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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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.
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DAA-1106 (Standard)
0 ImagesDAA-1106 (Standard) is the analytical standard of DAA-1106. This product is intended for research and analytical applications. 0
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DL-Menthol (Standard)
0 ImagesDL-Menthol (Standard) is the analytical standard of DL-Menthol. This product is intended for research and analytical applications. DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol relates to the activation of GABAA receptor.
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NS11394 (Standard)
0 ImagesCat. No.: HY-11048RCAS No.: 951650-22-9NS11394 (Standard) is the analytical standard of NS11394 (HY-11048). This product is intended for research and analytical applications. 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.
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Lesogaberan hydrochloride (Standard)
0 ImagesCat. No.: HY-10061BRCAS No.: 2925644-17-1Synonyms: AZD-3355 hydrochloride (Standard)Lesogaberan (hydrochloride) (Standard) is the analytical standard of Lesogaberan (hydrochloride) (HY-10061B). This product is intended for research and analytical applications. Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
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Vigabatrin hydrochloride (Standard)
0 ImagesCat. No.: HY-B0033RCAS No.: 1391054-02-6Synonyms: γ-Vinyl-GABA hydrochloride (Standard)Vigabatrin (hydrochloride) (Standard) is the analytical standard of Vigabatrin (hydrochloride). This product is intended for research and analytical applications. Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
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FG 7142 (Standard)
0 ImagesCat. No.: HY-100991RCAS No.: 78538-74-6Synonyms: ZK 39106 (Standard); LSU-65 (Standard)FG 7142 (Standard) is the analytical standard of FG 7142. This product is intended for research and analytical applications. FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex.
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Ricinine-d3
0 ImagesCat. No.: HY-121944SCAS No.: 1313734-77-8Ricinine-d3 is the d3-labeled Ricinine (HY-121944). Ricinine is a central nervous system stimulant found in Ricinus communis. Ricinine binds near the benzodiazepine site of the GABAA receptor, reducing benzodiazepine binding affinity through an allosteric effect, and shows no interaction with AMPA, 5-HT1A, muscarinic receptors, or α1 adrenergic receptors. Ricinine improves memory consolidation in mice at low doses, while at high doses it induces seizures, an effect that is selectively inhibited by diazepam. Ricinine shortens the lifespan of Anopheles mosquitoes through sugar feeding and promotes the development of Plasmodium falciparum in mosquitoes. Ricinine is used in research related to epilepsy, amnesia, and malaria.
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Flutoprazepam
0 ImagesCat. No.: HY-W681659CAS No.: 25967-29-7Synonyms: KB-509Flutoprazepam (KB-509), a benzodiazepine drug, possesses anticonflict effect. Flutoprazepam (KB-509) prevents maximal electroshock, pentetrazol, and strychnine-induced convulsions in mice.
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Valnoctamide (Standard)
0 ImagesCat. No.: HY-121877RCAS No.: 4171-13-5Synonyms: Valmethamide (Standard)Valnoctamide (Standard) is the analytical standard of Valnoctamide. This product is intended for research and analytical applications. Valnoctamide (Valmethamide), a derivative of valproate, suppresses benzodiazepine-refractory status epilepticus. Valnoctamide (Valmethamide) acts directly on GABAA receptors.
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Chlorothymol
0 ImagesChlothymol is a potent positive modulator of the GABAA receptor subunit LGC-37, anticonvulsant, and antibacterial agent. Chlothymol inhibits Pentylenetetrazol-induced c-fos expression. Chlothymol inhibits the growth of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA) strains, including LAC, with an MIC of 32 μg/mL. Chlorothymol has protective effects against epileptic seizures in various mouse models.
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Pynazolam
0 ImagesCat. No.: HY-184400CAS No.: 2034366-97-5Pynazolam is a predicted positive allosteric modulator of GABAA receptor. 3D-field QSAR and RVM models predict an IC50 of approximately 0.40 nM. Pynazolam can be used in studies related to GABAA receptor pharmacology.
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3-Methoxyphenol (Standard)
0 Images3-Methoxyphenol (Standard) is the analytical standard of 3-Methoxyphenol (HY-Y1840). This product is intended for research and analytical applications. 3-Methoxyphenol is an environmental pollutant. 3-Methoxyphenol occurs in the aroma components of dried bonito. 3-Methoxyphenol potentially enhances GABA-evoked responses of α1β1 GABAA receptors by increasing the affinity of GABA binding sites. 3-Methoxyphenol is used as a flavoring substance in food and animal feed. 3-Methoxyphenol prolongs pentobarbital-induced sleeping time and reduces elevated plus maze behavior.
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Chrodrimanin B
0 ImagesCat. No.: HY-N8472CAS No.: 132196-54-4Chrodrimanin B, a metabolite of a fungal, is a potent, non-open-channel-blocking antagonist on?B.?mori GABAR RDL with an IC50?of 1.13 nM. Chrodrimanin B attenuates the peak current amplitude of the GABA response of RDL with an IC50?of 1.66 nM.?Chrodrimanin B, a meroterpenoid, shows insecticidal activity.
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Flumazenil (Standard)
0 ImagesSynonyms: Ro 15-1788 (Standard)Flumazenil (Standard) is the analytical standard of Flumazenil. This product is intended for research and analytical applications. Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
