Table 2. Binding affinities and brain pharmacokinetics of [CpM(CO)3] complexes.
No. | Aβ1–42Ki (nM) | Brain uptake (% ID g–1) |
Ref. | |
2 min | 60 min | |||
40 | — | 0.25 | 0.11 | 60 |
42 | — | 0.25 a | 0.21 a , c | 61 |
— | 0.24 b | 0.19 b , c | 61 | |
45 | 162 | — | — | 62 |
46 | 37 | 0.18 | 0.08 | 62 |
47 | 366 | — | — | 62 |
48 | 78 | 0.24 | 0.10 | 62 |
49 | 106.0 | — | — | 63 |
50 | 45.3 | 0.80 | 0.69 | 63 |
51 | 46.0 | — | — | 63 |
52 | 61.9 | 0.61 | 0.24 | 63 |
53 | 85.1 | — | — | 63 |
54 | 50.8 | 0.88 | 0.15 | 63 |
55 | 56.6 | — | — | 63 |
56 | 42.2, 37.0, d 64.5 e | 1.21 | 0.06 | 63 |
57 | 142.6 | 0.50 | 0.18 | 64 |
58 | 75.8 | 0.36 | 0.19 | 64 |
59 | 64.1 | 0.26 | 0.11 | 64 |
60 | 24.0 | 0.37 | 0.14 | 64 |
61 | 18.8 | 1.06 | 0.39 | 65 |
62 | 22.8 | — | — | 65 |
63 | 12.4 | 0.70 | 0.17 | 65 |
64 | 22.3 | — | — | 65 |
65 | 204.1 | — | — | 65 |
66 | 42.0 | 0.69 | 0.31 | 65 |
67 | 130.6 | — | — | 65 |
68 | 15.1 | 0.54 | 0.10 | 65 |
aThe brain uptake was measured in WT mice.
bThe brain uptake was measured in 10 month-old APP/PS1 Tg mice.
cExpressed as brain uptake determined at 30 min post-injection.
dExpressed as IC50 values (nM) for Aβ1–40 aggregates.
eExpressed as IC50 values (nM).