Arylpiperazide derivatives of phenylpiperazines as a new class of potent and selective 5-HT1B receptor antagonists

被引：4

作者：

Jorand-Lebrun, C ^{[1
]}

Pauwels, PJ ^{[1
]}

Palmier, C ^{[1
]}

Chopin, P ^{[1
]}

Moret, C ^{[1
]}

Marien, M ^{[1
]}

Halazy, S ^{[1
]}

机构：

[1] Ctr Rech Pierre Fabre, Dept Mol & Cellular Biol, F-81106 Castres, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(97)10164-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of arylpiperazide derivatives of phenylpiperazines of general formula 4 has been prepared and evaluated as 5-HT1B receptor antagonists. In vitro experiments at human cloned 5-HT1B receptors show that these derivatives are potent and selective 5-HT1B receptor, antagonists. Among them, compound 4f was found to be orally active, to gain access to the CNS and more importantly to induce an increase in extracellular brain 5-HT upon systemic administration. (C) 1997 Elsevier Science Ltd.

引用

页码：3183 / 3188

页数：6

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