International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology最新文献_第10页

Synthesis, tissue distribution in rats and PET studies in baboon brain of no-carrier-added [18F]RU 52461: in vivo evaluation as a brain glucocorticoid receptor radioligand 无载体添加物ru52461的合成、大鼠组织分布及狒狒脑PET研究[18F]:脑糖皮质激素受体放射配体的体内评价

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-02-01 DOI: 10.1016/0883-2897(92)90004-I

Jean N. Dasilva , Christian Crouzel , Oscar Stulzaft , Marina Khalili-Varasteh , Philippe Hantraye

{"title":"Synthesis, tissue distribution in rats and PET studies in baboon brain of no-carrier-added [18F]RU 52461: in vivo evaluation as a brain glucocorticoid receptor radioligand","authors":"Jean N. Dasilva , Christian Crouzel , Oscar Stulzaft , Marina Khalili-Varasteh , Philippe Hantraye","doi":"10.1016/0883-2897(92)90004-I","DOIUrl":"10.1016/0883-2897(92)90004-I","url":null,"abstract":"<div>11,17β-Dihydroxy-6-methyl-17α -(3-[18F]fluoro-prop-1 -ynyl)androsta-1,4,6-trien-3-one ([18F]RU 52461), an 18F-analog of RU 28362, was synthesized by bromide displacement with [18F]fluoride in 12–30% overall radiochemical yield (decay-corrected) within 140 min from end of bombardment (EOB). The specific activity was 900–1500 mCi/μmol (33.3–55.5 GBq/μmol) at the end of synthesis (EOS). Biodistribution studies indicated high adrenal and pituitary retention, and uniformly low uptake of [18F]RU 52461 in all other brain regions of the rat. Except for the pituitary, no specific receptor-mediated uptake of [18F]RU 52461 could be demonstrated using saturating doses of unlabeled RU 52461 in rat brain. While no change was observed throughout the brain areas in adrenalectomized rats and in animals coinjected with dexamethasone, when compared to controls. PET studies revealed extremely low levels of radioactivity in baboon brain. Therefore, [18F]RU 52461 does not appear to cross the blood-brain barrier, suggesting that this radiopharmaceutical is not suitable to visualize the brain glucocorticoid binding sites by PET.</div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 2","pages":"Pages 167-173"},"PeriodicalIF":0.0,"publicationDate":"1992-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90004-I","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12768718","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 12

Synthesis, receptor binding and target-tissue uptake of carbon-11-labeled carbamate derivatives of estradiol and hexestrol 碳-11标记的雌二醇和己甾醇氨基甲酸酯衍生物的合成、受体结合和靶组织摄取

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-02-01 DOI: 10.1016/0883-2897(92)90005-J

H. Ali , J. Rousseau , M. Diksic , J.E. Van Lier

引用次数: 3

The use of 2-[18F]fluoro-2-deoxy-d-glucose as a potential in vitro agent for labelling human granulocytes for clinical studies by positron emission tomography 利用2-[18F]氟-2-脱氧-d-葡萄糖作为一种潜在的体外剂，通过正电子发射断层扫描为临床研究标记人粒细胞

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-02-01 DOI: 10.1016/0883-2897(92)90006-K

S. Osman, H.J. Danpure

{"title":"The use of 2-[18F]fluoro-2-deoxy-d-glucose as a potential in vitro agent for labelling human granulocytes for clinical studies by positron emission tomography","authors":"S. Osman, H.J. Danpure","doi":"10.1016/0883-2897(92)90006-K","DOIUrl":"10.1016/0883-2897(92)90006-K","url":null,"abstract":"<div>In this study, 2-[18F]fluoro-2-deoxy-d-glucose, ([18F]FDG) was used to radiolabel human granulocytes in vitro for possible clinical use by positron emission tomography (PET). Uptake of [18F]FDG was dependent on the amount of glucose in the labelling medium, e.g. when 1 × 107 granulocytes were incubated with [18F]FDG containing 15μg/mL glucose 80% of [18F]FDG was incorporated within 30 min, but in the presence of 1 mg/mL of glucose it was reduced to 2%. Increasing the cell concentration and activating the granulocytes with Streptococcus pneumoniae, opsonized zymosan or phorbol myristate acetate all increased the uptake of [18F]FDG. Retention of the [18F]FDG by the cells as [18F]FDG-6-phosphate was also dependent on the extracellular glucose concentration, 9% was released within 60 min in the absence of glucose, but 27% in the presence of 1 mg/mL glucose.</div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 2","pages":"Pages 183-190"},"PeriodicalIF":0.0,"publicationDate":"1992-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90006-K","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12768719","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 101

