Table 5. Permeability (Pe 10–6 cm·s–1) in the PAMPA-BBB Assay for 10 Commercial Drugs, Used in the Experiment Validation, and Different N-(Benzothiazolyl)-phenylamides with Their Predictive Penetration in the CNS.
| compd | bibl | Pea (10–6 cm·s–1) | BBB prediction |
|---|---|---|---|
| atenolol | 0.8 | 0.2 ± 0.1 | |
| caffeine | 1.3 | 0.9 ± 0.1 | |
| desipramine | 12 | 14.6 ± 0.6 | |
| enoxacine | 0.9 | 0.2 ± 0.1 | |
| hydrocortisone | 1.9 | 1.1 ± 0.8 | |
| ofloxacine | 0.8 | 0.4 ± 0.3 | |
| piroxicam | 2.5 | 0.5 ± 0.1 | |
| promazine | 8.8 | 12.7 ± 1.3 | |
| testosterone | 17 | 21.8 ± 4.0 | |
| verapamil | 16 | 24.6 ± 1.5 | |
| 17 | 5.6 ± 0.8 | CNS+ | |
| 20 | 11.2 ± 2.0 | CNS+ | |
| 27 | 9.6 ± 0.1 | CNS+ | |
| 34 | 11.2 ± 2.0 | CNS+ | |
| 38 | 11.2 ± 2.0 | CNS+ | |
| 41 | 6.4 ± 3.0 | CNS+ | |
| 42 | 14.6 ± 0.1 | CNS+ | |
| 46 | 4.4 ± 2.9 | CNS+ | |
| 47 | 1.4 ± 1.5 | CNS– | |
| 52 | 2.6 ± 0.8 | CNS+/CNS– | |
| 55 | 7.2 ± 2.5 | CNS+ |
a
PBS:EtOH (70:30) was used as solvent. Data are the mean ± SD of three independent experiments.