Kinetic parameters for P-gp–mediated transport of tested drugs
Each parameter represents the mean ± computer-calculated S.D. (n = 3).
| Compound | Vmaxa | Kma | Vmax/Km |
|---|---|---|---|
| pmol/min/106 cells | μM | μl/min/106 cells | |
| Celiprolol | — | — | 1.51 |
| Digoxin | — | — | 6.83 |
| Fexofenadine | 38.7 ± 13.1 | 25.9 ± 5.9 | 1.49 |
| Talinolol | 57.5 ± 17.8 | 11.2 ± 3.3 | 4.68 |
| Indinavir | 32.0 ± 28.8 | 5.94 ± 4.35 | 5.39 |
| Quinidine | 75.7 ± 2.3 | 1.26 ± 0.23 | 60.1 |
| Saquinavir | — | — | 63.6 |
| Verapamil | — | — | 1.18 |
—, Saturation kinetics was not observed.
↵a The Vmax and Km values with regard to unbound concentration in the cells were calculated based on the model analysis method (Tachibana et al., 2010). Vmax converted by 40 × 104 cells/0.33 cm2.