γ-氨基丁酸B（GABA(B)）受体激动剂巴氯芬对吗啡戒断症状的缓解作用

Attenuation of morphine withdrawal signs by the GABA(B) receptor agonist baclofen.

作者信息

Bexis S, Ong J, White J

机构信息

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

出版信息

Life Sci. 2001 Dec 14;70(4):395-401. doi: 10.1016/s0024-3205(01)01485-0.

DOI:10.1016/s0024-3205(01)01485-0

PMID:11798009

Abstract

The present study examined the effect of the gamma-aminobutyric acidB (GABA(B)) receptor agonist, baclofen on naloxone-induced withdrawal signs in morphine-dependent rats and modification by the antagonist, 3-aminopropyl-cyclohexylmethylphosphinic acid (CGP 46381). Morphine was administered via mini-osmotic pumps for 7 days to induce physical dependence. Baclofen (20 mg kg(-1)) decreased stereotyped head movements, chewing, chatter, ptosis and body weight loss, induced by naloxone (10 mg kg(-1)) in morphine-dependent rats. CGP 46381 (20 mg kg(-1)) reversed the effects exerted by baclofen on stereotyped head movements, ptosis, and weight loss and partially reversed the effect of baclofen on chewing. It can be concluded that baclofen has some potential in the treatment of opioid withdrawal and that GABA(B) receptors may be implicated in such a withdrawal.

摘要

本研究考察了γ-氨基丁酸B（GABA(B)）受体激动剂巴氯芬对吗啡依赖大鼠纳洛酮诱发的戒断症状的影响，以及拮抗剂3-氨基丙基-环己基甲基次膦酸（CGP 46381）对其的调节作用。通过微型渗透泵给予吗啡7天以诱导身体依赖性。巴氯芬（20 mg kg(-1)）减少了吗啡依赖大鼠中由纳洛酮（10 mg kg(-1)）诱发的刻板头部运动、咀嚼、颤搐、眼睑下垂和体重减轻。CGP 46381（20 mg kg(-1)）逆转了巴氯芬对刻板头部运动、眼睑下垂和体重减轻的作用，并部分逆转了巴氯芬对咀嚼的作用。可以得出结论，巴氯芬在治疗阿片类药物戒断方面具有一定潜力，且GABA(B)受体可能参与了此类戒断过程。