Synthesis of quinolinyl and isoquinolinyl phenyl ketones as novel agonists for the cannabinoid CB2 receptor.
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.
Reux
Bastien
B
Laboratory of Organic Chemistry, Helsinki University of Technology, Finland.
Nevalainen
Tapio
T
Raitio
Katri H
KH
Koskinen
Ari M P
AM
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*
D007546:Isoquinolines; D007659:Ketones; D011804:Quinolines; D043885:Receptor, Cannabinoid, CB2