短链巴氯芬类似物在豚鼠离体回肠中是γ-氨基丁酸B（GABAB）受体拮抗剂。

Short-chain baclofen analogues are GABAB receptor antagonists in the guinea-pig isolated ileum.

作者信息

Ong J, Kerr D I, Abbenante J, Prager R H

机构信息

Department of Anaesthesia and Intensive Care, University of Adelaide, Australia.

出版信息

Eur J Pharmacol. 1991 Dec 3;205(3):319-22. doi: 10.1016/0014-2999(91)90918-g.

DOI:10.1016/0014-2999(91)90918-g

PMID:1667917

Abstract

A new series of GABAB receptor antagonists, based on short-chain baclofen analogues has been investigated. In guinea-pig isolated ileal preparations, the GABAB receptor-mediated, baclofen-induced depression of cholinergic twitch responses was reversibly and competitively antagonised by the short-chain baclofen analogues 3-amino-3-(p-chlorophenyl)propionic acid (apparent pA2 = 3.5), 2-amino-2-(p-chlorophenyl)ethanephosphonic acid (apparent pA2 = 3.8), and 2-amino-2-(p-chlorophenyl)ethanesulphonic acid apparent pA2 = 4.0). The corresponding des-chloro analogues were all less active. These compounds represent another class of GABAB receptor antagonists which may cross the blood-brain barrier.

摘要

已对基于短链巴氯芬类似物的一系列新型GABAB受体拮抗剂进行了研究。在豚鼠离体回肠制备物中，短链巴氯芬类似物3-氨基-3-（对氯苯基）丙酸（表观pA2 = 3.5）、2-氨基-2-（对氯苯基）乙烷膦酸（表观pA2 = 3.8）和2-氨基-2-（对氯苯基）乙烷磺酸（表观pA2 = 4.0）可对GABAB受体介导的、巴氯芬诱导的胆碱能抽搐反应抑制作用产生可逆性竞争性拮抗。相应的去氯类似物活性均较低。这些化合物代表了另一类可能穿过血脑屏障的GABAB受体拮抗剂。