2006
Determination of nifedipine as a probe substrate of cytochrome P450 3A1/2 activity in rats
JUŘICA, Jan, Josef TOMANDL, Lucia ZAHRADNÍKOVÁ, Ondřej ZENDULKA, Eva HADAŠOVÁ et. al.Základní údaje
Originální název
Determination of nifedipine as a probe substrate of cytochrome P450 3A1/2 activity in rats
Název česky
Stanovení nifedipinu jako substrátu aktivity cytochromu P450 3A1/2 u potkanů
Autoři
Vydání
Bratislava, Proceedings from XX. Biochemický zjazd, s. 424-424, 2006
Nakladatel
Institute of Molecular Physiology and Genetics, Slovak Academy of Sciences
Další údaje
Jazyk
angličtina
Typ výsledku
Stať ve sborníku
Obor
10600 1.6 Biological sciences
Stát vydavatele
Slovensko
Utajení
není předmětem státního či obchodního tajemství
Organizační jednotka
Lékařská fakulta
ISBN
80-969532-6-5
Klíčová slova anglicky
cytochrome P450 - nifedipine - rat
Příznaky
Mezinárodní význam
Změněno: 12. 12. 2006 12:57, doc. PharmDr. Jan Juřica, Ph.D.
V originále
Nifedipine is a dihydropyridine calcium channel blocker used in the treatment of hypertension, acute coronary syndrom, stable angina pectoris and congestive heart failure. Oxidation of nifedipine to its pyridine metabolite is used as a valuable tool for the measurement of metabolic activity of the rat 3A1/2 or human 3A4/5 isoform of cytochrome P450. Due to high similarity in amino acid sequence between rat CYP3A1/2 and human CYP3A4/5 it is possible to predict the metabolic activity of human CYP3A4/5 by the measurement of rat CYP3A1/2 activity. Here we describe a new, very simple, rapid, sensitive and reproducible HPLC method for the determination of nifedipine and its pyridine metabolite in perfuse medium after rat liver perfusion. This method is applicable for modeling and description of possible pharmacological interactions on rat CYP3A1/2 or human CYP3A4/5, respectively.
Česky
Nifedipine is a dihydropyridine calcium channel blocker used in the treatment of hypertension, acute coronary syndrom, stable angina pectoris and congestive heart failure. Oxidation of nifedipine to its pyridine metabolite is used as a valuable tool for the measurement of metabolic activity of the rat 3A1/2 or human 3A4/5 isoform of cytochrome P450. Due to high similarity in amino acid sequence between rat CYP3A1/2 and human CYP3A4/5 it is possible to predict the metabolic activity of human CYP3A4/5 by the measurement of rat CYP3A1/2 activity. Here we describe a new, very simple, rapid, sensitive and reproducible HPLC method for the determination of nifedipine and its pyridine metabolite in perfuse medium after rat liver perfusion. This method is applicable for modeling and description of possible pharmacological interactions on rat CYP3A1/2 or human CYP3A4/5, respectively.
Návaznosti
| GA203/06/0047, projekt VaV |
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| LC06023, projekt VaV |
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| MSM0021622404, záměr |
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