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-138014
    Cinazepam
    		Agonist
    Cinazepam is a partial GABAA receptor agonist and a benzodiazepine derivative with anxiolytic and sedative properties. Cinazepam can be utilized in research related to sleep disorders.
    Cinazepam
  • HY-164322
    Cyproflanilide
    		Antagonist
    Cyproflanilide is an insecticide. Cyproflanilide is a GABAR antagonist. Cyproflanilide shows high activity against a variety of pests, including lepidopteran, coleopteran, and thysanopteran pests.
    Cyproflanilide
  • HY-B0122S1
    Topiramate-13C
    		Activator
    Topiramate-13C (McN 4853-13C) is 13C labeled Topiramate. 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-<sup>13</sup>C<sub>
  • HY-120276
    Golexanolone
    		Antagonist
    Golexanolone is a GABAA receptor modulating steroid antagonist. Golexanolone reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in hyperammonemic rats.
    Golexanolone
  • HY-114685
    S-8510 free base
    		Antagonist
    S-8510 free base is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.
    S-8510 free base
  • HY-101869R
    MK-0343 (Standard)
    		Agonist
    MK-0343 (Standard) is the analytical standard of MK-0343. This product is intended for research and analytical applications. MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic[1].
    MK-0343 (Standard)
  • HY-11065A
    (iodo-125)-CGP 71872
    		Antagonist
    (iodo-125)-CGP 71872 is a iodo-125-labeled CGP 71872 (GABABR1 receptor agonist),containing an azido group that can be photoactivated,and can be used to characterize GABAB receptors.
    (iodo-125)-CGP 71872
  • HY-N8852
    6-Methoxyflavanone
    		Modulator 98.95%
    6-Methoxyflavanone (6-MeOF) is an orally active flavonoid compound. 6-Methoxyflavanone has anxiolytic properties. 6-Methoxyflavanone targets unique sites on GABA-A receptors, different from traditional benzodiazepines. 6-Methoxyflavanone can be used to study anxiety disorders. 6-Methoxyflavanone readily crosses the blood brain barrier (BBB).
    6-Methoxyflavanone
  • HY-14843
    Imagabalin
    Imagabalin (PD-0332334 free base) is an active compound with activity for studying neurological diseases. The synthesis of imagabalin involves the reaction of 3-methylvaleric acid and Meldrum acid. During the synthesis of imagabalin, an acyl chloride intermediate species, 3-methylvaleryl chloride, was revealed for the first time. The synthesis of imagabalin also provided new information about the reaction mechanism, indicating that 3-methylvaleric anhydride is an important intermediate.
    Imagabalin
  • HY-106875
    Saripidem
    		Modulator
    Saripidem is a non-selective ligand for ω modulatory sites of GABA receptor.
    Saripidem
  • HY-114706
    Suritozole
    Suritozole (MGL-26479) is a cognitive enhancer that acts as a partial inverse agonist of benzodiazepine receptor sites on GABAA ion channel complexes. Suritozole can be used in the study of neurodegenerative diseases.
    Suritozole
  • HY-160105
    GABAB receptor antagonist 3
    		Antagonist
    GABAB receptor antagonist 3 (example 3) is a antagonist of GABAB receptor.
    GABAB receptor antagonist 3
  • HY-136942
    DS1
    		Agonist
    DS1 is a potent GABAA agonist. DS1 increases the activity of serum response element (SRE) and cAMP response element (CRE) promoters. DS1 induces luteinizing hormone beta (LHbeta) and follicle-stimulating hormone beta (FSHbeta) promoter activity.
    DS1
  • HY-167658
    Tuclazepam
    Tuclazepam (KC 1956) is a derivative of benzodiazepines that has anti-anxiety and sedative effects.
    Tuclazepam
  • HY-129710
    CGP47656
    		Agonist
    CGP47656 is a potent GABAB receptor agonist that inhibits Forskolin (HY-15371)-stimulated adenylyl cyclase activity and augments noradrenaline-stimulated adenylyl cyclase activity. CGP47656 is promising for research of brain function-related diseases.
    CGP47656
  • HY-101059R
    FGIN 1-27 (Standard)
    		Agonist
    FGIN 1-27 (Standard) is the analytical standard of FGIN 1-27. This product is intended for research and analytical applications. FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions[1].
    FGIN 1-27 (Standard)
  • HY-W765182
    Emamectin-d3
    		Agonist
    Emamectin-d3 is the deuterium labeled Emamectin. Radioactive isotopes labeled compounds can be used in metabolic analysis, allowing the movement of individual atoms to be precisely tracked and quantified. Emamectin is a macrocyclic lactone insecticide. Emamectin acts as agonist for GABA-gated chloride channels.
    Emamectin-d<sub>3</sub>
  • HY-14856
    Atagabalin
    		Agonist
    Atagabalin (PD 0200390) is a selective GABA (gamma-aminobutyric acid) receptor agonist with antianxiety and sedative effects. Atagabalin enhances the activity of the GABA receptor by binding to the α2δ subunit of the GABA receptor, thereby increasing the GABA mediated inhibition. This enhancement results in reduced excitability of neurons, helping to reduce anxiety and improve sleep. Atagabalin can be used to study neuropsychiatric disorders, anxiety or sleep disorders.
    Atagabalin
  • HY-17354A
    (R)-Baclofen hydrochloride
    		Agonist
    (R)-Baclofen hydrochloride (Arbaclofen hydrochloride) is a selective GABAB receptor agonist.
    (R)-Baclofen hydrochloride
  • HY-121877S
    Valnoctamide-d5
    Valnoctamide-d5 is the deuterium labeled Valnoctamide. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors[1][2].
    Valnoctamide-d<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity