3-苯并异噻唑基哌嗪衍生物作为潜在的非典型抗精神病药物。
3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
作者信息
Howard H R, Lowe J A, Seeger T F, Seymour P A, Zorn S H, Maloney P R, Ewing F E, Newman M E, Schmidt A W, Furman J S, Robinson G L, Jackson E, Johnson C, Morrone J
机构信息
Central Research Division, Pfizer Inc., Groton, Connecticut 06340, USA.
出版信息
J Med Chem. 1996 Jan 5;39(1):143-8. doi: 10.1021/jm950625l.
A series of substituted phenethyl derivatives of 3-benzisothiazolylpiperazine incorporating potent D2 and 5-HT2A antagonist activity was investigated as an approach to a novel atypical antipsychotic agent. The in vitro profile of 8e from this series is a combination of D2 receptor affinity comparable to the typical antipsychotic agent haloperidol and a 5-HT2A/D2 ratio comparable to the atypical agent clozapine. In vivo 8e possesses activity consistent with an efficacious antipsychotic agent with less tendency to induce extrapyramidal side effects in man.
研究了一系列具有强效D2和5-HT2A拮抗剂活性的3-苯并异噻唑基哌嗪取代苯乙胺衍生物，作为开发新型非典型抗精神病药物的一种途径。该系列中8e的体外特性是，其D2受体亲和力与典型抗精神病药物氟哌啶醇相当，5-HT2A/D2比值与非典型药物氯氮平相当。在体内，8e具有与有效抗精神病药物一致的活性，在人体中诱发锥体外系副作用的倾向较小。
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