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-118844
    Flumazenil acid
    		Antagonist 99.97%
    Flumazenil acid is a metabolite of Flumazenil. Flumazenil is a GABAA receptor antagonist.
    Flumazenil acid
  • HY-116813
    ZK 93423
    		Agonist 99.43%
    ZK 93423 is a potent benzodiazepine GABAA receptor agonist with a certain cooling effect on rodents.
    ZK 93423
  • HY-125296
    Fipronil sulfone
    		Inhibitor 99.75%
    Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
    Fipronil sulfone
  • HY-W009009
    L-838417
    		Modulator 99.22%
    L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.
    L-838417
  • HY-W105694
    3-Aminopropylphosphonic acid
    		Agonist ≥98.0%
    3-Aminopropylphosphonic acid ((3-Aminopropyl)phosphonic acid) is a phosphonic acid analogue of GABA and a GABAB receptor agonist.
    3-Aminopropylphosphonic acid
  • 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-115685
    3-Methyl-GABA
    		Activator 99.86%
    3-Methyl-GABA is a potent GABA aminotransferase activator. 3-Methyl-GABA can fit the binding pocket of GABAA receptor (GABAaR). 3-Methyl-GABA can activate L-glutamic acid decarboxylase (GAD). 3-Methyl-GABA has anticonvulsant activity.
    3-Methyl-GABA
  • 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-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-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-Y0313S
    p-Hydroxybenzaldehyde-d4
    		Antagonist 99.65%
    p-Hydroxybenzaldehyde-d4 is the deuterium labeled p-Hydroxybenzaldehyde. p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
    p-Hydroxybenzaldehyde-d<sub>4</sub>
  • HY-W008645
    NCS-382 sodium
    		Antagonist ≥99.0%
    NCS-382 (sodium) is a potent GABA receptor antagonist. NCS-382 (sodium) has anti-sedative and anti-hypnotic activities and can be used in research related to neurological diseases.
    NCS-382 sodium
  • 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-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-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-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
Cat. No. Product Name / Synonyms Application Reactivity