Prediction of BBB penetration of 2–11 and marketed drugs, expressed as Pe ± SEM (n = 2–3).
| Compound | BBB penetration estimation | |
|---|---|---|
| P e ± SEM (10−6 cm s−1) | CNS (+/−) | |
| LDT544 (2) | N.D.a | |
| LDT636 (3) | 9.6 ± 2.3 | CNS+ |
| LDT637 (4) | 23.1 ± 2.4 | CNS+ |
| LDT638 (5) | 19.5 ± 1.9 | CNS+ |
| LDT639 (6) | 18.8 ± 8.6 | CNS+ |
| LDT640 (7) | 32.0 ± 4.3 | CNS+ |
| LDT641 (8) | 15.3 ± 3.5 | CNS+ |
| LDT642 (9) | 39.3 ± 3.4 | CNS+ |
| LDT643 (10) | 21.7 ± 5.2 | CNS+ |
| LDT692 (11) | 12.0 ± 1.5 | CNS+ |
| Tacrine | 5.96 ± 0.59 | CNS+ |
| Donepezil | 21.49 ± 2.05 | CNS+ |
| Rivastigmine | 20.0 ± 2.07 | CNS+ |
| Chlorothiazide | 1.14 ± 0.53 | CNS− |
| Cefuroxime | 0.62 ± 0.16 | CNS− |
| Furosemide | 0.19 ± 0.07 | CNS− |
a
N.D. stands for not determined due to low solubility in the assay buffer.