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Gamma-aminobutyric acid type A receptor subunit theta (GABRQ) is a protein that forms part of the pentameric GABA(A) receptor complex, a ligand-gated chloride channel responsible for mediating fast inhibitory neurotransmission in the central nervous system[1][2][3][4][5]. GABRQ encodes the theta subunit, which can combine with alpha, beta, gamma, or epsilon subunits to form various receptor isoforms with distinct physiological and pharmacological properties. The GABA(A) receptor as a whole is a primary target for several classes of central nervous system drugs including benzodiazepines, barbiturates, and anesthetics[1][5]. Dysregulation or mutations in GABRQ have been implicated in neurodevelopmental disorders (such as autism and schizophrenia), epilepsy, and certain forms of cancer (notably hepatocellular carcinoma), where altered expression may influence disease phenotype or progression[2][4][5]. The theta subunit is located within a gene cluster on chromosome Xq28, and as part of the GABA(A) receptor, modulates chloride ion flux to regulate neuronal excitability and synaptic inhibition.
Positive allosteric modulation (benzodiazepines, barbiturates, neurosteroids, anesthetics enhance GABAergic currents); Direct agonism/antagonism at the GABA(A) receptor; Channel blockade. Note: Not all these drugs are specific to the theta subunit, but act via GABA(A) receptors as a whole.
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