3-THIENYLAMINOBUTYRIC AND 3-FURYLAMINOBUTYRIC ACIDS - SYNTHESIS AND BINDING GABA-B RECEPTOR STUDIES

被引：65

作者：

BERTHELOT, P

VACCHER, C

FLOUQUET, N

DEBAERT, M

LUYCKX, M

BRUNET, C

机构：

[1] FAC PHARM LILLE,PHARM CHIM LAB,3 RUE PROFESSEUR LAGUESSE,F-59045 LILLE,FRANCE

[2] FAC PHARM LILLE,PHARMACODYNAM LAB,F-59045 LILLE,FRANCE

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 08期

关键词：

D O I：

10.1021/jm00112a033

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Baclofen (beta-(p-chlorophenyl)-GABA) is a selective agonist for the bicuculline-insensitive GABA(B) receptor. The search for new compounds that bind to the GABA(B) receptor is very important to clarify structural requirements. We report herein the synthesis and the binding studies of variously substituted 3-thienyl- and 3-furylaminobutyric acids. 4-Amino-3-(5-methyl-2-thienyl)butyric acid (5d) and 4-amino-3-(5-chloro-2-thienyl)butyric acid (5h) are potent and specific ligands for GABA(B) receptor. The IC50 values for the displacement of (R)-(-)-[H-3]baclofen are 1.34 and 0.61-mu-M for 5d and 5h, respectively, as compared to 0.33-mu-M for baclofen.

引用

页码：2557 / 2560

页数：4