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Gamma-aminobutyric acid type A receptor subunit epsilon is a protein encoded by the GABRE gene and forms part of the heteropentameric GABA_A receptor, a chloride-selective ligand-gated ion channel that is critical for inhibitory synaptic transmission in the brain. The epsilon subunit contributes to the structural and functional heterogeneity of GABA_A receptors, which allow rapid hyperpolarization of neurons upon activation by GABA, the major inhibitory neurotransmitter. This subunit is primarily expressed in the brain but has been noted to participate in modulation of cardiac function as well. Variants in GABRE are associated with certain neuropsychiatric disorders, and the receptor as a whole is a major pharmacological target for diverse drug classes including anesthetics, benzodiazepines, and barbiturates.
Positive allosteric modulation (benzodiazepines, barbiturates, some anesthetics); Direct agonism/activation (GABA, muscimol); Competitive antagonism (bicuculline)
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