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

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• 作者：Cecilia Mattsson ; Clas Sonesson ; Anna Sandahl ; Hartmut E. Greiner ; Michael Gassen ; Jö ; rg Plaschke ; Joachim Leibrock and Henning Bö ; ttcher
• 关键词：5-HT₆ ; 5-Hydroxytryptamine₆ agonist ; 3-(1 ; 2 ; 3 ; 6-Tetrahydropyridin-4-yl)-1H-indole
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：2005
• 年：2005
• 卷：15
• 期：19
• 页码：4230-4234
• 全文大小：254 K

文摘

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.