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.

S3018

Niflumic acid

Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.

S4661

Tiagabine hydrochloride

Tiagabine Hydrochloride 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 is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.

S6470

Fluralaner

Fluralaner 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 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 is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

S7071

(+)-Bicuculline

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

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 is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.

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, 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 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 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.

S3072

(R)-baclofen

(R)-baclofen is a derivative of gamma-aminobutyric acid primarily used to treat spasticity.

S4574

Piperazine

Piperazine, 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, 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.

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.

S3663

Afloqualone

Afloqualone (AFQ) 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.

S6755New

NS 11394

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

S6611New

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.

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.

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, 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.

S3018

Niflumic acid

Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.

S4661

Tiagabine hydrochloride

Tiagabine Hydrochloride 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 is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.

S6470

Fluralaner

Fluralaner 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 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
S1332

Flumazenil

Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.

S7071

(+)-Bicuculline

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

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 is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.

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, 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 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 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.

S3072

(R)-baclofen

(R)-baclofen is a derivative of gamma-aminobutyric acid primarily used to treat spasticity.

S4574

Piperazine

Piperazine, 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, 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.

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.

S3663

Afloqualone

Afloqualone (AFQ) 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 Product Validations
S6755New

NS 11394

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

S6611New

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.

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.

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, 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.

Tags: GABA inhibition | GABA receptor activation | GABA function | GABA drugs | GABA activity | GABA pathway | GABA-A receptor function | GABA receptor function | GABA activation | gamma aminobutyric acid function | GABA cancer | GABA assay | GABA receptor drugs | GABA receptor inhibition | GABA receptor signaling | GABA receptors review | GABA agonists list | GABA antagonist drugs | GABA inhibitor drugs | GABA inhibitor review