TABLE 2.
Kinetic parameters for (S,S)- and (R,R)-hydroxybupropion formation from RS-bupropion by POR variants
| POR variant | (S,S)-hydroxybupropion formation from RS-bupropion | (R,R)-hydroxybupropion formation from RS-bupropion | ||||
|---|---|---|---|---|---|---|
| Vmax | Km | Clinta | Vmax | Km | Clint a | |
| pmol/min per picomole | µM | ml/min per nanomole | pmol/min per picomole | µM | ml/min per nanomole | |
| POR.1 | 26.4 ± 0.5 | 18.2 ± 1.5 | 1.45 (100) | 9.0 ± 0.1 | 11.4 ± 0.8 | 0.79 (100) |
| POR.5 | 21.0 ± 1.6 | 15.5 ± 3.1 | 1.35 (93) | 9.1 ± 0.1 | 10.5 ± 0.7 | 0.87 (110) |
| POR.28 | 21.4 ± 0.7 | 13.3 ± 1.1 | 1.61 (111) | 10.5 ± 0.1 | 8.9 ± 0.5 | 1.18 (149) |
| POR P228L | 21.3 ± 0.8 | 18.8 ± 1.8 | 1.13 (78) | 10.5 ± 0.1 | 13.0 ± 0.5 | 0.81 (103) |
a
Values in brackets represent percentages of CYP2B6.1 Clint.