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

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

  • Bioorg Med Chem Lett. 2005 Oct 1;15(19):4230-4. doi: 10.1016/j.bmcl.2005.06.067.
Cecilia Mattsson 1,  Clas Sonesson,  Anna Sandahl,  Hartmut E Greiner,  Michael Gassen,  Jörg Plaschke,  Joachim Leibrock,  Henning Böttcher
Affiliations

Affiliation

  • 1 Medicinal Chemistry, Carlsson Research AB, Biotech Center, Arvid Wallgrens Backe 20, SE-413 46 Goteborg, Sweden. cecilia.mattsson@carlssonresearch.se
PMID: 16055331 DOI: 10.1016/j.bmcl.2005.06.067
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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