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 (782)
Related Products (782)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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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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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.
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PF-0713
0 ImagesCat. No.: HY-117257CAS No.: 1083093-47-3PF 0713 is a GABAA receptor agonist..
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Loreclezole (Standard)
0 ImagesSynonyms: R 72063 (Standard)Loreclezole (Standard) is the analytical standard of Loreclezole. This product is intended for research and analytical applications. Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
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Imidazenil
0 ImagesImidazenil is a partial positive allosteric modulator of GABAA receptors with anxiolytic, antipanic and anticonvulsant activities.
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Cartazolate
0 ImagesCat. No.: HY-183471CAS No.: 34966-41-1Synonyms: SQ 65396Cartazolate (SQ 65396) is a pyrazolopyridine modulator with benzodiazepine receptor agonist activity and cyclic AMP phosphodiesterase inhibitory activity. Cartazolate enhances the affinity of 3H-diazepam for brain-specific binding sites, regulates the GABA/benzodiazepine receptor complex, reversibly increases Na+-independent GABA receptor binding sites, and stimulates the binding of [3H]flunitrazepam to cerebellar membranes. Cartazolate restores punishment-suppressed behavior and exhibits anxiolytic properties. Cartazolate is applicable to anxiety-related research.
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Tiagabine-d6
0 ImagesCat. No.: HY-B0696SCAS No.: 1217672-34-8Synonyms: NO050328-d6; NO328-d6; TGB-d6Tiagabine-d6 (NO050328-d6) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease.
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Thiocolchicoside (Standard)
0 ImagesThiocolchicoside (Standard) is the analytical standard of Thiocolchicoside. This product is intended for research and analytical applications. Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties.
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CPP-115 hydrochloride
0 ImagesCat. No.: HY-W1025152CAS No.: 760947-97-5CPP-115 hydrochloride is an orally active, selective GABA-AT inhibitor with a Ki value of 9.7 μM. CPP-115 hydrochloride blocks GABA degradation and increases GABA levels in the brain. CPP-115 hydrochloride does not bind to GABA transporters, does not displace GABA from GABAA/GABAB receptors, and does not act as an agonist/antagonist of GABAC receptors. CPP-115 hydrochloride reduces cocaine-induced dopamine release, blocks cocaine-induced conditioned place preference, and suppresses seizure activity in a rat model of infantile spasms. CPP-115 hydrochloride can be used in research related to infantile spasms and epilepsy.
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CGP52432 (Standard)
0 ImagesCat. No.: HY-103531RCAS No.: 139667-74-6
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Imepitoin (Standard)
0 ImagesSynonyms: AWD 131-138 (Standard)Imepitoin (Standard) is the analytical standard of Imepitoin. This product is intended for research and analytical applications. Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
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Afloqualone-d7
0 ImagesCat. No.: HY-B1833SSynonyms: HQ-495-d7Afloqualone-d7 (HQ-495-d7) is deuterium labeled Afloqualone. Afloqualone (HQ-495) is an orally active central muscle relaxant and antivertiginous agent that can increase the sensitivity of GABA receptors in neurons of the lateral vestibular nucleus. Afloqualone (HQ-495) can be used in the research of low back pain and neck-arm-shoulder syndrome.
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3,4,5-Trimethoxycinnamic acid (Standard)
0 Images3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits.
