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 (795)
Related Products (795)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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AZD7325 (Standard)
0 ImagesAZD7325 (Standard) is the analytical standard of AZD7325. This product is intended for research and analytical applications. AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
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Bemegride (Standard)
0 ImagesSynonyms: 3-Ethyl-3-methylglutarimide (Standard); Bemegrid (Standard)Bemegride (Standard) is the analytical standard of Bemegride. This product is intended for research and analytical applications. Bemegride (3-Ethyl-3-methylglutarimide) is a central nervous system stimulant and antidote for barbiturate poisoning.
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Miltirone (Standard)
0 ImagesCat. No.: HY-N1951RCAS No.: 27210-57-7Synonyms: Rosmariquinone (Standard)Miltirone is an orally active natural compound found in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM. Miltirone induces ROS - and-p53 dependent apoptosis. Miltirone inhibits carboxylesterase 2 (CES2; Ki = 0.04 μM) and SARS-CoV main protease (Mpro).
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RO 4938581 (Standard)
0 ImagesCat. No.: HY-107489RCAS No.: 883093-10-5RO 4938581 (Standard) is the analytical standard of RO 4938581 (HY-107489). This product is intended for research and analytical applications. RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
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CGP 62349
0 ImagesCat. No.: HY-120192CAS No.: 187608-26-0CGP 62349 is a selective and orally active GABAB receptor antagonist that improves cognitive performance in multiple learning paradigms.
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THIP (Standard)
0 ImagesSynonyms: Gaboxadol (Standard)THIP (Gaboxadol) Standard is the analytical standard of THIP (HY-10232). This product is intended for research and analytical applications. THIP (Gaboxadol) is a blood-brain barrier-penetrant, orally active selective GABAA receptor agonist. THIP exhibits EC50 values of 33 μM and 130 μM for α4β2δ and α4β1δ receptors, respectively. THIP activates extrasynaptic GABAA receptors to produce tonic inhibition and inhibits GABAergic interneurons to cause disinhibition. THIP is used in research on insomnia, sleep disorders, and addictive behaviors.
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Arecaidine hydrochloride (Standard)
0 ImagesCat. No.: HY-N2368ARCAS No.: 6018-28-6Arecaidine hydrochloride (Standard) is the analytical standard of Arecaidine hydrochloride (HY-N2368A). This product is intended for research and analytical applications. Arecaidine hydrochloride is a GABA transport system inhibitor. Arecaidine hydrochloride inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine hydrochloride inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine hydrochloride inhibits hPAT1-mediated L-[3H]proline uptake in cells. Arecaidine hydrochloride can be used in research related to neurological diseases.
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CGP 36742 (Standard)
0 ImagesCat. No.: HY-121599RCAS No.: 123690-78-8Synonyms: SGS-742 (Standard)CGP 36742 (Standard) is the analytical standard of CGP 36742. This product is intended for research and analytical applications. CGP 36742 (SGS-742) is an orally active and selective antagonist of GABAB receptor (IC50 = 36 µM). CGP 36742 is a brain-penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study.
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Topiramate-13C6-1
0 ImagesCat. No.: HY-B0122SS1Synonyms: McN 4853-13C6-1; RWJ 17021-13C6-1
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Ciclotizolam
0 ImagesCat. No.: HY-168363CAS No.: 58765-21-2Synonyms: WE-973Ciclotizolam (WE-973) is a thienotriazolodiazepine with anticonvulsant and anti-aggressive activities. Ciclotizolam binds to benzodiazepine receptors in the central nervous system. Ciclotizolam decreases total sleep time in cats.
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Etifoxine-d5
0 ImagesCat. No.: HY-16579AS2CAS No.: 1346598-10-4Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
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Ro15-4513 (Standard)
0 ImagesCat. No.: HY-103476RCAS No.: 91917-65-6Ro15-4513 (Standard) is the analytical standard of Ro15-4513. This product is intended for research and analytical applications. Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect. Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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ZAPA
0 ImagesCat. No.: HY-133722CAS No.: 92138-10-8ZAPA is a competitive GABAC receptor antagonist.
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CGS-9895
0 ImagesCat. No.: HY-129090CAS No.: 77779-50-1CGS-9895 is a GABA antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors.
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Clomethiazole (Standard)
0 ImagesClomethiazole (Standard) is the analytical standard of Clomethiazole. This product is intended for research and analytical applications. Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
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Flupirtine Maleate (Standard)
0 ImagesSynonyms: D 9998 Maleate (Standard)Flupirtine Maleate (Standard) is the analytical standard of Flupirtine Maleate (HY-17001). This product is intended for research and analytical applications. Flupirtine Maleate is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine Maleate is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine Maleate stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine Maleate exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine Maleate functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine Maleate can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis.
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JY-XHe-053
0 ImagesCat. No.: HY-123426CAS No.: 612526-36-0JY-XHe-053 is a potent and selective agonist of GABAA receptors containing the α5 subunit (Kis of 22.0 nM, 12.3 nM, 34.9 nM, 0.7 nM for α1, α2, α3, α5, respectively). JY-XHe-053 lacks significant anti-anxiety activity, despite its efficacy at α2- and α3-GABAA receptors.
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Y-23684
0 ImagesCat. No.: HY-19082CAS No.: 118288-67-8Y-23684 is a partial agonist of benzodiazepine receptor (BZR) with anticonvulsant and anxiolytic activities. Y-23684 can be used in the research of treatment of anxiety disorders.
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Alpidem (Standard)
0 ImagesCat. No.: HY-W013150RCAS No.: 82626-01-5Alpidem (Standard) is the analytical standard of Alpidem (HY-W013150). This product is intended for research and analytical applications. Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.
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Doxefazepam (Standard)
0 ImagesSynonyms: SAS-643 (Standard)Doxefazepam (Standard) (SAS-643 (Standard)) is the analytical standard of Doxefazepam (HY-101808). This product is intended for research and analytical applications. Doxefazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsan and skeletal muscle relaxant properties.