Amino acids for the measurement of protein synthesis in vivo by PET 用PET测定体内蛋白质合成的氨基酸

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-02-01 DOI: 10.1016/0883-2897(92)90011-M

W. Vaalburg , H.H. Coenen , C. Crouzel , Ph.H. Elsinga , B. Långström , C. Lemaire , G.J. Meyer

引用次数: 95

The evaluation of 186Re-labeled antibodies using N2S4 chelate in vitro and in vivo using tumor-bearing nude mice 用N2S4螯合物体外和体内对荷瘤裸鼠进行186re标记抗体的评价

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-02-01 DOI: 10.1016/0883-2897(92)90009-N

A. Najafi , M.M. Alauddin , A. Sosa , G.Q. Ma , D.C.P. Chen , A.L. Epstein , M.E. Siegel

引用次数: 18

Production of 6-[18F]fluoro-l-DOPA and its metabolism in vivo—a critical review 6-[18F]氟左旋多巴的产生及其体内代谢综述

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-02-01 DOI: 10.1016/0883-2897(92)90002-G

A. Luxen , M. Guillaume , W.P. Melega , V.W. Pike , O. Solin , R. Wagner

引用次数: 77

Synthesis of 18F-labeled fluconazole and positron emission tomography studies in rabbits 18f标记氟康唑的合成及家兔正电子发射断层扫描研究

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-02-01 DOI: 10.1016/0883-2897(92)90007-L

E. Livni , Alan J. Fischman , Stephen Ray , Ian Sinclair , David R. Elmaleh , Nathaniel M. Alpert , Stephen Weiss , John A. Correia , Douglas Webb , Robert Dahl , William Robeson , Donald Margouleff , Robert Liss , H.William Strauss , Robert H. Rubin

{"title":"Synthesis of 18F-labeled fluconazole and positron emission tomography studies in rabbits","authors":"E. Livni , Alan J. Fischman , Stephen Ray , Ian Sinclair , David R. Elmaleh , Nathaniel M. Alpert , Stephen Weiss , John A. Correia , Douglas Webb , Robert Dahl , William Robeson , Donald Margouleff , Robert Liss , H.William Strauss , Robert H. Rubin","doi":"10.1016/0883-2897(92)90007-L","DOIUrl":"10.1016/0883-2897(92)90007-L","url":null,"abstract":"<div>[4-18F]2-(2,4-difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)-2-propanol ([4-18F]fluconazole) was synthesized from its amino precursor. Fieldel-Crafts acylation of 3-fluoroacetanilide with chloroacetyl chloride produced 2′-fluoro-4′-acteamido-2-(1H-1,2,4-triazole-1-yl) acetophenone in 12% yield. Sequential reaction with (1) dimethylsulphoxonium methylide and (2) 1,2,4-triazole followed by in situ hydrolysis resulted in 2-(2-fluoro-4-aminophenyl)-1,3-bis(1H-1,2,4-triazol-l-yl)-2-propanol in 19% yield. A modified Schiemann reaction on this product resulted in [4-18F]fluconazole with a radiochemical yield of 1.0–2.0% (EOS) within 2 h. [4-18F]Fluconazole was used to measure the pharmacokinetics of fluconazole in rats by measurement of radioactivity in excised tissues and in rabbits by PET. In both species, there was rapid equilibration of [4-18F]fluconazole to a relatively uniform distribution of radioactivity in most organs.</div>","PeriodicalId":14328,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology","volume":"19 2","pages":"Pages 191-195, 197-199"},"PeriodicalIF":0.0,"publicationDate":"1992-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2897(92)90007-L","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"12768720","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 22

In vivo mapping of receptors with radiolabelled peptides by gamma scintigraphy 伽玛闪烁成像在体内用放射性标记肽定位受体

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-01-01 DOI: 10.1016/0883-2897(92)90229-R

Richard J Flanagan, Keith Hogan, Daniel Tartaglia, F.Peter Charleson, Jean-Marc Dufour, Rolland Limoges, Raymond Lambert, Johanne Tremblay, Jean Ethier, Pavel Hamet

引用次数: 0

Radiolabeled somatostatin analogues 放射性标记的生长抑素类似物

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-01-01 DOI: 10.1016/0883-2897(92)90232-N

E Deutsch

引用次数: 0

The medications development program — A new initiative of the National Institute on drug abuse 药物开发计划-国家药物滥用研究所的一项新倡议

International Journal of Radiation Applications and Instrumentation. Part B. Nuclear Medicine and Biology Pub Date : 1992-01-01 DOI: 10.1016/0883-2897(92)90214-J

Heinz Sorer Ph.D.

引用次数: 1