One of the most likely targets of ethanol in the central nervous system (CNS) is the GABA A receptor, a member of the ligand-gated ion channel superfamily of receptors. Gamma-aminobutyric acid (GABA), the neurotransmitter that activates GABA A receptors, is the major inhibitory neurotransmitter in the adult CNS (Barnard et al.,1998).

Alcohol alters the balance between γ-aminobutyric acid (GABA), the primary inhibitory neurotransmitter, and glutamate, the major excitatory neurotransmitter. Genetic vulnerability to alcoholism is therefore likely to be due to numerous genes of small to modest effects in many neurotransmitter systems and signal transduction pathways.

GABA as a neurotransmitter has been long known to be affected by alcohol consumption. Recently, two sub types of the GABAA receptor have come into the spotlight for showing what can possibly be a genetic predisposition to alcohol addiction. These two subtypes are namely GABA A receptor α1 (GABRA1) and GABA A receptor α6 (GABRA6).

2017年9月20日 · We further suggest that the GABA A receptors contributing to alcohol dependence in the rat and presumably in human alcohol use disorders (AUD) are the ethanol-induced up-regulated subtypes containing α4 and most importantly α2 subunits. These mediate critical aspects of the positive reinforcement of ethanol in the dependent chronic user while ...

2006年5月30日 · Thus, the authors provide exciting new evidence for a highly specific interaction of alcohol with a subtype of GABA A receptor that may mediate (at least in part) some of this drug's most important behavioral effects.

In functional studies, alcohol has been reported to potentiate GABA receptor-mediated 36Cl-flux in microsacs, neurosynaptosomes, and cultured spinal cord neurons at pharmacologically relevant concentrations. The potentiating effect of alcohol is blocked by GABA antagonists and the inverse agonists of the benzodiazepine receptor site.

2024年10月1日 · Here, we have discovered a transmembrane protein TMEM132B that is a GABA A receptor (GABA A R) auxiliary subunit. Functionally, TMEM132B promotes GABA A R expression at the cell surface, slows receptor deactivation, and enhances the allosteric effects of alcohol on the receptor.

2014年8月4日 · It has been recently shown that dihydromyricetin, a flavonoid purified from Hovenia, has unique effects on GABA A receptors and blocks ethanol intoxication and withdrawal in alcoholic animal...

Context: Alcohol facilitates gamma-aminobutyric acid (GABA) function, and GABA type A (GABA(A)) receptor-facilitating agents suppress alcohol withdrawal symptoms. Advances in molecular neuroscience, genetics, and neuroimaging provide new insights into the role of brain GABA systems in short- and long-term alcohol effects.

Ethanol, the main psychoactive molecule acting in alcoholic beverages, directly impacts the GABAergic system, contributing to GABAergic dysregulations that vary depending on the intensity and duration of alcohol consumption.