1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. 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 (135):

Cat. No. Product Name Effect Purity
  • 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-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-B0211
    Riluzole Inhibitor 98.52%
    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-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-N2482
    Guvacine Inhibitor
    Guvacine, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively[1].
  • HY-N2368
    Arecaidine Inhibitor
    Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitive inhibits L-proline uptake[1][2].
  • HY-133596
    12,14-Dichlorodehydroabietic acid Antagonist
    12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca2+-activated K+ (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca2+ and stimulates transmitter release[1][2].
  • 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-N0067
    γ-Aminobutyric acid Agonist
    γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
  • HY-17354
    (R)-Baclofen Agonist 99.49%
    (R)-Baclofen(STX209) is a selective GABAB receptor agonist[1].
  • HY-103531
    CGP52432 Antagonist 98.50%
    CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
  • HY-16716
    Basmisanil Inhibitor 99.49%
    Basmisanil is a highly selective GABAAα5 negative allosteric modulator.
  • HY-B0007
    Baclofen Agonist 99.42%
    Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant.
  • 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-100810
    Isoguvacine hydrochloride Agonist 98.80%
    Isoguvacine hydrochloride is a GABA receptor agonist.
  • HY-B0799
    Dihydroergotoxine mesylate Modulator >98.0%
    Dihydroergotoxine mesylate is a complex of closely related alkaloid salts; Binds with high affinity to the GABAA receptor Cl- channel, producing an allosteric interaction with the benzodiazepine site.
  • HY-B0009
    Flumazenil Antagonist 99.98%
    Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
  • HY-16579A
    Etifoxine Activator 99.87%
    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-13694
    Methionine Activator
    Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.