputs a feature subset. Experimental results demonstrate that the proposed method can identify a feature subset much faster than conventional multi-label feature selection methods for large multi-label datasets.