TABLE 2.
Nonspecific binding of cationic diamidines in mouse plasma and brain
| Compound | Concn (μM) | % fu (mean ± SD)a in: |
|
|---|---|---|---|
| Plasma | Brain | ||
| Pentamidine | 1 | 8.4 ± 1.2b | 0.3 ± 0.1 |
| 5 | 10 ± 1.2 | 0.5 ± 0.1 | |
| DB75 | 1 | 6.8 ± 0.7 | 0.1 ± 0.05 |
| 5 | 8.0 ± 0.4 | 0.09 ± 0.01 | |
| DB820 | 1 | 21 ± 2.0 | 0.2 ± 0.05c |
| 5 | 19 ± 2.4 | 0.4 ± 0.06c | |
| DB829 | 1 | 40 ± 8.2b | 1.5 ± 0.3 |
| 5 | 36 ± 3.3 | 1.4 ± 0.4 | |
a
fu, drug unbound fraction. Results are from triplicate determinations.
b
Previously published value (8).
c
The difference between the results at 1 and 5 μM was statistically significant (P < 0.05).