Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
| Contribuinte(s) |
Universidade Estadual Paulista (UNESP) |
|---|---|
| Data(s) |
20/05/2014
20/05/2014
01/11/2012
|
| Resumo |
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Processo FAPESP: 09/12664-5 Processo FAPESP: 10/12495-6 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. |
| Formato |
15305-15320 |
| Identificador |
http://dx.doi.org/10.3390/ijms131115305 International Journal of Molecular Sciences. Basel: Mdpi Ag, v. 13, n. 11, p. 15305-15320, 2012. 1422-0067 http://hdl.handle.net/11449/7922 10.3390/ijms131115305 WOS:000311425000095 WOS000311425000095.pdf |
| Idioma(s) |
eng |
| Publicador |
Mdpi Ag |
| Relação |
International Journal of Molecular Sciences |
| Direitos |
openAccess |
| Palavras-Chave | #NSAIDs #anti-inflammatory #diclofenac #prodrugs #molecular modification #lactam #COX-inhibitor #bioconversion #chronic inflammation |
| Tipo |
info:eu-repo/semantics/article |
