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 (271):

Cat. No. Product Name Effect Purity
  • HY-16716
    Basmisanil Inhibitor 99.89%
    Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders[1].
  • HY-B0211
    Riluzole Inhibitor
    Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
  • HY-107994
    Aminooxyacetic acid hemihydrochloride Inhibitor
    Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
  • HY-N0219
    Bicuculline Antagonist
    Bicuculline ((+)-Bicuculline; d-Bicuculline), as a convulsant alkaloid, is a competitive neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+-activated potassium (SK) channels and subsequently blocks the slow afterhyperpolarization (slow AHP) [1][2][3].
  • HY-103533
    Gabazine Antagonist
    Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
  • HY-103500
    Ro19-4603 Inhibitor
    Ro19-4603 is a benzodiazepine inverse agonist. Ro19-4603 antagonizes ethanol (EtOH) intake in alcohol-preferring rats[1].
  • HY-100799
    ZAPA sulfate Agonist
    ZAPA sulfate is an agonist at low affinity GABAA-receptors. ZAPA sulfate induces membrane hyperpolarization of the Ascaris muscle cell with an EC50 of 10.3 μM[1][2].
  • HY-111298
    TG 41 Modulator
    TG 41 is positive modulator of GABAA receptor. TG 41 enhances the binding both of GABA and of Flunitrazepam to rat cerebral cortical membranes[1].
  • HY-131941
    SJM-3 Agonist
    SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface[1].
  • HY-103510
    TB-21007 Agonist
    TB-21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptor with a Ki of 1.6 nM. TB-21007 enhanced spatial memory in rats[1].
  • HY-119687
    Bifenazate Agonist 99.65%
    Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm[1]. Bifenazate is a positive allosteric modulator of GABA receptor[2].
  • HY-12783
    SCH 50911 hydrochloride Antagonist
    SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM.
  • HY-118301
    ADX71441 Modulator
    ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity[1].
  • HY-B0122A
    Topiramate lithium Activator
    Topiramate (McN 4853) lithium is a broad-spectrum antiepileptic agent. Topiramate lithium 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[1][2][3].
  • HY-116622
    α5IA Agonist
    α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential[1].
  • 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[1].
  • HY-109077S
    Tigolaner-d4 Antagonist
    Tigolaner-d4 is deuterium labeled Tigolaner. Tigolaner is a GABA antagonist that regulates chloride channel. Tigolaner is an antiparasitic agent[1].
  • HY-132806
    Alogabat Activator 99.91%
    Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1)[1].
  • HY-129105
    Clomethiazole Agonist 99.75%
    Chlormethiazole is an potent and orally active GABAA agonist[1]. 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[2].
  • HY-100140A
    Pipequaline hydrochloride Agonist
    Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity[1][2].