Kinetic parameters for the formation of cisapride metabolites from each enantiomer by recombinant human CYP3A4 and CYP2C8 (3-F-4-OHCIS)
| P450 | NORCIS | 3-F-4-OHCIS | 4-F-2-OHCIS | ||||||
|---|---|---|---|---|---|---|---|---|---|
| Vmax | Km | Vmax/Km | Vmax | Km | Vmax/Km | Vmax | Km | Vmax/Km | |
| (−)-Cisapride | |||||||||
| CYP3A4 | 0.52 ± 0.2 | 5.6 ± 2.8 | 0.093 | 0.17 ± 0.01 | 5.8 ± 0.9 | 0.03 | 1.17 ± 0.02 | 9.9 ± 0.5 | 0.12 |
| CYP2C8 | 0.15 ± 0.01 | 13.3 ± 3.2 | 0.011 | ||||||
| (+)-Cisapride | |||||||||
| CYP3A4 | 1.17 ± 0.1 | 6.8 ± 2.9 | 0.17 | 0.40 ± 0.01 | 6.1 ± 0.27 | 0.07 | 1.43 ± 0.19 | 25 ± 6.7 | 0.06 |
| CYP2C8 | 0.24 ± 0.02 | 12.6 ± 2.5 | 0.02 | ||||||
Vmax (pmol/min/pmol of P450),Km (μM), andVmax/Km (μl/min/pmol of P450).