Summary of preincubation time, P450 inhibitors, substrates, and metabolites for specificity study
P450 Isozymes | Preincubation Time | Inactivators and Concentrations | Substrates | Metabolites | Mass Transitions of Metabolites |
---|---|---|---|---|---|
min | |||||
1A2 | 15 | 1 µM Furafylline | Phenacetin | Acetaminophen | 152 > 110 |
2B6 | 15 | 20 µM Phencyclidine | Bupropion | OH-bupropion | 256 > 238 |
2D6 | 15 | 1.8 µM Paroxetine | Dextromethorphan | Dextrorphan | 258 > 199 |
2C8 | 30 | 100 µM Gemfibrozil glucuronide | Amodiaquine | N-desethylamodiaquine | 328 > 283 |
2C9 | 30 | 15 µM Tienilic acid | Diclofenac | 4′-OH diclofenac | 312 > 231 |
2C19 | 15 | 8 µM Esomeprazole | Mephenytoin | 4′-OH-mephenytoin | 235 > 150 |
3A | 15 | 25 µM Troleandomycin | Midazolam | 1′-OH-midazolam | 324 > 203 |
3A4 | 15 | 2 µM CYP3cide | Midazolam | 1′-OH-midazolam | 342 > 203 |
Pan-CYP | 30 | 1 mM ABT, 15 µM tienilic acid | All substrates listed above | All metabolites listed above | NA |