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dc.contributor.authordos Santos, Jean Leandro-
dc.contributor.authorMoreira, Vanessa-
dc.contributor.authorCampos, Michel Leandro-
dc.contributor.authorChelucci, Rafael Consolin-
dc.contributor.authorBarbieri, Karina Pereira-
dc.contributor.authorMaggio de Castro Souto, Pollyana Cristina-
dc.contributor.authorMatsubara, Marcio Hideki-
dc.contributor.authorTeixeira, Catarina-
dc.contributor.authorBosquesi, Priscila Longhin-
dc.contributor.authorPeccinini, Rosangela Goncalves-
dc.contributor.authorChin, Chung Man-
dc.date.accessioned2014-05-20T13:25:02Z-
dc.date.available2014-05-20T13:25:02Z-
dc.date.issued2012-11-01-
dc.identifierhttp://dx.doi.org/10.3390/ijms131115305-
dc.identifier.citationInternational Journal of Molecular Sciences. Basel: Mdpi Ag, v. 13, n. 11, p. 15305-15320, 2012.-
dc.identifier.issn1422-0067-
dc.identifier.urihttp://hdl.handle.net/11449/7922-
dc.description.abstractLong-term nonsteroidal anti-inflammatory drugs (NSAIDs) therapy has been associated with several adverse effects such as gastric ulceration and cardiovascular events. Among the molecular modifications strategies, the prodrug approach is a useful tool to discover new safe NSAIDs. The 1-(2,6-dichlorophenyl)indolin-2-one is a diclofenac prodrug which demonstrated relevant anti-inflammatory properties without gastro ulceration effect. In addition, the prodrug decreases PGE(2) levels, COX-2 expression and cellular influx into peritoneal cavity induced by carrageenan treatment. Preliminary pharmacokinetic studies have shown in vivo bioconversion of prodrug to diclofenac. This prodrug is a new nonulcerogenic NSAID useful to treat inflammatory events by long-term therapy.en
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
dc.description.sponsorshipPADC-UNESP-
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)-
dc.description.sponsorshipInstituto Nacional de Ciência e Tecnologia-Inovacao Farmaceutica (INCT-if)-
dc.format.extent15305-15320-
dc.language.isoeng-
dc.publisherMdpi Ag-
dc.sourceWeb of Science-
dc.subjectNSAIDsen
dc.subjectanti-inflammatoryen
dc.subjectdiclofenacen
dc.subjectprodrugsen
dc.subjectmolecular modificationen
dc.subjectlactamen
dc.subjectCOX-inhibitoren
dc.subjectbioconversionen
dc.subjectchronic inflammationen
dc.titlePharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effecten
dc.typeoutro-
dc.contributor.institutionUniversidade Estadual Paulista (UNESP)-
dc.contributor.institutionInstituto Butantan-
dc.description.affiliationSch Pharmaceut Sci UNESP, Drugs & Med Dept, Lapdesf Lab Res & Drug Dev, BR-14801902 Araraquara, SP, Brazil-
dc.description.affiliationInstituto Butantan, Inflammat Unit, Pharmacol Lab, BR-05503900 São Paulo, Brazil-
dc.description.affiliationSch Pharmaceut Sci UNESP, Nat Act Principles & Toxicol Dept, BR-14801902 Araraquara, SP, Brazil-
dc.description.affiliationUnespSch Pharmaceut Sci UNESP, Drugs & Med Dept, Lapdesf Lab Res & Drug Dev, BR-14801902 Araraquara, SP, Brazil-
dc.description.affiliationUnespSch Pharmaceut Sci UNESP, Nat Act Principles & Toxicol Dept, BR-14801902 Araraquara, SP, Brazil-
dc.description.sponsorshipIdFAPESP: 09/12664-5-
dc.description.sponsorshipIdFAPESP: 10/12495-6-
dc.description.sponsorshipIdPADC-UNESP: 107/10-
dc.identifier.doi10.3390/ijms131115305-
dc.identifier.wosWOS:000311425000095-
dc.rights.accessRightsAcesso aberto-
dc.identifier.fileWOS000311425000095.pdf-
dc.relation.ispartofInternational Journal of Molecular Sciences-
Appears in Collections:Artigos, TCCs, Teses e Dissertações da Unesp

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