中文名 | AWD-131-138 |
英文名 | 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one |
别名 | 伊匹妥英 1-(4-氯苯基)-4-吗啉-1H-咪唑-2(5H)-酮 1-(4-氯苯基)-1,5-二氢-4-(4-吗啉基)-2H-咪唑-2-酮 |
英文别名 | IMEPITOIN Imepitoin AWD-131-138 AWD131-138 1-(4-CHLOROPHENYL)-4-MORPHOLINO-1H-IMIDAZOL-2(5H)-ONE 1-(4-chlorophenyl)-4-morpholin-4-yl-5H-imidazol-2-one 1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one 2H-Imidazol-2-one,1-(4-chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)- Imepitoin 1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one |
CAS | 188116-07-6 |
EINECS | 200-256-5 |
化学式 | C13H14ClN3O2 |
分子量 | 279.72 |
密度 | 1.42±0.1 g/cm3(Predicted) |
熔点 | 264℃ (ethanol ) |
沸点 | 421.8±55.0 °C(Predicted) |
酸度系数 | 4.39±0.20(Predicted) |
存储条件 | 2-8°C |
体外研究 | 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]. |
体内研究 | 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]. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.575 ml | 17.875 ml | 35.75 ml |
5 mM | 0.715 ml | 3.575 ml | 7.15 ml |
10 mM | 0.357 ml | 1.787 ml | 3.575 ml |
5 mM | 0.071 ml | 0.357 ml | 0.715 ml |
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