Gamma-aminobutyric acid type A receptor subunit rho-1 (GABRR1)

Gamma-aminobutyric acid type A receptor subunit rho-1 (GABRR1) is a protein subunit of the GABA(A) receptor that assembles as part of a pentameric, ligand-gated chloride channel mediating the fast inhibitory actions of the major neurotransmitter GABA in the central nervous system. Rho subunit-containing GABA(A) receptors, previously known as GABA(C) receptors, are classically found in the retina, where they contribute to visual signal processing, but are also present in the brain and in non-neural tissues. These receptors are highly selective to GABA and insensitive to classic benzodiazepines, differing in pharmacological profile from other GABA(A) receptor subtypes. GABRR1 variants are associated with several neuropsychiatric conditions, including autism spectrum disorder, epilepsy, bipolar disorder, schizoaffective disorder, and alcohol dependence. Recent research has also implicated GABRR1 in hematopoietic differentiation, especially in the development of megakaryocytes and platelet numbers. Its primary physiological functions include mediating synaptic and extrasynaptic inhibition by permitting chloride influx upon GABA binding, thereby hyperpolarizing neurons and reducing excitability.

Other names

Gamma-aminobutyric acid receptor subunit rho-1GABA(A) receptor subunit rho-1GABA(C) receptorGABA(A) receptor, rho 1GABAAR subunit rho-1gamma-aminobutyric acid (GABA) A receptor, rho 1gamma-aminobutyric acid (GABA) receptor, rho 1bA135P14.1

Drugs targeting GABRR1 may exert their effects through positive allosteric modulation, antagonism at the GABA binding site, or inhibition or alteration of chloride ion flow (channel blockade).