Otro
Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
Registro en:
International Journal of Molecular Sciences. Basel: Mdpi Ag, v. 13, n. 11, p. 15305-15320, 2012.
1422-0067
10.3390/ijms131115305
WOS:000311425000095
WOS000311425000095.pdf
Autor
dos Santos, Jean Leandro
Moreira, Vanessa
Campos, Michel Leandro
Chelucci, Rafael Consolin
Barbieri, Karina Pereira
Maggio de Castro Souto, Pollyana Cristina
Matsubara, Marcio Hideki
Teixeira, Catarina
Bosquesi, Priscila Longhin
Peccinini, Rosangela Goncalves
Chin, Chung Man
Resumen
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. Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)