Inhibition of CYP3A4 Activity by M3 in Human Liver Microsomes
| M3 Concentration | Testosterone 6β-hydroxylase activity | ||
|---|---|---|---|
| 40 μM | 80 μM | 200 μM | |
| μM | nmol/min/mg | ||
| 0 | 0.63 ± 0.04 | 1.17 ± 0.05 | 2.07 ± 0.03 |
| 0.5 | 0.59 ± 0.05 (7%) | 1.19 ± 0.00 (−2%) | 2.07 ± 0.06 (0%) |
| 5.0 | 0.56 ± 0.01 (11%) | 1.05 ± 0.02 (10%) | 2.02 ± 0.00 (3%) |
Activity is expressed as mean ± SD. Values in parentheses represent the percentage of inhibition of CYP3A4 by M3 in comparison with control samples that do not contain M3.