GABAA receptor Selective Activators | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S5049 Thiocolchicoside

Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) is a natural occuring glycoside originated from the flower seeds of superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.

S3663 Afloqualone

Afloqualone (AFQ, HQ-495) is a quinazolinone family GABAergic drug with muscle-relaxant and sedative effects, showing the agonist activity at the β subtype of the GABAa receptor.

S3634 6-Hydroxyflavone (6-HF)

6-Hydroxyflavone, a naturally occurring flavonoid, binds to GABAA receptors with moderate affinity and acts as a partial agonist of GABAA receptors.

S7071 (+)-Bicuculline

(+)-Bicuculline (d-Bicuculline) is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.

Selective GABAA receptor, IC50: 2 μM
S3786 Glabridin

Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.

Selective α1β1γ2 (GABAA receptor), EC50: 17.23 μM; α1β2 (GABAA receptor), EC50: 9.63 μM; α1β3γ2 (GABAA receptor), EC50: 6.83 μM; α1β2γ2 (GABAA receptor), EC50: 6.3 μM
S1329 Etomidate

Etomidate (R16659) is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.

S5194 Furosemide sodium

Furosemide (Frusemide) sodium is a potent and orally active inhibitor of Na-K-Cl cotransporter (NKCC). Furosemide sodium is a subtype-selective antagonist of gamma-aminobutyric acid type A (GABAA) receptor.

S2399 Dihydromyricetin

Dihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata.

S4494 Methionine

Methionine (MRX-1024, D-Methionine) is an activitor of GABAA receptor that modulates neuronal activity.

S4724 Etomidate hydrochloride

Etomidate (Amidate, R 16659) hydrochloride is a general anesthetic that produces its effects by enhancing GABA(A) receptor activity.

S1332 Flumazenil (RO 15-1788)

Flumazenil (RO 15-1788) is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

S4197 Bemegride

Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.

S2269 Baicalin (NSC-661431)

Baicalin (NSC-661431) is a known prolyl endopeptidase inhibitor and affects the GABA receptors.