Table 2. . Permeability values from the PAMPA-BBB assay.
| Ligand | Pe ± SEM (10-6 cm s-1)† | CNS predicted availability ‡ |
|---|---|---|
| 3a | 6.65 ± 1.58 | CNS+ |
| 3b | 4.94 ± 1.15 | CNS+ |
| 3c | 4.44 ± 1.32 | CNS+ |
| 3d | 6.64 ± 0.69 | CNS+ |
| 3e | 9.18 ± 1.67 | CNS+ |
| 3f | 17.4 ± 3.96 | CNS+ |
| 3g | 31.2 ± 6.72 | CNS+ |
| 4a | 3.10 ± 0.17 | CNS+/− |
| 4b | 6.70 ± 1.19 | CNS+ |
| 4c | 7.91 ± 1.59 | CNS+ |
| 4d | 9.09 ± 1.54 | CNS+ |
| 4e | 12.9 ± 3.19 | CNS+ |
| 4f | 12.9 ± 2.42 | CNS+ |
| Tacrine | 6.0 ± 0.6 | CNS+ |
| Donepezil | 21.9 ± 2.1 | CNS+ |
| Rivastigmine | 20.0 ± 2.1 | CNS+ |
| Ibuprofen | 18.0 ± 4.3 | CNS+ |
| Chlorothiazide | 1.1 ± 0.5 | CNS− |
| Furosemide | 0.2 ± 0.07 | CNS− |
| Ranitidine | 0.04 ± 0.02 | CNS− |
| Sulfasalazine | 0.09 ± 0.05 | CNS− |
†
Results are expressed as the mean of at least three experiments ± SEM.
‡
Classification of the prediction to cross the BBB: 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 [45].
BBB: Blood–brain barrier; PAMPA: Parallel artificial membrane permeability assay; Pe: Permeability coefficient; SEM: Standard error of the mean.