Cytochrome P-450, Percentage of Control | ||||||
---|---|---|---|---|---|---|
CYP3A4 | CYP3A4 | CYP1A2 | CYP2C19 | CYP2C9 | CYP2D6 | |
10 μM LOR | 118.6 | 86.9 | 99.4 | 26.4 | 68.7 | 45.1 |
IC50LOR | ≥10 μM | ≥10 μM | ≥10 μM | ≅0.76 μM | ≥10 μM | ≅8.1 μM |
10 μM DL | 84.0 | 80.0 | 110.4 | 112.5 | 106.3 | 86.3 |
IC50DL | ≥10 μM | ≥10 μM | ≥10 μM | ≥10 μM | ≥10 μM | ≥10 μM |
10 μM 3-OH-DL | 75.3 | 90.0 | 98.2 | 101.4 | 89.5 | 97.9 |
IC503-OH-DL | ≥10 μM | ≥10 μM | ≥10 μM | ≥10 μM | ≥10 μM | ≥10 μM |
Substrate | dextromethorphan | testosterone | 7-ethoxyresorufin | mephenytoin | diclofenac | dextromethorphan |
The IC50 experiments were run at approximateKm values established in our laboratory for pooled human liver microsomes and, in general, correspond withKm values found in the literature: [3A4-dextromethorphan] Schmider et al., 1997; [3A4-testosterone]Wang et al., 1997; [1A2] Lin et al., 2001; [2C19] Easterbrook et al., 2001; [2C9] Tang et al., 2000; [2D6] Hickman et al., 1998.