Role of the GABAB receptor in alcohol-seeking and drinking behavior
Role of the GABAB receptor in alcohol-seeking and drinking behavior
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DOI：
10.1016/j.alcohol.2009.09.030
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发表时间：
2009-11-01
期刊：
影响因子：
2.3
通讯作者：
Colombo, Giancarlo
中科院分区：
文献类型：
--
作者：
Maccioni, Paola;Colombo, Giancarlo
本文总结了γ -氨基丁酸(B) （GABA(B)）受体的直接激动剂和正变构调节剂（pam）对不同酒精相关行为的降低作用的实验数据。不同的证据表明，直接激动剂，包括巴氯芬，在大鼠和小鼠中有效地抑制饮酒行为的获得和维持、复发样饮酒以及酒精的强化、奖励、刺激和动机特性。最近，一个正变构调节结合位点的发现，以及体内有效配体的合成，开辟了GABAB药理学研究的新途径。越来越多的证据表明，PAMs保留了巴氯芬抑制酒精消费的能力，以及酒精在大鼠中的强化和激励特性；这些影响发生的剂量与产生行为毒性的剂量相差甚远。(C) 2009爱思唯尔公司版权所有。
The present paper summarizes experimental data demonstrating the reducing effect of direct agonists and positive allosteric modulators (PAMs) of the gamma-aminobutyric acid(B) (GABA(B)) receptor on different alcohol-related behaviors. Different lines of evidence indicate that direct agonists, including baclofen, effectively suppress acquisition and maintenance of alcohol drinking behavior, relapse-like drinking, and alcohol's reinforcing, rewarding, stimulating, and motivational properties in rats and mice. More recently, the discovery of a positive allosteric modulatory binding site, together with the synthesis of in vivo effective ligands, opened a new avenue of research in GABAB pharmacology. Accumulating lines of evidence suggest that PAMs retain baclofen's capcity to supprcss alcohol consumption and alcohol's reinforcing and motivational properties in rats; these effects occur at doses far from those producing behavioral toxicity. (C) 2009 Elsevier Inc. All rights reserved.