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新型抗精神病药物[2-氯-11-(2-二甲氨基乙氧基)二苯并[b,f]硫氮杂䓬](佐替平)的药理学研究

Pharmacological study of [2-chloro-11-(2-dimethylaminoethoxy) dibenzo[b,f]thiepine] (zotepine), a new neuroleptic drug.

作者信息

Uchida S, Honda F, Otsuka M, Satoh Y, Mori J, Ono T, Hitomi M

出版信息

Arzneimittelforschung. 1979;29(10):1588-94.

PMID:42413
Abstract

2-Chloro-11-(2-dimethyl-aminoethoxy)dibenzo [b,f]thiepine (zotepine) is a new neuroleptic drug with a chemical structure different from known neuroleptics. The psychopharmacological effects of zotepine in mice, rats and dogs were studied and compared with those of commercially available neuroleptics. Haloperidol and perphenazine were the most active and thioridazine was the least active in hibiting apomorphine-induced gnawing and circling movement, methamphetamine-induced gnawing and circling movement, conditioned avoidance response, motor activity, dopamine-induced pancreatic secretion and apomorphine-induced vomiting. These drugs also had the same order of potency in inducing catalepsy and increasing dopamine turnover and prolactin release. Chlorpromazine, propericiazine and thiothixene were intermediate in potency. Zotepine equalled chlorpromazine in most activities, however, it was clearly less active than chlorpromazine in potentiation of barbiturate sleep and cardiovascular effect.

摘要

2-氯-11-(2-二甲基氨基乙氧基)二苯并[b,f]硫氮䓬(佐替平)是一种新型抗精神病药物,其化学结构与已知的抗精神病药物不同。研究了佐替平在小鼠、大鼠和犬体内的精神药理作用,并与市售抗精神病药物进行了比较。在抑制阿扑吗啡诱导的啃咬和转圈运动、甲基苯丙胺诱导的啃咬和转圈运动、条件回避反应、运动活性、多巴胺诱导的胰腺分泌以及阿扑吗啡诱导的呕吐方面,氟哌啶醇和奋乃静活性最强,硫利达嗪活性最弱。这些药物在诱导僵住症、增加多巴胺代谢及催乳素释放方面的效价顺序也相同。氯丙嗪、丙嗪和替沃噻吨的效价居中。佐替平在大多数活性方面与氯丙嗪相当,然而,在增强巴比妥类药物睡眠和心血管效应方面,它明显不如氯丙嗪活跃。

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