THIOETHER ANALOGS OF BACLOFEN, PHACLOFEN AND SACLOFEN

被引：5

作者：

ALLAN, RD

DREW, CA

ONG, J

TRAN, HW

机构：

[1] Department of Pharmacology, The University of Sydney, Sydney, NSW

来源：

NEUROSCIENCE LETTERS | 1990年 / 112卷 / 2-3期

基金：

英国医学研究理事会;

关键词：

(-)-[[!sup]3[!/sup]H]Baclofen binding study; Baclofen; Guinea pig ileum; Rat cortical slice; Vas deferens; γ-Aminobutyric acid-B receptor antagonist;

D O I：

10.1016/0304-3940(90)90207-P

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Analogues of baclofen, phaclofen and saclofen, incorporating a sulfur atom within the methylene chain, have been tested against responses induced by baclofen for activity at γ-aminobutyric acid-B (GABAB) receptor sites, using a number of preparations including the guinea-pig isolated ileum and vas deferens, rat brain cortical slices and displacement of (-)-[3H]baclofen in rat cerebellar membranes. Results indicate that 2-{[2-amino-1-(4-chlorophenyl)ethyl]thio}ethanephosphonic acid 2d is the most active of the new compounds. 2d is some 2-5 times weaker than phaclofen as a GABAB antagonist and approximately half as potent as phaclofen as an inhibitor of GABAB binding. © 1990.

引用

页码：223 / 228

页数：6

共 7 条

[1] GABA-A AND GABA-B RECEPTOR-SITE DISTRIBUTION IN THE RAT CENTRAL-NERVOUS-SYSTEM [J].