1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. GABA Receptor

GABA Receptor

Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor

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-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-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-B0649
    Propofol
    Activator 99.52%
    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-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-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-123801
    MIDD0301
    Modulator 98.14%
    MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABAA receptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guinea pig and human tracheal smooth muscle for the study of bronchial systolic diseases.
    MIDD0301
  • HY-W105694
    3-Aminopropylphosphonic acid
    Agonist
    3-Aminopropylphosphonic acid is a GABAB receptor agonist with IC50 value of 1.5 μM.
    3-Aminopropylphosphonic acid
  • 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-B0135
    Furosemide
    Antagonist 99.90%
    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-103533
    Gabazine
    Antagonist 99.05%
    Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
    Gabazine
  • HY-B0007
    Baclofen
    Agonist 99.81%
    Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. 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 99.81%
    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-103531
    CGP52432
    Antagonist 98.16%
    CGP52432 is a GABAB receptor antagonist, with an IC50 of 85 nM.
    CGP52432
  • HY-B0009
    Flumazenil
    Antagonist 99.97%
    Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
    Flumazenil
  • HY-15399
    Vigabatrin
    Inhibitor ≥98.0%
    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-B0211A
    Riluzole hydrochloride
    Inhibitor 99.88%
    Riluzole hydrochloride 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 hydrochloride
  • HY-13694
    Methionine
    Activator 99.09%
    Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
    Methionine
  • HY-N0659
    Jujuboside A
    Agonist 99.88%
    Jujuboside A is a glycoside extracted from Semen Ziziphi Spinosae, a Chinese herbal medicine used to treat insomnia and anxiety.
    Jujuboside A
  • HY-10232
    THIP
    Antagonist 99.93%
    THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders.
    THIP
  • HY-113320
    Etiocholanolone
    Modulator 99.31%
    Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form.
    Etiocholanolone
Cat. No. Product Name / Synonyms Application Reactivity