Effects of P450 isoform-specific inhibitors on the formation of M1, M2, and M3 in HLM incubations of glafenine
Values are an average of duplicated measurements and expressed as percentage relative to the control without inhibitors.
| P450 Inhibitor | M1 Formation | M2 Formation | M3 Formation | P450 Activitya |
|---|---|---|---|---|
| α-Naphthoflavone (CYP1A2) | 97.4 | 95.8 | 92.4 | 15.8 |
| Sulfaphenazole (CYP2C9) | 95.8 | 93.6 | 95.6 | 28.2 |
| Tranylcypromine (CYP2C19) | 87.6 | 84.9 | 89.5 | 24.2 |
| Quinidine (CYP2D6) | 92.2 | 95.1 | 91.7 | 10.7 |
| Ketoconazole (CYP3A4) | 14.5 | 12.2 | 20.2 | 16.4 |
a P450 activities were determined using known P450 substrates.