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Gamma-aminobutyric acid receptor subunit rho-3 (GABRR3) is a protein encoded by the GABRR3 gene in humans and belongs to the rho subunit family of ionotropic GABA receptors, sometimes referred to as GABA(C) receptors. These receptors are pentameric ligand-gated chloride channels that mediate inhibitory neurotransmission in the central nervous system. Rho-containing GABA receptors form a subclass distinct from classical GABA(A) receptors due to the presence of rho subunits, which confer unique pharmacological and physiological properties. Rho-3 subunits are predominantly expressed in the retina but are also found in other CNS regions. Abnormalities in GABRR3 and GABAergic signaling are implicated in several neurological and psychiatric disorders, including epilepsy, restless legs syndrome, autism, and mood disorders. Drugs targeting GABA receptors are clinically important for the treatment of anxiety, epilepsy, insomnia, and anesthesia, but specificity for the rho-3 subunit is less common. Safety concerns for therapeutics targeting this class of receptors generally include CNS depression and visual effects.
Chloride channel modulation, Allosteric modulation by ligands resulting in enhanced or decreased inhibitory neurotransmission, Antagonism (inhibition of chloride conductance), Agonism (activation leading to increased chloride conductance)
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