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 (786)
Related Products (786)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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Riluzole-13C,15N2
0 ImagesSynonyms: PK 26124-13C,15N2Riluzole-13C,15N2 is the 13C and 15N labeled Riluzole. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
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Glutamate decarboxylase
0 ImagesGlutamate decarboxylase is an enzyme that catalyzes the decarboxylation of glutamate to gamma-aminobutyric acid (GABA) and carbon dioxide (CO2). Many gut microbes can metabolize glutamate via their Glutamate decarboxylase in a pyridoxal-5′-phosphate (PLP) dependent manner.
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Ocinaplon
0 ImagesSynonyms: DOV 273547Ocinaplon (DOV 273547) is an orally active positive allosteric modulator of GABAA receptor, with an EC50 ranging from 3.07 μM (α1β2γ2 subtype) to 10.03 μM (α1β2γ3 subtype). Ocinaplon enhances GABA-stimulated chloride currents across multiple GABAA receptor subtypes, with varying potency between different subtypes. Ocinaplon exerts anxiolytic and anticonvulsant effects, and causes motor impairment at high doses. Ocinaplon can be used for research on generalized anxiety disorder.
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6,2'-Dihydroxyflavone
0 Images6,2'-Dihydroxyflavone is a novel antagonist of GABAA receptor.
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Dehydroepiandrosterone sulfate-d6 sodium dihydrate
0 ImagesCat. No.: HY-113416ASPurity: 98.00%Synonyms: DHEA sulfate-d6 sodium dihydrate; Prasterone sulfate-d6 sodium dihydrateDehydroepiandrosterone sulfate sodium dihydrate-d6 sodium dihydrate is the deuterium labeled Dehydroepiandrosterone sulfate sodium dihydrate. Dehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) sodium dihydrate is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate sodium dihydrate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate sodium dihydrate can partially penetrate the blood-brain barrier, inhibit GABAA receptor-mediated chloride influx, enhance NMDA receptor activity through σ1 receptors, exert anti-inflammatory, anti-glucocorticoid and antidepressant effects, and increase convulsive sensitivity. Dehydroepiandrosterone sulfate sodium dihydrate participates in neuroprotection, neurite growth regulation and catecholamine secretion regulation, and can be used in the study of depression, post-traumatic stress disorder (PTSD), Alzheimer's disease, etc. Dehydroepiandrosterone sulfate sodium dihydrate may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
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Temgicoluril
0 ImagesSynonyms: TetramethylglycolurilTemgicoluril (Tetramethylglycoluril) is an orally active antianxiety and antidepressant. Temgicoluril acts on GABA receptors to enhance GABA neurotransmission.
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SSD114 hydrochloride
0 ImagesSSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
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mNLS-CPP-WSTF TFA
0 ImagesCat. No.: HY-P11208CmNLS-CPP-WSTF TFA is the trifluoroacetate salt of mNLS-CPP-WSTF (HY-P11208). mNLS-CPP-WSTF is a nuclear localization signal (NLS)-cell-penetrating peptide based on the mouse WSTF sequence. mNLS-CPP-WSTF significantly inhibits the GABARAP-WSTF interaction, WSTF degradation and inflammatory gene expression. mNLS-CPP-WSTF effectively attenuates chronic inflammation, liver fibrosis and cartilage damage in metabolic-dysfunction-associated steatohepatitis (MASH) and osteoarthritis (OA) mice model. mNLS-CPP-WSTF is promising for research of chronic inflammatory diseases such as MASH and OA.
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Anisatin
0 ImagesAnisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM.
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SL651498
0 ImagesSL651498 is a full agonist of α2 and α3 GABAA receptors, and a partial agonist of α1 and α5 GABAA receptors. SL651498 shows anxiolytic and anticonvulsant activities.
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FGIN-1-43
0 ImagesFGIN-1-43 is an effective and specific ligand for the mitochondrial diazepam binding inhibitor (DBI) receptor (related to the production of neurosteroids). FGIN 1-43 enhances the transmission of GABA by inducing the production of neurosteroids, which can be used for research on anti-anxiety.
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17β-Estradiol sulfate-d4 sodium
0 ImagesSynonyms: 17β-Estradiol 3-sulfate-d4 sodium17β-Estradiol sulfate-d4 (sodium) is the deuterium labeled 17β-Estradiol sulfate 17β-Estradiol sulfate (sodium), also known as β-Estradiol 3-sulfate sodium salt, is a neuroactive steroid.
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AZD6280
0 ImagesAZD6280 is an orally active, blood-brain barrier-permeable GABAA receptor modulator, with Ki values of 21 nM, 31 nM and 1680 nM against human receptors containing α2, α3 and α5 subtypes, respectively, and subtype-specific Ki values of < 30 nM for α2 and α3 subtypes. AZD6280 selectively potentiates GABAA receptors containing α2/α3 subtypes with higher potency than α1/α5 subtypes, exerts no modulatory effect on receptors containing α1 subtypes, and regulates the tuberoinfundibular dopaminergic pathway. AZD6280 decreases peak saccadic velocity, increases serum and plasma prolactin levels, rescues dendritic abnormalities of cortical neurons induced by DISC1 knockdown. AZD6280 can be used in studies related to anxiety disorders.
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mNLS-CPP-scramble TFA
0 ImagesCat. No.: HY-P11208BPurity: 98.44%mNLS-CPP-scramble (TFA) is the trifluoroacetate salt of mNLS-CPP-scramble (HY-P11208A). mNLS-CPP-scramble is a negative control peptide of mNLS-CPP-WSTF. mNLS-CPP-scramble is promising for research of chronic inflammatory diseases (e.g., MASH, osteoarthritis).
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Epiallopregnanolone
0 ImagesEpiallopregnanolone (5α,3β-THDOC), a 3β-hydroxy neurosteroid, an antagonist at GABAA receptors and a NMDA receptor enhancer.
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CGS 20625
0 ImagesCGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 enhances GABA in Xenopus laevis oocytes . CGS 20625 can be used for the research of pentylenetetrazol-induced seizures and anxiety.
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RuBi-Glutamate hexafluorophosphate sodium
0 ImagesCat. No.: HY-131885CAS No.: 2417096-44-5RuBi-Glutamate hexafluorophosphate sodium is a neuronal activator. RuBi-Glutamate hexafluorophosphate sodium photocleaves to release glutamate upon one- or two-photon excitation, activating glutamate receptors in cortical pyramidal neurons. RuBi-Glutamate hexafluorophosphate sodium reduces peak amplitude of evoked GABAergic inhibitory postsynaptic currents in its caged form. RuBi-Glutamate hexafluorophosphate sodium can be used for the research of Huntington's disease.
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CGS 8216
0 ImagesCGS 8216 is a non-benzodiazepine brain benzodiazepine receptor ligand that binds to rat forebrain membranes with high affinity and specificity. CGS 8216 also inhibits 3H-flunitrazepam (3H-FLU) binding to rat synaptosomal membranes and blocks 3H-FLU labeling of brain benzodiazepine receptors in vivo with potency equivalent to Diazepam.
