Table 2.
In vitro BBB permeability prediction for (±)-1·HCl and (±)-HupY·HCl as positive reference compound.
| Compound | BBB Penetration Estimation | |
|---|---|---|
| Pe ± SEM (10−6 cm·s−1) a | CNS (+/−) b | |
| (±)-1·HCl | 7.64 ± 0.22 | CNS + |
| (±)-HupY·HCl | 5.89 ± 0.36 | CNS + |
| THA | 5.30 ± 0.20 c | CNS + |
| Donepezil | 7.3 ± 0.9 | CNS + |
| 7-MEOTA | 6.50 ± 1.85 | CNS + |
| 6-chlorotacrine | 5.00 ± 0.45 c | CNS + |
| Cefuroxim | 2.70 ± 0.1 | CNS − |
| Piroxicam | 2.20 ± 0.15 | CNS − |
a Results are expressed as the mean of at least three experiments; b CNS +: high BBB permeation predicted with Pe (10−6 cm·s−1) > 4.0, CNS −: low BBB permeation predicted with Pe (10−6 cm·s−1) < 2.0, CNS +/−: BBB permeation uncertain with Pe (10−6 cm·s−1) from 4.0 to 2.0; c taken from references [52,53].