Positron emission tomography (PET) studies of the monoamine neurotransmitter systems in the human brain employ a variety of radiotracers targeting the many receptors, transporters, and enzymes present in monoaminergic neurons. One of these is the vesicular monoamine transporter 2 (VMAT2), the protein responsible for the energy-dependent accumulation of monoamines into synaptic vesicles. The development of in vivo imaging radiotracers for VMAT2 is a story of starting with a well-characterized clinically used drug (tetrabenazine) which had a pharmacologically active metabolite: that metabolite that was in stepwise fashion refined and modified to provide both carbon-11 and fluorine-18 labeled VMAT2 radiotracers that are now used for human PET studies of neurodegenerative and psychiatric diseases. The design approach taken, which involved understanding the metabolism of the radiotracers and identification of the optimal ligand stereochemistry, are representative of important steps in the general concepts behind successful in vivo radiotracer design for brain imaging agents.

中文翻译：

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神经影像学的经典：囊泡单胺转运蛋白的放射性配体2。

对人脑中单胺神经递质系统的正电子发射断层扫描（PET）研究采用了针对单胺能神经元中存在的许多受体，转运蛋白和酶的多种放射性示踪剂。其中之一是囊泡单胺转运蛋白2（VMAT2），该蛋白负责能量依赖的单胺积累到突触小泡中。VMAT2体内成像放射性示踪剂的开发是从具有良好药理活性代谢产物的特征明确的临床使用药物（丁苯那嗪）开始的故事：逐步代谢的代谢产物经过精制和修饰以提供碳11和氟-18个标记的VMAT2放射性示踪剂，现已用于人类PET研究神经退行性疾病和精神疾病。采用的设计方法，