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 Verwandte Produkte (793)
Verwandte Produkte (793)
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Antibodies (14)
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Related Compound Screening Libraries (1)
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γ-Aminobutyric acid
0 Imagesγ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors. γ-Aminobutyric acid shows calming effect by blocking specific signals of central nervous system.
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Bicuculline
0 ImagesBicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice.
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Aminooxyacetic acid hemihydrochloride
0 ImagesSynonyms: Carboxymethoxylamine hemihydrochloride; Aminooxyacetate hemihydrochlorideAminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
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Gabazine
0 ImagesSynonyms: SR95531Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
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Furosemide
0 ImagesFurosemide is an orally active GABAA receptor antagonist. Furosemide inhibits carbonic anhydrase, the sodium-chloride cotransporter, sodium reabsorption, tubuloglomerular feedback, and GABA-induced chloride flux. Furosemide can be used as a diuretic reagent. Furosemide is applied in the research of hepatic necrosis, sepsis-associated acute kidney injury, hypoalbuminemia-related fluid retention, and congestive heart failure.
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Dehydroepiandrosterone sulfate
0 ImagesDehydroepiandrosterone sulfate (DHEA sulfate; Prasterone sulfate) is a neurosteroid and the main secretion product of the adrenal gland. Dehydroepiandrosterone sulfate has both non-competitive antagonist activity of GABAA receptor and agonist activity of σ1 receptor. Dehydroepiandrosterone sulfate 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 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 may also be a biomarker for cardiovascular disease mortality, and its concentration is independently and negatively correlated with mortality.
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Cyclothiazide
0 ImagesCyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures.
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tert-Butyl 3,9-diazaspiro[5.5]undecane-3-carboxylate
![tert-Butyl 3,9-diazaspiro[5.5]undecane-3-carboxylate](https://file.medchemexpress.com/product_pic/hy-30536.gif "Click to View tert-Butyl 3,9-diazaspiro[5.5]undecane-3-carboxylate Product Detail")
0 Imagestert-Butyl 3,9-diazaspiroundecane-3-carboxylate is a 3,9-diazaspiroundecane-based building block and precursor for synthesizing γ-aminobutyric acid type A (GABAA) receptor antagonists.
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Baclofen
0 ImagesBaclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist with blood-brain barrier permeability. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research.
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Amentoflavone
0 ImagesAmentoflavone (Didemethyl-ginkgetin) is a potent and orally active GABA(A) negative modulator. Amentoflavone also shows anti-inflammatory, antioxidative, anti-viral, anti-tumor, anti-radiation, anti-fungal, antibacterial activity. Amentoflavone induces apoptosis and cell cycle arrest at sub-G1 phase.
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Vigabatrin
0 ImagesSynonyms: γ-Vinyl-GABAVigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin 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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Cefepime
0 ImagesSynonyms: BMY-28142Cefepime (BMY-28142) is a broad-spectrum, blood-brain barrier-permeable cephalosporin antibiotic with hPON1 inhibitory activity, with an IC50 of 21.115 mM and a Ki of 35.092 mM. Cefepime inhibits hPON1 via a non-competitive mechanism and blocks GABAA receptors. Cefepime penetrates the outer membrane of Gram-negative bacteria, inhibits the growth of Gram-positive and Gram-negative bacteria, and does not induce the production of β-lactamase.
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Creatinine
0 ImagesCreatinine (NSC13123) is an orally active, blood-brain barrier-permeable modulator of GABAA and NMDA receptors, with activities of antioxidation and metabolic regulation. Creatinine is generated via non-enzymatic conversion of creatine and phosphocreatine in muscle. Creatinine serum levels correlate with muscle mass, glomerular filtration rate, and extrarenal clearance, serving as an evaluation biomarker for renal function, muscle mass, and clinical outcomes, and used for perioperative renal risk assessment. In addition, Creatinine can induce specific Cryptococcus species to produce creatinine deiminase and act as their nitrogen source, while it can be secreted via renal tubules. Creatinine is widely used in research related to various diseases such as neurodegenerative diseases, psychiatric disorders, acute kidney injury, chronic kidney disease, and renal failure.
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Flumazenil
0 ImagesSynonyms: Ro 15-1788Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
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Picrotoxinin
0 ImagesPicrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
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Bicuculline methiodide
0 ImagesSynonyms: (-)-Bicuculline methiodideBicuculline methiodide ((-)-Bicuculline methiodide) is a potent GABAA blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current.
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Topiramate
0 ImagesSynonyms: McN 4853; RWJ 17021Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.
