Kinetic parameters and corresponding CLint and fm values for 4′-hydroxydiazepam, 3-hydroxydiazepam, and nordiazepam in rat liver microsomes and rat hepatocytes Data represent a mean ± S.D. (n = 4).
Parameter | Microsomesa | Hepatocytesb | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 4′-HDZ | 3-HDZ | NDZ | Total | 4′-HDZ | 3-HDZ | NDZ | Total | |||||||
| Vmax (nmoles/min) | 0.4 ± 0.03 | 3.5 ± 0.09 | 0.8 ± 0.04 | - | 0.4 ± 0.05 | 2.2 ± 0.4 | 0.6 ± 0.05 | - | ||||||
| Km (μM) | 1.9 ± 0.6 | 83.5 ± 6.9 | 19.7 ± 3.8 | - | 2.7 ± 0.9 | 51.5 ± 10.1 | 18.4 ± 4.5 | - | ||||||
| CLint (μl/min) | 237.2 ± 56.6 | 41.6 ± 2.9 | 44.2 ± 9.9 | 322.9 ± 64.5 | 167.8 ± 49.8 | 45.1 ± 19.5 | 34.6 ± 12.7 | 247.5 ± 31.9 | ||||||
| fm (fraction of 1) | 0.73 ± 0.04 | 0.13 ± 0.03 | 0.14 ± 0.02 | 1 | 0.67 ± 0.14 | 0.19 ± 0.09 | 0.14 ± 0.05 | 1 | ||||||