Synthesis of quinolinyl and isoquinolinyl phenyl ketones as novel agonists for the cannabinoid CB2 receptor

Article abstract of DOI:10.1016/j.bmc.2009.05.013

A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB₂ receptor-dependent G-protein activities were determined using the [³⁵S]GTPγS 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.