Title : Formation of a dihydroxy metabolite of phenytoin in human liver microsomes/cytosol: roles of cytochromes P450 2C9, 2C19, and 3A4.

Pub. Date : 2000 Nov

PMID : 11038165






4 Functional Relationships(s)
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1 In the presence of liver cytosol, 3",4"-diHPPH formation activity from 100 microM 4"-HPPH was correlated with testosterone 6beta-hydroxylation activity and CYP3A4 content. hydroxyphenytoin cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 Of 10 cDNA-expressed human P450 enzymes examined, CYP2C19, CYP2C9, and CYP3A4 catalyzed 3",4"-diHPPH formation from the primary hydroxylated metabolites (3"-hydroxy-DPH and 4"-HPPH). hydroxyphenytoin cytochrome P450 family 3 subfamily A member 4 Homo sapiens
3 Fluvoxamine and anti-CYP2C antibody inhibited 3",4"-diHPPH formation from 10 microM 4"-HPPH in a human liver sample that contained relatively high levels of CYP2C, whereas ketoconazole and anti-CYP3A antibody showed inhibitory effects on the activities in liver microsomal samples in which CYP3A4 levels were relatively high. hydroxyphenytoin cytochrome P450 family 3 subfamily A member 4 Homo sapiens
4 Fluvoxamine and anti-CYP2C antibody inhibited 3",4"-diHPPH formation from 10 microM 4"-HPPH in a human liver sample that contained relatively high levels of CYP2C, whereas ketoconazole and anti-CYP3A antibody showed inhibitory effects on the activities in liver microsomal samples in which CYP3A4 levels were relatively high. hydroxyphenytoin cytochrome P450 family 3 subfamily A member 4 Homo sapiens