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用于脑内多巴胺活体研究的[18F]氟-L-多巴

[18F]fluoro-L-dopa for the in vivo study of intracerebral dopamine.

作者信息

Firnau G, Garnett E S, Chirakal R, Sood S, Nahmias C, Schrobilgen G

出版信息

Int J Rad Appl Instrum A. 1986;37(8):669-75. doi: 10.1016/0883-2889(86)90260-1.

DOI:10.1016/0883-2889(86)90260-1
PMID:3021668
Abstract

6-[18F]Fluoro-L-dopa was designed to trace the dopamine metabolism in the brain with positron tomography. 6-[18F]Fluoro-L-dopa resembles natural L-dopa biochemically, it crosses the blood-brain barrier with the similar kinetics, it is decarboxylated by dopa decarboxylase and is stored intraneuronally in vesicles. In addition the rate of O-methylation of 6-[18F]fluoro-L-dopa by catechol-O-methyl transferase is only 1/4 of that of natural L-dopa. The low rate of O-methylation, especially in the periphery, is particularly beneficial for PT investigations of the brain. The radiotracer has been synthesized using a variety of electrophilic fluorinating agents.

摘要

6-[18F]氟-L-多巴旨在通过正电子断层扫描追踪大脑中的多巴胺代谢。6-[18F]氟-L-多巴在生化方面类似于天然L-多巴,它以相似的动力学穿过血脑屏障,被多巴脱羧酶脱羧并储存在神经元内的囊泡中。此外,儿茶酚-O-甲基转移酶对6-[18F]氟-L-多巴的O-甲基化速率仅为天然L-多巴的1/4。低O-甲基化速率,尤其是在外周,对大脑的PET研究特别有利。该放射性示踪剂已使用多种亲电氟化剂合成。

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