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-143831S
    Cefepime-d8 sulfate
    		Inhibitor 99.21%
    Cefepime-d8 (BMY-28142-d8) sulfate is deuterium labeled Cefepime sulfate. Cefepime sulfate is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC50 of 21.115 mM and a Ki of 35.092 mM. Cefepime sulfate inhibits hPON1 via a non-competitive mechanism and blocks GABAA receptors. Cefepime sulfate penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.
    Cefepime-d<sub>8</sub> sulfate
  • HY-B0616R
    Cefepime Dihydrochloride Monohydrate (Standard)
    		Inhibitor
    Cefepime (BMY-28142) Dihydrochloride Monohydrate (Standard) is the analytical standard of Cefepime Dihydrochloride Monohydrate. This product is intended for research and analytical applications. Cefepime Dihydrochloride Monohydrate is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC50 of 21.115 mM and a Ki of 35.092 mM. Cefepime Dihydrochloride Monohydrate inhibits hPON1 via a non-competitive mechanism and blocks GABAA receptors. Cefepime Dihydrochloride Monohydrate penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.
    Cefepime Dihydrochloride Monohydrate (Standard)
  • 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-177552
    4''-Oxoavermectin B1a
    		Ligand 98.0%
    4''-Oxoavermectin B1a is a potentiator targeting GABA (γ-aminobutyric acid) and glutamate-gated chloride channels with insecticidal and acaricidal activities. 4''-Oxoavermectin B1a is promising for research of agricultural pests.
    4''-Oxoavermectin B1a
  • 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-B0822S1
    Fipronil-13C6
    		Antagonist 98%
    Fipronil-13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
    Fipronil-<sup>13</sup>C<sub>6</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-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-129927
    Thiomuscimol
    		Agonist 99.90%
    Thiomuscimol is a GABAA receptor agonist (IC50=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.
    Thiomuscimol
  • 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-E70570
    Glutamate decarboxylase
    Glutamate decarboxylase is an enzyme that catalyzes the decarboxylation of glutamate to gamma-aminobutyric acid (GABA) and carbon dioxide (CO2). Many gut microbes can metabolize glutamate via their Glutamate decarboxylase in a pyridoxal-5′-phosphate (PLP) dependent manner.
    Glutamate decarboxylase
  • HY-117979
    Alphadolone
    		Agonist 98.71%
    Alphadolone is a GABAA receptor positive allosteric modulator. Alphadolone has antinociceptive effects. Alphadolone causes general anaesthesia.
    Alphadolone
  • 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-N10887
    Withasomniferolide B
    Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera.
    Withasomniferolide B
  • HY-N1745
    2'-O-Methylisoliquiritigenin
    		Activator 99.06%
    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-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-101414A
    L-DABA hydrobromide
    		Inhibitor 98.0%
    L-DABA (L-2,4-Diaminobutyric acid) hydrobromide is a week GABA transaminase inhibitor with an IC50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.
    L-DABA hydrobromide
Cat. No. Product Name / Synonyms Application Reactivity