γ-胍基巴氯芬是一种外周GABAB受体激动剂。

Gamma-guanidinobaclofen is a peripheral GABAB receptor agonist.

作者信息

Kerr D I, Humeniuk R E, Ong J

机构信息

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

出版信息

Eur J Pharmacol. 1994 Sep 1;262(1-2):189-92. doi: 10.1016/0014-2999(94)90046-9.

DOI:10.1016/0014-2999(94)90046-9

PMID:7813573

Abstract

In the guinea-pig isolated ileum, both baclofen and gamma-guanidinobaclofen elicited dose-dependent depression of cholinergic twitch contractions, sensitive to the GABAB receptor antagonists phaclofen and 2-hydroxysaclofen. gamma-Guanidinobaclofen was 5 times less potent than R,S-(+/-)-baclofen in depressing the contractions. The corresponding GABA analogs, guanidinoacetic acid, beta-guanidinopropionic acid and gamma-guanidinobutanoic acid were inactive. In rat neocortical slices maintained in Mg(2+)-free medium, baclofen (1-50 microM) reduced the amplitude and rate, whilst gamma-guanidinobaclofen (1 mM) has a very weak GABAB receptor agonist action, 100 times weaker than baclofen. gamma-Guanidinobaclofen is therefore a GABAB receptor agonist, more potent at peripheral than central GABAB receptors.

摘要

在豚鼠离体回肠中，巴氯芬和γ-胍基巴氯芬均可引起胆碱能抽搐收缩呈剂量依赖性抑制，且对GABAB受体拮抗剂法氯芬和2-羟基氯苯氨丁酸敏感。γ-胍基巴氯芬在抑制收缩方面的效力比R,S-(+/-)-巴氯芬低5倍。相应的GABA类似物胍基乙酸、β-胍基丙酸和γ-胍基丁酸无活性。在无镁培养基中培养的大鼠新皮质切片中，巴氯芬（1 - 50μM）可降低振幅和速率，而γ-胍基巴氯芬（1 mM）具有非常弱的GABAB受体激动作用，比巴氯芬弱100倍。因此，γ-胍基巴氯芬是一种GABAB受体激动剂，在外周GABAB受体上比在中枢GABAB受体上更有效。