Table 2

Kinetic analysis of 7-ethoxyresorufin O-deethylation by recombinant human P450 enzymes and by human liver microsomes

Enzymes7-EthoxyresorufinO-Deethylation
Km (μM)Vmax (nmol/min/nmol P450)
Human enzymes
 CYP1A12.8  ± 0.518.2  ± 1.2
 CYP1A23.0  ± 0.60.23  ± 0.02
 CYP1B11.0  ± 0.21.33  ± 0.06
 Liver chromosomes2.9  ± 0.50.21  ± 0.01
Rat enzymes
 CYP1A13.3  ± 0.611.4  ± 0.9
 CYP1A22.3  ± 0.40.83  ± 0.05
  • Kinetic analysis was determined using P450 concentrations of 5 nM for human CYP1A1 and 1B1 and rat CYP1A1 and 1A2 and 20 nM for human CYP1A2 and liver microsomes. Values are means ± SEM of duplicate determinations at substrate concentrations between 2∼16 μM (using a nonlinear kinetic analysis).