2-烷基-3-(1,2,3,6-四氢吡啶-4-基)-1H-吲哚作为新型5-HT6受体激动剂。
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.
作者信息
Mattsson Cecilia, Sonesson Clas, Sandahl Anna, Greiner Hartmut E, Gassen Michael, Plaschke Jörg, Leibrock Joachim, Böttcher Henning
机构信息
Medicinal Chemistry, Carlsson Research AB, Biotech Center, Arvid Wallgrens Backe 20, SE-413 46 Goteborg, Sweden.
出版信息
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。
Zotero 插件