Avaliação do potencial antinociceptivo e mecanismo de ação do 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1hpirazol- 1-il] 4-(4 bromofenil)- 5 metiltiazol (b50) em camundongos

Detalhes bibliográficos
Autor(a) principal: Souza, Alessandra Hübner de
Data de Publicação: 2005
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Manancial - Repositório Digital da UFSM
dARK ID: ark:/26339/00130000172z1
Texto Completo: http://repositorio.ufsm.br/handle/1/11110
Resumo: Pain is a common symptom in the clinical practice. Therefore, novel analgesic drugs, with more favorable pharmacological properties have been searched. Previous studies from our group showed that the systemic administration of the 2-[5-triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1H-pyrazole-1-yl]-4-(4-bromophenyl)-5-metyl-thiazole(B50) causes antinociception in the acetic acid writhing test. However, it is not know whether such an antinociceptive action involves central or peripheral mechanisms. In this study we investigated the antinociceptive effect of the intrathecal administration of the new pyrazole derivative 2-[5-triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1H-pyrazole-1-yl]-4-(4- bromophenyl)-5-metyl-thiazole (B50) in adult male mice, using the acetic acid writhing induced by acetic acid and hot-plate tests, in order to determine its putative site of action. B50 caused antinociception (200 nmol/ 5 μl, i.t.), 120 minutes after its administration, in the acetic acid writhing assay and 90 minutes after its administration in the hot plate test. Naloxone (8.25 μmol/kg, s.c.) reverted the antinociceptive action of B50 (200 nmol/ 5 μl, i.t.) in the acetic acid writhing assay, suggesting that opioid mechanisms are involved in the antinociception caused by B50. B50 had no effect on spontaneous locomotion or rotarod performance, indicating that the currently reported antinociceptive effect of B50 is not related to unspecific motor effects.
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spelling Avaliação do potencial antinociceptivo e mecanismo de ação do 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1hpirazol- 1-il] 4-(4 bromofenil)- 5 metiltiazol (b50) em camundongosAntinociceptive evaluation of 2-[5- triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1hpyrazole- 1-yl]-4-(4-bromophenyl)-5-metylthiazole( b50) and its mechanism of action in miceAnalgesiaAntinocicepçãoHeterociclosCNPQ::CIENCIAS BIOLOGICAS::BIOQUIMICAPain is a common symptom in the clinical practice. Therefore, novel analgesic drugs, with more favorable pharmacological properties have been searched. Previous studies from our group showed that the systemic administration of the 2-[5-triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1H-pyrazole-1-yl]-4-(4-bromophenyl)-5-metyl-thiazole(B50) causes antinociception in the acetic acid writhing test. However, it is not know whether such an antinociceptive action involves central or peripheral mechanisms. In this study we investigated the antinociceptive effect of the intrathecal administration of the new pyrazole derivative 2-[5-triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1H-pyrazole-1-yl]-4-(4- bromophenyl)-5-metyl-thiazole (B50) in adult male mice, using the acetic acid writhing induced by acetic acid and hot-plate tests, in order to determine its putative site of action. B50 caused antinociception (200 nmol/ 5 μl, i.t.), 120 minutes after its administration, in the acetic acid writhing assay and 90 minutes after its administration in the hot plate test. Naloxone (8.25 μmol/kg, s.c.) reverted the antinociceptive action of B50 (200 nmol/ 5 μl, i.t.) in the acetic acid writhing assay, suggesting that opioid mechanisms are involved in the antinociception caused by B50. B50 had no effect on spontaneous locomotion or rotarod performance, indicating that the currently reported antinociceptive effect of B50 is not related to unspecific motor effects.Trabalhos realizados em nosso laboratório, demonstraram que a administração sistêmica do pirazoltiazol 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1h-pirazol-1-il] 4-(4 bromofenil)- 5 metiltiazol (B50) provocou