检测方案
~95% (HPLC)
形式
powder
颜色
yellow
mp
100-105 °C
储存温度
2-8°C
SMILES字符串
COC(=O)c1c(C)nc(C)c(C(=O)OC)c1-c2ccccc2[N+]([O-])=O
InChI
1S/C17H16N2O6/c1-9-13(16(20)24-3)15(14(10(2)18-9)17(21)25-4)11-7-5-6-8-12(11)19(22)23/h5-8H,1-4H3
InChI key
UMQHJQGNGLQJPF-UHFFFAOYSA-N
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应用
Oxidized Nifedipine may be used:
- to study enzyme kinetics using UV high-performance liquid chromatography (UV-HPLC)
- as a standard in calibration curve preparation in high-performance liquid chromatography (HPLC) for the quantification of cytochrome P450 3A4 (CYP3A4)-mediated nifedipine oxidation in human microsomes
- in nifedipine metabolism activity assay of Hep G2 cells transfected with hepatocyte nuclear factor-1α(HNF1α)
Oxidized nifedipine has been used for apoptotic signaling studies in dopaminergic neurons.
生化/生理作用
Nifedipine is a dihydropyridine derivative and a calcium channel blocker. It is used in treating hypertension and angina pectoris. Oxidized Nifedipine is an oxidation product of nifedipine generated either by exposure to UV or day light. The enzyme cytochrome P450 3A (CYP3A4) metabolizes nifedipine.
CYP3A4 nifedipine metabolite. Nifedipine (parent compound) is an antianginal and antihypertensive agent.
包装
Bottomless glass bottle. Contents are inside inserted fused cone.
警示用语：
Danger
危险声明
危险分类
Eye Dam. 1
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
CYP3As catalyze nifedipine oxidation in pig liver microsomes: Enzyme kinetics, inhibition and functional expression
Jiang J, et al.
Catalysis Communications, 12(8), 694-697 (2011)
Gabriel A de Erausquin et al.
Molecular pharmacology, 63(4), 784-790 (2003-03-20)
We describe a new molecular mechanism of cell death by excitotoxicity mediated through nuclear transcription factor kappa B (NF kappa B) in rat embryonic cultures of dopaminergic neurons. Treatment of mesencephalic cultures with alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) resulted in a number
Wiriyaporn Sumsakul et al.
Asian Pacific journal of tropical medicine, 8(11), 914-918 (2015-11-29)
To investigate the propensity of plumbagin to inhibit the three isoforms of human cytochrome P450 (CYP), i.e., CYP1A2, CYP2C19, and CYP3A4 using human liver microsomes in vitro. Inhibitory effects of plumbagin on the three human CYP isoforms were investigated using pooled
D G Waller et al.
British journal of clinical pharmacology, 18(6), 951-954 (1984-12-01)
Oral administration of nifedipine (20 and 30 mg tablets) to six volunteers was associated with a bioavailability of 0.43 and the presence of its nitropyridine analogue in the plasma. This metabolite was present in only trace amounts in samples taken
J L Born et al.
Chemical research in toxicology, 2(1), 57-59 (1989-01-01)
The primary deuterium isotope effect on Vm for the microsomal oxidation of the dihydropyridine calcium entry blocker nifedipine [4-(2-nitrophenyl)-2,6-dimethyl-3,5- bis(methoxycarbonyl)-1,4-dihydropyridine] has been measured. The magnitude of the kinetic isotope effect, 6.7, suggests that the rate-limiting step in the mechanism of
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