Table 1.
|
Octanol/water partition coefficient |
Brain uptakes (%ID/g) |
Ki values for Aβ fibrils (nm) |
Fluorescence assay |
|
||
---|---|---|---|---|---|---|---|
|
2 min |
30 min |
Ec50 for Aβ fibrils (nm) |
EC50 for τ fibrils (nm) |
|||
BF-126 | 12.5 | 7.2 ± 0.49 | 0.16 ± 0.030 | 1.2 ± 0.68 | 1280 ± 1.64 | 583 ± 2.07 | |
BF-158 | 47.4 | 11.3 ± 0.81 | 3.1 ± 0.61 | >5000 | 659 ± 2.04 | 399 ± 2.41 | |
BF-170 | 70.3 | 9.1 ± 1.2 | 0.25 ± 0.027 | >5000 | 786 ± 1.79 | 221 ± 2.31 | |
BF-168 |
62.6 |
3.9 ± 0.22a
|
1.6 ± 0.0071a
|
6.4 ± 1.0a
|
346 ± 2.21 |
1010 ± 1.72 |
Brain uptake and EC50 values are shown as the mean ± SEM. Ki values for Aβ fibrils are shown as the mean ± SD.
From Okamura et al., 2004a.