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GABA Receptor GABA Receptor

Inhibitors

Cat.No.  Name Information
M2347 (+)-Bicuculline (+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.
M21509 Afizagabar Afizagabar (S44819) is a first-in-class, competitive and selective α5-GABAAR antagonist with an IC50 value of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2.
M20865 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.
M20438 Phenibut Phenibut, a GABA analogue, is a central nervous system depressant with anxiolytic and sedative effects.
M14224 Vigabatrin hydrochloride Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor.
M14222 Valerenic acid Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors.
M14221 THIP THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist, functionally selective GABAAR ligand, exhibits agonism at α4β1δ, α4β3δ and weak antagonism at αβγ and α4β2δ GABAARs.
M14220 Picrotoxin Picrotoxin (Cocculin) is a natural noncompetitive antagonist of GABAA receptor, binds to the interface pocket on the GABAR. Picrotoxin (Cocculin) causes overstimulation and induces convulsions.
M14219 NS11394 NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM.
M14218 Etifoxine Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
M14217 DL-Borneol DL-Borneol is a racemic mixture of D-Borneol and L-Borneol. DL-Borneol is widely used for the treatment of cardiovascular and cerebrovascular diseases in China.
M14216 DAA-1106 DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.
M14215 4-Acetamidobutanoic acid 4-Acetamidobutanoic acid (N-acetyl GABA), the main metabolite of GABA, exhibits antioxidant and antibacterial activities.
M14214 γ-Aminobutyric acid γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors).
M11530 Guvacine Guvacine, an alkaloid found in areca nut, is an effective inhibitor of GABA uptake. Guvacine inhibited rat GAT-1 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.
M10326 Zuranolone Zuranolone also known as SAGE-217, is a potent GABAA receptor agonist with EC50 values of 296 nM and 163 nM for α1β2γ2 and α4β3δ GABAA receptors.
M9874 SSD114 hydrochloride SSD114 hydrochloride is a GABAB receptor positive allosteric modulator.
M9856 Pipequaline Pipequaline (PK-8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
M9411 AZD-7325 AZD-7325 is a GABA-Aα2,3 -selective receptor modulator.
M9127 ONO-8590580 ONO-8590580 is a GABAAα5 negative allosteric modulator which enhances long-term potentiation and improves cognitive deficits in preclinical models.
M9114 LAU159 LAU159 is a potent, functionally selective α6β3γ2 GABAA receptor modulator.



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