2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists |
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| Authors: | Mattsson Cecilia Sonesson Clas Sandahl Anna Greiner Hartmut E Gassen Michael Plaschke Jörg Leibrock Joachim Böttcher Henning |
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| Institution: | Medicinal Chemistry, Carlsson Research AB, Biotech Center, Arvid Wallgrens Backe 20, SE-413 46 Goteborg, Sweden. cecilia.mattsson@carlssonresearch.se |
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| Abstract: | 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. |
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