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-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-107482
    Picamilon
    		Agonist 98.25%
    Picamilon is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats.
    Picamilon
  • 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. Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form.
    Etiocholanolone-d<sub>5</sub>
  • HY-N8852
    6-Methoxyflavanone
    		Modulator 98.95%
    6-Methoxyflavanone (6-MeOF) is a flavonoid compound that can cross the blood-brain barrier. 6-Methoxyflavanone is a positive allosteric modulator of GABAA receptors. 6-Methoxyflavanone exhibits positive allosteric regulatory effects on human recombinant α1β2γ2L and α2β2γ2L GABAA receptors, and is relatively inactive on the α1β2 GABAA receptor. 6-Methoxyflavanone showes inhibitory behavior towards the activation of bitter receptor hTAS2R39 and hTAS2R14, demonstrating a reversible and non-overcome antagonistic effect. 6-Methoxyflavanone has the effects of anti-anxiety, analgesia and relief of neuropathic pain.
    6-Methoxyflavanone
  • HY-11048
    NS11394
    		Modulator 99.77%
    NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
    NS11394
  • HY-W015793
    6-Aminonicotinic acid
    		Agonist 99.26%
    6-Aminonicotinic acid is a GABAA receptor agonist with Ki value of 4.4 nM. 6-Aminonicotinic acid can be formed via electrocatalytic synthesis at silver cathodes. 6-Aminonicotinic acid has a variety of biological properties, such as protein synthesis inhibitor, vitamin B3 agonist, and modulating agent in chemotherapy.
    6-Aminonicotinic acid
  • HY-B0696
    Tiagabine
    		Inhibitor 98.49%
    Tiagabine (NO050328) is a potent and selective GABA reuptake inhibitor, used as an anticonvulsant agent, with IC50s of 67, 446 and 182 nM for [3H]GABA uptake in Synaptosomes, Neurons and Glia, respectively.
    Tiagabine
  • HY-128174
    β-CCM
    		Antagonist 98.95%
    β-CCM is a benzodiazepine receptor inverse agonist with anxiogenic and proconvulsant effects. β-CCM enhances emotional reactivity and reduces vulnerability to interference in spatial working memory tasks. β-CCM can be used for research on anxiety-related disorders.
    β-CCM
  • 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-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-101411R
    4-Acetamidobutanoic acid (Standard)
    		Agonist
    Josamycin propionate (Standard) is the analytical standard of Josamycin propionate. This product is intended for research and analytical applications. Josamycin propionate is classified as a macrolide antibiotic.
    4-Acetamidobutanoic acid (Standard)
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity