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 関連製品 (776)
関連製品 (776)
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抗体 (14)
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関連化合物スクリーニングライブラリー (1)
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γ-Aminobutyric acid
(γ-アミノ酪酸)
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
(ビククリン)
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
(Carboxymethoxylamine (hemihydrochloride))
0 Images別名: Aminooxyacetic acid (hemihydrochloride); Aminooxyacetate (hemihydrochloride); (アミノオキシ)酢酸 ヘミ塩酸塩; カルボキシメトキシルアミン ヘミ塩酸塩Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.
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Gabazine
(Gabazine)
0 Images別名: SR95531Gabazine is a selective and competitive antagonist of GABAA receptor, with an IC50 of ~0.2 μM for GABA receptor.
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ASP8062
0 Images製品番号: HY-184060CAS 番号: 1704716-36-8ASP8062 is an orally active, blood-brain barrier-permeable selective GABAB receptor positive allosteric modulator. ASP8062 enhances GABA-mediated activation of GABAB receptors and strengthens GABAergic neurotransmission. ASP8062 reverses Reserpine (HY-N0480)-induced myalgia, regulates the sleep-wake cycle, increases delta wave power during non-REM sleep, and impairs motor coordination at high doses. ASP8062 penetrates the central nervous system with a half-life of 40-50 h. ASP8062 can be used in research related to opioid use disorder, fibromyalgia, chronic pain, and alcohol use disorder.
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Scoulerine hydrochloride
0 Images製品番号: HY-N1255ACAS 番号: 51486-68-1別名: (-)-Scoulerine hydrochloride; Discretamine hydrochlorideScoulerine ((-)-Scoulerine; Discretamine) hydrochloride is a multi-target inhibitor with anti-tumor and antioxidant activities. Scoulerine hydrochloride mainly targets the PI3K/Akt/mTOR signaling axis and α1D-adrenergic receptor, disrupts microtubule structure, and induces cell cycle arrest and apoptosis. Scoulerine hydrochloride effectively inhibits mitochondrial dehydrogenase activity, targets GABA receptors and BACE1, and suppresses the proliferation, migration, invasion, epithelial-mesenchymal transition and stem cell properties of cancer cells. Scoulerine hydrochloride also exhibits multiple pharmacological activities including anti-Plasmodium falciparum, antibacterial, antiemetic and antitussive effects, and regulates endoplasmic reticulum stress and mitochondrial function (modulates Bax, Bcl-2 and cytochrome c). Scoulerine hydrochloride is applicable to research related to leukemia, ovarian cancer, and colorectal cancer.
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GABAA receptor modulator-14
0 Images製品番号: HY-184478CAS 番号: 3103822-75-6GABAA receptor modulator-14 is an orally active, blood-brain barrier permeable selective positive allosteric modulator (PAM) of extrasynaptic δ-containing GABAA receptors (α4β3δ subtype) with an EC50 of 0.8 μM. GABAA receptor modulator-14 selectively enhances tonic neuronal inhibition by potentiating GABA-evoked currents mediated by extrasynaptic δ-GABAARs, produces rapid sustained antidepressant effects, elevates slow-wave NREM sleep and shows no addiction liability in mice. GABAA receptor modulator-14 can be applied to major depressive disorder (MDD) and comorbid insomnia research.
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Furosemide
(フロセミド)
0 ImagesFurosemide is a potent and orally active inhibitor of Na+/K+/2Cl- (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
- Riluzole (リルゾール)
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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
(バクロフェン)
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
(アメントフラボン)
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
(Vigabatrin)
0 Images別名: 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 Images別名: 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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Dehydroepiandrosterone sulfate
(DHEA 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.
- Methionine (Methionine)
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Creatinine
(クレアチニ)
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
(フルマゼニル)
0 Images別名: Flumazenil; Ro 15-1788Flumazenil is a competitive GABAA receptor antagonist, used in the treatment of benzodiazepine overdoses.
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Picrotoxinin
(Picrotoxinin)
0 Images別名: ピクロトキシニンPicrotoxinin, 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.
