| 货号 | 16235-50mg |
| 描述 | AWD 131-138 is a partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM.1 This effect is blocked by the benzodiazepine antagonist flumazenil (Item No. 14252).1 AWD 131-138 displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or abuse.2,3,4 It has a superior pharmacokinetic profile in dogs vs.humans.3,5 |
| 别名 | ELB138;Imepitoin; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Sigel, E.,Baur, R.,Netzer, R., et al. The antiepileptic drug AWD 131-138 stimulates different recombinant isoforms of the rat GABAA receptor through the benzodiazepine binding site. Neuroscience Letters 245(2), 85-88 (1998). 2.Rundfeldt, C.,Gasparic, A. and Wlaz, P. Imepitoin as novel treatment option for canine idiopathic epilepsy: Pharmacokinetics, distribution, and metabolism in dogs. J.Vet.Pharmacol.Therap. 37, 421-434 (2015). 3.Rundfeldt, C. and Löscher, W. The pharmacology of imepitoin: The first partial benzodiazepine receptor agonist developed for the treatment of epilepsy. CNS Drugs 28(1), 29-43 (2014). 4.Yasar, S.,Bergman, J.,Munzar, P., et al. Evaluation of the novel antiepileptic drug, AWD 131-138, for benzodiazepine-like discriminative stimulus and reinforcing effects in squirrel monkeys. European Journal of Pharmacology 465(3), 257-265 (2003). 5.Patterson, E.E. Canine epilepsy: An underutilized model. ILAR J. 55(1), 182-186 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 279.7 |
| 分子式 | C13H14ClN3O2 |
| CAS号 | 188116-07-6 |
| 稳定性 | ≥ 2 years |
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