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1: Bioorg Med Chem Lett. 2005 Oct 1;15(19):4230-4.Click here to read Links

2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.

Mattsson C, Sonesson C, Sandahl A, Greiner HE, Gassen M, Plaschke J, Leibrock J, Böttcher H.

Medicinal Chemistry, Carlsson Research AB, Biotech Center, Arvid Wallgrens Backe 20, SE-413 46 Goteborg, Sweden. cecilia.mattsson@carlssonresearch.se

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.

PMID: 16055331 [PubMed - indexed for MEDLINE]