- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S1168||Valproic acid sodium salt (Sodium valproate)||33 mg/mL||33 mg/mL||33 mg/mL|
|S3018||Niflumic acid||<1 mg/mL||56 mg/mL||<1 mg/mL|
|S4661||Tiagabine hydrochloride||11 mg/mL||82 mg/mL||82 mg/mL|
|S1969||Nefiracetam||5 mg/mL||49 mg/mL||49 mg/mL|
|S1332||Flumazenil||<1 mg/mL||5 mg/mL||<1 mg/mL|
|S9249||Securinine||-1 mg/mL||44 mg/mL||-1 mg/mL|
|S9176||Pimpinellin||-1 mg/mL||49 mg/mL||-1 mg/mL|
|s9065||Songorine||-1 mg/mL||71 mg/mL||-1 mg/mL|
|S5049||Thiocolchicoside||100 mg/mL||100 mg/mL||2 mg/mL|
|S7071||(+)-Bicuculline||<1 mg/mL||21 mg/mL||<1 mg/mL|
|S2026||Ginkgolide A||<1 mg/mL||81 mg/mL||2 mg/mL|
|S4587||Pentylenetetrazol||27 mg/mL||27 mg/mL||27 mg/mL|
|S4197||Bemegride||<1 mg/mL||31 mg/mL||31 mg/mL|
|S1338||Gabapentin HCl||42 mg/mL||<1 mg/mL||<1 mg/mL|
|S1329||Etomidate||<1 mg/mL||49 mg/mL||49 mg/mL|
|S2133||Gabapentin||34 mg/mL||<1 mg/mL||<1 mg/mL|
|S4840||Baclofen||0.1 mg/mL||<1 mg/mL||<1 mg/mL|
|S4892||Phenibut||-1 mg/mL||35 mg/mL||-1 mg/mL|
|S3072||(R)-baclofen||8 mg/mL||<1 mg/mL||<1 mg/mL|
|S4574||Piperazine||17 mg/mL||8 mg/mL||17 mg/mL|
|S3634||6-Hydroxyflavone (6-HF)||<1 mg/mL||47 mg/mL||<1 mg/mL|
|S2269||Baicalin||<1 mg/mL||89 mg/mL||<1 mg/mL|
|S3786||Glabridin||-1 mg/mL||64 mg/mL||-1 mg/mL|
|S2399||Dihydromyricetin||<1 mg/mL||64 mg/mL||64 mg/mL|
|S3663||Afloqualone||<1 mg/mL||56 mg/mL||28 mg/mL|
|S4270||Oxiracetam||31 mg/mL||31 mg/mL||<1 mg/mL|
|S4700||4-Aminobutyric acid (GABA)||20 mg/mL||<1 mg/mL||<1 mg/mL|
|S3748||Acamprosate Calcium||40 mg/mL||<1 mg/mL||<1 mg/mL|
|S5805||Allopregnanolone||<1 mg/mL||64 mg/mL||31 mg/mL|
- GABA Receptor Inhibitors (31)
- New GABA Receptor Products
|Catalog No.||Information||Product Use Citations||Product Validations|
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.
(A,B) Wild-type C57BL/6 male mice were treated with vehicle (saline) or 10 mg/kg of paraquat (PQ) for 3 days, and mice received VPA (3.5 mg/kg) or anacardic acid (5 mg/kg) starting 24 and 1 h before PQ injection. IL-6 mRNA expression was determined by real-time PCR.
Niflumic acid is an inhibitor of cyclooxygenase-2 used for joint and muscular pain.
Tiagabine Hydrochloride is the hydrochloride salt form of tiagabine, a nipecotic acid derivative with anticonvulsant property. A selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
Tiagabine is an anti-convulsive medication and a selective gamma-aminobutyric acid (GABA) reuptake inhibitor.
Nefiracetam is a GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. Phase 2.
Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
Securinine, a major natural alkaloid product from the root of the plant Securinega suffruticosa, acts as a γ-amino butyric acid (GABA) receptor antagonist.
Pimpinellin is a furocoumarin that acts as antagonist of proteins with GABA receptor activity.
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.
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.
(+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
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.
Ginkgolide A is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.
Pentylenetetrazol displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GABA(A) receptor antagonist.
Bemegride is a central nervous system stimulant and antidote for barbiturate poisoning.
Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
Etomidate is a GABAA receptor agonist, used as a short-acting anaesthetic agent or sedative.
Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
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.
Phenibut, a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.
(R)-baclofen is a derivative of gamma-aminobutyric acid primarily used to treat spasticity.
Piperazine, GABA receptor agonist, is an anthelmintic used in the treatment of the intestinal nematodes Ascaris lumbricoides and Enterobius vermicularis.
6-Hydroxyflavone, a naturally occurring flavonoid, binds to GABAA receptors with moderate affinity and acts as a partial agonist of GABAA receptors.
Baicalin is a known prolyl endopeptidase inhibitor and affects the GABA receptors.
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.
Dihydromyricetin (Ampelopsin, Ampeloptin) is a natural antioxidant flavonoid from Ampelopsis grossedentata.
A. Cal27 cells transfected with GFP-LC3 plasmid were treated with different concentration of DHM for 24 h. The formation of GFP-LC3 puncta were examined using immunofluorescence and quantified. Scale bar 50 μm.
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.
Oxiracetam, a cyclic derivative of gamma-aminobutyric acid (GABA), is used as a nootropic drug to improve memory and learning.
Gamma-Aminobutyric Acid is a naturally occurring neurotransmitter with central nervous system (CNS) inhibitory activity.
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.
Allopregnanolone, a neurosteroid synthesized from progesterone in brain, acts as a highly potent positive allosteric modulator of the GABAA receptor.
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.