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-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-100812
    2-Hydroxysaclofen
    		Antagonist ≥98.0%
    2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats.
    2-Hydroxysaclofen
  • HY-103512
    TP003
    		Agonist 98.99%
    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-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-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-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-B1229
    Isovaleramide
    		Modulator ≥98.0%
    Isovaleramide (3-Methylbutanamide) is an orally active anticonvulsant. Isovaleramide inhibits alcohol dehydrogenase (ADH) activity and regulates GABAergic system. Isovaleramide reduces acute kidney injury. Isovaleramide has antiepileptic, anxiolytic, sedative and hypnotic effects[1].
    Isovaleramide
  • HY-118635
    Cyprodenate
    		Antagonist ≥98.0%
    Cyprodenate (Actebral) is an orally active psychotonic brain activator. Cyprodenate can be used for the research of metabolism.
    Cyprodenate
  • HY-107482
    Picamilon
    		Agonist 98.25%
    Picamilon is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.
    Picamilon
  • HY-133594
    Sandaracopimaric acid
    		Inhibitor 98.86%
    Sandaracopimaric acid is a diterpenoid with anti-inflammatory effect. Sandaracopimaric acid reduces the contraction of phenylephrine-induced pulmonary arteries with an EC50 of 43.93 μM.
    Sandaracopimaric acid
  • HY-100140
    Pipequaline
    		Agonist 99.77%
    Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
    Pipequaline
  • HY-11048
    NS11394
    		Modulator 99.77%
    NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
    NS11394
  • 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-137494
    Ethyl β-carboline-3-carboxylate
    		99.75%
    Ethyl β-carboline-3-carboxylate (fl-CCE) is a ligand and short-acting antagonist of benzodiazepine receptors. Ethyl β-carboline-3-carboxylate did not affect cerebellar cGMP levels when used alone, but when taken together with Diazepam, it significantly inhibited the cGMP levels that were upregulated by Diazepam.
    Ethyl β-carboline-3-carboxylate
  • HY-101639
    CP-409092
    		Agonist
    CP-409092 is a partial agonist of GABAA receptor, with anti-anxiety activity.
    CP-409092
Cat. No. Product Name / Synonyms Application Reactivity