| CAS NO: | 188116-07-6 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 279.08 |
|---|---|
| Formula | C13H14ClN3O2 |
| CAS No. | 188116-07-6 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 10 mM |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Solubility (In vivo) | O=C1N=C(N2CCOCC2)CN1C3=CC=C(Cl)C=C3 |
| Synonyms | AWD 131-138; AWD-131-138; AWD131-138; ELB 138; ELB-138; ELB138; AWD 131138; Imepitoin |
| In Vitro | In vitro activity: Imepitoin, formerly known as AWD 131-138 and ELB 138, is a novel partial BZD (benzodiazepine) receptor agonist that has the potential use as an antiepileptic drug for the treatment of canine idiopathic epilepsy. Imepitoin is a centrally acting anti-epileptic which crosses the blood brain barrier. It inhibits seizures via potentiation of the GABA a receptor-mediated inhibitory effects on the neurones. Kinase Assay: 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. Cell Assay: |
|---|---|
| In Vivo | Imepitoin exerts significant anticonvulsant efficacy without tolerance in a dog seizure model as well as in epileptic dogs with spontaneously recurrent seizures. These data thus substantiate that partial agonism at the BZD site of GABAA receptors offers advantages versus full agonism and constitutes a valuable approach for treatment of seizures. 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. 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 |
| Animal model | Dog seizure model |
| Formulation & Dosage | 10-100 microg/kg/injection |
| References | Epilepsia. 2004 Oct;45(10):1228-39. |
m.cnreagent.com