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 (778)
Related Products (778)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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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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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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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.
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CGP35348 (Standard)
0 ImagesCat. No.: HY-103530RCAS No.: 123690-79-9CGP35348 (Standard) is the analytical standard of CGP35348. This product is intended for research and analytical applications. CGP 35348?is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM.?CGP 35348 shows affinity for the GABAB receptor only. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage.
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Saclofen (Standard)
0 ImagesCat. No.: HY-100813RCAS No.: 125464-42-8Saclofen (Standard) is the analytical standard of Saclofen.
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7-Keto-DHEA (Standard)
0 ImagesSynonyms: 7-Oxo-DHEA (Standard); 7-Ketodehydroepiandrosterone (Standard); 7-Oxodehydroepiandrosterone (Standard)7-Keto-DHEA (Standard) (7-Oxo-DHEA (Standard)) is the analytical standard of 7-Keto-DHEA (HY-N9483). This product is intended for research and analytical applications. 7-Keto-DHEA binds to GABA Receptor, and reduces the ethanol intake in rats. 7-Keto-DHEA exhibits potential in investigation of alcohol dependence disorders.
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Fluxametamide (Standard)
0 ImagesCat. No.: HY-108690RCAS No.: 928783-29-3Fluxametamide (Standard) is the analytical standard of Fluxametamide (HY-108690). This product is intended for research and analytical applications. Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
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PNU-107484A
0 ImagesCat. No.: HY-117106CAS No.: 200266-76-8PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl- currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes.
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CI-966 hydrochloride (Standard)
0 ImagesCat. No.: HY-103534RCAS No.: 110283-66-4CI-966 hydrochloride (Standard) is the analytical standard of CI-966 hydrochloride (HY-103534). This product is intended for research and analytical applications. CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities.
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TACA (Standard)
0 ImagesCat. No.: HY-100800RCAS No.: 38090-53-8Synonyms: trans-4-Aminocrotonic acid (Standard)TACA (Standard) is the analytical standard of TACA (HY-100800). This product is intended for research and analytical applications. TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons.
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Etifoxine (Standard)
0 ImagesSynonyms: HOE 36-801 (Standard)Etifoxine (Standard) is the analytical standard of Etifoxine. This product is intended for research and analytical applications. 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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Ethyl dirazepate
0 ImagesCat. No.: HY-101596CAS No.: 23980-14-5Ethyl dirazepate is a agent which is a benzodiazepine derivative. It has anxiolytic and possibly other characteristic benzodiazepine properties.
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Ru-32514
0 ImagesCat. No.: HY-19065CAS No.: 90807-98-0Ru-32514 is an agonist of benzodiazepine receptor.
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U-101017
0 ImagesCat. No.: HY-19250CAS No.: 170568-47-5Synonyms: PNU 101017U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.
