Mattsson Cecilia, Sonesson Clas, Sandahl Anna, Greiner Hartmut E, Gassen Michael, Plaschke Jörg, Leibrock Joachim, Böttcher Henning
Medicinal Chemistry, Carlsson Research AB, Biotech Center, Arvid Wallgrens Backe 20, SE-413 46 Goteborg, Sweden.
Bioorg Med Chem Lett. 2005 Oct 1;15(19):4230-4. doi: 10.1016/j.bmcl.2005.06.067.
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.
合成了一系列2-烷基-3-(1,2,3,6-四氢吡啶-4-基)-1H-吲哚，并对其5-HT6活性进行了评估。该系列中最有效的激动剂是5-氯-2-甲基-3-(1,2,3,6-四氢吡啶-4-基)-1H-吲哚，在3H-LSD结合实验中的IC50 = 7.4 nM，在测量环磷酸腺苷生成的功能实验中的EC50 = 1.0 nM。
