Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 50, Issue 16, Pages 3851-3856Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm070317a
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Selective activation of peripheral cannabinoid CB, 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, naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone (13), which displays good oral bioavailability, potent antihyperalgesic activity in animal models, and limited brain penetration.
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