Table 6

Correlation of the in vitro N-dehydroxylation of guanoxabenz to guanabenz with known isoenzyme-specific P450 marker activities in 10 different samples of human hepatic microsomes

Marker ReactionResponsible P450 Isoenzymer
7-EthoxyresorufinO-deethylationCYP1A20.33
Caffeine N-demethylationCYP1A20.36
Coumarin 7-hydroxylationCYP2A60.36
Tolbutamide-methylhydroxylationCYP2C9/100.48
(S)-Mephenytoin 4′-hydroxylationCYP2C190.06
Dextrometorphan O-demethylationCYP2D60.14
Chlorzoxazone 6-hydroxylationCYP2E10.03
Testosterone 6β-hydroxylationCYP3A40.43
Lauric acid 12-hydroxylationCYP4A0.04
  • For incubation procedure, sample work-up, and analysis seeMaterials and Methods.