Gamma-aminobutyric acid type A receptor subunit alpha4 (GABRA4)

Gamma-aminobutyric acid type A receptor subunit alpha4 (GABRA4) is a protein subunit that forms part of the pentameric GABA-A receptor complex, a ligand-gated chloride channel and the principal mediator of rapid inhibitory neurotransmission in the central nervous system[1][2][3][4][5]. The alpha4 subunit can combine with other subunits such as beta and delta or gamma to form receptor isoforms with distinctive functional and pharmacological properties; most importantly, receptors containing alpha4 often mediate *extrasynaptic* (tonic) inhibition, are insensitive to classical benzodiazepines, but are highly sensitive to neurosteroids, ethanol, and certain hypnotics such as gaboxadol[2]. These receptors play important roles in controlling neuronal excitability in brain regions such as the thalamus and hippocampal dentate gyrus, and alterations in GABRA4-containing receptors have been implicated in several neurological and psychiatric diseases[2][5]. This subunit is encoded by the human GABRA4 gene located on chromosome 4p12[5].

Other names

GABA-A receptor subunit alpha4GABRA4Gamma-aminobutyric acid (GABA) A receptor, alpha4GABA-A α4

Positive or negative allosteric modulation (for neurosteroids, ethanol, etomidate) Agonism/partial agonism at GABA binding site (gaboxadol/THIP) Alteration of tonic and phasic chloride current to modulate neuronal excitability