STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CENTRAL-NERVOUS-SYSTEM AGENTS .13. 4-[3-(BENZOTRIAZOL-1-YL)PROPYL]-1-(2-METHOXYPHENYL)PIPERAZINE, A NEW PUTATIVE 5-HT1A RECEPTOR ANTAGONIST, AND ITS ANALOGS

被引：65

作者：

MOKROSZ, JL ^{[1
]}

PALUCHOWSKA, MH ^{[1
]}

CHOJNACKAWOJCIK, E ^{[1
]}

FILIP, M ^{[1
]}

CHARAKCHIEVAMINOL, S ^{[1
]}

DERENWESOLEK, A ^{[1
]}

MOKROSZ, MJ ^{[1
]}

机构：

[1] POLISH ACAD SCI,INST PHARMACOL,NEW DRUGS LAB,PL-31343 KRAKOW,POLAND

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1994年 / 37卷 / 17期

关键词：

D O I：

10.1021/jm00043a014

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new set of 4-alkyl-1-(o-methoxyphenyl)piperazines containing a terminal benzotriazole fragment were synthesized, and their 5-HT1A and 5-HT2 affinity was determined. It was shown that the benzotriazole moiety contributes to both the 5-HT1A and 5-HT2 receptor affinity. It was demonstrated in several behavioral models that 4-[3(benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine (11) is a new, potent presynaptic and postsynaptic 5-HT1A receptor antagonist. However, it is not selective For 5-HT1A versus alpha(1) receptors.

引用

页码：2754 / 2760

页数：7

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