P450 inhibition of m/z 217 formation by liver microsomes from BNF-treated mice
Incubations were conducted for 30 min at 37°C with 0.06 mM IQ. Furafylline was preincubated for 10 min before addition of IQ. For those incubations, the control microsomal activity was 0.31 ± 0.02 nmol, which is not different from the control value above. Data are expressed as mean nanomole of m/z 217 ± S.E. with n = 3 to 6.
Test Agents | Type of P450 Inhibitor | Concentration | Activity | % of Total |
|---|---|---|---|---|
| μM | nmol | |||
| Control | 0.29 ± 0.02 | 100 | ||
| Ellipticine | 1A | 10 | N.D. | 0 |
| 20 | N.D. | 0 | ||
| Furafylline | 1A2 | 20 | 0.16 ± 0.04* | 55 |
| α-Naphthoflavone | 1A | 20 | 0.07 ± 0.04* | 24 |
| 100 | N.D. | 0 | ||
| SKF-525A | Nonspecific | 20 | 0.19 ± 0.01* | 66 |
| 100 | 0.18 ± 0.01* | 62 | ||
| Ketoconazole | 3A | 20 | 0.17 ± 0.01* | 59 |
| 100 | 0.07 ± 0.04* | 24 | ||
| Sulfaphenazole | 2C | 20 | 0.27 ± 0.02 | 93 |
|
|
| 100 | 0.26 ± 0.01 | 90 |
N.D., not detected.
↵* p < 0.05 compared with control.