TY - JOUR T1 - Investigations on the 4-quinolone-3-carboxylic acid motif. 4. Identification of new potent and selective ligands for the cannabinoid type 2 receptor with diverse substitution patterns and antihyperalgesic effects in mice. AU - Pasquini,Serena, AU - De Rosa,Maria, AU - Pedani,Valentina, AU - Mugnaini,Claudia, AU - Guida,Francesca, AU - Luongo,Livio, AU - De Chiaro,Maria, AU - Maione,Sabatino, AU - Dragoni,Stefania, AU - Frosini,Maria, AU - Ligresti,Alessia, AU - Di Marzo,Vincenzo, AU - Corelli,Federico, Y1 - 2011/07/06/ PY - 2011/6/28/entrez PY - 2011/6/28/pubmed PY - 2011/10/8/medline SP - 5444 EP - 53 JF - Journal of medicinal chemistry JO - J Med Chem VL - 54 IS - 15 N2 - Experimental evidence suggests that selective CB2 receptor modulators may provide access to antihyperalgesic agents devoid of psychotropic effects. Taking 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. SN - 1520-4804 UR - https://www.unboundmedicine.com/medline/citation/21702498/Investigations_on_the_4_quinolone_3_carboxylic_acid_motif__4__Identification_of_new_potent_and_selective_ligands_for_the_cannabinoid_type_2_receptor_with_diverse_substitution_patterns_and_antihyperalgesic_effects_in_mice_ L2 - https://doi.org/10.1021/jm200476p DB - PRIME DP - Unbound Medicine ER -