Inhibition of estradiol-17β-glucuronide metabolite formation in human microsomes or using yeast-expressed CYP 2C8
Thirty-minute incubations were performed using the indicated inhibitor concentrations and 1 μM P450 liver microsomes, or 0.5 μM expressed P450 and 50 μM substrate. Data are means of two independent determinations.
Concentration | Percentage Inhibition | |||
|---|---|---|---|---|
| Human Microsomes | CYP 2C8 | |||
| μM | ||||
| O2/CO gas | 87 | |||
| Miconazole | 2 | 40 | ||
| Sulfaphenazone | 10 | 26 | ||
| Furafylline | 10 | 19 | ||
| Quinidine | 10 | 21 | ||
| Bromocriptine | 10 | 65 | 3 | |
| Ketoconazole | 10 | 100 | ||
| 2 | 39 | 10 | ||
| Chlorzoxazone | 10 | 13 | ||
| Quercetin | 10 | 60 | 14 | |
| Paclitaxel | 10 | 46 | 31 | |