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The GABAA receptor is a major inhibitory neurotransmitter receptor in the mammalian brain. It is an ionotropic, ligand-gated chloride channel that mediates fast synaptic inhibition upon activation by its endogenous ligand, gamma-aminobutyric acid (GABA). The alpha subunit is one of several types of subunits that assemble to form functional GABAA receptors. Different combinations of alpha isoforms confer distinct pharmacological properties. Synaptic receptors containing α(1/2/3) mediate phasic inhibition, while extrasynaptic receptors with certain alpha isoforms like α4 or α6 contribute to tonic inhibition due to higher sensitivity for ambient GABA concentrations.
Binding of GABA to the α/β subunit interface leads to chloride channel opening and neuronal hyperpolarization.
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