TABLE 1

P450-selective probe reactions and their parameters that derive the RAF values for various P450 isoforms

P450 IsoformProbe ReactionHLMsrP450RAF
Km,uVmaxfuKm,uVmaxfu
µMµM/minµMµM/min
CYP1A2Phenacetin O-deethylation66.30.5141.005.70.7331.000.061
CYP2C9Diclofenac 4′-hydroxylation22.40.0400.807.90.0340.840.415
Tolbutamide 4-hydroxylation236.50.0580.9576.70.1140.920.164
S-Warfarin 7-hydroxylation10.20.0020.836.90.0040.950.289
CYP2C19S-Mephenytoin 4′-hydroxylation56.80.0390.9119.80.8870.950.015
CYP2D6Bufuralol 1′-hydroxylation5.40.0600.576.71.1350.780.066
CYP3A4Midazolam 1′-hydroxylation4.83.8780.603.32.9810.700.904
Nifedipine dehydrogenation8.40.7540.586.30.7700.770.734
Testosterone 6β-hydroxylation10.20.6680.788.017.9600.820.029