GABA_A-ρ Receptors

GABA_A-ρ receptors are Cys-loop ionotropic ligand-gated ion channels mediating the fast synaptic inhibitory effects of GABA. They were previously known as GABA_C receptors, but IUPHAR now considers them to be a subtype of GABA_A receptors.

GABA_A-ρ receptors differ from other GABA_A receptors in pharmacology, physiology and biochemistry. Most GABA_A receptors are heteromeric pentamers, generally comprising two α, two β and one other subunit, whereas GABA_A-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 GABA_A 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 GABA_A-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.

External sources of pharmacological information for GABA_A-ρ Receptors :

• IUPHAR Receptor Code

• BJP Guide

Literature for GABA_A-ρ Receptors

Tocris offers the following scientific literature for GABA_A-ρ Receptors to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

GABA Receptors Scientific Review

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.

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GABA_A-ρ Receptor Gene Data