Drug metabolism and disposition: the biological fate of chemicals · 1999
Role of human CYP2B6 in S-mephobarbital N-demethylation.
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Kobayashi K, Abe S, Nakajima M, Shimada N, Tani M, Chiba K, Yamamoto T
Аннотация
The role of cytochrome P-450s (CYPs) in S-mephobarbital N-demethylation was investigated by using human liver microsomes and cDNA-expressed CYPs. Among the 10 cDNA-expressed CYPs studied (CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4), only CYP2B6 could catalyze S-mephobarbital N-demethylation. The apparent K(m) values of human liver microsomes for S-mephobarbital N-demethylation were close to that of cDNA-expressed CYP2B6 (about 250 microM). The N-demethylase activity of S-mephobarbital in 10 human liver microsomes was strongly correlated with immunodetectable CYP2B6 levels (r = 0.920, p<.001). Orphenadrine (300 microM), a CYP2B6 inhibitor, inhibited the N-demethylase activity of S-mephobarbital in human liver microsomes to 29% of control activity. Therefore, it appears that CYP2B6 mainly catalyzes S-mephobarbital N-demethylation in human liver microsomes.
Предметные рубрики MeSH
AnticonvulsantsAryl Hydrocarbon HydroxylasesB-LymphocytesCytochrome P-450 CYP2B6Cytochrome P-450 Enzyme InhibitorsCytochrome P-450 Enzyme SystemDNA, ComplementaryHumansIn Vitro TechniquesKineticsMephobarbitalMethylationMicrosomes, LiverOxidoreductases, N-DemethylatingStatistics as TopicTransfectionTumor Cells, Cultured