GABA Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

GABA Receptor Products

Catalog No.	Information	Product Use Citations	Product Validations
S1168	Valproic acid sodium salt (Sodium valproate) Valproic acid sodium salt (Sodium valproate) is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.	Theranostics, 2020, 10(15):6790-6805 J Cell Physiol, 2020, 10.1002/jcp.29443 Biochem Pharmacol, 2020, 3;178:114067	Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
S3018	Niflumic acid Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.	Oncol Lett, 2020, 20(4):39
S4661	Tiagabine hydrochloride Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S4675	Tiagabine Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S6470	Fluralaner Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally.Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls)
S1969	Nefiracetam Nefiracetam (DZL 221) is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.
S4772	alpha-Asarone Alpha (α)-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.
S5319	AWD 131-138 AWD 131-138 is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy. AWD 131-138 (Imepitoin) is an antiepileptic and antianxietic drug, AWD 131-138 can stimulate different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site.
S1332	Flumazenil Flumazenil (RO 15-1788) is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.	Biomed Pharmacother, 2018, 107:1674-1681 Holist Nurs Pract, 2017, 31(3):193-203
S0303^New	CGP52432 CGP52432 is a potent and selective antagonist of GABA_B autoreceptor with IC50 of 0.085 μM.
S7071	(+)-Bicuculline (+)-Bicuculline is a competitive antagonist of GABA_A receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.	Front Cell Neurosci, 2020, 14:24 Cancer Discov, 2020, CD-20-0160 Am J Physiol Lung Cell Mol Physiol, 2019, 316(1):L20-L34	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.
S9249	Securinine Securinine, a major natural alkaloid product from the root of the plant Securinega suffruticosa, acts as a γ-amino butyric acid (GABA) receptor antagonist.
S2026	Ginkgolide A Ginkgolide A (BN52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a K_i of 14.5 μM.	Cell Rep, 2020, 21;31(3):107521
S4587	Pentylenetetrazol Pentylenetetrazol displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.
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.
S4197	Bemegride Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
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.
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.
S1338	Gabapentin HCl Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
S1329	Etomidate Etomidate (R16659) is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.
S2133	Gabapentin Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.	Cell Death Dis, 2020, 11(9):764 Int J Clin Exp Pathol, 2018, 11(12):5536-5546
S3072	(R)-baclofen (R)-baclofen (STX 209) is a derivative of gamma-aminobutyric acid primarily used to treat spasticity.
S4574	Piperazine Piperazine (1,4-Diazacyclohexane, Diethylenediamine, exahydropyrazine, Piperazidine), GABA receptor agonist, is an anthelmintic used in the treatment of the intestinal nematodes Ascaris lumbricoides and Enterobius vermicularis.
S4840	Baclofen Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.
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.
S4892	Phenibut Phenibut (Aminophenylbutyric acid, Fenibut, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA), a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.
S2269	Baicalin Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.	Reprod Fertil Dev, 2019, 31(5):983-992 J Nutr Biochem, 2013, 24(11):1953-62
S4961	3,4,5-Trimethoxycinnamic acid 3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.
S3786	Glabridin Glabridin, 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.	Cell Signal, 2020, 65:109431 Fundam Clin Pharmacol, 2016, 30(6):596-606 Oncotarget, 2016, 10.18632/oncotarget.10836	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.
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.
S4270	Oxiracetam Oxiracetam, a cyclic derivative of gamma-aminobutyric acid (GABA), is used as a nootropic drug to improve memory and learning.
S4700	4-Aminobutyric acid (GABA) Gamma-Aminobutyric Acid is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity.
S3748	Acamprosate Calcium Acamprosate, calcium acetylhomotaurinate, is a synthetic compound with a chemical structure similar to the amino acid neurotransmitter gamma-aminobutyric acid (GABA) and the amino acid neuromodulator taurine.
S5612	Isonipecotic acid Isonipecotic acid is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist.
S6755^New	NS 11394 NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes.
S5131	Homotaurine Homotaurine is a synthetic organic compound that has GABAergic activity by mimicking GABA. It is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy.
S3959	(+)-Borneol (+)-Borneol is one of enantiomers of borneol which is a valuable medical material, senior aromatic spice, and chemical material and has been used in food and also folk medicine.
S5596	(1S)-(-)-α-Pinene α-Pinene is found in the oils of many species of many coniferous trees, notably the pine and has insecticidal activity. (1S)-(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site.
S5805	Allopregnanolone Allopregnanolone, a neurosteroid synthesized from progesterone in brain, acts as a highly potent positive allosteric modulator of the GABAA receptor.
S6611	Cyclothiazide Cyclothiazide is a positive allosteric modulator of ionotropic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-type glutamate receptors with critical roles in neurological development and function.	Cell Death Dis, 2020, 24;11(1):63 Eur J Med Chem, 2020, 15;192:112199 Int J Biol Sci, 2020, 25;16(11):1774-1784
S9409	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.
S3977	(-)-Borneol (-)-Borneol (L-Borneol), one of enantiomers of borneol, has a camphoraceous and evident woody odor. (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.

