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-W050122
    S-(+)-GABOB
    S-(+)-GABOB is an endogenous ligand with antiepileptic activity. S-(+)-GABOB is a metabolite of GABA and may function as a neurotransmitter. S-(+)-GABOB behaves as a full agonist when bound to the ρ(1) wild-type receptor. S-(+)-GABOB acts as a competitive antagonist in the ρ(1) T244S mutant receptor.
    S-(+)-GABOB
  • HY-N2368A
    Arecaidine hydrochloride
    		Inhibitor 98.00%
    Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
    Arecaidine hydrochloride
  • HY-U00315
    Gidazepam
    		Agonist 98.03%
    Gidazepam is an agonist of GABA receptor channels (GABA RCs).
    Gidazepam
  • HY-W103105
    R 29676
    		Antagonist
    R 29676 is a neuroleptic agent and inhibits sodium-dependent GABA binding (GABA uptake).
    R 29676
  • 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-W015793
    6-Aminonicotinic acid
    		Agonist 99.86%
    6-Aminonicotinic acid is a GABAA receptor agonist with Ki value of 4.4 nM.
    6-Aminonicotinic acid
  • HY-B0007C
    Baclofen hydrochloride
    		Agonist 99.20%
    Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research.
    Baclofen hydrochloride
  • 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-103534
    CI-966 hydrochloride
    		Inhibitor ≥99.0%
    CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities.
    CI-966 hydrochloride
  • HY-W008645
    NCS-382 sodium
    		Antagonist ≥99.0%
    NCS-382 (sodium) is a potent GABA receptor antagonist. NCS-382 (sodium) has anti-sedative and anti-hypnotic activities and can be used in research related to neurological diseases.
    NCS-382 sodium
  • 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-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-105056
    Bretazenil
    		Agonist 99.13%
    Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects.
    Bretazenil
  • 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-15831
    L-838417-d9
    		99.71%
    L-838417-d9 is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].
    L-838417-d<sub>9</sub>
  • HY-108295
    Pivagabine
    		Antagonist ≥98.0%
    Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain.
    Pivagabine
  • HY-107151
    ABP-700
    		Agonist 98.53%
    ABP-700, an Etomidate analog and anesthetic, is a γ-aminobutyric acid type receptor agonist.
    ABP-700
  • 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
Cat. No. Product Name / Synonyms Application Reactivity