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-N0067
    γ-Aminobutyric acid
    		Agonist 99.71%
    γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system.
    γ-Aminobutyric acid
  • HY-N0219
    Bicuculline
    		Antagonist 99.97%
    Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice.
    Bicuculline
  • HY-107994
    Aminooxyacetic acid hemihydrochloride
    		Inhibitor ≥98.0%
    Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
    Aminooxyacetic acid hemihydrochloride
  • HY-B0649
    Propofol
    		Activator 99.82%
    Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
    Propofol
  • HY-103533
    Gabazine
    		Antagonist 98.72%
    Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
    Gabazine
  • HY-W015050
    1-Anthramine
    		Agonist 98.74%
    1-Anthramine (1-aminoanthracene) is a fluorescent general anesthetic. potentiates GABAergic transmission with Kd = 0.1 mM, for binding to the general anesthetic site in horse spleen apoferritin (HSAF). 1-Anthramine fluorescence is enhanced when bound to HSAF. 1-Anthramine potentiates chloride currents elicited by GABA. 1-Anthramine can reversibly inhibit the movement of Xenopus laevis, with an EC50 value of 16 μM.
    1-Anthramine
  • HY-179215
    OV329 hydrochloride
    		Inhibitor 99.83%
    OV329 hydrochloride is a potent GABA aminotransferase inactivator. OV329 hydrochloride is a Vigabatrin (HY-15399) analogue. OV329 hydrochloride can increase brain GABA levels and block abnormal intracerebral hyperexcitability. OV329 hydrochloride exhibits anticonvulsant and antiepileptic activities. OV329 hydrochloride can be used for the research of neurological disease, such as seizure.
    OV329 hydrochloride
  • HY-179215A
    OV329
    		Inhibitor
    OV329 is a potent GABA aminotransferase inactivator. OV329 is a Vigabatrin (HY-15399) analogue. OV329 can increase brain GABA levels and block abnormal intracerebral hyperexcitability. OV329 exhibits anticonvulsant and antiepileptic activities. OV329 can be used for the research of neurological disease, such as seizure.
    OV329
  • HY-B0211
    Riluzole
    		Inhibitor 99.80%
    Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
    Riluzole
  • HY-B0135
    Furosemide
    		Antagonist 99.83%
    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
  • HY-B0007
    Baclofen
    		Agonist 99.98%
    Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist with blood-brain barrier permeability. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.
    Baclofen
  • HY-N0662
    Amentoflavone
    		Modulator 99.66%
    Amentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase.
    Amentoflavone
  • HY-15399
    Vigabatrin
    		Inhibitor 99.91%
    Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
    Vigabatrin
  • HY-B0692
    Cefepime
    		Inhibitor 99.86%
    Cefepime (BMY-28142) is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC50 of 21.115 mM and a Ki of 35.092 mM. Cefepime inhibits hPON1 via a non-competitive mechanism and blocks GABAA receptors. Cefepime penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.
    Cefepime
  • HY-113416
    Dehydroepiandrosterone sulfate
    		Antagonist 99.93%
    Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate 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 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 may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
    Dehydroepiandrosterone sulfate
  • HY-13694
    Methionine
    		Activator 99.91%
    Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
    Methionine
  • HY-B0504
    Creatinine
    		Modulator 99.92%
    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
  • HY-B0009
    Flumazenil
    		Antagonist 99.99%
    Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
    Flumazenil
  • HY-B1494
    Picrotoxinin
    		Antagonist 99.91%
    Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
    Picrotoxinin
  • HY-B0122
    Topiramate
    		Activator 99.76%
    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
Cat. No. Product Name / Synonyms Application Reactivity