Table 1. Binding Data of the Synthesized Compounds 11–31 for 5-HT6R.
compd | Q | R | R1 | 5-HT6Ki [nM]a |
---|---|---|---|---|
Ib | 2-napthtyl | H | H | 27 ± 6 |
11 | 3-quinolinyl | H | H | 13 ± 3 |
12 | 6-quinolinyl | H | H | 20 ± 4 |
13 | 7-quinolinyl | H | H | 7 ± 2 |
14 | 3-isoquinolinyl | H | H | 12 ± 1 |
15 | 4-isoquinolinyl | H | H | 5 ± 1 |
16 | 3-quinolinyl | 5-Cl | H | 11 ± 2 |
17 | 5-quinolinyl | 5-Cl | H | 11 ± 3 |
18 | 7-quinolinyl | 5-Cl | H | 9 ± 2 |
19 | 4-isoquinolinyl | 5-Cl | H | 18 ± 3 |
IIb | 2-napthtyl | 5-MeO | H | 19 ± 2 |
20 | 3-quinolinyl | 5-MeO | H | 8 ± 1 |
21 | 5-quinolinyl | 5-MeO | H | 4 ± 1 |
22 | 6-quinolinyl | 5-MeO | H | 14 ± 3 |
23 | 7-quinolinyl | 5-MeO | H | 2 ± 0.4 |
24 | 3-isoquinolinyl | 5-MeO | H | 6 ± 1 |
25 | 4-isoquinolinyl | 5-MeO | H | 3 ± 0.2 |
26 | 3-quinolinyl | 6-Cl | H | 37 ± 5 |
27 | 6-quinolinyl | 6-Cl | H | 112 ± 9 |
28 | 7-quinolinyl | 6-Cl | H | 22 ± 2 |
29 | 3-isoquinolinyl | 6-Cl | H | 102 ± 12 |
30 | 7-quinolinyl | H | Me | 18 ± 3 |
31 | 3-isoquinolinyl | H | Me | 20 ± 2 |
Mean Ki values ± SEM based on three independent binding experiments.
Data from ref (13).