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| 产地 | 中国 |
| 品牌 | Chemstan |
| 货号 | LC-01 |
| 用途 | 中间体 |
| 包装规格 | 20mg |
| 纯度 | 98%% |
| CAS编号 | 188116-07-6 |
| 是否进口 | 否 |
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Fields of Application :
AWD 131-138(Imepitoin) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
| CAS Number: | 188116-07-6 |
| Purity: | >98% |
| Molecular Weight: | 279.72 |
| Molecular Formula: | C13H14ClN3O2 |
Quality Control: HPLC、NMR、 LC/MS(Please contact us to get the QC report)
| Synonyms: | Imepitoin; AWD131-138 |
| Chemical Name: | |
| Storage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
Note: Products for research use only, not for human use
Description:
AWD 131-138 is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models. IC50 Value: Target: GABA receptor in 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 . 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 . 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 .For the detailed information of AWD 131-138(Imepitoin), the solubility of AWD 131-138(Imepitoin) in water, the solubility of AWD 131-138(Imepitoin) in DMSO, the solubility of AWD 131-138(Imepitoin) in PBS buffer, the animal experiment (test) of AWD 131-138(Imepitoin), the cell expriment (test) of AWD 131-138(Imepitoin), the in vivo, in vitro and clinical trial test of AWD 131-138(Imepitoin), the EC50, IC50,and Affinity of AWD 131-138(Imepitoin).
References:
C(=O)1N(C2=CC=C(Cl)C=C2)CC(N2CCOCC2)=N1