Catalog No.	Information	Product Use Citations	Product Validations
S1168	Valproic acid sodium salt (Sodium valproate) Valproic acid sodium salt (Sodium valproate) is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches. Valproic acid induces Notch1 signaling in small cell lung cancer (SCLC) cells. Valproic acid is under investigation for treatment of HIV and various cancers. Valproic acid (VPA) induces autophagy and mitophagy by upregulation of BNIP3 and mitochondrial biogenesis by upregulating PGC-1α.	Theranostics, 2020, 10(15):6790-6805 J Cell Physiol, 2020, 10.1002/jcp.29443 Biochem Pharmacol, 2020, 3;178:114067	Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
S3018	Niflumic acid Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.	Oncol Lett, 2020, 20(4):39
S4661	Tiagabine hydrochloride Tiagabine Hydrochloride (Gabitril, NO050328, NO328, TGB) is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S4675	Tiagabine Tiagabine (Gabitril, NO050328, NO328, TGB) is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
S6470	Fluralaner Fluralaner (A1443, AH252723) is a systemic insecticide and acaricide that is administered orally.Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls)

Catalog No.	Information	Product Use Citations	Product Validations
S1969	Nefiracetam Nefiracetam (DZL 221) is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.
S4772	alpha-Asarone Alpha (α)-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.
S5319	AWD 131-138 AWD 131-138 is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy. AWD 131-138 (Imepitoin) is an antiepileptic and antianxietic drug, AWD 131-138 can stimulate different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site.

Catalog No.

Information

Product Use Citations

Product Validations

S1969

Nefiracetam

Nefiracetam (DZL 221) is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.

S4772

Alpha (α)-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.

S5319

AWD 131-138

AWD 131-138 is a centrally acting anti-epileptic which crosses the blood brain barrier and is used for the treatment of canine idiopathic epilepsy. AWD 131-138 (Imepitoin) is an antiepileptic and antianxietic drug, AWD 131-138 can stimulate different recombinant isoforms of the rat GABA(A) receptor through the benzodiazepine binding site.

