Gamma-aminobutyric acid type A receptor alpha 3 subunit (GABRA3)

The Gamma-aminobutyric acid type A (GABA_A) receptor alpha 3 subunit (GABRA3) is a key component of the heteropentameric GABA_A receptor, a ligand-gated ion channel that mediates the majority of fast inhibitory neurotransmission in the central nervous system (UniProt P34903). This subunit is predominantly expressed in the cerebral cortex, thalamus, and the dorsal horn of the spinal cord, where it plays a vital role in modulating neuronal excitability and sensory processing (NCBI Gene ID: 2556). GABA_A receptors containing the alpha 3 subunit are involved in the regulation of anxiety, muscle relaxation, and the processing of painful stimuli. Unlike the alpha 1 subunit, which is primarily associated with sedation, the alpha 3 subunit is a target for developing non-sedating anxiolytics and analgesics (PubMed: 21948512). Pharmacological agents like TP003 and KRM-II-81 act as positive allosteric modulators at the benzodiazepine binding site of these receptors, enhancing the inhibitory effects of GABA to treat conditions such as chronic pain and generalized anxiety disorder (PubMed: 28438437). Mutations in the GABRA3 gene have also been linked to X-linked neurodevelopmental disorders characterized by epilepsy and cognitive impairment (PubMed: 28190456).

Other names

GABA(A) receptor subunit alpha-3GABRA3GABA-A receptor alpha-3 subunitGABA_A receptor alpha 3

Positive allosteric modulation of the GABA-induced chloride current at the benzodiazepine binding site.