Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2

Bastien Reux, Tapio Nevalainen, Katri H. Raitio, Ari M.P. Koskinen

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    Abstract

    A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB2 receptor-dependent G-protein activities were determined using the [35S]GTPcS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor.
    Original languageEnglish
    Pages (from-to)4441-4447
    JournalBIOORGANIC AND MEDICINAL CHEMISTRY
    Volume17
    Issue number13
    DOIs
    Publication statusPublished - 2009
    MoE publication typeA1 Journal article-refereed

    Keywords

    • cannabinoid
    • receptor CB2
    • quinoline
    • isoquinoline

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