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http://acervodigital.unesp.br/handle/11449/7922- Title:
- Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
- Universidade Estadual Paulista (UNESP)
- Instituto Butantan
- 1422-0067
- Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
- PADC-UNESP
- Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
- Instituto Nacional de Ciência e Tecnologia-Inovacao Farmaceutica (INCT-if)
- FAPESP: 09/12664-5
- FAPESP: 10/12495-6
- PADC-UNESP: 107/10
- Long-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.
- 1-Nov-2012
- International Journal of Molecular Sciences. Basel: Mdpi Ag, v. 13, n. 11, p. 15305-15320, 2012.
- 15305-15320
- Mdpi Ag
- NSAIDs
- anti-inflammatory
- diclofenac
- prodrugs
- molecular modification
- lactam
- COX-inhibitor
- bioconversion
- chronic inflammation
- http://dx.doi.org/10.3390/ijms131115305
- http://hdl.handle.net/11449/7922
- Acesso aberto
- outro
- http://repositorio.unesp.br/handle/11449/7922
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