Catalog No.	Information	Product Use Citations	Product Validations
S1332	Flumazenil Flumazenil (RO 15-1788) is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.	Biomed Pharmacother, 2018, 107:1674-1681 Holist Nurs Pract, 2017, 31(3):193-203
S0303^New	CGP52432 CGP52432 is a potent and selective antagonist of GABA_B autoreceptor with IC50 of 0.085 μM.
S7071	(+)-Bicuculline (+)-Bicuculline is a competitive antagonist of GABA_A receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.	Front Cell Neurosci, 2020, 14:24 Cancer Discov, 2020, CD-20-0160 Am J Physiol Lung Cell Mol Physiol, 2019, 316(1):L20-L34	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.
S9249	Securinine Securinine, a major natural alkaloid product from the root of the plant Securinega suffruticosa, acts as a γ-amino butyric acid (GABA) receptor antagonist.
S2026	Ginkgolide A Ginkgolide A (BN52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a K_i of 14.5 μM.	Cell Rep, 2020, 21;31(3):107521
S4587	Pentylenetetrazol Pentylenetetrazol displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.
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.
S4197	Bemegride Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
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.
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
S1338	Gabapentin HCl Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
S1329	Etomidate Etomidate (R16659) is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.
S2133	Gabapentin Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.	Cell Death Dis, 2020, 11(9):764 Int J Clin Exp Pathol, 2018, 11(12):5536-5546
S3072	(R)-baclofen (R)-baclofen (STX 209) is a derivative of gamma-aminobutyric acid primarily used to treat spasticity.
S4574	Piperazine Piperazine (1,4-Diazacyclohexane, Diethylenediamine, exahydropyrazine, Piperazidine), GABA receptor agonist, is an anthelmintic used in the treatment of the intestinal nematodes Ascaris lumbricoides and Enterobius vermicularis.
S4840	Baclofen Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant and central nervous system depressant. It activates GABA receptors, specifically the GABAB receptors.
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.
S4892	Phenibut Phenibut (Aminophenylbutyric acid, Fenibut, Phenigam, Phenybut, PhGABA, β-Phenyl-γ-aminobutyric acid, β-Phenyl-GABA), a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.
S2269	Baicalin Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.	Reprod Fertil Dev, 2019, 31(5):983-992 J Nutr Biochem, 2013, 24(11):1953-62
S4961	3,4,5-Trimethoxycinnamic acid 3,4,5-Trimethoxycinnamic acid (TMCA) is one of the constituents of Polygalae Radix and may exert anti-seizure activity by acting at the GABAA/BZ receptor complex.
S3786	Glabridin Glabridin, 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.	Cell Signal, 2020, 65:109431 Fundam Clin Pharmacol, 2016, 30(6):596-606 Oncotarget, 2016, 10.18632/oncotarget.10836	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.
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.
S4270	Oxiracetam Oxiracetam, a cyclic derivative of gamma-aminobutyric acid (GABA), is used as a nootropic drug to improve memory and learning.
S4700	4-Aminobutyric acid (GABA) Gamma-Aminobutyric Acid is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity.
S3748	Acamprosate Calcium Acamprosate, calcium acetylhomotaurinate, is a synthetic compound with a chemical structure similar to the amino acid neurotransmitter gamma-aminobutyric acid (GABA) and the amino acid neuromodulator taurine.
S5612	Isonipecotic acid Isonipecotic acid is a heterocyclic compound that mainly acts as a GABAA receptor partial agonist.

Catalog No.	Information	Product Use Citations
S6755^New	NS 11394 NS11394 is a subtype-selective positive allosteric modulator at GABAA receptors, with selectivity for the α3 and α5 subtypes.
S5131	Homotaurine Homotaurine is a synthetic organic compound that has GABAergic activity by mimicking GABA. It is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy.
S3959	(+)-Borneol (+)-Borneol is one of enantiomers of borneol which is a valuable medical material, senior aromatic spice, and chemical material and has been used in food and also folk medicine.
S5596	(1S)-(-)-α-Pinene α-Pinene is found in the oils of many species of many coniferous trees, notably the pine and has insecticidal activity. (1S)-(-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site.
S5805	Allopregnanolone Allopregnanolone, a neurosteroid synthesized from progesterone in brain, acts as a highly potent positive allosteric modulator of the GABAA receptor.
S6611	Cyclothiazide Cyclothiazide is a positive allosteric modulator of ionotropic α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA)-type glutamate receptors with critical roles in neurological development and function.	Cell Death Dis, 2020, 24;11(1):63 Eur J Med Chem, 2020, 15;192:112199 Int J Biol Sci, 2020, 25;16(11):1774-1784
S9409	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.
S3977	(-)-Borneol (-)-Borneol (L-Borneol), one of enantiomers of borneol, has a camphoraceous and evident woody odor. (-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.