GABA Receptor

Inhibitory Selectivity

Isoform-specific Inhibitors

GABA Receptor Products

All (26) GABA Receptor Inhibitors (4) GABA Receptor Activators (4) GABA Receptor Antagonists (7) GABA Receptor Agonists (5) GABA Receptor Modulators (5) GABA Receptor Chemicals (1) New GABA Receptor Products

Catalog No.	Information	Product Use Citations	Product Validations
E1247^New	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.
E0599^New	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.
E2232^New	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).
E2354^New	Valepotriate Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABA_A, 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 GABA_A receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.	Acta Pharmacol Sin, 2022, 10.1038/s41401-021-00854-7 Biomedicines, 2021, 9(12)1927 Neurobiol Dis, 2021, 156:105407	Effects of antagonists on the anti-hyperalgesic effects of sinomenine in CCI rats. * P<0.05 as compared to vehicle control group (N=8 per group). The GABAA receptor antagonist bicuculline but not the opioid receptor antagonist naltrexone nor the 5-HT1A receptor antagonist WAY100635 blocked the antinociceptive effects of 40 mg/kg sinomenine.
S0303	CGP52432 CGP52432 is a potent and selective antagonist of GABA_B autoreceptor with IC50 of 0.085 μM.	J Cell Biochem, 2022, 10.1002/jcb.30231 Front Neurosci, 2021, 15:741214
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.	Life Sci, 2021, S0024-3205(20)31752-5
S2399	Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata.	Molecules, 2021, 26(5)1210 Cell Signal, 2020, 65:109431 J Med Virol, 2019, 91(8):1440-1447	ADH and ALDH expressions in 40% ethanol loaded mice for three hours. Group 1, 500 lM taraxerone; Group 2, 1 mM taraxerone; Group 3, 3 mM DHM (positive control); Group 4, DMSO (control); Group 5, saline. Taraxerone and DHM were dissolved in DMSO, and all treated samples (ethanol, taraxerone, DHM, DMSO, and saline) were administered orally (5 mL/kg body weight). The same letters denote significant differences at p < 0.05, and the error bar represents standard deviation.
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.
E0101^New	AZD-6280 AZD-6280 is a selective GABAA (α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
E0960^New	RO5186582 RO5186582 (Basmisanil, RG1662) is a highly selective GABA_Aα5 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
E1247^New	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.
E0599^New	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.
E2232^New	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
E2354^New	Valepotriate Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABA_A, 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 GABA_A receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.	Acta Pharmacol Sin, 2022, 10.1038/s41401-021-00854-7 Biomedicines, 2021, 9(12)1927 Neurobiol Dis, 2021, 156:105407	Effects of antagonists on the anti-hyperalgesic effects of sinomenine in CCI rats. * P<0.05 as compared to vehicle control group (N=8 per group). The GABAA receptor antagonist bicuculline but not the opioid receptor antagonist naltrexone nor the 5-HT1A receptor antagonist WAY100635 blocked the antinociceptive effects of 40 mg/kg sinomenine.
S0303	CGP52432 CGP52432 is a potent and selective antagonist of GABA_B autoreceptor with IC50 of 0.085 μM.	J Cell Biochem, 2022, 10.1002/jcb.30231 Front Neurosci, 2021, 15:741214
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.	Life Sci, 2021, S0024-3205(20)31752-5
S2399	Dihydromyricetin Dihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata.	Molecules, 2021, 26(5)1210 Cell Signal, 2020, 65:109431 J Med Virol, 2019, 91(8):1440-1447	ADH and ALDH expressions in 40% ethanol loaded mice for three hours. Group 1, 500 lM taraxerone; Group 2, 1 mM taraxerone; Group 3, 3 mM DHM (positive control); Group 4, DMSO (control); Group 5, saline. Taraxerone and DHM were dissolved in DMSO, and all treated samples (ethanol, taraxerone, DHM, DMSO, and saline) were administered orally (5 mL/kg body weight). The same letters denote significant differences at p < 0.05, and the error bar represents standard deviation.
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
E0101^New	AZD-6280 AZD-6280 is a selective GABAA (α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
E0960^New	RO5186582 RO5186582 (Basmisanil, RG1662) is a highly selective GABA_Aα5 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.

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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.

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GABA Receptor

Inhibitory Selectivity

Isoform-specific Inhibitors

GABA Receptor Products