Effect of preadministration of various compounds at 5 mM on [3H]PGE2 elimination from brain across the BBB in mice
Each compound or ECF buffer (control) was administered at 5 min before administration of [3H]PGE2. Clarithromycin, itraconazole, indomethacin, ketoprofen, dipyridamole, or celecoxib was administered with ECF buffer containing 0.25% DMSO. As a control for these compounds, ECF buffer containing 0.25% DMSO was injected. The BEI value was determined 40 min after intracerebral microinjection of [3H]PGE2. Each value represents the mean ± S.E.M.
| Compound | No. Studied | BEI | %Control |
|---|---|---|---|
| % | |||
| Antibiotics and antifungals | |||
| Control | 7 | 65.3 ± 1.6 | 100 ± 3 |
| Cefmetazole | 6 | 40.2 ± 3.2 | 61.5 ± 4.8** |
| Cefazolin | 5 | 44.5 ± 4.3 | 68.2 ± 6.6** |
| Cefotaxime | 3 | 32.0 ± 2.0 | 49.0 ± 3.0** |
| Ceftriaxone | 4 | 39.9 ± 7.0 | 61.0 ± 10.7** |
| Benzylpenicillin | 4 | 46.5 ± 4.7 | 71.2 ± 7.1** |
| Cefotiam | 3 | 63.9 ± 4.7 | 97.9 ± 5.2 |
| Cefsulodin | 4 | 58.3 ± 3.4 | 89.3 ± 5.2 |
| Control (0.25% DMSO) | 8 | 62.6 ± 3.5 | 100 ± 6 |
| Clarithromycin (0.25% DMSO) | 5 | 55.3 ± 5.7 | 88.3 ± 9.1 |
| Itraconazole (0.25% DMSO) | 7 | 51.4 ± 3.8 | 82.1 ± 6.1 |
| Inhibitors of organic anion transporters and NSAIDs | |||
| Control (0.25% DMSO) | 8 | 62.6 ± 3.5 | 100 ± 6 |
| Indomethacin (0.25% DMSO) | 3 | 13.0 ± 5.6 | 20.8 ± 9.0** |
| Ketoprofen (0.25% DMSO) | 3 | 30.1 ± 4.4 | 48.1 ± 7.1** |
| Dipyridamole (0.25% DMSO) | 3 | 61.4 ± 5.4 | 98.1 ± 8.6 |
| Celecoxib (0.25% DMSO) | 3 | 63.9 ± 5.7 | 102 ± 9 |
↵** p < 0.01, significantly different from control.