巴氯芬、苯氯芬和氯苯氨丁酸的硫醚类似物。

Thioether analogues of baclofen, phaclofen and saclofen.

作者信息

Allan R D, Drew C A, Ong J, Tran H W

机构信息

Department of Pharmacology, University of Sydney, N.S.W., Australia.

出版信息

Neurosci Lett. 1990 May 4;112(2-3):223-8. doi: 10.1016/0304-3940(90)90207-p.

DOI:10.1016/0304-3940(90)90207-p

PMID:2163039

Abstract

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 gamma-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.

摘要

巴氯芬、苯氯芬和沙氯芬的类似物，在亚甲基链中引入了硫原子，已使用多种制剂进行测试，以检测它们对巴氯芬诱导反应的γ-氨基丁酸B（GABAB）受体位点活性，这些制剂包括豚鼠离体回肠和输精管、大鼠脑皮质切片以及大鼠小脑膜中（-）-[3H]巴氯芬的置换。结果表明，2-([2-氨基-1-(4-氯苯基)乙基]硫代)乙膦酸2d是新化合物中活性最高的。作为GABAB拮抗剂，2d的活性比苯氯芬弱约2-5倍，作为GABAB结合抑制剂，其效力约为苯氯芬的一半。