Gamma-aminobutyric acid (GABA) A receptors are GABA gated chloride channels, which are important mediators of neuronal inhibition in the mammalian central nervous system. Activation of the GABAA site results in increased intracellular chloride concentration and hyperpolarization of the cell. GABAA receptors are pentameric structures assembled from a family of distinct subunits. At least fourteen distinct subunits have been identified, which show distinct patterns of temporal and spatial expression. GABAA receptors may be modulated by several drug types including benzodiazepines and barbiturates, and by phosphorylation by protein kinase C (PKC) and protein kinase A (PKA). The GABA-A receptors are important targets for a variety of drugs such as benzodiazepines, barbiturates, steroids, anaesthetics and convulsants.
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