Gamma-aminobutyric acid type A receptor alpha-1 beta-1 (GABA_A alpha1beta1) (GABA_A alpha1beta1)

The GABA_A receptor alpha-1 beta-1 is a specific heteromeric subtype of the ionotropic gamma-aminobutyric acid (GABA) receptor, which functions as the primary inhibitory neurotransmitter receptor in the mammalian central nervous system [1.1.1, 1.2.1]. It is a ligand-gated chloride channel composed of alpha-1 (GABRA1) and beta-1 (GABRB1) subunits [1.1.2, 1.2.2]. While the most common native GABA_A receptors are pentamers typically containing alpha, beta, and gamma subunits (e.g., alpha-1 beta-2 gamma-2), the alpha-1 beta-1 configuration is a functional assembly used extensively in pharmacological research to characterize subunit-specific drug binding and channel kinetics [1.2.3, 1.2.5]. Activation of this receptor by GABA triggers the influx of chloride ions, leading to neuronal hyperpolarization and the suppression of action potentials [1.2.1, 1.4.1]. This receptor subtype is a target for several classes of psychotropic and anesthetic drugs, including barbiturates, etomidate, and propofol, which act as positive allosteric modulators at the alpha-beta interface or within transmembrane domains [1.3.1, 1.3.4]. Unlike gamma-containing receptors, pure alpha-beta assemblies are generally insensitive to classical benzodiazepines [1.3.2]. Mutations or expression changes in the alpha-1 and beta-1 subunits are linked to various neurological disorders, including juvenile myoclonic epilepsy, childhood absence epilepsy, and schizophrenia [1.1.2, 1.2.2].

Other names

GABRA1/GABRB1 receptorGABA(A) receptor alpha1/beta1Alpha1-beta1 GABA-A receptorGABA-A receptor subunit alpha-1 and beta-1

Positive allosteric modulation of the chloride channel, increasing the frequency or duration of channel opening in response to GABA.