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 (136):

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-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-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-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-107198
    (2S)-6-Prenylnaringenin Agonist 98.56%
    (2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface.
  • HY-B0822
    Fipronil Antagonist >98.0%
    Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC500s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
  • HY-116702
    Flufiprole Inhibitor
    Flufiprole is a nonsystemic phenylpyrazole insecticide targeting the GABA receptor used in the rice field. Flufiprole is excellent in controlling a wide range of pests.
  • HY-15399
    Vigabatrin Inhibitor >98.0%
    Vigabatrin (γ-Vinyl-GABA), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting 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, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors).
  • HY-17354
    (R)-Baclofen Agonist 99.49%
    (R)-Baclofen(STX209) is a selective GABAB receptor agonist.
  • 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, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA-B receptor (GABABR) agonist. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.
  • HY-B0211A
    Riluzole hydrochloride Inhibitor 99.96%
    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-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-100810
    Isoguvacine hydrochloride Agonist 98.80%
    Isoguvacine hydrochloride is a GABA receptor agonist.
  • HY-B0122
    Topiramate Activator >98.0%
    Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
  • HY-16579A
    Etifoxine Activator 99.87%
    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.
  • HY-B0649
    Propofol Activator 99.52%
    Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
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