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-103502
    CGP7930
    		Modulator ≥99.0%
    CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons.
    CGP7930
  • HY-131941
    SJM-3
    		Agonist
    SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface.
    SJM-3
  • HY-N2160
    6'''-Feruloylspinosin
    		99.62%
    6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons.
    6'''-Feruloylspinosin
  • HY-B0135R
    Furosemide (Standard)
    		Antagonist 99.95%
    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-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-W015595
    L-Allylglycine HCl
    		Antagonist
    L-Allylglycine HCl is an amino acid derivative. L-Allylglycine HCl is an inhibitor for glutamate decarboxylase (GAD) that reduces the GABA biosynthesis in the brain. L-Allylglycine HCl exhibits convulsant activity.
    L-Allylglycine HCl
  • HY-N1745
    2'-O-Methylisoliquiritigenin
    		Activator 98.44%
    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-B0649S1
    Propofol-d18
    		Activator
    Propofol-d18 is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission[1].
    Propofol-d<sub>18</sub>
  • HY-P2602
    α-Casozepine
    		99.36%
    α-Casozepine is a bioactive peptide derived from the α protein S1 casein in milk and has an affinity for γ-aminobutyric acid (GABA) receptors in the brain. α-Casozepine has anti-anxiety effects.
    α-Casozepine
  • HY-113320S
    Etiocholanolone-d5
    		Modulator 99.20%
    Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].
    Etiocholanolone-d<sub>5</sub>
  • HY-103511
    TCS1105
    		99.66%
    TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion.
    TCS1105
  • 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-137429
    Valiloxibic acid
    Valiloxibic acid is a proagent of γ-Hydroxybutyric acid (GHB).GHB is a naturally occurring neurotransmitter and a psychoactive agent, it acts on the GHB receptor and is a weak agonist at the GABAB receptor.
    Valiloxibic acid
  • 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-B0211R
    Riluzole (Standard)
    		Inhibitor
    Riluzole (Standard) is the analytical standard of Riluzole. This product is intended for research and analytical applications. 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 (Standard)
  • 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-W050162
    (E)-3,4,5-Trimethoxycinnamic acid
    		Agonist 99.95%
    (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-19872
    AZD-6280
    		Modulator 99.09%
    AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
    AZD-6280
  • HY-121116
    CGS 8216
    		Antagonist 99.85%
    CGS 8216, a benzodiazepine receptor antagonist, inhibits 3H-flunitrazepam (3H-FLU) binding to rat synaptosomal membranes in vitro at subnanomolar concentrations.
    CGS 8216
  • HY-W067716
    Spinacine
    		Inhibitor
    Spinacine is an alkaloid inhibitor of GABA (γ-aminobutyric acid) absorption that can be isolated from spinach leaf extract.
    Spinacine
Cat. No. Product Name / Synonyms Application Reactivity