Name | 3-(4-chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one |
---|---|
Synonyms |
2H-Imidazol-2-one, 1-(4-chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-
1-(4-Chlorophenyl)-1,5-dihydro-4-(4-morpholinyl)-2H-imidazol-2-one 1-(4-Chlorophenyl)-4-(4-morpholinyl)-1,5-dihydro-2H-imidazol-2-one UNII-19V39682LI 1-(4-Chlorophenyl)-4-(morpholin-4-yl)-1,5-dihydro-2H-imidazol-2-one AWD 131-138 Imepitoin |
Description | 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]. |
---|---|
Related Catalog | |
References |
Density | 1.4±0.1 g/cm3 |
---|---|
Boiling Point | 421.8±55.0 °C at 760 mmHg |
Molecular Formula | C13H14ClN3O2 |
Molecular Weight | 279.722 |
Flash Point | 208.9±31.5 °C |
Exact Mass | 279.077454 |
PSA | 45.14000 |
LogP | 0.04 |
Appearance | white solid |
Vapour Pressure | 0.0±1.0 mmHg at 25°C |
Index of Refraction | 1.664 |
Storage condition | -20℃ |