Design and structure-activity relationship analysis of ligands of gamma-hydroxybutyric acid receptors

被引：23

作者：

Bourguignon, JJ ^{[1
]}

Schmitt, M ^{[1
]}

Didier, B ^{[1
]}

机构：

[1] Fac Pharm, Lab Pharmacochim Commun Cellulaire, ERS 655, CNRS, F-67401 Illkirch Graffenstaden, France

来源：

ALCOHOL | 2000年 / 20卷 / 03期

关键词：

gamma-hydroxybutyric acid; derivatives; lactone; alcohol; drug design; crotonic acids; ligands; receptors; antagonist;

D O I：

10.1016/S0741-8329(99)00086-5

中图分类号：

R194 [卫生标准、卫生检查、医药管理];

学科分类号：

摘要：

With the use of [H-3]gamma-hydroxybutyric acid, binding experiments allowed the screening of new compounds as ligands of gamma-hydroxybutyric acid receptors. Starting from the acid-alcohol gamma-hydroxybutyric acid structure, structure-activity relation analysis and lead optimization highlighted gamma-hydroxybutyric acid derivatives with significantly increased affinities, when compared with the affinity of gamma-hydroxybutyric acid. Further pharmacological studies with the use of gamma-hydroxybutyric acid derivatives allowed the characterization of the first competitive antagonist acting at gamma-hydroxybutyric acid receptors (NCS 382). (C) 2000 Elsevier Science Inc. All rights reserved.

引用

页码：227 / 236

页数：10

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