Table 2

Individual enzyme kinetic parameters for (−)-OSU6162 N-despropylation

P450 EnzymesKmVmaxVmax/Km
μM pmol/pmol P450/min
CYP1A178.9  ± 8.77.23  ± 0.210.091
CYP1A2591.4  ± 146.72.58  ± 0.380.0043
CYP2C19194.7  ± 7.810.60  ± 0.140.054
CYP2D64.0  ± 0.31.41  ± 0.040.351
CYP3A4439.6  ± 44.71.06  ± 0.0510.0024

Michaelis-Menten parameters (Vmax andKm) and intrinsic clearance (Vmax/Km) were determined from recombinant baculovirus-insect cell microsomes expressing human P450 enzymes.