VERAPAMIL IMPURITY J
| 中文名稱 | VERAPAMIL IMPURITY J |
|---|---|
| 中文同義詞 | 鹽酸維拉帕米雜質(zhì)J(EP) 標(biāo)準(zhǔn)品;化合物 T12244;維拉帕米EP雜質(zhì)J;維拉帕米雜質(zhì)10 單體(維拉帕米EP雜質(zhì)J 單體);維拉帕米雜質(zhì)10 甲酸鹽(維拉帕米EP雜質(zhì)J 甲酸鹽);化合物 NORVERAPAMIL;去甲維拉帕米標(biāo)準(zhǔn)品 |
| 英文名稱 | NORVERAPAMIL |
| 英文同義詞 | NORVERAPAMIL;Benzeneacetonitrile, a-[3-[[2-(3,4-dimethoxyphenyl)-ethyl]amino]propyl]-3,4-dimethoxy-a-(1-methylethyl)-;D591;2-(3,4-Dimethoxyphenyl)-2-isopropyl-5-(3,4-dimethoxyphenethylamino)valeronitrile;α-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-α-isopropylbenzeneacetonitrile;Verapamil Impurity J;Norverapamil D6;5-[(3,4-dimethoxyphenethyl)amino]-2-(3,4-dimethoxyphenyl)-2-isopropylvaleronitrile |
| CAS號(hào) | 67018-85-3 |
| 分子式 | C26H36N2O4 |
| 分子量 | 440.58 |
| EINECS號(hào) | 266-544-8 |
| 相關(guān)類(lèi)別 | |
| Mol文件 | 67018-85-3.mol |
| 結(jié)構(gòu)式 |  |
VERAPAMIL IMPURITY J 性質(zhì)
| 沸點(diǎn) | 586.1±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.063±0.06 g/cm3(Predicted) |
| 酸度系數(shù)(pKa) | 9.79±0.19(Predicted) |
| CAS 數(shù)據(jù)庫(kù) | 67018-85-3 |
| EPA化學(xué)物質(zhì)信息 | Benzeneacetonitrile, .alpha.-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-.alpha.-(1-methylethyl)- (67018-85-3) |
Calcium channel blocker
P-glycoprotein (P-gp) inhibitor
Norverapamil ((±)-Norverapamil) is similarly effective as verapamil at inhibiting isoniazid and rifampicin tolerance and killing of intracellular M. tuberculosis in the absence of other drugs. norverapamil, also inhibits macrophage-induced tolerance and achieves similar serum levels to verapamil.
Verapamil and its major metabolite Norverapamil were identified to be both mechanism-based inhibitors and substrates of CYP3A and reported to have non-linear pharmacokinetics in clinic.
Norverapamil (9 mg/kg; p.o.), a major metabolite of verapamil, has terminal half-life, AUC and Cmax values of 9.4 hours, 260 ng?h/ml, and 41.6 ng/mL, respectively.
| Animal Model: | Male Sprague-Dawley rats |
| Dosage: | 9 mg/kg (Pharmacokinetic Study) |
| Administration: | Oral administration |
| Result: | t 1/2 =9.4 hours; AUC=260 ng?h/mL; C max =41.6 ng/mL. |