Gamma-aminobutyric acid type A receptor alpha-1 beta-3 gamma-2 (GABA_A receptor α1β3γ2)

The GABA_A receptor α1β3γ2 is a heteropentameric ligand-gated ion channel and the most prevalent subtype of GABA_A receptor in the vertebrate central nervous system [1, 11]. It is composed of two α1, two β3, and one γ2 subunits arranged around a central chloride-selective pore [1, 4]. This receptor mediates fast inhibitory neurotransmission, known as phasic inhibition, by allowing chloride ion influx upon binding of the endogenous neurotransmitter gamma-aminobutyric acid (GABA) [6, 7]. It serves as a primary therapeutic target for a wide range of drugs, including benzodiazepines like diazepam and alprazolam, which act as positive allosteric modulators at the α+/γ2- interface, as well as general anesthetics such as propofol and etomidate [1, 2, 12]. Dysfunction of this receptor complex is implicated in various neurological and psychiatric conditions, including epilepsy, anxiety disorders, and insomnia [1, 7, 11]. Clinical use of drugs targeting this receptor is often limited by safety concerns such as respiratory depression, sedation, and the risk of developing tolerance or dependence [12, 13].

Other names

GABA(A) receptor alpha1beta3gamma2GABRA1-GABRB3-GABRG2 complexBZ1 receptorBenzodiazepine receptor 1Alpha-1 beta-3 gamma-2 GABA-A receptor

Positive allosteric modulation of GABA-induced chloride currents; direct channel activation at high concentrations of certain anesthetics; competitive antagonism; non-competitive pore blockade.