10 - （烷基氨基）-4H - 噻吩并[3,4 - b][1,5]苯并二氮杂䓬类。一类新型潜在抗精神病药物。

10-(Alkylamino)-4H-thieno[3,4-b][1,5]benzodiazepines. A novel class of potential neuroleptic agents.

作者信息

Press J B, Hofmann C M, Eudy N H, Fanshawe W J, Day I P, Greenblatt E N, Safir S R

出版信息

J Med Chem. 1979 Jun;22(6):725-31. doi: 10.1021/jm00192a020.

DOI:10.1021/jm00192a020

PMID:37338

Abstract

An investigation of the structural requirements for CNS activity of the title compounds was undertaken. A synthesis of the precursor dihydro-10H-thieno[3,4-b][1,5]benzodiazepin-10-ones was achieved and three routes for their conversion to the title compounds were developed. The compounds were tested for neuroleptic activity by means of the blockade or d-amphetamine lethality in aggregated mice and/or effects on locomotor activity in rats. Antidepressant activity was examined using inhibition of tetrabenazine-induced depression in mice. Most of the compounds were found to be potent neuroleptic agents with several exhibiting additional antidepressant activity.

摘要

对标题化合物中枢神经系统活性的结构要求进行了研究。实现了前体二氢-10H-噻吩并[3,4-b][1,5]苯二氮䓬-10-酮的合成，并开发了三种将其转化为标题化合物的路线。通过阻断聚集小鼠的d-苯丙胺致死性和/或对大鼠运动活性的影响来测试这些化合物的抗精神病活性。使用小鼠中丁苯那嗪诱导的抑郁抑制来检查抗抑郁活性。发现大多数化合物是有效的抗精神病药物，其中几种还表现出额外的抗抑郁活性。

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