Recommended in vitro probe substrates and inactivators for evaluation of TDI (including MBI) of P450 enzymes
Isoform | Substrate | Positive Control TDI | Reference |
|---|---|---|---|
| CYP1A2 | Phenacetin | Furafylline | Kunze and Trager, 1993 |
| Ethoxyresorufin | |||
| CYP2B6 | Bupropion | Ticlopidine | Richter et al., 2004 |
| thioTEPA | Richter et al., 2005 | ||
| CYP2C8 | Paclitaxel | Gemfibrozil-glucuronide | Ogilvie et al., 2006 |
| Amodiaquine | Phenelzine | Polasek et al., 2004 | |
| CYP2C9 | Diclofenac | Tienilic acid | Jean et al., 1996 |
| Tolbutamide | |||
| S-Warfarin | |||
| CYP2C19 | S-Mephenytoin | Ticlopidine | Ha-Duong et al., 2001 |
| Omeprazole | |||
| CYP2D6 | Dextromethorphan | Paroxetine | Bertelsen et al., 2003 |
| Bufuralol | |||
| CYP3A4 | Testosterone | Mifepristone | He et al., 1999 |
| Midazolam | Verapamil | Wang et al., 2004 | |
| Troleandomycin | Atkinson et al., 2005 | ||
|
|
| Erythromycin |
McConn, et al., 2004
|
TEPA, N,N′,N″-triethylenethiophosphoramide.