Potentiation of Gamma Aminobutyric Acid Receptors (GABAAR) by Ethanol: How Are Inhibitory Receptors Affected?
Potentiation of Gamma Aminobutyric Acid Receptors (GABAAR) by Ethanol: How Are Inhibitory Receptors Affected?
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DOI：
10.3389/fncel.2016.00114
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发表时间：
2016
影响因子：
5.3
通讯作者：
Aguayo LG
中科院分区：
文献类型：
--
作者：
Förstera B;Castro PA;Moraga-Cid G;Aguayo LG
近年来，乙醇对五聚体配体门控离子通道（pLGIC）的成员之一--A型γ-氨基丁酸氯通道（GABAAR）的作用的了解有所增加。然而，乙醇增强复合物的机制仍然没有完全理解，许多出版物显示出相互矛盾的结果。因此，许多问题仍然没有得到解决，需要进一步的研究，以更好地理解这种影响。本综述集中在乙醇的急性行动中的GABAAR的参与，并特别侧重于即时的，直接或间接的，突触和突触外的调节作用。要详细说明的即时，直接调制的GABAAR急性乙醇暴露，电生理研究调查不同亚基的重要性，并从受体突变体的数据将进行检查。我们还将讨论的性质，乙醇的推定结合位点的基础上获得的结构数据从其他成员的pLGICs家族。最后，我们将简要强调甘氨酸门控氯离子通道（GlyR），pLGIC家族的另一个成员，作为一个合适的目标，为新的药理学工具的发展。
In recent years there has been an increase in the understanding of ethanol actions on the type A γ-aminobutyric acid chloride channel (GABAAR), a member of the pentameric ligand gated ion channels (pLGICs). However, the mechanism by which ethanol potentiates the complex is still not fully understood and a number of publications have shown contradictory results. Thus many questions still remain unresolved requiring further studies for a better comprehension of this effect. The present review concentrates on the involvement of GABAAR in the acute actions of ethanol and specifically focuses on the immediate, direct or indirect, synaptic and extra-synaptic modulatory effects. To elaborate on the immediate, direct modulation of GABAAR by acute ethanol exposure, electrophysiological studies investigating the importance of different subunits, and data from receptor mutants will be examined. We will also discuss the nature of the putative binding sites for ethanol based on structural data obtained from other members of the pLGICs family. Finally, we will briefly highlight the glycine gated chloride channel (GlyR), another member of the pLGIC family, as a suitable target for the development of new pharmacological tools.