Plasma and brain concentrations in wild-type and knockout mice after oral (20 mg/kg) administration of GDC-0980
Results presented as mean of three animals ± S.D.
| Mice | Time | Total | Free | ||||
|---|---|---|---|---|---|---|---|
| Brain | Plasma | Brain-to-Plasma Ratio | Brain | Plasma | Brain-to-Plasma Ratio | ||
| h | μM | μM | μM | μM | |||
| FVBn | 1 | 0.52 ± 0.055 | 6.4 ± 1.1 | 0.082 ± 0.0087 | 0.042 ± 0.0044 | 1.9 ± 0.32 | 0.022 ± 0.0023 |
| Mdr1a/1b(−/−)/Bcrp1(−/−) | 1 | 9.9 ± 5.2 | 9.5 ± 4.6 | 1.0 ± 0.20 | 0.78 ± 0.41 | 2.8 ± 1.3 | 0.27 ± 0.054 |
| FVBn | 6 | 0.83 ± 0.31 | 10 ± 2.9 | 0.081 ± 0.0071 | 0.065 ± 0.024 | 2.9 ± 0.84 | 0.021 ± 0.0020 |
| Mdr1a/1b(−/−)/Bcrp1(−/−) | 6 | 10 ± 2.8 | 10 ± NC | 1.1 ± NC | 0.79 ± 0.23 | 2.9 ± NC | 0.30 ± NC |
NC, not calculated; n = 2.