Metabolite (Enzyme Involved) | Activity 0–3 h | Activity 24–27 h | % Initial Metabolic Rate after 24-h Preincubation | |
---|---|---|---|---|
pmol/mg protein/min | ||||
1-Hydroxymidazolam (CYP3A4/5) | 11 ± 2 | 5 ± 1 | 42 | |
4-Hydroxydiclofenac (CYP2C9) | 7 ± 1 | 0.6 ± 0.2 | 9 | |
1-Hydroxybufuralol (CYP2D6) | 1.1 ± 0.3 | 0.4 ± 0.04 | 39 | |
Androstenedione (mainly 17β-HSD) | 308 ± 38 | 234 ± 32 | 76 | |
2β-TOH (CYP3A4) | 10 ± 1 | 3 ± 1 | 32 | |
6β-TOH (CYP3A4) | 48 ± 5 | 11 ± 2 | 22 | |
16α-TOH (CYP2Ba) | 9 ± 1 | 5 ± 1 | 51 | |
7-HC (mainly CYP1A1) | 33 ± 14 | 13 ± 7 | 38 | |
7-HC-GLUC (UGT1A6) | 248 ± 29 | 189 ± 38 | 76 | |
7-HC-SULF (SULT) | 42 ± 3 | 23 ± 4 | 53 |
7-HC-SULF, 7-hydroxycoumarin-sulfate; SULT, sulfotransferase
↵ a In rodents