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

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-dichlorop...

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Autores principales: dos Santos, Jean Leandro, Moreira, Vanessa, Campos, Michel Leandro, Chelucci, Rafael Consolin, Barbieri, Karina Pereira, de Castro Souto, Pollyana Cristina Maggio, Matsubara, Márcio Hideki, Teixeira, Catarina, Bosquesi, Priscila Longhin, Peccinini, Rosângela Gonçalves, Chin, Chung Man
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International (MDPI) 2012
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Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3509643/
https://www.ncbi.nlm.nih.gov/pubmed/23203127
http://dx.doi.org/10.3390/ijms131115305
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author dos Santos, Jean Leandro
Moreira, Vanessa
Campos, Michel Leandro
Chelucci, Rafael Consolin
Barbieri, Karina Pereira
de Castro Souto, Pollyana Cristina Maggio
Matsubara, Márcio Hideki
Teixeira, Catarina
Bosquesi, Priscila Longhin
Peccinini, Rosângela Gonçalves
Chin, Chung Man
author_facet dos Santos, Jean Leandro
Moreira, Vanessa
Campos, Michel Leandro
Chelucci, Rafael Consolin
Barbieri, Karina Pereira
de Castro Souto, Pollyana Cristina Maggio
Matsubara, Márcio Hideki
Teixeira, Catarina
Bosquesi, Priscila Longhin
Peccinini, Rosângela Gonçalves
Chin, Chung Man
author_sort dos Santos, Jean Leandro
collection PubMed
description 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.
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spelling pubmed-35096432013-01-09 Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect dos Santos, Jean Leandro Moreira, Vanessa Campos, Michel Leandro Chelucci, Rafael Consolin Barbieri, Karina Pereira de Castro Souto, Pollyana Cristina Maggio Matsubara, Márcio Hideki Teixeira, Catarina Bosquesi, Priscila Longhin Peccinini, Rosângela Gonçalves Chin, Chung Man Int J Mol Sci Article 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. Molecular Diversity Preservation International (MDPI) 2012-11-19 /pmc/articles/PMC3509643/ /pubmed/23203127 http://dx.doi.org/10.3390/ijms131115305 Text en © 2012 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0 This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0).
spellingShingle Article
dos Santos, Jean Leandro
Moreira, Vanessa
Campos, Michel Leandro
Chelucci, Rafael Consolin
Barbieri, Karina Pereira
de Castro Souto, Pollyana Cristina Maggio
Matsubara, Márcio Hideki
Teixeira, Catarina
Bosquesi, Priscila Longhin
Peccinini, Rosângela Gonçalves
Chin, Chung Man
Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
title Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
title_full Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
title_fullStr Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
title_full_unstemmed Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
title_short Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
title_sort pharmacological evaluation and preliminary pharmacokinetics studies of a new diclofenac prodrug without gastric ulceration effect
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3509643/
https://www.ncbi.nlm.nih.gov/pubmed/23203127
http://dx.doi.org/10.3390/ijms131115305
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