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

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dc.contributor.authordos Santos, Jean Leandro [UNESP]
dc.contributor.authorMoreira, Vanessa
dc.contributor.authorCampos, Michel Leandro [UNESP]
dc.contributor.authorChelucci, Rafael Consolin [UNESP]
dc.contributor.authorBarbieri, Karina Pereira [UNESP]
dc.contributor.authorMaggio de Castro Souto, Pollyana Cristina
dc.contributor.authorMatsubara, Marcio Hideki
dc.contributor.authorTeixeira, Catarina
dc.contributor.authorBosquesi, Priscila Longhin [UNESP]
dc.contributor.authorPeccinini, Rosangela Goncalves [UNESP]
dc.contributor.authorChin, Chung Man [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionInstituto Butantan
dc.date.accessioned2014-05-20T13:25:02Z
dc.date.available2014-05-20T13:25:02Z
dc.date.issued2012-11-01
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.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.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.description.sponsorshipIdFAPESP: 09/12664-5
dc.description.sponsorshipIdFAPESP: 10/12495-6
dc.description.sponsorshipIdPADC-UNESP: 107/10
dc.format.extent15305-15320
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.doi10.3390/ijms131115305
dc.identifier.fileWOS000311425000095.pdf
dc.identifier.issn1422-0067
dc.identifier.lattes1066743423929093
dc.identifier.lattes9734333607975413
dc.identifier.orcid0000-0003-4141-0455
dc.identifier.urihttp://hdl.handle.net/11449/7922
dc.identifier.wosWOS:000311425000095
dc.language.isoeng
dc.publisherMdpi Ag
dc.relation.ispartofInternational Journal of Molecular Sciences
dc.relation.ispartofjcr3.687
dc.relation.ispartofsjr1,260
dc.rights.accessRightsAcesso abertopt
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.typeArtigopt
dcterms.licensehttp://www.mdpi.com/about/openaccess
dcterms.rightsHolderMdpi Ag
dspace.entity.typePublication
relation.isDepartmentOfPublicatione214da1b-9929-4ae9-b8fd-655e9bfeda4b
relation.isDepartmentOfPublication.latestForDiscoverye214da1b-9929-4ae9-b8fd-655e9bfeda4b
relation.isOrgUnitOfPublication95697b0b-8977-4af6-88d5-c29c80b5ee92
relation.isOrgUnitOfPublication.latestForDiscovery95697b0b-8977-4af6-88d5-c29c80b5ee92
unesp.author.lattes1066743423929093
unesp.author.lattes9734333607975413[11]
unesp.author.orcid0000-0001-5887-7663[8]
unesp.author.orcid0000-0003-4141-0455[11]
unesp.author.orcid0000-0002-2460-2829[1]
unesp.author.orcid0000-0002-7147-7637[3]
unesp.author.orcid0000-0001-5579-3069[2]
unesp.author.orcid0000-0002-2692-8101[10]
unesp.campusUniversidade Estadual Paulista (UNESP), Faculdade de Ciências Farmacêuticas, Araraquarapt
unesp.departmentFármacos e Medicamentos - FCFpt
unesp.departmentPrincípios Ativos Naturais e Toxicologia - FCFpt

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Araraquara - FCF - Faculdade de Ciências Farmacêuticas