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-N2482A
    Guvacine hydrobromide
    		Inhibitor 98.0%
    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 98.00%
    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
  • HY-139584
    Temgicoluril
    		Inhibitor 98.03%
    Temgicoluril (Tetramethylglycoluril) is an orally active antianxiety and antidepressant. Temgicoluril acts on GABA receptors to enhance GABA neurotransmission.
    Temgicoluril
  • HY-103503
    CGP13501
    		Modulator 98.01%
    CGP13501 is a positive allosteric modulator of GABAB receptor. CGP13501 is a structural analogue of propofol.
    CGP13501
  • HY-137204
    COR659
    		Activator 99.94%
    COR659 is a potent and effective GABAB positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats.
    COR659
  • HY-N1745
    2'-O-Methylisoliquiritigenin
    		Activator 99.06%
    2'-O-Methylisoliquiritigenin, isolated from the Arachis species, up-regulates 5-HT, NE, DA and GABA pathways, but does not put a very significant effect on ne NE pathway.
    2'-O-Methylisoliquiritigenin
  • HY-100982
    (E) -4-Hydroxycrotonic acid
    		98.0%
    (E)-4-Hydroxycrotonic acid (T-HCA) is a high-affinity ligand for GHB binding sites, with a ki value of 1.1 μM. The introduction of diaryl substituents into (E)-4-Hydroxycrotonic acid significantly enhances its affinity for GHB binding sites, with ki values ranging from 0.023 to 0.075 μM. (E)-4-Hydroxycrotonic acid holds promise for optimizing GHB ligand structures and assisting in the development of effective three-dimensional pharmacophore models.
    (E) -4-Hydroxycrotonic acid
  • HY-123801
    MIDD0301
    		Modulator 98.14%
    MIDD0301 (GL-II-93) is an orally available, active γ-aminobutyric acid type A receptor (GABAAR) inhibitor and anti-asthmatic agent. MIDD0301 exhibits biological and immunotoxicological safety in mice and does not affect the number of circulating lymphocytes, monocytes, and granulocytes. MIDD0301 has no significant adverse immune response at repeated doses, which is better than Prednisone (HY-B0214). MIDD0301 relaxes histamine-contracted guinea pig and human airway smooth muscle and is used in the study of bronchoconstrictive diseases.
    MIDD0301
  • HY-B1326
    Bemegride
    		Antagonist 99.96%
    Bemegride (3-Ethyl-3-methylglutarimide) is a central nervous system stimulant and antidote for barbiturate poisoning.
    Bemegride
  • HY-101060
    FGIN 1-43
    		Inhibitor 98.96%
    FGIN 1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety.
    FGIN 1-43
  • HY-101060
    FGIN 1-43
    		Activator 98.96%
    FGIN 1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety.
    FGIN 1-43
  • 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-141672S1
    17β-Estradiol sulfate-d4 sodium
    		99.57%
    17β-Estradiol sulfate-d4 (sodium) is the deuterium labeled 17β-Estradiol sulfate 17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid.
    17β-Estradiol sulfate-d<sub>4</sub> sodium
  • 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 98.53%
    Tigolaner (BAY-1272858) acts on γ-aminobutyric acid (GABA) and glutamate-gated chloride channels. Tigolaner has antiparasitic activity.
    Tigolaner
  • HY-14953
    Imepitoin
    		Agonist 99.87%
    Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
    Imepitoin
  • 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-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-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
Cat. No. Product Name / Synonyms Application Reactivity