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-119404
    Diproqualone
    		Agonist 99.9%
    diproqualone is methaqualone analogous with sedative, anxiolytic, anti-inflammatory and analgesic properties.
    Diproqualone
  • HY-P5964A
    K1 peptide TFA
    		Ligand 98.22%
    K1 peptide TFA is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP).
    K1 peptide TFA
  • HY-110234
    Topiramate D12
    		Activator 99.90%
    Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate 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 D12
  • HY-100799
    ZAPA sulfate
    		Agonist 99.25%
    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.
    ZAPA sulfate
  • 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-108034
    GET73
    		98.69%
    GET73 is a γ-hydroxybutyric acid (GHB) analog, a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties. GET73 significantly affects glutamate transmission in the hippocampus.
    GET73
  • HY-A0198
    Adinazolam
    		Agonist ≥99.0%
    Adinazolam (U 41123) is a triazolobenzodiazepine. Adinazolam binds to peripheral-type benzodiazepine receptors which interact allosterically with GABA receptors. Adinazolam has dual anxiolytic and antidepressant activities.
    Adinazolam
  • HY-10061
    Lesogaberan
    		Agonist
    Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
    Lesogaberan
  • HY-133486
    GABAA receptor agent 1
    		98.93%
    GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity.
    GABAA receptor agent 1
  • HY-100664
    Zopiclone N-oxide
    		Agonist ≥98.0%
    Zopiclone N-oxide (RP 29753) is a less active metabolite of Zopiclone. Zopiclone N-oxide is also an impurity of Eszopiclone and is formed by the oxidation of Eszopiclone.
    Zopiclone N-oxide
  • HY-109077
    Tigolaner
    		Antagonist 98.53%
    Tigolaner (BAY-1272858) acts on γ-aminobutyric acid (GABA) and glutamate-gated chloride channels. Tigolaner has antiparasitic activity.
    Tigolaner
  • HY-163855
    KGP-25
    KGP-25 is an inhibitor of voltage-gated sodium channel 1.8 (Nav1.8), which can be used for analgesia by targeting Nav1.8 in the peripheral nervous system (PNS). KGP-25 can also target γ-aminobutyric acid subtype A receptor (GABAA) in the central nervous system (CNS) for general anesthesia.
    KGP-25
  • HY-N2368B
    Arecaidine hydrobromide
    		Inhibitor 98.0%
    Arecaidine hydrobromide, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrobromide is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
    Arecaidine hydrobromide
  • HY-154436
    Anticonvulsant agent 2
    		Inhibitor
    Anticonvulsant agent 2 is a potent and orally active anticonvulsant agent. Anticonvulsant agent 2 shows antiepileptic activity.
    Anticonvulsant agent 2
  • HY-19872
    AZD-6280
    		Modulator 99.09%
    AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
    AZD-6280
  • HY-B2090
    Pipazethate
    		Antagonist ≥99.0%
    Pipazethate (SKF 70230A), a pyridobenzothiazine derivative, is a potent GABA antagonist. Pipazethate has antitussive activity. Pipazethate can be used in research in cough supressant.
    Pipazethate
  • HY-106316
    CGS 20625
    		Agonist 99.80%
    CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 can be used for the research of pentylenetetrazol-induced seizures.
    CGS 20625
  • HY-131885
    RuBi-Glutamate hexafluorophosphate sodium
    RuBi-Glutamate hexafluorophosphate sodium is a novel cage glutamate compound based on ruthenium photochemistry. RuBi-Glutamate hexafluorophosphate sodium can be excited at visible wavelengths and release glutamate after single or two-photon excitation. It has high quantum efficiency and can be used at low concentrations, partially avoiding the blocking of GABA energy transmission by other cage compounds. Two-photon release of RuBi-Glutamate hexafluorophosphate sodium has high spatial resolution and produces a physiodynamic excitatory response in a single dendritic spine.
    RuBi-Glutamate hexafluorophosphate sodium
  • HY-124534
    (1S,3R)-3-Aminocyclopentane carboxylic acid
    		≥98.0%
    (1S,3R)-3-Aminocyclopentane carboxylic acid has GABAA receptor activity.
    (1S,3R)-3-Aminocyclopentane carboxylic acid
  • HY-123840
    MRK-623
    		Agonist
    MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect.
    MRK-623
Cat. No. Product Name / Synonyms Application Reactivity