新型8α-氨基麦角灵CQP 201-403的药效学特征

Pharmacodynamic profile of CQP 201-403, a novel 8 alpha-amino-ergoline.

作者信息

Flückiger E, Briner U, Clark B, Closse A, Enz A, Gull P, Hofmann A, Markstein R, Tolcsvai L, Wagner H R

机构信息

Preclinical Research, Pharma, Sandoz Ltd., Basel, Switzerland.

出版信息

Experientia. 1988 May 15;44(5):431-6. doi: 10.1007/BF01940539.

DOI:10.1007/BF01940539

PMID:3371446

Abstract

The profile of action in animals of CQP 201-403, a novel 8 alpha-amino-ergoline, is in most aspects that of a very potent dopaminomimetic, both as a prolactin secretion inhibitor, and at the levels of the CNS and the cardiovascular system. Qualitatively CQP 201-403 differs slightly from bromocriptine and apomorphine in its effects on the CNS (no influence on serotonin metabolism in the rat cortex; induction of masculine mounting behavior in rats) and the cardiovascular system of the dog (reflex tachycardia in response to a blood-pressure fall). In man the new compound proved to be highly active in lowering prolactin serum levels and be more potent than bromocriptine (Parlodel).

摘要

新型8α-氨基麦角灵CQP 201 - 403在动物体内的作用概况在大多数方面表现为一种非常强效的多巴胺模拟物，无论是作为催乳素分泌抑制剂，还是在中枢神经系统和心血管系统层面。在对中枢神经系统（对大鼠皮层中5-羟色胺代谢无影响；诱导大鼠出现雄性爬跨行为）和犬类心血管系统（对血压下降产生反射性心动过速）的作用上，CQP 201 - 403在性质上与溴隐亭和阿扑吗啡略有不同。在人体中，这种新化合物被证明在降低血清催乳素水平方面具有高度活性，且比溴隐亭（帕罗西汀）更有效。