Comparison of kinetic parameter data on pranidipine dehydrogenation and de-esterification of dehydrogenated pranidipine
| Kinetic Parameter | Pranidipine Dehydrogenation3-a | Dehydrogenated Pranidipine De-esterification | |
|---|---|---|---|
| CYP3A4 | CYP2D6 | CYP3A4 | |
| K m (μM) | 21.4 | 11.8 | 8.7 |
| V max (nmol/min/nmol P-450) | 1.96 | 0.47 | 0.84 |
| CLintrinsic (μl/min/nmol P-450) | 91.6 | 39.8 | 96.6 |
The formation rates of dehydrogenated pranidipine were determined over the pranidipine concentration range of 50 to 200 μM in a reaction mixture containing 0.4 mg/ml of microsomal protein (22.4 pmol of P-450) expressing CYP3A4. Enzyme incubation and metabolite analyses were carried out in triplicate and the apparent Kmand Vmax values for pranidipine dehydrogenation by the enzyme were determined using a Lineweaver-Burk reciprocal plot.
↵3-a Referred to the paper described by Kudo et al. (1998).