Table 1.
Structures and Binding Affinity for Scopolamine (1), Compounds 8, and 17–36 at the hM1 and hM5 mAcChRsa
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---|---|---|---|---|
compd | R1 |
Ki, nM
|
hM1/hM5 | |
hM1 | hM5 | |||
1 | - | 7.5 | 17.6 | 0.4 |
8 |
![]() |
170 | 420 | 0.4 |
17 |
![]() |
1,730 | 1,250 | 1.4 |
18 |
![]() |
470 | 150 | 3.1 |
19 |
![]() |
3,060 | 3,610 | 0.8 |
20 |
![]() |
3,290 | 470 | 7.0 |
21 |
![]() |
>100,000 | >100,000 | - |
22 |
![]() |
200 | 290 | 0.7 |
23 |
![]() |
100 | 190 | 0.5 |
24 |
![]() |
560 | 410 | 1.4 |
25 |
![]() |
240 | 370 | 0.6 |
26 |
![]() |
810 | 440 | 1.8 |
27 |
![]() |
>100,000 | >100,000 | - |
28 |
![]() |
1,390 | 230 | 6.0 |
29 |
![]() |
200 | 280 | 0.7 |
30 |
![]() |
60 | 120 | 0.5 |
31 |
![]() |
11,700 | 2,460 | 4.8 |
32 |
![]() |
>100,000 | >100,000 | - |
33 |
![]() |
>100,000 | >100,000 | - |
34 |
![]() |
410 | 760 | 0.5 |
35 |
![]() |
370 | 140 | 2.6 |
36 |
![]() |
140 | 190 | 0.7 |
At least three independent experiments with samples evaluated in duplicate were performed to obtain the Ki value.