Gamma-aminobutyric acid type A receptor alpha1beta2gamma2S subtype (GABA_A receptor alpha1beta2gamma2S)

The Gamma-aminobutyric acid type A receptor alpha1beta2gamma2S subtype is a pentameric ligand-gated ion channel that serves as the primary mediator of fast inhibitory neurotransmission in the mammalian central nervous system [1, 2]. It is composed of two alpha-1, two beta-2, and one gamma-2S (short splice variant) subunits arranged around a central chloride-selective pore [2, 7]. Activation by the endogenous neurotransmitter GABA leads to chloride influx, resulting in membrane hyperpolarization and a subsequent decrease in neuronal firing [1, 6]. This specific receptor configuration is the most abundant GABA_A receptor subtype in the brain and is the principal target for benzodiazepines, which bind at the alpha/gamma subunit interface to enhance GABA-mediated currents [2, 4]. The alpha-1 subunit within this complex is specifically linked to the sedative, hypnotic, and anticonvulsant properties of GABAergic drugs, while the gamma-2S subunit is crucial for receptor clustering at synapses and benzodiazepine sensitivity [4, 6]. Clinically, this receptor is targeted to treat conditions such as insomnia, anxiety, and epilepsy, though its modulation is also associated with side effects like sedation, ataxia, and the potential for physical dependence [6].

Other names

GABAA receptor alpha1beta2gamma2Salpha1beta2gamma2S GABA(A) receptorBZ1 receptorBenzodiazepine receptor type 1GABRA1-GABRB2-GABRG2S complex

Positive allosteric modulation of the GABA-induced chloride current