Gamma-aminobutyric acid type A receptor alpha-3 beta-2 gamma-2 (GABA_A receptor α3β2γ2) (GABA_A receptor α3β2γ2)

The Gamma-aminobutyric acid type A (GABA_A) receptor alpha-3 beta-2 gamma-2 is a heteropentameric ligand-gated ion channel that serves as a primary mediator of fast inhibitory neurotransmission in the central nervous system [1, 2]. It is composed of two alpha-3, two beta-2, and one gamma-2 subunits, forming a central pore permeable to chloride and bicarbonate ions [4, 9]. Upon binding of the endogenous neurotransmitter GABA, the channel opens, leading to hyperpolarization of the postsynaptic neuron and a decrease in its excitability [6, 7]. This specific subtype is notably expressed in the reticular nucleus of the thalamus, the spinal cord dorsal horn, and the basal ganglia, playing a critical role in sensory processing, muscle tone, and anxiety regulation [9, 31]. Pharmacologically, it is a target for benzodiazepines and other allosteric modulators, which enhance the receptor's response to GABA [12, 15]. Research into alpha-3-selective modulators aims to develop treatments for chronic pain and anxiety that lack the sedative side effects typically associated with alpha-1-containing GABA_A receptors [25, 32]. Dysregulation or mutations in the subunits of this receptor are linked to conditions such as epilepsy, autism, and chronic pain syndromes [8, 11, 32].

Other names

GABRA3/GABRB2/GABRG2 receptorα3β2γ2 GABA-A receptorGamma-aminobutyric acid receptor subunit alpha-3/beta-2/gamma-2 complexGABRA3-GABRB2-GABRG2

Positive allosteric modulation of the GABA-A receptor chloride channel, increasing chloride ion conductance and causing neuronal hyperpolarization.