“杜松子酒加奎宁水”的新含义：强直抑制作为大脑中乙醇作用的靶点。
A new meaning for "Gin & Tonic": tonic inhibition as the target for ethanol action in the brain.
作者信息
Mody Istvan, Glykys Joseph, Wei Weizheng
机构信息
Department of Neurology, The David Geffen School of Medicine at UCLA, 635 Charles Young Dr S, University of California, Los Angeles, CA 90095, USA.
出版信息
Alcohol. 2007 May;41(3):145-53. doi: 10.1016/j.alcohol.2007.03.009. Epub 2007 May 23.
Gamma-aminobutyric acid (GABA) is the main chemical inhibitory neurotransmitter in the brain. In the central nervous system, it acts on two distinct types of receptor: an ion channel, that is, an "ionotropic" receptor permeable to Cl- and HCO3- (GABAA receptors [GABAARs]) and a G-protein coupled "metabotropic" receptor that is linked to various effector mechanisms (GABAB receptors). This review will summarize novel developments in the physiology and pharmacology of GABAARs, specifically those found outside synapses. The focus will be on a particular combination of GABAAR subunits responsible for mediating tonic inhibition and sensitive to concentrations of ethanol legally considered to be sobriety impairing. Since the same receptors are also a preferred target for the metabolites of steroid hormones synthesized in the brain (neurosteroids), the ethanol-sensitive tonic inhibition may be a common pathway for interactions between the effects of alcohol and those of ovarian and stress-related neurosteroids.
γ-氨基丁酸（GABA）是大脑中主要的化学抑制性神经递质。在中枢神经系统中，它作用于两种不同类型的受体：一种离子通道，即对Cl-和HCO3-通透的“离子otropic”受体（GABAA受体[GABAARs]），以及一种与各种效应机制相关联的G蛋白偶联“代谢otropic”受体（GABAB受体）。本综述将总结GABAARs生理学和药理学的新进展，特别是突触外发现的那些进展。重点将放在负责介导强直抑制并对法律上认为会损害清醒度的乙醇浓度敏感的GABAAR亚基的特定组合上。由于相同的受体也是大脑中合成的类固醇激素（神经类固醇）代谢产物的首选靶点，乙醇敏感的强直抑制可能是酒精效应与卵巢和应激相关神经类固醇效应之间相互作用的共同途径。
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