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Anti-hyperalgesic effects of two sphingosine derivatives in different acute and chronic models of hyperalgesia in mice.
Cavichioli, Felipe J; Bernal, Graylin N B; Holzmann, Iandra; Klein, Juliana Bagatini; Escarcena, Ricardo; Del Olmo, Esther; San Feliciano, Arturo; Cechinel Filho, Valdir; Quintão, Nara L M.
Afiliação
  • Cavichioli FJ; Biomedicine Course, Universidade do Vale do Itajaí, Santa Catarina, Brazil.
  • Bernal GNB; Biomedicine Course, Universidade do Vale do Itajaí, Santa Catarina, Brazil.
  • Holzmann I; Postgraduate Program in Pharmaceutical Science, Universidade do Vale do Itajaí, Santa Catarina, Brazil.
  • Klein JB; Postgraduate Program in Pharmaceutical Science, Universidade do Vale do Itajaí, Santa Catarina, Brazil.
  • Escarcena R; Departament of Pharmaceutical Chemistry, Faculty of Pharmacy-CIETUS, University of Salamanca, Salamanca, Spain.
  • Del Olmo E; Departament of Pharmaceutical Chemistry, Faculty of Pharmacy-CIETUS, University of Salamanca, Salamanca, Spain.
  • San Feliciano A; Departament of Pharmaceutical Chemistry, Faculty of Pharmacy-CIETUS, University of Salamanca, Salamanca, Spain.
  • Cechinel Filho V; Postgraduate Program in Pharmaceutical Science, Universidade do Vale do Itajaí, Santa Catarina, Brazil; Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí, Santa Catarina, Brazil.
  • Quintão NLM; Biomedicine Course, Universidade do Vale do Itajaí, Santa Catarina, Brazil; Postgraduate Program in Pharmaceutical Science, Universidade do Vale do Itajaí, Santa Catarina, Brazil. Electronic address: nara.quintao@univali.br.
Pharmacol Rep ; 70(4): 753-759, 2018 Aug.
Article em En | MEDLINE | ID: mdl-29936362
BACKGROUND: The study evaluated the effects of two sphingosine derivatives N-(2-tert-butoxycarbamylhexadecyl)glutaramide (AA) and N-(1-benzyloxyhexadec-2-yl)glutaramide (OA) in different models of hypersensitivity in mice. METHODS: Male Swiss mice were orally pre-treated with AA or OA (0.3-3mg/kg). After 1h, they received λ-carrageenan (300µg/paw), lipopolysaccharide (LPS; 100ng/paw), bradykinin (BK; 500ng/paw) or prostaglandin E2 (PGE2; 0.1nmol/paw) or epinephrine (100ng/paw), and the mechanical withdrawal thresholds were evaluated using von Frey filament (0.6g) at different time points. The effect of the compounds against inflammatory and neuropathic pain was also evaluated using complete Freund's adjuvant (CFA), or by performing partial sciatic nerve ligation (PSNL). RESULTS: Animals pre-treated with AA and OA reduced hypersensitivity induced by carrageenan, LPS and BK, and modest inhibition of PGE2-induced hypersensitivity and carrageenan-induced paw oedema were observed in mice treated with OA. Though the partial effect presented by AA and OA, when dosed once a day, both compounds were able to significantly reduce the persistent inflammatory and neuropathic pain induced by CFA and PSNL, respectively. CONCLUSION: These results demonstrate that the sphingosine derivatives AA and OA present important anti-hypersensitive effects, suggesting a possible interaction with the kinin signalling pathway. This may represent an interesting tool for the management of acute and chronic pain, with good bioavailability and safety.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Medição da Dor / Hiperalgesia / Neuralgia Limite: Animals Idioma: En Revista: Pharmacol Rep Assunto da revista: FARMACOLOGIA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Brasil País de publicação: Suíça

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Medição da Dor / Hiperalgesia / Neuralgia Limite: Animals Idioma: En Revista: Pharmacol Rep Assunto da revista: FARMACOLOGIA Ano de publicação: 2018 Tipo de documento: Article País de afiliação: Brasil País de publicação: Suíça