In vitro PAMPA-BBB penetration results.
| Compounds label | Permeability (PAMPA-BBB)aPe(tested) (10−6 cm s−1) | Prediction of CNS penetration |
|---|---|---|
| 23 | 5.9 | High |
| 25 | 6.4 | High |
| 27b | 0.01 | No |
| 28 | 5.0 | High |
| 29 | 0.37 | No |
| Donepezil | 16.7 | High |
| Validation of the model by seven commercial drugs | ||
| Diazepam | 15.30 | High |
| Atenolol | 0.75 | No |
| Alprazolam | 5.60 | High |
| Lomefloxacin | 1.12 | No |
a
Data represent are the assay mean for the marketed drugs (n = 3). b‘CNS+’ (prediction of high BBB permeation); Pe (10−6 cm s−1) > 4.39. c‘CNS−’ (prediction of low BBB permeation); Pe (10−6 cm s−1) < 1.78.
b
Italics cells showed compounds with no BBB permeability.