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GABA Receptor

GABA Receptor相关产品(49)
货号 产品名 中文名称 产品描述
SJ-MX0468 Furosemide (NSC 269420) 呋塞米

Furosemide 是 Na+/K+/2Cl- (NKCC),NKCC1 和 NKCC2 共转运蛋白的有效的和具有口服活性抑制剂。Furosemide 也是 GABAA 受体拮抗剂,对含 α6 受体的选择性是含 α1 受体的 100 倍。Furosemide 用作利尿试剂,用于充血性心力衰竭,高血压和水肿的研究。

SJ-MX3293 Imepitoin 伊匹妥英 Imepitoin, formerly known as AWD 131-138 and ELB 138, is a novel partial BZD (benzodiazepine) receptor agonist that has the potential use as an antiepileptic drug for the treatment of canine idiopathic epilepsy. Imepitoin is a centrally acting anti-epileptic which crosses the blood brain barrier. It inhibits seizures via potentiation of the GABA a receptor-mediated inhibitory effects on the neurones. Imepitoin exerts significant anticonvulsant efficacy without tolerance in a dog seizure model as well as in epileptic dogs with spontaneously recurrent seizures. These data thus substantiate that partial agonism at the BZD site of GABAA receptors offers advantages versus full agonism and constitutes a valuable approach for treatment of seizures.
SJ-MX3500 DMCM hydrochloride DMCM hydrochloride 是一种苯二氮杂 (benzodiazepine) 非选择性全反向激动剂。DMCM 对人重组GABAA αxβ3γ2 受体亚型具有亲和力,对 α1,α2,α3 和 α5 受体的 Ki 值分别为 10 nM,13 nM,7.5 nM,2.2 nM。
SJ-MX3584 MRK-016 MRK-016 是一种选择性的,可口服的,可透过血脑屏障的 GABAA α5 receptor 拮抗剂,对 GABAA α5 的 EC50 值为 3 nM,对人 GABAA α1β3γ2,GABAA α2β3γ2,GABAA α3β3γ2 和 GABAA α5β3γ2 的 Ki 值分别为 0.83,0.85,0.77 和 1.4 nM。
SJ-MX3639 Lorediplon Lorediplon是一种新型非苯并二氮卓类,充当GABAA受体调节剂。
SJ-MX3742 CGP52432 CGP52432 是一种 GABAB 受体拮抗剂,IC50 值为 85 nM。
SJ-MX3813 Fluxametamide 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.
SJ-MX2566 Clomethiazole 氯美噻唑 Clomethiazole is a positive allosteric modulator at the barbiturate/picrotoxin site of the GABAA receptor. It acts as a sedative and hypnotic agent.
SJ-MX1340 L-Cycloserine L-环丝氨酸 L-Cycloserine ((S)-4-Amino-3-isoxazolidone) 作用于大肠杆菌和各种动物大脑,不可逆地抑制 GABA 5'-磷酸吡哆醛氨基转移酶,这种作用具有时间依赖性,导致了γ-氨基丁酸 (GABA) 含量增高, GABA 在体内抑制性神经递质。
SJ-MN1004 Cirsimaritin Cirsimaritin binds weakly to the benzodiazepine site on GABAA receptors, with antidepressant, anxiolytic and antinociceptive activities.
SJ-MX2488 Acamprosate calcium 阿坎酸钙 Acamprosate calcium(Campral EC)是GABA受体激动剂和谷氨酸能系统调节剂。
SJ-MX2494 Afloqualone 氟喹酮 Afloqualone, also known as HQ-495, is a centrally acting muscle relaxant. Afloqualone inhibits vestibular nystagmus probably due to both inhibition of selective polysynaptic transmission and enhancement of the effects of GABA and glycine in the lateral vestibular nucleus (LVN), and its GABA-enhancing effect is thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site.
SJ-MX2547 Baclofen 巴氯芬 Baclofen (also known as STX 209) is a derivative of gamma-aminobutyric acid and a selective GABAB receptor agonist.primarily used to treat spasticity. Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing It acts at spinal and supraspinal sites, reducing excitatory transmission. GABAB receptors are metabotropic receptors which produce slow inhibitory signals.
SJ-MX2611 Chlormezanone 氯美扎酮 Chlormezanone is a non-benzodiazepine that is used in the management of anxiety. Chlormezanone is a skeletal muscle relaxant, acting at the benzodiazepine site of GABAA receptors. Chlormezanone is a substrate of GABA receptor. It has been suggested for use in the treatment of muscle spasm.
SJ-MX2664 Nefiracetam 奈非西坦 Nefiracetam (DZL-221; DM9384; DZL221; DM 9384; Translon) is a potent GABAergic, cholinergic, and monoaminergic neuronal system enhancer for Ro 5-4864-induced convulsions. It is a nootropic (cognition-enhancing) agent with antidementia activity. Nefiracetam at a concentration of 1 μM increases a long-lasting component of calcium channel currents two-fold without affecting a transient component. Nefiracetam induces a short-term depression of ACh-evoked currents at submicromolar concentrations (0.01–0.1 μM) and a long-term enhancement of the currents at micromolar concentrations (1–10 μM).
SJ-MX3370 Flumazenil 氟马西尼 Flumazenil (Flumazepil, Anexate, Romazicon, Lanexat; Ro-15-1788; Ro-15 1788) is a specific and competitive GABAA receptor antagonist that has been used for the treatment of benzodiazepine overdoses. Flumazenil is a specific benzodiazepine receptor antagonist primarily administered by injection. It is the only benzodiazepine receptor antagonist on the market today. Flumazenil is of benefit in patients who become excessively drowsy after benzodiazepines are used for either diagnostic or therapeutic procedures.
SJ-MX3423 Bemegride 贝美格 Bemegride (3-Ethyl-3-methylglutarimide; Antibarbi; Agipnon; Ahypnon; Eukraton; Malysol; Mikedimide; Zentraleptin) is apotent central nervous system stimulant and effective antidote for barbiturate poisoning. Ethinamate is a short-acting carbamate-derivative, sedative-hypnotic medication used to treat insomnia. Regular use leads to tolerance, and it is usually not effective for more than 7 days. Structurally, it does not resemble the barbituates, but it shares many effects with this class of drugs. The depressant effects of ethinamate are, however, generally milder than those of most barbiturates.
SJ-MX2212 Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride 氨氧基乙酸半盐酸盐 Aminooxyacetic acid (Carboxymethoxylamine) hemihydrochloride 是苹果酸-天冬氨酸穿梭 (MAS) 抑制剂,也能抑制 GABA 降解酶 GABA-T。
SJ-MN1127 α-Asarone α-细辛脑 α-Asarone (alpha-Asarone;trans-Asarone) 是菖蒲属中主要的活性物质,具有抗抑等功效。
SJ-MN0619 γ-Aminobutyric acid γ-氨基丁酸 γ-Aminobutyric acid (4-Aminobutyric acid) 是成年哺乳动物大脑中主要的抑制性神经递质,能够与离子移变 GABA 受体 (GABAA) 受体和促代谢受体 (GABAB) 受体结合发挥作用。