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[18F]N-3-氟丙基-2-β-甲氧基羰基-3-β-(4-碘苯基)去甲托烷的放射性合成及首次正电子发射断层扫描人体研究。

Radiosynthesis of [18F] N-3-fluoropropyl-2-beta-carbomethoxy-3-beta-(4-iodophenyl) nortropane and the first human study with positron emission tomography.

作者信息

Chaly T, Dhawan V, Kazumata K, Antonini A, Margouleff C, Dahl J R, Belakhlef A, Margouleff D, Yee A, Wang S, Tamagnan G, Neumeyer J L, Eidelberg D

机构信息

Department of Research, North Shore University Hospital/Cornell University Medical College, Manhasset, NY 11030, USA.

出版信息

Nucl Med Biol. 1996 Nov;23(8):999-1004. doi: 10.1016/s0969-8051(96)00155-2.

DOI:10.1016/s0969-8051(96)00155-2
PMID:9004288
Abstract

A procedure for the routine preparation of [18F]FP-CIT has been developed. Purification of the final product was achieved by preparative HPLC using phenethyl column without decomposition or epimerization. [18F] labeled-N-fluoropropyl-2 beta-carbomethoxy-3 beta-(4-iodophenyl) nortropane was prepared and PET imaging was performed on human subjects. A high uptake into striatal regions was observed. HPLC plasma analysis using [18F]FP-CIT indicated the presence of only one metabolite. By directly comparing the behavior of these three radiotracers ([18F]DOPA, [123I]FP-CIT, and [18F]FP-CIT) in the same subjects, we can enhance our understanding of the dopaminergic system as well as the relative potential of these techniques in a clinical research setting.

摘要

已经开发出一种用于常规制备[18F]FP-CIT的方法。最终产物通过使用苯乙基柱的制备型高效液相色谱法进行纯化,未发生分解或差向异构化。制备了[18F]标记的N-氟丙基-2β-甲氧羰基-3β-(4-碘苯基)去甲托烷,并对人体进行了PET成像。观察到纹状体区域有高摄取。使用[18F]FP-CIT进行的高效液相色谱血浆分析表明仅存在一种代谢物。通过在同一受试者中直接比较这三种放射性示踪剂([18F]多巴、[123I]FP-CIT和[18F]FP-CIT)的行为,我们可以增强对多巴胺能系统以及这些技术在临床研究环境中的相对潜力的理解。

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