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

GABA Receptor

Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor

GABA Receptor

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-124467
    Difludiazepam
    		Ligand 98.9%
    Difludiazepam (Ro 07-4065), a benzodiazepine derivative, is a GABAA receptor ligand with an IC50 of 4.1 nM. Difludiazepam binds to an allosteric site on the GABAA receptor to potentiate the receptor's response to GABA, reducing neuron excitability. Difludiazepam contains halogenated groups at the ortho position of its phenyl ring.
    Difludiazepam
  • HY-18715
    Ornidazole (Levo-)
    		98.86%
    Levo-ornidazole ((S)-Ornidazole) is the L-isomer of Ornidazole. Ornidazole (Levo-) increases GAD 65/67 expression and decreases brain Glu/GABA ratio. Ornidazole (Levo-) has a mild sedative effect. Levo-ornidazole can be used in the research of anti-anaerobic and anti-parasitic agents.
    Ornidazole (Levo-)
  • HY-B0822R
    Fipronil (Standard)
    		Antagonist
    Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes.
    Fipronil (Standard)
  • HY-N2338
    Cholesterol myristate
    		98.0%
    Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
    Cholesterol myristate
  • HY-109077
    Tigolaner
    		Antagonist 99.37%
    Tigolaner (BAY-1272858) acts on γ-aminobutyric acid (GABA) and glutamate-gated chloride channels. Tigolaner has antiparasitic activity.
    Tigolaner
  • HY-103512
    TP003
    		Agonist 98.09%
    TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors.
    TP003
  • HY-108068
    Alphadolone acetate
    		Agonist 98.50%
    Alphadolone acetate (Alfadolone acetate) is a steroid agent that can suppress or relieve pain, with antinociception.
    Alphadolone acetate
  • HY-103507
    N-Arachidonyl-GABA
    		Activator ≥99.0%
    N-Arachidonoyl-GABA is one member of a new class of lipoamino acids related to anandamide identified in bovine brain. N-Arachidonoyl-GABA displays analgesic activity.
    N-Arachidonyl-GABA
  • HY-120837
    PZ-II-029
    		Agonist 99.23%
    PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects.
    PZ-II-029
  • HY-W033027
    BGT1-IN-1
    		Inhibitor
    BGT1-IN-1 (compound 9) is a potent BGT1 inhibitor with IC50 value of 13.9, 58.3 µM for hBGT1, GAT3, respectively. BGT1-IN-1 shows no cytotoxic. BGT1-IN-1 shows neuroprotective activity.
    BGT1-IN-1
  • HY-N13742
    Dihydrohonokiol B
    		Agonist 99.29%
    Dihydrohonokiol B (Dihydrohonokiol) is an anxiolytic agent. Dihydrohonokiol B can reduce the neurotoxicity induced by amyloid β protein by stimulating the GABAC receptor. Dihydrohonokiol B can be used in the research of neurodegenerative diseases such as Alzheimer's disease.
    Dihydrohonokiol B
  • HY-W103105
    R 29676
    		Antagonist 99.80%
    R 29676 is a neuroleptic agent and inhibits sodium-dependent GABA binding (GABA uptake).
    R 29676
  • HY-B0122R
    Topiramate (Standard)
    		Activator
    Topiramate (Standard) is the analytical standard of Topiramate. This product is intended for research and analytical applications. 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.
    Topiramate (Standard)
  • HY-B0211S
    Riluzole-13C,15N2
    		99.90%
    Riluzole-13C,15N2 is the 13C and 15N labeled Riluzole. 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.
    Riluzole-<sup>13</sup>C,<sup>15</sup>N<sub>2</sub>
  • HY-112788
    ONO-8590580
    		Modulator 99.84%
    ONO-8590580 is a GABAA α5 negative allosteric modulator.
    ONO-8590580
  • HY-P5188A
    Waglerin-1
    		Inhibitor 98.71%
    Waglerin-1, a 22-amino acid peptide, is a competitive antagonist of the muscle nicotinic receptor (nAChR).
    Waglerin-1
  • HY-W001692
    Ocinaplon
    		Modulator 99.58%
    Ocinaplon (DOV 273547) is an orally active positive allosteric modulator of GABAA receptor, with an EC50 ranging from 3.07 μM (α1β2γ2 subtype) to 10.03 μM (α1β2γ3 subtype). Ocinaplon enhances GABA-stimulated chloride currents across multiple GABAA receptor subtypes, with varying potency between different subtypes. Ocinaplon exerts anxiolytic and anticonvulsant effects, and causes motor impairment at high doses. Ocinaplon can be used for research on generalized anxiety disorder.
    Ocinaplon
  • HY-N6628
    6,2'-Dihydroxyflavone
    		Antagonist 99.54%
    6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.
    6,2'-Dihydroxyflavone
  • HY-N2482A
    Guvacine hydrobromide
    		Inhibitor 99.86%
    Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine hydrobromide inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.
    Guvacine hydrobromide
  • HY-113416AS
    Dehydroepiandrosterone sulfate-d6 sodium dihydrate
    		Antagonist 99.9%
    Dehydroepiandrosterone sulfate sodium dihydrate-d6 sodium dihydrate is the deuterium labeled Dehydroepiandrosterone sulfate sodium dihydrate. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium dihydrate is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium dihydrate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium dihydrate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium dihydrate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium dihydrate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate-d<sub>6</sub> sodium dihydrate
Cat. No. Product Name / Synonyms Application Reactivity