title: Synthesis of quinolinyl and isoquinolinyl phenyl ketones as novel agonists for the cannabinoid CB2 receptor.
abstract: A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB(2) receptor-dependent G-protein activities were determined using the [(35)S]GTPgammaS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB(2) receptor agonist activity, the most potent ligands being the 2-(Me(2)N)-phenyl substituted derivatives, which were also full agonists at the CB(2)-receptor.
authors.affiliation: Laboratory of Organic Chemistry, Helsinki University of Technology, Finland.
authors.forename: Bastien
authors.initials: B
authors.lastname: Reux
authors.forename: Tapio
authors.initials: T
authors.lastname: Nevalainen
authors.forename: Katri H
authors.initials: KH
authors.lastname: Raitio
authors.forename: Ari M P
authors.initials: AM
authors.lastname: Koskinen
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007659:Ketones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011485:Protein Binding; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists* / Q000378:metabolism*
chemical_list: D007546:Isoquinolines; D007659:Ketones; D011804:Quinolines; D043885:Receptor, Cannabinoid, CB2