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[莫沙必利代谢物的合成。II. 莫沙必利酚类代谢物的合成及其药理活性]

[Synthesis of metabolites of mosapramine. II. Synthesis of phenolic metabolites of mosapramine and their pharmacological activities].

作者信息

Tashiro C, Yuasa S, Fukuda T

机构信息

Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd., Fukuoka, Japan.

出版信息

Yakugaku Zasshi. 1992 Sep;112(9):615-21. doi: 10.1248/yakushi1947.112.9_615.

Abstract

Four phenolic metabolites of (+-)-3-chloro-5-[3-(2-oxo-1,2,3,5,6,7,8,8a-octahydroimidazo[1,2- a]pyridine-3-spiro-4'-piperidino)propyl]-10,11-dihydro-5H-dibenz [b,f]azepine (mosapramine), a new antipsychotic drug, were synthesized in order to determine their chemical structures. Pharmacological activities of the three main metabolites were compared with those of mosapramine. The activities of the metabolites were far less potent than those of mosapramine.

摘要

为确定新型抗精神病药物(±)-3-氯-5-[3-(2-氧代-1,2,3,5,6,7,8,8a-八氢咪唑并[1,2-a]吡啶-3-螺-4'-哌啶基)丙基]-10,11-二氢-5H-二苯并[b,f]氮杂卓(莫沙帕明)的四种酚类代谢产物的化学结构,对其进行了合成。将三种主要代谢产物的药理活性与莫沙帕明的药理活性进行了比较。这些代谢产物的活性远低于莫沙帕明。

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