TABLE 2

Probe drug and activity used to measure microsomal P450 enzyme activity rate (pmol/mg protein/min) and interindividual variability therein

Liver microsomes were prepared and P450 enzyme activity rates were determined as described under Materials and Methods.


Enzyme

Probe Drug/Activity

Minimum

Maximum

Variability (-Fold)

Mean Activity Level

S.D.
pmol/mg protein/min
CYP1A2 7-Ethoxyresorufin O-dealkylation 5.9 175 30 39 43
CYP2A6 Coumarin 7-hydroxylation 91.5 4000 44 958 1179
CYP2B6 S-Mephenytoin N-demethylation 13 1280 98 191 315
CYP2C8 Paclitaxel 6α-hydroxylation 37.4 2040 55 512 623
CYP2C9 Diclofenac 4′-hydroxylation 210 3530 17 1748 774
CYP2C19 S-Mephenytoin 4′-hydroxylation 2.69 344 128 94 89
CYP2D6 Dextromethorphan O-demethylation 85.5 870 10 392 170
CYP2E1 Chlorzoxazone 6-hydroxylation 358 4270 12 2057 974
CYP3A4/5
Testosterone 6β-hydroxylation
201
20,300
101
5081
6196