γ-Aminobutyric acid type A receptor subunit alpha5 (GABRA5)

γ-Aminobutyric acid type A receptor subunit alpha5 is one of six alpha subunits that can be incorporated into the heteropentameric GABA(A) receptor, the major inhibitory neurotransmitter receptor in the central nervous system[1][2][5]. GABA(A) receptors are ligand-gated chloride ion channels typically composed of two alpha (α1–6), two beta (β1–3), and one gamma (γ1–3) or other accessory subunit; the α5 subunit is primarily expressed in the hippocampus and plays important roles in both phasic and tonic inhibition[1]. The α5-containing GABA(A) receptors are involved in synaptic and extrasynaptic inhibition and are modulated by clinically relevant drugs, most notably acting as a binding site for benzodiazepines and other allosteric ligands[1][5][6]. Dysfunction of these receptors is implicated in cognitive and neuropsychiatric disorders, making the α5 subunit a therapeutic target for drugs aiming to address memory impairment, epilepsy, schizophrenia, and neurodegeneration[1][4][5].

Other names

GABA(A) receptor subunit alpha5GABAA receptor α5 subunitGABRA5

Positive allosteric modulation at benzodiazepine site; Negative allosteric modulation (inverse agonism); Direct agonism (GABA binding); Modulation by neurosteroids and barbiturates at distinct sites