Mean enzyme kinetic parameters of the formation of metabolites from benidipine and its enantiomers in HLMs
Values are mean ± S.D. of estimates from four different HLMs.
(+)-α-Benidipine | Racemic Benidipine | (−)-α-Benidipine | |
|---|---|---|---|
| N-Debenzylation | |||
| V max a | 7.7 ± 3.4 | 9.8 ± 4.9 | 12.9 ± 10.1 |
| K m | 10.1 ± 13.8 | 3.8 ± 0.9 | 6.9 ± 5.9 |
| CLint | 2.3 ± 2.3 | 3.0 ± 2.3 | 1.9 ± 0.1 |
| n | 0.9 | 0.8 | 0.9 |
| Dehydrogenation | |||
| V max a | 8.7 ± 2.9 | 8.4 ± 4.7 | 10.7 ± 7.6 |
| K m | 23.6 ± 12.9 | 17.3 ± 11.3 | 21.7 ± 7.2 |
| CLint | 0.6 ± 0.6 | 0.8 ± 0.9 | 0.5 ± 0.2 |
|
n
| 0.8 | 0.9 | 1.0 |
↵ a Vmax is expressed as pmol/min/pmol P450, Km as μM, and CLint as Vmax/Km (μl/min/ pmol P450), n as Hill coefficient.