Effect of clorgyline and selegiline on the metabolism of [14C]bicifadine to M2 by human liver microsomes and mitochondrial preparations
Pooled human liver microsomes (0.5 mg/ml) and mitochondria (1 mg/ml) were incubated with increasing concentrations of clorgyline or selegiline for 37°C for 20 min. [14C]Bicifadine (1 μM) was then added and the incubation continued for an additional 30 min. The incubations were assayed for metabolites as detailed under Materials and Methods.
Conc. | Activity ± S.D. | |||
|---|---|---|---|---|
| Microsomes | Mitochondria | |||
| μM | pmol/min/mg protein | |||
| Control | 0.0 | 37.7 ± 1.1 | 17.3 ± 0.06 | |
| Selegiline | 0.001 | 40.2 ± 1.9 | 13.9 ± 3.2 | |
| 0.01 | 37.1 ± 3.2 | 14.6 ± 2.9 | ||
| 0.1 | 4.30 ± 0.95 | 3.56 ± 0.41 | ||
| 1 | 2.35 ± 0.05 | 2.67 ± 0.30 | ||
| Clorgyline | 0.001 | 40.5 ± 1.7 | 15.8 ± 1.5 | |
| 0.01 | 38.9 ± 1.3 | 17.8 ± 1.1 | ||
| 0.1 | 36.3 ± 0.3 | 14.4 ± 0.3 | ||
|
| 1 | 33.6 ± 0.5 | 14.0 ± 0.5 | |