CYP3A4 | CYP3A5 | |||||
---|---|---|---|---|---|---|
(+)-α-Benidipine | (−)-α-Benidipine | (+)-α-Benidipine | (−)-α-Benidipine | |||
N-Debenzylation | ||||||
V max a | 62.7 ± 1.2 | 89.0 ± 6.3 | 25.7 ± 1.3 | 17.9 ± 1.4 | ||
K m | 5.5 ± 2.3 | 5.9 ± 2.2 | 2.5 ± 0.7 | 2.2 ± 0.1 | ||
CLint | 12.3 ± 4.9 | 16.1 ± 5.0 | 10.4 ± 2.1 | 8.1 ± 0.1 | ||
n | 1.2 | 1.2 | 1.6 | 0.9 | ||
Dehydrogenation | ||||||
V max | 31.7 ± 2.5 | 33.6 ± 0.2 | 9.1 ± 0.1 | 8.9 ± 1.4 | ||
K m | 15.2 ± 0.5 | 20.8 ± 2.4 | 15.4 ± 0.9 | 38.2 ± 12.7 | ||
CLint | 2.1 ± 0.1 | 1.6 ± 0.2 | 0.6 ± 0.1 | 0.2 ± 0.1 | ||
n
| 1.5 | 1.3 | 1.3 | 1.0 |
↵ a Vmax is expressed as pmol/min/pmol P450, Km as μM, and CLint as Vmax/Km (μl/min/pmol of P450), n as Hill coefficient.