Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect

dc.contributorUniversidade Estadual Paulista (UNESP)
dc.creatordos Santos, Jean Leandro
dc.creatorMoreira, Vanessa
dc.creatorCampos, Michel Leandro
dc.creatorChelucci, Rafael Consolin
dc.creatorBarbieri, Karina Pereira
dc.creatorMaggio de Castro Souto, Pollyana Cristina
dc.creatorMatsubara, Marcio Hideki
dc.creatorTeixeira, Catarina
dc.creatorBosquesi, Priscila Longhin
dc.creatorPeccinini, Rosangela Goncalves
dc.creatorChin, Chung Man
dc.date2014-05-20T13:25:02Z
dc.date2014-05-20T13:25:02Z
dc.date2012-11-01
dc.date.accessioned2017-04-05T20:02:11Z
dc.date.available2017-04-05T20:02:11Z
dc.identifierInternational Journal of Molecular Sciences. Basel: Mdpi Ag, v. 13, n. 11, p. 15305-15320, 2012.
dc.identifier1422-0067
dc.identifierhttp://hdl.handle.net/11449/7922
dc.identifier10.3390/ijms131115305
dc.identifierWOS:000311425000095
dc.identifierWOS000311425000095.pdf
dc.identifierhttp://dx.doi.org/10.3390/ijms131115305
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/856442
dc.descriptionLong-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.
dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.languageeng
dc.publisherMdpi Ag
dc.relationInternational Journal of Molecular Sciences
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectNSAIDs
dc.subjectanti-inflammatory
dc.subjectdiclofenac
dc.subjectprodrugs
dc.subjectmolecular modification
dc.subjectlactam
dc.subjectCOX-inhibitor
dc.subjectbioconversion
dc.subjectchronic inflammation
dc.titlePharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
dc.typeOtro


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