Conversion of cisapride (0.1 and 1.0 μM) to Nor, 3F, and 4F and (±)-norcisapride (0.1 and 1.0 μM) to UNK by heterologously expressed human P450 enzymes
| Expressed Human P450 Enzyme | Metabolite Formation | |||||||
|---|---|---|---|---|---|---|---|---|
| Nor | 3F | 4F | UNK | |||||
| 0.1 μM | 1.0 μM | 0.1 μM | 1.0 μM | 0.1 μM | 1.0 μM | 0.1 μM | 1.0 μM | |
| pmol/nmol P450/min | ||||||||
| CYP1A2 | <0.1 | 0.88 ± 0.06 | <0.1 | <0.1 | <0.1 | <0.1 | <0.005 | <0.005 |
| CYP2B6 | 0.18 ± 0.02 | 1.66 ± 0.05 | <0.1 | <0.1 | <0.1 | <0.1 | <0.005 | <0.005 |
| CYP2C8 | 0.53 ± 0.07 | 5.38 ± 1.10 | 1.17 ± 0.54 | 15.5 ± 2.6 | 0.14 ± 0.12 | 1.51 ± 1.31 | <0.005 | <0.005 |
| CYP2C9 | <0.1 | <0.1 | <0.1 | <0.1 | <0.1 | <0.1 | <0.005 | <0.005 |
| CYP2C19 | <0.1 | 0.31 ± 0.10 | <0.1 | 0.57 ± 0.39 | <0.1 | 0.20 ± 0.15 | <0.005 | <0.005 |
| CYP2D6 | <0.1 | <0.1 | <0.1 | 0.32 ± 0.19 | <0.1 | 0.28 ± 0.21 | <0.005 | <0.005 |
| CYP2E1 | <0.1 | <0.1 | <0.1 | <0.1 | <0.1 | <0.1 | <0.005 | <0.005 |
| CYP3A4 | 130 ± 4 | 950 ± 164 | 59.8 ± 12.9 | 341 ± 124 | 46.8 ± 10.5 | 338 ± 39 | 0.092 ± 0.003 | 0.339 ± 0.019 |
| CYP3A5 | 0.41 ± 0.03 | 4.04 ± 0.70 | 0.19 ± 0.02 | 1.90 ± 0.89 | 0.46 ± 0.10 | 5.37 ± 2.71 | <0.005 | <0.005 |
| CYP3A7 | 2.26 ± 0.10 | 17.6 ± 2.05 | <0.1 | 0.49 ± 0.11 | 0.11 ± 0.09 | 1.44 ± 0.94 | <0.005 | <0.005 |