Gamma-aminobutyric acid type A receptor alpha1beta3gamma2 subtype (GABA-A receptor α1β3γ2)

The GABA-A receptor α1β3γ2 subtype is a heteropentameric ligand-gated chloride channel and the most prevalent GABA-A receptor isoform in the mammalian central nervous system [2, 5]. It is composed of two α1, two β3, and one γ2 subunit arranged around a central ion-conducting pore [3, 5]. This receptor mediates fast inhibitory synaptic transmission, known as phasic inhibition, by facilitating chloride ion influx upon binding of the neurotransmitter γ-aminobutyric acid (GABA) [6, 7]. This influx leads to membrane hyperpolarization and a subsequent reduction in neuronal excitability [6, 7]. The α1β3γ2 subtype is a major therapeutic target for various classes of drugs, including benzodiazepines, non-benzodiazepine hypnotics, barbiturates, and general anesthetics [4, 8]. Specifically, the α1 subunit is linked to the sedative, anticonvulsant, and amnestic properties of these agents [4]. Dysregulation or genetic mutations in the subunits of this receptor are associated with several CNS disorders, including epilepsy, insomnia, and anxiety [7, 10].

Other names

α1β3γ2 GABA-A receptorGABAA receptor alpha1beta3gamma2BZ1-type GABA-A receptorGABRA1-GABRB3-GABRG2 complex

Positive allosteric modulation of the chloride channel