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 (789)
Related Products (789)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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(+)-Bicuculline methochloride
0 ImagesCat. No.: HY-100783ACAS No.: 53552-05-9(+)-Bicuculline methobromide is a potent GABAA blocker. (+)-Bicuculline methobromide alters membrane properties and firing pattern. (+)-Bicuculline methobromide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. (+)-Bicuculline methobromide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.
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Nav1.2-IN-4
0 ImagesCat. No.: HY-189470Nav1.2-IN-4 is a blood-brain barrier-penetrant NaV1.2 inhibitor (IC50 = 31.21 μM). Nav1.2-IN-4 preferentially blocks the inactivated state of the neuronal voltage-gated sodium channel NaV1.2, inhibiting persistent and resurgent sodium currents associated with epileptogenesis. Nav1.2-IN-4 restores the GABA-glutamate balance by enhancing GABA and reducing glutamate. Nav1.2-IN-4 reduces oxidative stress in brain tissue by increasing GSH and decreasing MDA. Nav1.2-IN-4 protects mice against MES-induced tonic hindlimb extensor seizures and attenuates hippocampal neuronal degeneration in the PTZ kindling model. Nav1.2-IN-4 can be used for research on epilepsy.
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17β-Estradiol sulfate-d6 sodium
0 ImagesCat. No.: HY-W743264Synonyms: 17β-Estradiol 3-sulfate-d3 sodium17β-Estradiol sulfate-d3 sodium (17β-Estradiol 3-sulfate-d3 sodium) is the deuterium labeled 17β-Estradiol sulfate sodium (HY-141672). 17β-Estradiol sulfate sodium, also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid.
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Fominoben
0 ImagesCat. No.: HY-A0177CAS No.: 18053-31-1Fominoben is a type of benzamide-based antitussive agent. Fominoben works by acting on the central nervous system to increase alveolar ventilation, thereby improving the blood oxygen levels in patients with pulmonary diseases (COLD). Fominoben can bind to the benzodiazepine receptor binding sites in the brain and also has anti-anxiety and anti-convulsant effects. Fominoben can be used in research on hypoxemia.
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T-2000
0 ImagesCat. No.: HY-118490CAS No.: 97846-21-4Synonyms: DMMDPBT-2000 (DMMDPB) is an orally active GABA receptor agonist with anticonvulsant activities.
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ENX-101
0 ImagesCat. No.: HY-173251SENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models.
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GABA-IN-2
0 ImagesCat. No.: HY-149400CAS No.: 2363715-13-1GABA-IN-2 (Compound 5) is a GABA inhibitor. GABA-IN-2 has larvicidal activity and insecticidal effect, with mortality rates of 87% at 50 mg/L.
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NNC 05-2090
0 ImagesCat. No.: HY-120146CAS No.: 184845-43-0
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Suriclone
0 ImagesCat. No.: HY-106635CAS No.: 53813-83-5Synonyms: RP31264Suriclone (RP31264) is a GABA receptor agonist. Suriclone is an anxiolytic agent with a high affinity for the benzodiazepine receptors. Suriclone has oral activity.
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GABA-AT-IN-1
0 ImagesCat. No.: HY-147982CAS No.: 242148-96-5GABA-AT-IN-1 (Compound 6) is a γ-aminobutyric acid aminotransferase (GABA-AT) inhibitor and significantly elevates the mouse brain GABA level. GABA-AT-IN-1 has the ability to cross the BBB and can be used as an anticonvulsant.
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Bicyclo-GABA
0 ImagesCat. No.: HY-181135CAS No.: 1615763-33-1Bicyclo-GABA is a selective betaine/GABA transporter 1 (BGT1) competitive, non-transported inhibitor with an IC50 of 590 nM. Bicyclo-GABA exhibits low micromolar agonistic activity at α1β2γ2 GABAA receptors with an EC50 of 5.1 μM. Bicyclo-GABA displays 129 times higher activity for BGT1 than GAT3. Bicyclo-GABA serves as a valuable tool compound for deciphering its elusive pharmacological role in the brain and periphery.
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DOV51892
0 ImagesCat. No.: HY-118502CAS No.: 864673-91-6DOV51892 is a GABAA receptor modulator. DOV51892 has a specific effect on GABAA receptors containing the α1 subunit. DOV51892 exhibits non-sedative anti-anxiety effects. DOV51892 can be used for in-depth research on the function of GABAA receptors.
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GABAA receptor modulator-13
0 ImagesCat. No.: HY-181552GABAA receptor modulator-13 is an orally active, blood-brain barrier-permeable α4β1δ GABAA receptor modulator (IC50 = 9.02 μM). GABAA receptor modulator-13 reduces GABA-induced currents, impairs the stability of the transmembrane domain M2-M3 loop of α4β1δ GABAA receptors, and exhibits selectivity for γ2-containing GABAA receptor subtypes and α6β3δ GABAA receptor subtypes. GABAA receptor modulator-13 is applicable to the research of nervous system diseases with altered tonic inhibition, such as neurodevelopmental disorders and epilepsy.
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Fipronil sulfone (Standard)
0 ImagesCat. No.: HY-125296RCAS No.: 120068-36-2Fipronil sulfone (Standard) is the analytical standard of Fipronil sulfone. This product is intended for research and analytical applications. Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibitsGABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
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L-Cycloserine (Standard)
0 ImagesSynonyms: (S)-Cycloserine (Standard); (S)-4-Amino-3-isoxazolidone (Standard)L-Cycloserine (Standard) is the analytical standard of L-Cycloserine. This product is intended for research and analytical applications. L-Cycloserine ((S)-4-Amino-3-isoxazolidone) is an oral inhibitor of the enzyme gamma-aminobutyric acid (GABA) transaminase (GABA-t) and branched-chain transaminases in Mycobacterium tuberculosis. L-Cycloserine has anticonvulsant properties and inhibits the synthesis of neurotensin in mouse brains[1][2][3][4].
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Kavain (Standard)
0 ImagesKavain (Standard) is the analytical standard of Kavain. This product is intended for research and analytical applications. Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.
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Refisolone
0 ImagesCat. No.: HY-172433CAS No.: 202718-04-5Refisolone is an antagonist of the GABAA receptor.
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GMA-839
0 ImagesCat. No.: HY-117955CAS No.: 162882-76-0Synonyms: WAY 141839; Co 2-6749GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics.
