GABA Receptor

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

click to view more

Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

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.

S4675New

Tiagabine

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

S4661New

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.

S4587New

Pentylenetetrazol

Pentylenetetrazol displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.

S3018

Niflumic acid

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

S4270

Oxiracetam

Oxiracetam, a cyclic derivative of gamma-aminobutyric acid (GABA), is used as a nootropic drug to improve memory and learning.

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.

S4700New

4-Aminobutyric acid

Gamma-Aminobutyric Acid is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity.

S4644New

Zolpidem

Zolpidem is a benzodiazepine agonist with high selectivity for α1-subunit-containing GABAA receptors.

S3072

(R)-baclofen

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

S2269

Baicalin

Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.

S2399

Dihydromyricetin

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

S1969

Nefiracetam

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

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.

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.

S4197

Bemegride

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

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.

S4675New

Tiagabine

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

S4661New

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.

S4587New

Pentylenetetrazol

Pentylenetetrazol displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.

S3018

Niflumic acid

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

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.

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.

2014, 4:7270

2016, 173(10):1693-702

2016, 6: 19266

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.

S4197

Bemegride

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

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.

S4700New

4-Aminobutyric acid

Gamma-Aminobutyric Acid is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity.

S4644New

Zolpidem

Zolpidem is a benzodiazepine agonist with high selectivity for α1-subunit-containing GABAA receptors.

S3072

(R)-baclofen

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

S2269

Baicalin

Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.

2013, 24(11):1953-62

S2399

Dihydromyricetin

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

2016, 10.18632/oncotarget.10836

2012, 50(7):2508-14

Catalog No. Information Product Use Citations Product Validations
S4270

Oxiracetam

Oxiracetam, a cyclic derivative of gamma-aminobutyric acid (GABA), is used as a nootropic drug to improve memory and learning.

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