Inhibition of human cytochrome P450 activities in pooled human liver microsomes by montelukast
P450 | Activity | Microsomal Protein Concentration | IC50 (Mean ± S.E.) |
|---|---|---|---|
| mg/ml | μM | ||
| CYP1A2 | Phenacetin O-deethylase | 0.03 | 16 ± 0 |
| CYP2A6 | Coumarin 7-hydroxylase | 0.03 | 11 ± 2 |
| CYP2B6 | Bupropion hydroxylase | 0.05 | 11 ± 2 |
| CYP2C8 | Amodiaquine N-deethylase | 0.025 | 0.020 ± 0.002 |
| CYP2C9 | Diclofenac 4′-hydroxylase | 0.03 | 1.2 ± 0.1 |
| CYP2C19 | (S)-Mephenytoin 4′-hydroxylase | 0.20 | 32 ± 3 |
| CYP2D6 | Dextromethorphan O-demethylase | 0.03 | 11 ± 1 |
| CYP2E1 | Chlorzoxazone 6-hydroxylase | 0.05 | 180 ± 20 |
| CYP3A | Felodipine dehydrogenase | 0.01 | 1.2 ± 0.2 |
| CYP3A | Midazolam 1′-hydroxylase | 0.03 | 7.9 ± 0.9 |
| CYP3A | Testosterone 6β-hydroxylase | 0.03 | 7.9 ± 1.1 |