| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1379574 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
A series of 2-alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles were synthesized and evaluated for their 5-HT6 activity. The most potent agonist in this series was 5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole with an IC50 = 7.4 nM in 3H-LSD binding and an EC50 = 1.0 nM in a functional assay measuring production of cyclic AMP.
Graphical abstractA series of 2-alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles was synthesized and evaluated for their 5-HT6 activity. The most potent agonist in this series was 5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole with an IC50 = 7.4 nM in 3H-LSD-binding and an EC50 = 1.0 nM in a functional assay measuring production of cyclic AMP.Figure optionsDownload full-size imageDownload as PowerPoint slide
