TABLE 4.
Metabolic stability of sPBTZ derivatives measured in mouse and human microsomes
| Compound | CLint (μl/min/mg protein) |
Source or reference | |
|---|---|---|---|
| Mouse microsome | Human microsome | ||
| 11326059 | 18.6 | 16.8 | This study |
| 11326127 | 19 | 21.5 | This study |
| 11626091 | 2.7 | 9.7 | This study |
| 11626092 | 3 | 1.4 | This study |
| 11626093 | 42 | 6.4 | This study |
| 11626094 | 24 | 277 | This study |
| 11626095 | 0.9 | 1.0 | This study |
| Carbamazepine | 0.6 | 0.4 | This study |
| Nifedipine | 105 | 121.1 | This study |
| PBTZ169 | 36.7 | 28 | 5 |
| BTZ043 | 16.5 | 4.20 | 5 |