Activities for APZ and MDZ metabolite formation in liver and small intestinal microsomes from humans and cynomolgus monkeys
Activity was measured at a substrate concentration of 10 μM. Each value represents the mean of duplicate incubations.
| Metabolite | Liver Microsomes | Intestinal Microsomes | ||
|---|---|---|---|---|
| Human | Monkey | Human | Monkey | |
| nmol/(min · mg protein) | ||||
| 1′-OH APZ | 0.0062 | 0.0094 | 0.0015 | 0.0042 |
| 4-OH APZ | 0.030 | 0.097 | 0.012 | 0.041 |
| 1′-OH MDZ | 1.1 | 3.1 | 0.40 | 1.0 |
| 4-OH MDZ | 0.10 | 1.0 | 0.050 | 0.28 |