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.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
3618 Acamprosate calcium
GABA agonist and glutamatergic modulator
0344 GABA
Endogenous agonist
0289 Muscimol
Partial GABAA-ρ agonist
4709 RuBi GABA trimethylphosphine
Caged GABA; inhibits neural activity
0181 TACA
GABAA-ρ agonist

Antagonists

Cat No Product Name / Activity
0379 SKF 97541
GABAA-ρ antagonist. Also potent GABAB agonist
0807 THIP hydrochloride
GABAA-ρ antagonist
1040 TPMPA
Selective GABAA-ρ antagonist
0180 ZAPA sulfate
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

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    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