Assay conditions used to measure microsomal P450 enzyme activity and inhibition
| Enzyme | Substrate | Substrate Concentration (µM) | Incubation Time (min) | Type of Inhibitor | Positive Control Inhibitor |
|---|---|---|---|---|---|
| CYP1A2 | Phenacetin | 60 | 10 | Reversible | α-Naphthoflavone |
| TDI | Furafylline | ||||
| CYP2B6 | Bupropion | 80 | 15 | Reversible | Sertraline |
| TDI | ThioTEPA | ||||
| CYP2C8 | Amodiaquine | 2 | 10 | Reversible | Montelukast |
| TDI | Phenelzine | ||||
| CYP2C9 | Diclofenac | 5 | 15 | Reversible | Sulfphenazole |
| TDI | Tienilic acid | ||||
| CYP2C19 | S-Mephenytoin | 80 | 25 | Reversible | Benzylnirvanol |
| TDI | Ticlopidine | ||||
| CYP2D6 | Dextromethorphan | 5 | 10 | Reversible | Quinidine |
| TDI | Paroxetine | ||||
| CYP3A4/5 | Midazolam | 2 | 5 | Reversible | Ketoconazole |
| TDI | Azamulin | ||||
| Testosterone | 50 | 10 | Reversible | Ketoconazole | |
| TDI | Azamulin |
ThioTEPA, N,N′,N′′-triethylenethiophosphoramide.