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Sites of alcohol and volatile anaesthetic action on GABA(A) and glycine receptors

机译：酒精和挥发性麻醉药对GABA（A）和甘氨酸受体的作用部位

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Volatile anaesthetics have historically been considered to act in a nonspecific manner on the central nervous system. More recent studies, however, have revealed that the receptors for inhibitory neurotransmitters such as gamma-aminobutyric acid (GABA) and glycine are sensitive to clinically relevant concentrations of inhaled anaesthetics. The function of GABA(A) and glycine receptors is enhanced by a number of anaesthetics and alcohols, whereas activity of the related GABA rho1 receptor is reduced. We have used this difference in pharmacology to investigate the molecular basis for modulation of these receptors by anaesthetics and alcohols. By using chimaeric receptor constructs, we have identified a region of 45 amino-acid residues that is both necessary and sufficient for the enhancement of receptor function. Within this region, two specific amino-acid residues in transmembrane domains 2 and 3 are critical for allosteric modulation of both GABA(A) and glycine receptors by alcohols and two volatile anaesthetics. These observations support the idea that anaesthetics exert a specific effect on these ion-channel proteins, and allow for the future testing of specific hypotheses of the action of anaesthetics.
机译：过去，挥发性麻醉剂被认为以非特异性方式作用于中枢神经系统。但是，最近的研究表明，抑制性神经递质的受体（如γ-氨基丁酸（GABA）和甘氨酸）对吸入麻醉剂的临床相关浓度敏感。许多麻醉剂和酒精会增强GABA（A）和甘氨酸受体的功能，而相关的GABA rho1受体的活性会降低。我们已经使用药理学上的这种差异来研究麻醉药和酒精对这些受体进行调节的分子基础。通过使用chimaeric受体构建体，我们已经确定了45个氨基酸残基的区域，这对于增强受体功能既必要又足够。在该区域内，跨膜结构域2和3中的两个特定氨基酸残基对于酒精和两种挥发性麻醉剂对GABA（A）和甘氨酸受体的变构调节至关重要。这些观察结果支持了麻醉药对这些离子通道蛋白产生特定作用的想法，并允许将来对麻醉药作用的特定假设进行检验。

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