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

The Gamma-aminobutyric acid receptor subunit rho-1 (GABRR1) is a member of the Cys-loop family of ligand-gated ion channels and is a primary component of the GABA_A-rho receptor complex, formerly classified as the GABA_C receptor (UniProt P24198). These receptors are characterized by their unique pharmacological profile, including resistance to common GABA_A modulators like bicuculline and benzodiazepines, and their slow desensitization kinetics (IUPHAR/BPS Guide to Pharmacology). GABRR1 is highly enriched in the retina, specifically within bipolar and horizontal cells, where it mediates lateral inhibition and shapes visual signal transmission to the brain (PMID: 11578309). Beyond the visual system, GABRR1 expression in the brainstem and hippocampus suggests roles in sleep regulation, memory, and anxiety (PMID: 21822247). Therapeutic interest in GABRR1 stems from its involvement in retinal pathologies, myopia, and its potential as a target for non-benzodiazepine sedatives or anxiolytics. Drugs such as TPMPA act as selective antagonists, while muscimol serves as a potent agonist, providing tools to modulate inhibitory tone in specific neural circuits.

Other names

GABA(A) receptor subunit rho-1GABA-C receptorRho1 GABA receptorGABRR1GABA receptor rho 1

GABRR1 forms chloride-selective ion channels that open upon GABA binding, leading to neuronal hyperpolarization and inhibition (IUPHAR/BPS Guide to Pharmacology).