Imepitoin
Modify Date: 2024-01-08 13:50:28
Imepitoin structure
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Common Name | Imepitoin | ||
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| CAS Number | 188116-07-6 | Molecular Weight | 279.722 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 421.8±55.0 °C at 760 mmHg | |
| Molecular Formula | C13H14ClN3O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 208.9±31.5 °C | |
Use of ImepitoinAWD 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]. |
| Name | 3-(4-chlorophenyl)-5-morpholin-4-yl-4H-imidazol-2-one |
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| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
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| 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 of Characters | white solid |
| Vapour Pressure | 0.0±1.0 mmHg at 25°C |
| Index of Refraction | 1.664 |
| Storage condition | -20℃ |
| 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 |