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-B0211S
    Riluzole-13C,15N2
    		99.90%
    Riluzole-13C,15N2 is the 13C and 15N labeled Riluzole. 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-<sup>13</sup>C,<sup>15</sup>N<sub>2</sub>
  • 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-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-P5188A
    Waglerin-1
    		Inhibitor 98.71%
    Waglerin-1, a 22-amino acid peptide, is a competitive antagonist of the muscle nicotinic receptor (nAChR).
    Waglerin-1
  • HY-P5305A
    GAD65(247-266) epitope TFA
    GAD65(247-266) epitope TFA is the T cell epitopes of islet antigens，binding to I-Ag7 (type I diabetes-associated molecule) competitively with poor affinity. GAD65 refers to Glutamic Acid Decarboxylase 65，involved in the conversion of glutamate to gamma-aminobutyric acid (GABA).
    GAD65(247-266) epitope TFA
  • HY-W001692
    Ocinaplon
    		Agonist 99.70%
    Ocinaplon (DOV 273547) is a partial GABAA receptor positive allosteric modulator with relatively high efficacy at the α1 subunit.
    Ocinaplon
  • HY-N2482A
    Guvacine hydrobromide
    		Inhibitor 98.0%
    Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine hydrobromide inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively.
    Guvacine hydrobromide
  • HY-101665
    Pagoclone
    		Agonist ≥98.0%
    Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial GABA(A) receptor agonist used for the treatment of panic and anxiety disorders.
    Pagoclone
  • HY-129636A
    (E/Z)-CLH304a
    		Antagonist
    (E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors.
    (E/Z)-CLH304a
  • HY-103668A
    SSD114 hydrochloride
    		Agonist 99.13%
    SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
    SSD114 hydrochloride
  • HY-101639A
    CP-409092 hydrochloride
    		Agonist 99.79%
    CP-409092 hydrochloride is a partial agonist of GABAA receptor, with anti-anxiety activity.
    CP-409092 hydrochloride
  • HY-131693
    γ-Acetylenic GABA
    		Inhibitor
    γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain. γ-Acetylenic GABA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    γ-Acetylenic GABA
  • HY-100686
    U93631
    		Inhibitor 99.85%
    U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.
    U93631
  • HY-B1018AS
    Phenelzine-d5 sulfate
    		Inhibitor 99.97%
    Phenelzine-d5 sulfate is the deuterium labeled Phenelzine sulfate (HY-B1018A). Phenelzine sulfate, an antidepressant agent, is an irreversible and orally active monoamine oxidase (MAO-A and MAO-B) inhibitor. Phenelzine sulfate inhibits GABA transaminase and primary amine oxidase (PrAO), and sequester reactive aldehydes. Phenelzine sulfate also inhibits LSD1 (Ki: 5.6 μM) and suppresses oxidative stress and lipogenesis. Phenelzine sulfate elevates neurotransmitters (serotonin, norepinephrine, dopamine). Phenelzine sulfate is studied in neurological, metabolic and cancer diseases for depression and anxiety disorders, stroke, spinal cord injury, traumatic brain injury, multiple sclerosis, Parkinson’s disease, Alzheimer’s disease, inflammatory pain, obesity and prostate cancer.
    Phenelzine-d<sub>5</sub> sulfate
  • HY-19271
    NS-2710
    		Agonist 99.21%
    NS-2710 is a high-efficacy GABAAα3 agonist with a Ki of 9.2 nM. NS-2710 can be used for anxiety research.
    NS-2710
  • HY-N9506
    Anisatin
    		Antagonist ≥99.0%
    Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM.
    Anisatin
  • HY-124467
    Difludiazepam
    Difludiazepam (Ro 07-4065), a benzodiazepine, has binding affinity (0.613) to GABAA receptors.
    Difludiazepam
  • HY-W005749
    (R)-4-Amino-3-hydroxybutyric acid
    		Agonist
    (R)-4-Amino-3-hydroxybutyric acid ((R)-GABOB) is a 4-aminobutyric acids (GABAB) agonist. (R)-4-Amino-3-hydroxybutyric acid is promising for research of nervous disorders.
    (R)-4-Amino-3-hydroxybutyric acid
  • HY-106025
    Radequinil
    		Antagonist 99.25%
    Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively.
    Radequinil
  • HY-103527
    RuBi-GABA
    RuBi-GABA is a new ruthenium-based caged GABA compound. RuBi-GABA photocleaves and releases GABA after being excited with visible wavelengths. RuBi-GABA produces gaba receptor-mediated currents.
    RuBi-GABA
Cat. No. Product Name / Synonyms Application Reactivity