CGS 10746B：一种非典型抗精神病药物候选物，在行为有效剂量下可选择性降低多巴胺释放。

CGS 10746B: an atypical antipsychotic candidate that selectively decreases dopamine release at behaviorally effective doses.

作者信息

Altar C A, Wasley A M, Liebman J, Gerhardt S, Kim H, Welch J J, Wood P L

出版信息

Life Sci. 1986 Aug 25;39(8):699-705. doi: 10.1016/0024-3205(86)90017-2.

Abstract

CGS 10746B, a benzothiadiazepine, has a behavioral profile in mice and monkeys similar to the atypical antipsychotic clozapine. Unlike clozapine, CGS 10746B suppresses dopamine neuron firing rates and, when administered at behaviorally effective doses by the oral or intraperitoneal route, decreases neostriatal dopamine release without changing dopamine metabolism or occupying D2 receptors. CGS 10746B is the first atypical antipsychotic candidate that selectively decreases dopamine release.

摘要

CGS 10746B是一种苯并噻二氮卓类药物，在小鼠和猴子身上的行为表现与非典型抗精神病药物氯氮平相似。与氯氮平不同的是，CGS 10746B能抑制多巴胺神经元的放电频率，并且当通过口服或腹腔注射给予行为有效剂量时，它能降低新纹状体多巴胺的释放，而不改变多巴胺代谢或占据D2受体。CGS 10746B是首个选择性降低多巴胺释放的非典型抗精神病候选药物。