Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/5768
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dc.contributor.authorPasquini, Serenaen_us
dc.contributor.authorLigresti, Aen_us
dc.contributor.authorMugnaini, Claudiaen_us
dc.contributor.authorSemeraro, Teresaen_us
dc.contributor.authorCicione, Len_us
dc.contributor.authorDE ROSA, Mariaen_us
dc.contributor.authorGuida, Fen_us
dc.contributor.authorLuongo, Len_us
dc.contributor.authorDE CHIARO, Men_us
dc.contributor.authorCASCIO M., Gen_us
dc.contributor.authorBolognini, Den_us
dc.contributor.authorMarini, Pen_us
dc.contributor.authorPertwee, Ren_us
dc.contributor.authorMaione, Sen_us
dc.contributor.authorDI MARZO, Ven_us
dc.contributor.authorCorelli, Federicoen_us
dc.date.accessioned2021-03-30T15:55:00Z-
dc.date.available2021-03-30T15:55:00Z-
dc.date.issued2010-
dc.identifier.issn0022-2623en_US
dc.identifier.urihttp://hdl.handle.net/20.500.12779/5768-
dc.description34986en_US
dc.description.abstractA set of quinolone-3-carboxamides 2 bearing diverse substituents at position 1, 3, and 6 of the bicyclicnucleus was prepared. Except for six compounds exhibiting Ki >100 nM, all the quinolone-3-carboxamides 2 proved to be high affinity CB2 ligands, with Ki values ranging from 73.2 to 0.7 nMand selectivity [SI=Ki(CB1)/Ki(CB2)] varying from >14285 to 1.9, with only 2ah exhibiting a reverseselectivity (SI<1). In the formalin test of peripheral acute and inflammatory pain in mice, 2ae showedanalgesic activity that was antagonized by a selective CB2 antagonist. By contrast, 2e was inactive per seand antagonized the effect of a selective CB2 agonist. Finally, 2g and 2p exhibited CB2 inverse agonistlikebehavior in this in vivo test. However, two different functional assays carried out in vitro on 2e and2g indicated for both compounds an overall inverse agonist activity at CB2 receptors.en_US
dc.language.isoenen_US
dc.relationNoneen_US
dc.relation.ispartofJOURNAL OF MEDICINAL CHEMISTRYen_US
dc.titleInvestigations on the 4-Quinolone-3-carboxylic Acid Motif. 3. Synthesis, Structure-Affinity Relationships, and Pharmacological Characterization of 6-Substituted 4-Quinolone-3-carboxamides as Highly Selective Cannabinoid-2 Receptor Ligandsen_US
dc.typeArticleen_US
dc.identifier.pmid20718492en_US
dc.identifier.scopus2-s2.0-77955866101en_US
dc.identifier.isiWOS:000280962700003en_US
dc.relation.volume53en_US
dc.relation.issue16en_US
dc.description.firstpage5915en_US
dc.description.lastpage5928en_US
dc.description.thirdmissionNot applicableen_US
item.cerifentitytypePublications-
item.grantfulltextnone-
item.languageiso639-1en-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.openairetypeArticle-
item.fulltextNo Fulltext-
crisitem.author.orcid0000-0003-1998-732X-
crisitem.author.orcid0000-0002-5750-4504-
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