Model parameters for DTZ and nd-DTZ
Parameters | Values | References |
|---|---|---|
| PK parameters | ||
| DTZ | ||
| Ka (h-1) | 0.9 | Hermann et al., 1983 |
| Tlag (h) | 0.5 | Hermann et al., 1983 |
| Vc (liters) | 120 | Hermann et al., 1983 |
| Vp (liters) | 141 | Hermann et al., 1983 |
| CLr (l/h) | 0.06 | Hermann et al., 1983 |
| CLint (l/h) | 900 | Hermann et al., 1983 |
| CLint, 3A (l/h) | 360a | |
| CLint, non3A (l/h) | 540 | |
| Vmax, 3A (mg/h) | 432 | |
| Vmax, non3A (mg/h) | 648 | |
| Vmax, GW (mg/h) | 432 | |
| Km (mg/l) | 1.2 | Jones et al., 1999 |
| fu | 0.2 | Piepho et al., 1982 |
| nd-DTZ | ||
| Vnd-DTZ (liters) | 261b | |
| t1/2 (h) | 5 | Höglund and Nilsson, 1989 |
| CLnd-DTZ (liters) | 36c | |
| fu | 0.2b | |
| Physiological parameters | ||
| VGW (livers) | 0.25 | Chien et al., 2006 |
| VPV (liters) | 0.07 | Ito et al., 2003 |
| VLIV (liters) | 2.8 | Ito et al., 2003 |
| kdeg (h-1) | 0.03 | Greenblatt et al., 2003 |
| Enzyme inhibition parametersd | ||
| DTZ | ||
| Ki (μM) | 41 | |
| kinact (h-1) | 4.2 | |
| KI (μM) | 3 | |
| nd-DTZ | ||
| Ki (μM) | 0.8 | |
| kinact (h-1) | 3 | |
| KI (μM) | 0.3 |
|