用于多巴胺D2受体研究的放射性溴代螺哌啶醇

Radiobrominated spiroperidol for the study of dopamine D2 receptors.

作者信息

De Jesus O T, Friedman A M

出版信息

Int J Rad Appl Instrum A. 1986;37(8):719-26. doi: 10.1016/0883-2889(86)90266-2.

Abstract

Some neuropsychiatric disorders have been suggested to be related to the CNS dopaminergic system. In order to probe this neurotransmitter system, radiobrominated spiroperidol, a potent dopamine (DA) D2-receptor antagonist, was developed. This review deals with the routine synthesis of [75, 76, or 77Br]-p-bromospiroperidol (BrSP), its validation as a radiopharmaceutical directed to DA D2 receptors, and the imaging studies which have been done using this radioligand with either single photon tomography (SPECT) or positron tomography (PET). [*Br]BrSP will be compared to other D2 ligands currently available. The present state and future direction of DA receptor research, in particular, the quantitative aspects, will be discussed.

摘要

一些神经精神疾病被认为与中枢神经系统多巴胺能系统有关。为了探究这个神经递质系统，研发了放射性溴化螺哌啶醇，一种强效的多巴胺（DA）D2受体拮抗剂。本综述涉及[75, 76, 或77Br]-对溴螺哌啶醇（BrSP）的常规合成、其作为靶向DA D2受体的放射性药物的验证，以及使用这种放射性配体通过单光子断层扫描（SPECT）或正电子断层扫描（PET）所进行的成像研究。[*Br]BrSP将与目前可用的其他D2配体进行比较。将讨论DA受体研究的现状和未来方向，特别是定量方面。