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[11C]N,N-二甲基苯乙胺在小鼠和人体中的动力学:测量脑单胺氧化酶B活性的潜力

Kinetics of [11C]N,N-dimethylphenylethylamine in mice and humans: potential for measurement of brain MAO-B activity.

作者信息

Shinotoh H, Inoue O, Suzuki K, Yamasaki T, Iyo M, Hashimoto K, Tominaga T, Itoh T, Tateno Y, Ikehira H

出版信息

J Nucl Med. 1987 Jun;28(6):1006-11.

PMID:3495646
Abstract

Carbon-11-labeled N,N-dimethylphenylethylamine ([11C]DMPEA) was synthesized by the reaction of N-methylphenylethylamine with [11C]methyl iodide. This newly synthesized radiotracer was developed for the purpose of in vivo measurement of monoamine oxidase-B activity in the brain using a metabolic trapping method. Initially, biodistribution was investigated in mice. The rapid and high uptake of 11C radioactivity in the brain was observed following intravenous injection of [11C]DMPEA, the peak of which was reached at 1 min, followed by a decrease at 1-5 min and slowly thereafter. The kinetics of [11C]DMPEA in the human brain were determined using positron emission tomography (PET) and showed that 11C radioactivity increased gradually over 60 min following initial rapid uptake of 11C radioactivity, with basal ganglia and thalamus showing high accumulation.

摘要

碳-11标记的N,N-二甲基苯乙胺([11C]DMPEA)通过N-甲基苯乙胺与[11C]碘甲烷反应合成。这种新合成的放射性示踪剂是为使用代谢捕获法在体内测量大脑中单胺氧化酶-B活性而开发的。最初,在小鼠中研究了生物分布。静脉注射[11C]DMPEA后,观察到大脑中11C放射性快速且高度摄取,其峰值在1分钟时达到,随后在1至5分钟时下降,此后缓慢下降。使用正电子发射断层扫描(PET)确定了[11C]DMPEA在人脑中的动力学,结果表明,在11C放射性最初快速摄取后,11C放射性在60分钟内逐渐增加,基底神经节和丘脑显示出高积累。

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