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-B0504S1
    Creatinine-13C
    		Modulator 99.93%
    Creatinine-13C is the 13C-labeled Creatinine. Creatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure.
    Creatinine-<sup>13</sup>C
  • HY-W041333
    Phenibut hydrochloride
    		Agonist 98.0%
    Phenibut (β-Phenyl-GABA) hydrochloride is an orally active GABA-B agonist. Phenibut hydrochloride acts as a GABA-mimetic, primarily at GABAB?receptors. Phenibut hydrochloride has anxiolytic and nootropic (cognition enhancing) effects.
    Phenibut hydrochloride
  • HY-100783
    (-)-Bicuculline methobromide
    		Antagonist 99.94%
    (-)-Bicuculline methobromide is a potent GABAA blocker. (-)-Bicuculline methobromide alters membrane properties and firing pattern. (-)-Bicuculline methobromide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. (-)-Bicuculline methobromide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.
    (-)-Bicuculline methobromide
  • HY-141921S
    Dehydroepiandrosterone sulfate sodium-d6
    		Antagonist 99.61%
    Dehydroepiandrosterone sulfate sodium salt-d6 (DHEA sulfate sodium salt-d6; Prasterone sulfate sodium salt-d6) is the deuterium labeled Dehydroepiandrosterone sulfate sodium salt (HY-B0765). Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium salt is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium salt has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium salt 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 salt 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 salt may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate sodium-d<sub>6</sub>
  • HY-N6630
    6-Methylflavone
    		Activator 99.77%
    6-Methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.
    6-Methylflavone
  • HY-Y1683
    DL-Menthol
    		Activator 98.0%
    DL-Menthol (Racementhol) is an orally active, GABAaR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABAAR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production.
    DL-Menthol
  • HY-W012738S
    DL-Pyroglutamic acid-d5
    		99.21%
    DL-Pyroglutamic acid-d5 is the deuterium labeled DL-Pyroglutamic acid.
    DL-Pyroglutamic acid-d<sub>5</sub>
  • HY-A0173
    Progabide
    		Agonist 98.50%
    Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.
    Progabide
  • HY-103528
    SCS
    		Inhibitor 98.68%
    SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions.
    SCS
  • HY-108403
    Phenibut
    		Agonist 99.88%
    Phenibut (β-Phenyl-GABA) is a GABA-B agonist. Phenibut acts as a GABA-mimetic, primarily at GABAB receptors. Phenibut has anxiolytic and nootropic (cognition enhancing) effects.
    Phenibut
  • HY-B0135R
    Furosemide (Standard)
    		Antagonist
    Furosemide (Standard) is the analytical standard of Furosemide. This product is intended for research and analytical applications. Furosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
    Furosemide (Standard)
  • HY-N0449
    Nordihydrocapsaicin
    		Modulator 99.82%
    Nordihydrocapsaicin, an analog of Capsaicin (HY-10448), is an orally active compound with pungent properties and anti-cancer activities, which is found in fresh and processed peppers. Nordihydrocapsaicin can cause a burning sensation when consumed.
    Nordihydrocapsaicin
  • HY-B1671
    (+)-Kavain
    		99.98%
    (+)-Kavain, a main kavalactone that can be extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.
    (+)-Kavain
  • HY-B0339R
    Primidone (Standard)
    		Antagonist
    Primidone (Standard) is the analytical standard of Primidone. This product is intended for research and analytical applications. Primidone is the orally active inhibitor for TRPM3 (IC50 = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent.
    Primidone (Standard)
  • 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-W050162
    (E)-3,4,5-Trimethoxycinnamic acid
    		Agonist 99.90%
    (E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A receptor, with IC50 values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy.
    (E)-3,4,5-Trimethoxycinnamic acid
  • HY-108690
    Fluxametamide
    		Antagonist 99.45%
    Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
    Fluxametamide
  • HY-13694S1
    Methionine-d4
    		Activator 99.76%
    Methionine-d4 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
    Methionine-d<sub>4</sub>
  • HY-15377
    DL-Gabaculine hydrochloride
    		Inhibitor 99.90%
    DL-Gabaculine hydrochloride is a neurotoxin that irreversibly inhibits bacterial pyridoxal phosphate linked γ-aminobutyric acid-α-ketoglutaric acid transaminase with a Ki of 2.86 μM.
    DL-Gabaculine hydrochloride
  • 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
Cat. No. Product Name / Synonyms Application Reactivity