A study of the Antinociceptive, Anti-Inflammatory, and Toxicological Activity of a Promising Thiophene Derivative

Clelia A. X. Mota, Antonia R. S. Penha,Alisson M. Oliveira, Diogo V. Fonseca, Ana K. H. L. Maia, Aldeide O. B. Rocha,Ricardo O. Moura,Francisco J. B. Mendonca Junior,Liana C. M. Pordeus,Reinaldo N. Almeida,Margareth F. F. M. Diniz

LATIN AMERICAN JOURNAL OF PHARMACY(2018)

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摘要
This study aims to investigate the effects of the thiophene derivative 2-[(4-nitro-3-benzylidene)-amino]-4,5,6,7-tetrahydro-4H-benzo[b] thiophene-3-carbonitrile (6CN10) in experimental models of nociception and inflammation. Acute treatment with 6CN10 (25, 50, and 100 mg/kg, i.p.) showed antinociceptive activity by a mechanism of action that is most likely to be independent of opioid receptors. Evaluation of anti-inflammatory activity showed an inhibition of neutrophil migration into the intraperitoneal cavity of animals treated with the test substance. In the acute toxicological study of 6CN10 (1000 mg/kg, i.p.), a reduction in food intake and body weight of the treated females were observed. The analyzed hema-tological parameters were unaffected, but treatment with 6CN10 increased the levels of alanine transaminase and aspartate aminotransferase, corroborating the histopathological findings that showed evidence of hepatotoxicity. The results presented in this study show 6CN10 to have promising analgesic activity; however, the safety of the compound should be better investigated.
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关键词
antinociception,anti-inflammatory,thiophene derivative,toxicity
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