GABAA-ρ receptors are Cys-loop ionotropic ligand-gated ion channels mediating the fast synaptic inhibitory effects of GABA. They were previously known as GABAC receptors, but IUPHAR now considers them to be a subtype of GABAA receptors.
GABAA-ρ receptors differ from other GABAA receptors in pharmacology, physiology and biochemistry. Most GABAA receptors are heteromeric pentamers, generally comprising two α, two β and one other subunit, whereas GABAA-ρ receptors are homomeric pentamers assembled from ρ subunits only. There are three known ρ subunits, ρ1, ρ2, ρ3, and while heteromeric oligomers of these subunits have been proposed, only one receptor, made up solely of ρ1 subunits has been definitively identified to date. The resulting ion channel is not blocked or modulated by GABAA receptor ligands, but is 10 times more sensitive to the effects of GABA and selectively blocked by TPMPA. It is relatively insensitive to benzodiazepines, barbiturates and general anesthetics. In addition, the GABAA-ρ receptor has a longer channel opening time and is slower to desensitize. These receptors are expressed in various brain regions and particularly high levels are found in the retina and cerebellum.
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Literature for GABAA-ρ Receptors
A collection of over 250 products for pain research, the guide includes research tools for the study of:
- Ion Channels
- G-Protein-Coupled Receptors
- Intracellular Signaling
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.Request copy | Download PDF | View all reviews