Results of blood-brain barrier penetration studies for five Y2R antagonists and BIIE0246
| ID | Brain Penetration Studies | ||
|---|---|---|---|
| Plasma Concentration | Brain Concentration | Ratio [B]/[P] | |
| μM | % | ||
| SF-11 | 8.5 ± 3.3 | 3.7 ± 1.7 | 44 |
| SF-21 | 1.1 ± 0.1 | 0.4 ± 0.03 | 36 |
| SF-22 | 1.6 ± 0.6 | 1.7 ± 0.6 | 106 |
| SF-31 | 9.0 ± 0.7 | 4.5 ± 0.3 | 50 |
| SF-41 | 1.3 ± 0.3 | 1.5 ± 0.2 | 115 |
| BIIE0246 | 12 ± 2 | 0.2 ± 0.1 | 2 |