Table 2.
Kinetic parameters for biotransformation of DZN and DZO in liver and plasma
| Pathway | Rat | Human |
|---|---|---|
| Liver | ||
| DZN to DZO | ||
| Vmax (nmol/min/mg microsomal protein) | 0.288 | 0.187 |
| Km (µM) | 4.745 | 59.600 |
| CE (ml/min/mg microsome protein)a | 0.060 | 0.003 |
| DZN to IMHP | ||
| Vmax (nmol/min/mg microsomal protein) | 1.098 | 0.665 |
| Km (µM) | 1.764 | 16.340 |
| CE (ml/min/mg microsome protein) a | 0.620 | 0.041 |
| DZO to IMHP | ||
| Vmax (nmol/min/mg microsomal protein) | 691.100 | 53.490 |
| Km (µM) | 668.000 | 557.400 |
| CE (ml/min/mg microsome protein) a | 1.030 | 0.096 |
| Plasma | ||
| DZO to IMHP | ||
| Vmax (nmol/min/mg plasma protein) | 431.400 | 124.000 |
| Km (µM) | 535.600 | 701.000 |
| CE (ml/min/mg plasma protein) a | 0.810 | 0.180 |
| Total protein concentration (mg/ml) | 60.000 | 77.000 |
aCE = catalytic efficiency (ml/min/mg microsome protein or ml/min/mg plasma protein) calculated as Vmax/Km