GABA Receptor
Gamma-aminobutyric acid Receptor; γ-Aminobutyric acid Receptor
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.
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GABA Receptor Inhibitors
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GABA Receptor Agonists
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GABA Receptor Antagonists
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GABA Receptor Activators
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GABA Receptor Modulators
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GABA Receptor Controls
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GABA Receptor Ligands
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GABA Receptor Related Products (788)
Related Products (788)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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Withasomniferolide B
0 ImagesCat. No.: HY-N10887CAS No.: 2365386-75-8Withasomniferolide B is a withanolide. Withasomniferolide B can be isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera.
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COR659
0 ImagesCOR659 is a potent and effective GABAB positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats.
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2'-O-Methylisoliquiritigenin
0 Images2'-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.
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γ-Acetylenic GABA
0 ImagesCat. No.: HY-131693CAS No.: 57659-38-8Synonyms: GAGγ-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.
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U93631
0 ImagesU93631 is a GABAA receptor inhibitor targeting the picrotoxin (HY-101391) site, which exhibits higher inhibitory potency in receptors lacking α subunits. U93631 blocks GABA-induced chloride currents, exerts a mild initial stimulatory effect on activated currents, but its activity decreases in β2T246F mutant receptors. U93631 can serve as a ligand for the convulsant site of GABAA receptors in relevant studies.
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L-DABA hydrobromide
0 ImagesSynonyms: L-2,4-Diaminobutyric acid hydrobromideL-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.
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Phenelzine-d5 sulfate
0 ImagesPhenelzine-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.
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NS-2710
0 ImagesNS-2710 is a high-efficacy GABAAα3 agonist with a Ki of 9.2 nM. NS-2710 can be used for anxiety research.
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Caramboxin
0 ImagesCaramboxin is a phenylalanine-like α-amino acid neurotoxin found in star fruit (Averrhoa carambola) with glutamatergic ionotropic action. Caramboxin activates NMDA, AMPA, and kainate receptors while inhibiting GABA binding to synaptic membranes, shifting the CNS toward an excitatory state and exerting neurotoxic effects linked to star fruit ingestion. Caramboxin can be used for research on neurotoxicity and as a reference standard for toxicological studies.
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Bis(7)-tacrine dihydrochloride
0 ImagesBis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABAAreceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .
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MIDD0301
0 ImagesSynonyms: GL-II-93MIDD0301 (GL-II-93) is an orally available, active γ-aminobutyric acid type A receptor (GABAAR) inhibitor and anti-asthmatic agent. MIDD0301 exhibits biological and immunotoxicological safety in mice and does not affect the number of circulating lymphocytes, monocytes, and granulocytes. MIDD0301 has no significant adverse immune response at repeated doses, which is better than Prednisone (HY-B0214). MIDD0301 relaxes histamine-contracted guinea pig and human airway smooth muscle and is used in the study of bronchoconstrictive diseases.
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Radequinil
0 ImagesSynonyms: AC-3933Radequinil (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.
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RuBi-GABA
0 ImagesCat. No.: HY-103527CAS No.: 1028141-88-9RuBi-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.
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CGP46381
0 ImagesCat. No.: HY-103532CAS No.: 123691-14-5CGP 46381 is an orally active GABAB receptor antagonist with IC50 of 4.9 μM. CGP 46381 blocks the neuronal depression induced by iontophoretically applied baclofen (HY-B0007) .
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Abecarnil
0 ImagesSynonyms: ZK 112119Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.
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Diproqualone
0 ImagesSynonyms: (±)-Diproqualonediproqualone is methaqualone analogous with sedative, anxiolytic, anti-inflammatory and analgesic properties.
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Topiramate D12
0 ImagesCat. No.: HY-110234CAS No.: 1279037-95-4Synonyms: McN 4853 D12 ; RWJ 17021 D12Topiramate D12 (McN 4853 D12) is a deuterium labeled Topiramate. Topiramate is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
