Inhibitor |
µM |
Enzyme Inhibited |
Percent Inhibition of NODV Formationa |
Percent Inhibition of Benzyl Hydroxyl Desvenlafaxine Formationa |
α-Naphthoflavone |
1 |
CYP1A2 |
0 |
0 |
Coumarin |
100 |
CYP2A6 |
0 |
0 |
Sulfaphenazole |
10 |
CYP2C9 |
21 |
0 |
S(+)-Mephenytoin |
100 |
CYP2C19 |
0 |
0 |
Quinidine |
10 |
CYP2D6 |
4 |
0 |
Diethyldithiocarbamate |
100 |
CYP2E1 |
15 |
19 |
Ketoconazole |
50
5
1 |
CYP3A4
CYP3A4
CYP3A4 |
76
65
29 |
58
29
0 |
Benzylimidazole |
1000 |
All CYPs |
87 |
99 |
Heat inactivation |
1 min at 50°C |
FMO |
0 |
0 |
aValues are expressed as percent inhibition relative to a control reaction using the formula: % inhibition = ([a - b]/a * 100%), where a = peak area of metabolite with no
inhibitor present, and b = peak area of metabolite with inhibitor present.
Abbreviations: CYP, cytochrome P450; FMO, flavin-containing monooxygenase. |
