Table 2

Selectivity of probe substrate catalysis by the five major human hepatic CYPs

Probe ReactionSubstrate ConcentrationV
CYP1A2CYP2C9CYP2C19CYP2D6CYP3A4
pmol · min−1 · pmol−1
EROD30.400.010.05NDND
10.30NDNDNDND
NaproxenO-demethylation20003.906.804.800.08ND
3003.462.360.87NDND
DiazepamN-demethylation100ND0.032.61ND1.43
20ND0.021.47ND0.48
DextromethorphanO-demethylation30ND0.671.814.000.04
3ND0.030.212.90ND
ErythromycinN-demethylation300ND0.090.230.312.59
40NDND 0.030.031.62
  • ND not detectable (< 0.005 min−1).

  • Enzyme sources were E. coli membranes expressing CYP1A2, CYP2C9, CYP2C19 (single plasmid), CYP2D6, and CYP3A4 as described inMaterials and Methods.