Tiurenkov I N, Perfilova V N
Eksp Klin Farmakol. 2010 Oct;73(10):43-8.
Data on the structure, localization, physiology, and pharmacology of GABA receptors are reviewed. These receptors belong to cis-loop receptors and consist of 16 subunits in various combinations and occur in both central nervous system and peripheral organs. There are a great number of their allosteric modulators, agonists and antagonists. Activation of GABA receptors is accompanied by changes in the permeability of plasmatic membranes for chloride ions, which is followed by depolarization (presynaptic inhibition) or hyperpolarization (postsynaptic inhibition). GABA receptors contain some topographically different binding sites, intended for the interaction both with the main mediator (GABA) and with allosteric regulators such as benzodiazepines, barbiturates, convulsants, ethanol, and neurosteroids.