Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl) methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted …

…, LJ Edwards, AJ Fisher, AJ Fox, C Gentry…

文献索引：Dziadulewicz, Edward K.; Bevan, Stuart J.; Brain, Christopher T.; Coote, Paul R.; Culshaw, Andrew J.; Davis, Andrew J.; Edwards, Lee J.; Fisher, Adrian J.; Fox, Alyson J.; Gentry, Clive; Groarke, Alex; Hart, Terance W.; Huber, Werner; James, Iain F.; Kesingland, Adam; La Vecchia, Luigi; Loong, Yvonne; Lyothier, Isabelle; McNair, Kara; O'Farrell, Cathal; Peacock, Marcus; Portmann, Robert; Schopfer, Ulrich; Yaqoob, Mohammed; Zadrobilek, Jiri Journal of Medicinal Chemistry, 2007 , vol. 50, # 16 p. 3851 - 3856

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被引用次数: 62

摘要

Selective activation of peripheral cannabinoid CB1 receptors has the potential to become a valuable therapy for chronic pain conditions as long as central nervous system effects are attenuated. A new class of cannabinoid ligands was rationally designed from known aminoalkylindole agonists and showed good binding and functional activities at human CB1 and CB2 receptors. This has led to the discovery of a novel CB1/CB2 dual agonist, ...