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.
|Product Name / Activity
|GABAA-ρ partial agonist; also GABAA agonist
|RuBi GABA trimethylphosphine
|Caged GABA; inhibits neural activity
|GABAA-ρ agonist; also GABAA agonist, GABA-T substrate and GABA uptake inhibitor
|Product Name / Activity
|GABAA-ρ antagonist; also highly potent GABAB agonist
|GABAA-ρ antagonist; also GABAA agonist
|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
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
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