To further investigate the structure–activity relationship (SAR) of the 5-hydroxytryptamine type 6 (5-HT6) receptor agonist 5-chloro-2-methyl-3-(1, 2, 3, 6-tetrahydropyridin-4-yl)-1H- indole (EMD386088, 6), a series of 2-methyl-3-(1, 2, 3, 6-tetrahydropyridin-4-yl)-1H-indoles were synthesized, and in vitro affinity to, and functional activity at 5-HT6 receptors was tested. We focused on substituents made at the indole N1-, 2-and 5-positions and these ...
