Metabolic stability of BBR and 6-F-BBR in liver microsomes
The units of t1/2 and CLint are in minutes and ml/min per milligram protein, respectively; *P < 0.05, **P < 0.01, and ***P < 0.001 compared with BBR.
| Compound | Concentration | MLM | RLM | HLM | |||
|---|---|---|---|---|---|---|---|
| t1/2 | CLint | t1/2 | CLint | t1/2 | CLint | ||
| μM | |||||||
| BBR | 1 | 5.6 | 0.124 | 4.2 | 0.163 | 8.6 | 0.081 |
| 10 | 10.9 | 0.064 | 11.3 | 0.061 | >60 | — | |
| 6-F-BBR | 1 | >60 | — | 8.4** | 0.082*** | 13.6* | 0.051* |
| 10 | >60 | — | 15.1 | 0.046 | >60 | — | |
CLint, intrinsic clearance.
—, CLint was not calculated