antinocicepção no teste das contorções abdominais induzidas por ácido acético 0,8%. Porém, não se sabe se a ação antinociceptiva do B50 é central ou periférica. Nesse estudo, nós investigamos o efeito antinociceptivo da administração intratecal do composto B50 em camundongos adultos machos, usando os testes de contorções abdominais induzidos por ácido acético e o teste da placa quente a ± 50 ºC. O B50 (200 nmol/5 μl, i.t.) causou antinocicepção 120 minutos depois de sua administração no teste das contorções abdominais induzidas por ácido acético e 90 minutos depois de sua administração no teste da placa quente. A Naloxona (8,25 μmol/kg, s.c.) reverteu a ação antinociceptiva do B50 (200 nmol/5 μl, i.t.) no teste das contorções abdominais induzidas por ácido acético, sugerindo que mecanismos opióides estão envolvidos na antinocicepção causada pelo B50. Este pirazol-tiazol não alterou a locomoção espontânea e nem a performance dos animais no cilindro giratório, indicando que o efeito antinociceptivo do B50 não é relacionado a efeitos motores inespecíficos.Universidade Federal de Santa MariaBRBioquímicaUFSMPrograma de Pós-Graduação em Ciências Biológicas: Bioquímica ToxicológicaRubin, Maribel Antonellohttp://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4794806H7Barreto, Katia Padilhahttp://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4727510Z9Zanatta, Nilohttp://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4783100P9Souza, Alessandra Hübner de2017-04-112017-04-112005-07-21info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfapplication/pdfSOUZA, Alessandra Hübner de. Antinociceptive evaluation of 2-[5- triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1hpyrazole- 1-yl]-4-(4-bromophenyl)-5-metylthiazole( b50) and its mechanism of action in mice. 2005. 81 f. Dissertação (Mestrado em Bioquímica) - Universidade Federal de Santa Maria, Santa Maria, 2005.http://repositorio.ufsm.br/handle/1/11110ark:/26339/00130000172z1porinfo:eu-repo/semantics/openAccessreponame:Manancial - Repositório Digital da UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSM2017-07-25T15:09:57Zoai:repositorio.ufsm.br:1/11110Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/ONGhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.comopendoar:2017-07-25T15:09:57Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)false
dc.title.none.fl_str_mv Avaliação do potencial antinociceptivo e mecanismo de ação do 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1hpirazol- 1-il] 4-(4 bromofenil)- 5 metiltiazol (b50) em camundongos
Antinociceptive evaluation of 2-[5- triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1hpyrazole- 1-yl]-4-(4-bromophenyl)-5-metylthiazole( b50) and its mechanism of action in mice
title Avaliação do potencial antinociceptivo e mecanismo de ação do 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1hpirazol- 1-il] 4-(4 bromofenil)- 5 metiltiazol (b50) em camundongos
spellingShingle Avaliação do potencial antinociceptivo e mecanismo de ação do 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1hpirazol- 1-il] 4-(4 bromofenil)- 5 metiltiazol (b50) em camundongos
Souza, Alessandra Hübner de
Analgesia
Antinocicepção
Heterociclos
CNPQ::CIENCIAS BIOLOGICAS::BIOQUIMICA
title_short Avaliação do potencial antinociceptivo e mecanismo de ação do 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1hpirazol- 1-il] 4-(4 bromofenil)- 5 metiltiazol (b50) em camundongos
title_full Avaliação do potencial antinociceptivo e mecanismo de ação do 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1hpirazol- 1-il] 4-(4 bromofenil)- 5 metiltiazol (b50) em camundongos
title_fullStr Avaliação do potencial antinociceptivo e mecanismo de ação do 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1hpirazol- 1-il] 4-(4 bromofenil)- 5 metiltiazol (b50) em camundongos
title_full_unstemmed Avaliação do potencial antinociceptivo e mecanismo de ação do 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1hpirazol- 1-il] 4-(4 bromofenil)- 5 metiltiazol (b50) em camundongos
title_sort Avaliação do potencial antinociceptivo e mecanismo de ação do 2-[5-triclorometil-5-hidroxi-3-fenil-4,5-dihidro-1hpirazol- 1-il] 4-(4 bromofenil)- 5 metiltiazol (b50) em camundongos
