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.

Pasquini, S., De Rosa, M., Pedani, V., Mugnaini, C., Guida, F., Luongo, L., et al. (2011). 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. JOURNAL OF MEDICINAL CHEMISTRY, 54(15), 5444-5453 [10.1021/jm200476p].

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

Pasquini, Serena;De Rosa, Maria;Pedani, Valentina;Mugnaini, Claudia;Dragoni, Stefania;Frosini, Maria;Corelli, Federico
2011-01-01

Abstract

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.
2011
Pasquini, S., De Rosa, M., Pedani, V., Mugnaini, C., Guida, F., Luongo, L., et al. (2011). 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. JOURNAL OF MEDICINAL CHEMISTRY, 54(15), 5444-5453 [10.1021/jm200476p].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/4091
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