The kinetic parameters for the inactivation of the 7-EFC O-deethylation activity of P450 2B6 when incubated with the six different phenyl diaziridine compounds
The kinetic constants were derived from the double reciprocal plots of the rates of inactivation of 7-EFC O-deethylation activity as a function of the inactivator concentrations. The kinetic constants represent the mean and standard error from three different experiments.
Substituted Phenyl Diaziridines | KI | kinact | t1/2 | ||
|---|---|---|---|---|---|
| μM | min-1 | min | |||
| 4-Methoxy (1a) | 7.1 ± 1.9 | 0.042 | 16.5 | ||
| 4-Ethoxy (1b) | 2 ± 0.7 | 0.079 | 8.8 | ||
| 3,4-Dimethoxy (1c) | 2.5 ± 1.2 | 0.06 | 11.4 | ||
| 4-Methylthio (1d) | No inactivation | ||||
| 3-Methyl,4-methoxy (1e) | 1.7 ± 0.2 | 0.066 | 10.5 | ||
| 3,4,5-Trimethoxy (1f) | 2.7 ± 0.9 | 0.05 | 14 | ||