author Souza, Alessandra Hübner de
author_facet Souza, Alessandra Hübner de
author_role author
dc.contributor.none.fl_str_mv Rubin, Maribel Antonello
http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4794806H7
Barreto, Katia Padilha
http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4727510Z9
Zanatta, Nilo
http://buscatextual.cnpq.br/buscatextual/visualizacv.do?id=K4783100P9
dc.contributor.author.fl_str_mv Souza, Alessandra Hübner de
dc.subject.por.fl_str_mv Analgesia
Antinocicepção
Heterociclos
CNPQ::CIENCIAS BIOLOGICAS::BIOQUIMICA
topic Analgesia
Antinocicepção
Heterociclos
CNPQ::CIENCIAS BIOLOGICAS::BIOQUIMICA
description Pain is a common symptom in the clinical practice. Therefore, novel analgesic drugs, with more favorable pharmacological properties have been searched. Previous studies from our group showed that the systemic administration of the 2-[5-triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1H-pyrazole-1-yl]-4-(4-bromophenyl)-5-metyl-thiazole(B50) causes antinociception in the acetic acid writhing test. However, it is not know whether such an antinociceptive action involves central or peripheral mechanisms. In this study we investigated the antinociceptive effect of the intrathecal administration of the new pyrazole derivative 2-[5-triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1H-pyrazole-1-yl]-4-(4- bromophenyl)-5-metyl-thiazole (B50) in adult male mice, using the acetic acid writhing induced by acetic acid and hot-plate tests, in order to determine its putative site of action. B50 caused antinociception (200 nmol/ 5 μl, i.t.), 120 minutes after its administration, in the acetic acid writhing assay and 90 minutes after its administration in the hot plate test. Naloxone (8.25 μmol/kg, s.c.) reverted the antinociceptive action of B50 (200 nmol/ 5 μl, i.t.) in the acetic acid writhing assay, suggesting that opioid mechanisms are involved in the antinociception caused by B50. B50 had no effect on spontaneous locomotion or rotarod performance, indicating that the currently reported antinociceptive effect of B50 is not related to unspecific motor effects.
publishDate 2005
dc.date.none.fl_str_mv 2005-07-21
2017-04-11
2017-04-11
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/masterThesis
format masterThesis
status_str publishedVersion
dc.identifier.uri.fl_str_mv SOUZA, Alessandra Hübner de. Antinociceptive evaluation of 2-[5- triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1hpyrazole- 1-yl]-4-(4-bromophenyl)-5-metylthiazole( b50) and its mechanism of action in mice. 2005. 81 f. Dissertação (Mestrado em Bioquímica) - Universidade Federal de Santa Maria, Santa Maria, 2005.
http://repositorio.ufsm.br/handle/1/11110
dc.identifier.dark.fl_str_mv ark:/26339/00130000172z1
identifier_str_mv SOUZA, Alessandra Hübner de. Antinociceptive evaluation of 2-[5- triclorometyl-5-hidroxy-3-phenyl-4,5-dihydro-1hpyrazole- 1-yl]-4-(4-bromophenyl)-5-metylthiazole( b50) and its mechanism of action in mice. 2005. 81 f. Dissertação (Mestrado em Bioquímica) - Universidade Federal de Santa Maria, Santa Maria, 2005.
ark:/26339/00130000172z1
url http://repositorio.ufsm.br/handle/1/11110
dc.language.iso.fl_str_mv por
language por
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Universidade Federal de Santa Maria
BR
Bioquímica
UFSM
Programa de Pós-Graduação em Ciências Biológicas: Bioquímica Toxicológica
publisher.none.fl_str_mv Universidade Federal de Santa Maria
BR
Bioquímica
UFSM
Programa de Pós-Graduação em Ciências Biológicas: Bioquímica Toxicológica
dc.source.none.fl_str_mv reponame:Manancial - Repositório Digital da UFSM
instname:Universidade Federal de Santa Maria (UFSM)
instacron:UFSM
instname_str Universidade Federal de Santa Maria (UFSM)
instacron_str UFSM
institution UFSM
reponame_str Manancial - Repositório Digital da UFSM
collection Manancial - Repositório Digital da UFSM
repository.name.fl_str_mv Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)
repository.mail.fl_str_mv atendimento.sib@ufsm.br||tedebc@gmail.com
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