| 常用名 | 伊匹妥英 | CAS号 | 188116-07-6 |
|---|---|---|---|
| 价格 | ¥需询单/1g ¥需询单/1mg | 纯度 | 98.0% |
| 备货期 | 需询单 | 库存 | 询单 |
| 产品详情(用途,包装等)
用途: AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.IC50 Value: Target: GABA receptorin vitro: AWD 131-138 dose-dependently stimulated GABA currents(Recombinant gamma-aminobutyric acid A (GABA(A)) receptors of the subunit compositions alpha1beta2gamma2, alpha1beta3gamma2, alpha2beta2gamma2, alpha3beta2gamma2 and alpha5beta2gamma2). At 10 microM AWD 131-138, this allosteric stimulation amounted in average to about 12-21% of the maximal stimulation achieved using diazepam. The threshold of stimulation was about 0.3-1.0 microM [1]. in vivo: AWD 131-138 did not produce midazolam-like responding or alter response rates at cumulative doses up to 18.0 mg/kg i.m. (plasma levels over 2100 ng/ml). When AWD 131-138 (10-100 microg/kg/injection) was studied by substitution, responding declined to vehicle substitution levels within three sessions. At the dose of 100 microg/kg i.v. AWD 131-138, sufficient drug was self-administered during the first session (about 3.5 mg/kg) to produce plasma levels above 1000 ng/ml, yet responding over the next two sessions dropped to vehicle levels [2]. Prolonged oral administration with twice-daily dosing of ELB 138 with either 5 or 40 mg/kg over a 5-week period was not associated with loss of anticonvulsant efficacy in the PTZ dog model [3]. 物理化学性质: CAS号:188116-07-6 常用中文名:伊匹妥英 常用英文名:Imepitoin 分子式:C13H14ClN3O2 分子量:279.722 密度:1.4±0.1 g/cm3 沸点:421.8±55.0 °C at 760 mmHg 熔点:N/A 闪点:208.9±31.5 °C 储存条件:-20℃ |