| 中文名称 | 伊匹妥英 |
| 英文名称 | 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one |
| CAS号 | 188116-07-6 |
| 分子式 | C13H14ClN3O2 |
| 分子量 | 279.72 |
| EINECS号 | 200-256-5 |
| 熔点 | 264℃ (ethanol ) |
| 沸点 | 421.8±55.0 °C(Predicted) |
| 密度 | 1.42±0.1 g/cm3(Predicted) |
| 溶解度 | DMF:10.0(最大浓度 mg/mL);35.75(最大浓度 mM)DMSO:17.5(最大浓度 mg/mL);62.56(最大浓度 mM)DMSO:PBS ( pH 7.2) (1:1):0.5(最大浓度 mg/mL);1.79(最大浓度 mM)乙醇:1.13(最大浓度 mg/mL);4.02(最大浓度 mM) |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 4.39±0.20(Predicted) |
| 颜色 | 白色至米白色 |
GABA receptor
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].
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].