67018-85-3
67018-85-3 結(jié)構(gòu)式
基本信息
化合物 T12244
鹽酸維拉帕米雜質(zhì)J(EP) 標(biāo)準(zhǔn)品
NORVERAPAMIL
Norverapamil D6
Verapamil Impurity J
Verapamil EP Impurity J Monomer
(2RS)-2-(3,4-Dimethoxy-phenyl)-5-[[
2-(3,4-Dimethoxyphenyl)-2-isopropyl-5-(3,4-dimethoxyphenethylamino)valeronitrile
5-[(3,4-dimethoxyphenethyl)amino]-2-(3,4-dimethoxyphenyl)-2-isopropylvaleronitrile
α-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-α-isopropylbenzeneacetonitrile
Benzeneacetonitrile, α-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-α-(1-methylethyl)-
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
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. |