1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. GABA Receptor

GABA Receptor

GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). It has long been recognized that the fast response of neurons to GABA that is blocked by bicuculline and picrotoxin is due to direct activation of an anion channel. This channel was subsequently termed the GABAA receptor. Fast-responding GABA receptors are members of family of Cys-loop ligand-gated ion channels. A slow response to GABA is mediated by GABAB receptors, originally defined on the basis of pharmacological properties.

GABA Receptor Related Products (120):

Cat. No. Product Name Effect Purity
  • HY-101391
    Picrotoxin Antagonist >98.0%
    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.
  • HY-N0219
    (+)-Bicuculline Antagonist 99.97%
    (+)-Bicuculline is a light-sensitive competitive antagonist of GABA-A receptor.
  • HY-107994
    Aminooxyacetic acid hemihydrochloride Inhibitor >98.0%
    Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
  • HY-108690
    Fluxametamide Antagonist 99.74%
    Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
  • HY-15399
    Vigabatrin Inhibitor >98.0%
    Vigabatrin(γ-Vinyl-GABA; Sabril) is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase.
  • HY-129105
    Clomethiazole Agonist 98.19%
    Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
  • HY-N2096
    Kavain Activator
    Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic and sedative properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
  • HY-16974
    Afoxolaner Inhibitor 99.53%
    Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.
  • HY-B0211
    Riluzole Inhibitor 99.83%
    Riluzole is an anticonvulsant drug and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
  • HY-103533
    Gabazine Antagonist >98.0%
    Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
  • HY-17354
    (R)-Baclofen Agonist 99.49%
    (R)-Baclofen(STX209) is a selective GABAB receptor agonist.
  • HY-B0211A
    Riluzole hydrochloride Inhibitor 99.94%
    Riluzole hydrochloride is an anticonvulsant drug and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
  • HY-16716
    Basmisanil Inhibitor 99.49%
    Basmisanil is a highly selective GABAAα5 negative allosteric modulator.
  • HY-N0067
    γ-Aminobutyric acid Agonist
    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).
  • HY-103531
    CGP52432 Antagonist 98.50%
    CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
  • HY-103040
    Zuranolone Agonist 99.93%
    Zuranolone is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
  • HY-B0009
    Flumazenil Antagonist 99.98%
    Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
  • HY-14426
    L-655708 Inhibitor 99.25%
    L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki = 0.45 nM).
  • HY-16579A
    Etifoxine Activator 99.94%
    Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors.
  • HY-B0696A
    Tiagabine hydrochloride Inhibitor 99.78%
    Tiagabine hydrochloride is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively.
Isoform Specific Products

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