TABLE 6

N-De-ethylating activities by rat recombinant CYP3A forms. The enzyme activity was measured using 50 μg of microsomal protein of COS-1 cells described in detail under Materials and Methods. Activities represented are the mean and the standard deviation of three different experiments by nmol/min/nmol P450.


P450

Substrate
Amiodarone
Lidocaine
CYP3A62 0.008 ± 0.008 0.054 ± 0.012
CYP3A1 0.038 ± 0.005 0.081 ± 0.004
CYP3A2 0.018 ± 0.015 0.174 ± 0.006
CYP3A9 0.156 ± 0.010 0.178 ± 0.007
CYP3A18
0.084 ± 0.008
0.067 ± 0.006