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新型精神活性药物他克拉明(AY-22,214)对儿茶酚胺和5-羟色胺代谢的影响。

Effects of taclamine (AY-22,214), a new psychoactive agent, on catecholamine and serotonin metabolism.

作者信息

Pugsley T A, Lippmann W

出版信息

Arch Int Pharmacodyn Ther. 1975 Jan;213(1):73-87.

PMID:1156020
Abstract

The effects of a new psychopharmacologically-active agent taclamine (AY-22,214 (AY)(a dibenzocycloheptaisoquinolines)) on noradrenaline (NA), dopamine (DA) and serotonin(5-HT) turnover in the brains of normal and/or stressed animals were determined by the use of both non-isotopic and isotopic techniques; a comparison with chlordiazepoxide (CL) was carried out. Both AY and CL antagonized the increase in NA and 3H-NA turnover due to immobilization stress in whole, and selected regions, of the rat brain. AY, unlike CL did not decrease 3H-NA turnover in brains of non-stressed animals. AY accelerated the turnover of DA in whole brain and 3H-DA in the striatum. In contrast, CL decreased turnover of each. AY did not alter 5-HT turnover. CL decreased 14C-5-HT turnover in regions of rat brain; in addition, it antagonized the pargyline-induced rise in 5-HT and potentiated the subsequent fall in levels of 5-HIAA. Neither AY nor CL affected the 5-HT uptake in the mouse brain. It is concluded that AY appears to exhibit both similarities and differences to CL with regard to its effects on biogenic amine turnover.

摘要

通过使用非同位素和同位素技术,测定了一种新型精神药理学活性药物他克拉明(AY - 22,214(AY),一种二苯并环庚异喹啉)对正常和/或应激动物大脑中去甲肾上腺素(NA)、多巴胺(DA)和5 - 羟色胺(5 - HT)周转的影响;并与氯氮卓(CL)进行了比较。AY和CL均拮抗了因大鼠全脑及选定区域的固定应激而导致的NA和3H - NA周转增加。与CL不同,AY并未降低非应激动物大脑中的3H - NA周转。AY加速了全脑DA和纹状体中3H - DA的周转。相比之下,CL降低了二者的周转。AY未改变5 - HT周转。CL降低了大鼠脑区14C - 5 - HT的周转;此外,它拮抗了优降宁诱导的5 - HT升高,并增强了随后5 - 羟吲哚乙酸(5 - HIAA)水平的下降。AY和CL均未影响小鼠脑内的5 - HT摄取。结论是,就其对生物胺周转的影响而言,AY与CL既有相似之处,也有不同之处。

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