The inhibitory effect of (−)-OSU6162 on specific P450 enzyme activities in recombinant P450 microsomes
| P450 Enzyme | % Control of P450 Marker Substrate Metabolism Mean ± S.D. | ||
|---|---|---|---|
| (−)-OSU6162 1 μM | (−)-OSU6162 10 μM | (−)-OSU6162 100 μM | |
| CYP1A2 | 104.2 ± 4.4 | 106.4 ± 2.3 | 99.8 ± 4.8 |
| CYP2C9 | 93.7 ± 0.6 | 88.5 ± 2.7 | 86.9 ± 2.7 |
| CYP2C19 | 99.8 ± 4.8 | 104.9 ± 0.5 | 99.7 ± 4.9 |
| CYP2D6 | 98.9 ± 3.1 | 72.9 ± 5.0 | 19.1 ± 3.9 |
| CYP2E1 | 107.9 ± 13.1 | 114.7 ± 8.3 | 110.7 ± 7.7 |
| CYP3A4 | 110.6 ± 7.4 | 106.4 ± 2.3 | 94.7 ± 3.4 |
Values are the mean ± S.D. of triplicate determinations. Incubation conditions and concentrations of P450 marker substrates are as described under Experimental Procedures.