Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue 15, Pages 5444-5453Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm200476p
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Funding
- Siena Biotech SpA
- University of Siena [PAR Progetti 2006]
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Experimental evidence suggests that selective CB2 receptor modulators may provide access to antihyperalgesic agents devoid of psychotropic effects. Talcing advantage of previous findings on structure-activity/selectivity relationships for a class of 4-quinolone-3-carboxamides, further structural modifications of the heterocyclic scaffold were explored, leading to the discovery of the 8-methoxy derivative 4a endowed with the highest affinity and selectivity ever reported for a CB2 ligand. The compound, evaluated in vivo in the formalin test, behaved as an inverse agonist by reducing at a dose of 6 mg/kg the second phase of the formalin-induced nocifensive response in mice.
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