GABAA-ρ Receptors

GABAA-ρ receptors, previously known as GABAC receptors, are Cys-loop ionotropic ligand-gated ion channels mediating the fast synaptic inhibitory effects of GABA. Despite differing in pharmacology, physiology and biochemistry, they are viewed as a subclass of GABAA receptors.

Literature (1)
Gene Data

GABAA-ρ Receptor Agonists

Cat. No. Product Name / Activity
0344 GABA
Endogenous agonist
0289 Muscimol
GABAA-ρ partial agonist; also GABAA agonist
4709 RuBi GABA trimethylphosphine
Caged GABA; inhibits neural activity
0181 TACA
GABAA-ρ agonist; also GABAA agonist, GABA-T substrate and GABA uptake inhibitor

GABAA-ρ Receptor Antagonists

Cat. No. Product Name / Activity
0379 SKF 97541
GABAA-ρ antagonist; also highly potent GABAB agonist
0807 THIP hydrochloride
GABAA-ρ antagonist; also GABAA agonist
1040 TPMPA
Selective GABAA-ρ antagonist

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.

External sources of pharmacological information for GABAA-ρ Receptors :

Literature for GABAA-ρ Receptors

Tocris offers the following scientific literature for GABAA-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

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.

GABAA-ρ Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
GABAA ρ1 Human GABRR1 NM_002042 P24046
Mouse Gabrr1 NM_008075 P56475
Rat Gabrr1 NM_017291 P50572
GABAA ρ2 Human GABRR2 NM_002043 P28476
Mouse Gabrr2 NM_001081141 Q80T41
Rat Gabrr2 NM_017292 P47742
GABAA ρ3 Human GABRR3 NM_001105580 A8MPY1
Mouse Gabrr3 NM_001081190 NP_001074659
Rat Gabrr3 NM_138897 P50573