Metabolism of quinoline and isoquinoline by P450 enzymes Values are mean rates ± the standard deviation of triplicate incubations. Rates are expressed in pmol product/nmol P450/min.
P450 | Substrate | N-oxide | 5-OH | 3-OH |
|---|---|---|---|---|
| 3A4a | Quinoline | 1798 ± 180 | 183 | 86 |
| Isoquinoline | 1437 ± 127 | 0 | 0 | |
| 2E1a | Quinoline | 30 ± 3 | 371 | 3012 ± 390 |
| Isoquinoline | 965 ± 172 | 0 | 0 | |
| 2B4 | Quinoline | 221 ± 32 | 85 | 2620 ± 762 |
| Isoquinoline | 3292 ± 388 | 0 | 0 | |
| Cam | Quinoline | 516 ± 9 | 1376 ± 42 | 0 |
|
| Isoquinoline | 4538 ± 45 | 615 ± 38 | 0 |
↵ a Larger values were obtained for the rate of quinoline oxidation with CYP2E1 and 3A4 when the PanVera RECO system was thawed and used for the first time, since the P450 concentration was more accurate. Therefore, to compare rates to those of isoquinoline, the quinoline incubations were performed again, this time with the isoquinoline incubations, using the same tube of enzyme mix