GABA Receptor

Inhibitory Selectivity

Isoform-specific Inhibitors

GABA Receptor Products

New GABA Receptor Products
Catalog No. Information Product Use Citations Product Validations
E1247New

SR95531

Gabazine(SR95531) is a potent competitive and allosteric antagonist of the GABAA receptor, with an IC50 for the GABA receptor of 9 µM.

S2996

L-DAB HBR

L-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) is an inhibitor of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. L-DAB HBR exhibits antitumor activity.

E0599New

Arecaidine hydrochloride

Arecaidine hydrochloride, a constituent of the nut of Areca catechu, inhibits the uptake of GABA and beta-alanine, but not that of glycine.

E2232New

Guvacine hydrochloride

Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and displays modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).

E2354New

Valepotriate

Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABAA, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.

S4772

alpha-Asarone

Alpha (α)-asarone (trans-Asarone) is one of the main pharmacologically active compounds present in Acorus calamus Linn (Acoraceae), Acorus tatarinowii Schott (Acoraceae), and Acorus gramineus Solander. It has anticonvulsant, neuroprotective, anxiolytic and nootropic effects.

S4423

Emamectin Benzoate

Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.

S4494

Methionine

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

S7071

(+)-Bicuculline

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

S0303

CGP52432

CGP52432 is a potent and selective antagonist of GABAB autoreceptor with IC50 of 0.085 μM.

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.

S6008

p-Hydroxybenzaldehyde

p-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol), which can be found in the orchids Gastrodia elata, Galeola faberi and vanilla, is a hydroxybenzaldehyde that reacts with NAD+ and H2O to produce 4-hydroxybenzoate, NADH, and 2 protons. p-Hydroxybenzaldehyde at 101.7 μM can significantly reduce the GABA-induced chloride current of GABAA receptors(α1β2γ2S subtype) expressed.

S9065

Songorine

Songorine, a ubiquitous alkaloid in the genus Aconitum, is a novel antagonist of the GABAA receptor in rat brain and has antiarrhythmic, antinociceptive, anti-inflammatory, regenerative and CNS-modulating properties.

S6094

Imidazole-4(5)-acetic Acid Hydrochloride

Imidazole-4(5)-acetic Acid Hydrochloride is a competitive antagonist at GABAC receptors.

S9176

Pimpinellin

Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.

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.

S4724

Etomidate hydrochloride

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

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.

S2399

Dihydromyricetin

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

S5612

Isonipecotic acid

Isonipecotic acid (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid) is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist.

E0101New

AZD-6280

AZD-6280 is a selective GABAA (α2/3) receptor modulator, used for treatment of generalized anxiety disorder.

E0960New

RO5186582

RO5186582 (Basmisanil, RG1662) is a highly selective GABAAα5 negative allosteric modulator.

S0164

AZD-7325

AZD7325 is a potent and orally active partial selective Positive allosteric modulator (PAM) of GABAAα2 and Aα3 receptor with Ki=0.3 and 1.3 nM, respectively, and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes.

S9409

Kavain

Kavain ((+)-Kavain), the main kavalactone found mostly in the roots of the kava plant, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.

S6755

NS 11394

NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes.

S1989

GABAA receptor agent 1

GABAA receptor agent 1 is a high affinity ligand for Gamma-aminobutyric acid A (GABAA) receptor that exerts potent anticonvulsant activity.

Catalog No. Information Product Use Citations Product Validations
E1247New

SR95531

Gabazine(SR95531) is a potent competitive and allosteric antagonist of the GABAA receptor, with an IC50 for the GABA receptor of 9 µM.

S2996

L-DAB HBR

L-DAB HBR (L-Dab Hydrobromide, L-2,4-Diaminobutyric acid hydrobromide) is an inhibitor of GABA (Gamma-aminobutyric acid) transaminase with IC50 of >500 μM. L-DAB HBR exhibits antitumor activity.

E0599New

Arecaidine hydrochloride

Arecaidine hydrochloride, a constituent of the nut of Areca catechu, inhibits the uptake of GABA and beta-alanine, but not that of glycine.

E2232New

Guvacine hydrochloride

Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and displays modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).

Catalog No. Information Product Use Citations Product Validations
E2354New

Valepotriate

Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABAA, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.

S4772

alpha-Asarone

Alpha (α)-asarone (trans-Asarone) is one of the main pharmacologically active compounds present in Acorus calamus Linn (Acoraceae), Acorus tatarinowii Schott (Acoraceae), and Acorus gramineus Solander. It has anticonvulsant, neuroprotective, anxiolytic and nootropic effects.

S4423

Emamectin Benzoate

Emamectin Benzoate (EMB, MK-244) activates gamma-amino butyric acid (GABA) transporter. Emamectin Benzoate induces of reactive oxygen species (ROS)-mediated DNA damage and apoptosis.

S4494

Methionine

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

Catalog No. Information Product Use Citations Product Validations
S7071

(+)-Bicuculline

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

S0303

CGP52432

CGP52432 is a potent and selective antagonist of GABAB autoreceptor with IC50 of 0.085 μM.

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.

S6008

p-Hydroxybenzaldehyde

p-Hydroxybenzaldehyde (4-Hydroxybenzaldehyde, 4-Formylphenol, p-Formylphenol), which can be found in the orchids Gastrodia elata, Galeola faberi and vanilla, is a hydroxybenzaldehyde that reacts with NAD+ and H2O to produce 4-hydroxybenzoate, NADH, and 2 protons. p-Hydroxybenzaldehyde at 101.7 μM can significantly reduce the GABA-induced chloride current of GABAA receptors(α1β2γ2S subtype) expressed.

S9065

Songorine

Songorine, a ubiquitous alkaloid in the genus Aconitum, is a novel antagonist of the GABAA receptor in rat brain and has antiarrhythmic, antinociceptive, anti-inflammatory, regenerative and CNS-modulating properties.

S6094

Imidazole-4(5)-acetic Acid Hydrochloride

Imidazole-4(5)-acetic Acid Hydrochloride is a competitive antagonist at GABAC receptors.

S9176

Pimpinellin

Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.

Catalog No. Information Product Use Citations Product Validations
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.

S4724

Etomidate hydrochloride

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

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.

S2399

Dihydromyricetin

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

S5612

Isonipecotic acid

Isonipecotic acid (4-Piperidinecarboxylic acid, 4-Carboxypiperidine, Hexahydroisonicotinic acid) is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist.

Catalog No. Information Product Use Citations Product Validations
E0101New

AZD-6280

AZD-6280 is a selective GABAA (α2/3) receptor modulator, used for treatment of generalized anxiety disorder.

E0960New

RO5186582

RO5186582 (Basmisanil, RG1662) is a highly selective GABAAα5 negative allosteric modulator.

S0164

AZD-7325

AZD7325 is a potent and orally active partial selective Positive allosteric modulator (PAM) of GABAAα2 and Aα3 receptor with Ki=0.3 and 1.3 nM, respectively, and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes.

S9409

Kavain

Kavain ((+)-Kavain), the main kavalactone found mostly in the roots of the kava plant, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.

S6755

NS 11394

NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes.

Catalog No. Information Product Use Citations Product Validations
S1989

GABAA receptor agent 1

GABAA receptor agent 1 is a high affinity ligand for Gamma-aminobutyric acid A (GABAA) receptor that exerts potent anticonvulsant activity.