Side-effects of analgesic kyotorphin derivatives : advantages over clinical opioid drugs

Detalhes bibliográficos
Autor(a) principal: Ribeiro, Marta M. B.
Data de Publicação: 2013
Outros Autores: Santos, Sónia Sá, Sousa, David S. C., Oliveira, Margarida, Santos, Sara M., Heras, Montserrat, Bardaji, Eduard, Tavares, Isaura, Castanho, Miguel A. R. B.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10451/10689
Resumo: © Springer-Verlag 2013
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spelling Side-effects of analgesic kyotorphin derivatives : advantages over clinical opioid drugsKyotorphinAnalgesic peptidesOpioidsSide-effectsMorphineConstipation© Springer-Verlag 2013The adverse side-effects associated with opioid administration restrain their use as analgesic drugs and call for new solutions to treat pain. Two kyotorphin derivatives, kyotorphin-amide (KTP–NH2) and ibuprofen–KTP–NH2 (IbKTP–NH2) are promising alternatives to opioids: they trigger analgesia via an indirect opioid mechanism and are highly effective in several pain models following systemic delivery. In vivo side-effects of KTP–NH2 and IbKTP–NH2 are, however, unknown and were evaluated in the present study using male adult Wistar rats. For comparison purposes, morphine and tramadol, two clinically relevant opioids, were also studied. Results showed that KTP-derivatives do not cause constipation after systemic administration, in contrast to morphine. Also, no alterations were observed in blood pressure or in food and water intake, which were only affected by tramadol. A reduction in micturition was detected after KTP–NH2 or tramadol administrations. A moderate locomotion decline was detected after IbKTP–NH2-treatment. The side-effect profile of KTP–NH2 and IbKTP–NH2 support the existence of opioid-based mechanisms in their analgesic actions. The conjugation of a strong analgesic activity with the absence of the major side-effects associated to opioids highlights the potential of both KTP–NH2 and IbKTP–NH2 as advantageous alternatives over current opioids.Fundação para a Ciência e Tecnologia (Portugal) is acknowledged for funding: SFRH/BD/42158/2007 fellowship to M. Ribeiro and SFRH/BI/51213/2010 fellowship (for doctorate) to S. Sá Santos associated to Marie Curie IAPP. Marie Curie Industry-Academia Partnerships and Pathways (European Commission) is also acknowledged for funding (FP7-PEOPLE-2007-3-1-IAPP. Project 230654). The authors acknowledge and appreciate the financial support received from Faculdade de Medicina da Universidade de Lisboa and Fundação Amadeu Dias, Portugal (Project No. 2010029)SpringerRepositório da Universidade de LisboaRibeiro, Marta M. B.Santos, Sónia SáSousa, David S. C.Oliveira, MargaridaSantos, Sara M.Heras, MontserratBardaji, EduardTavares, IsauraCastanho, Miguel A. R. B.2014-03-05T16:55:58Z20132013-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10451/10689engAmino Acids (2013) 45:171–1780939-4451http://dx.doi.org/10.1007/s00726-013-1484-2metadata only accessinfo:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-11-08T15:56:21Zoai:repositorio.ul.pt:10451/10689Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T21:34:37.729457Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Side-effects of analgesic kyotorphin derivatives : advantages over clinical opioid drugs
title Side-effects of analgesic kyotorphin derivatives : advantages over clinical opioid drugs
spellingShingle Side-effects of analgesic kyotorphin derivatives : advantages over clinical opioid drugs
Ribeiro, Marta M. B.
Kyotorphin
Analgesic peptides
Opioids
Side-effects
Morphine
Constipation
title_short Side-effects of analgesic kyotorphin derivatives : advantages over clinical opioid drugs
title_full Side-effects of analgesic kyotorphin derivatives : advantages over clinical opioid drugs
title_fullStr Side-effects of analgesic kyotorphin derivatives : advantages over clinical opioid drugs
title_full_unstemmed Side-effects of analgesic kyotorphin derivatives : advantages over clinical opioid drugs
title_sort Side-effects of analgesic kyotorphin derivatives : advantages over clinical opioid drugs
author Ribeiro, Marta M. B.
author_facet Ribeiro, Marta M. B.
Santos, Sónia Sá
Sousa, David S. C.
Oliveira, Margarida
Santos, Sara M.
Heras, Montserrat
Bardaji, Eduard
Tavares, Isaura
Castanho, Miguel A. R. B.
author_role author
author2 Santos, Sónia Sá
Sousa, David S. C.
Oliveira, Margarida
Santos, Sara M.
Heras, Montserrat
Bardaji, Eduard
Tavares, Isaura
Castanho, Miguel A. R. B.
author2_role author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Repositório da Universidade de Lisboa
dc.contributor.author.fl_str_mv Ribeiro, Marta M. B.
Santos, Sónia Sá
Sousa, David S. C.
Oliveira, Margarida
Santos, Sara M.
Heras, Montserrat
Bardaji, Eduard
Tavares, Isaura
Castanho, Miguel A. R. B.
dc.subject.por.fl_str_mv Kyotorphin
Analgesic peptides
Opioids
Side-effects
Morphine
Constipation
topic Kyotorphin
Analgesic peptides
Opioids
Side-effects
Morphine
Constipation
description © Springer-Verlag 2013
publishDate 2013
dc.date.none.fl_str_mv 2013
2013-01-01T00:00:00Z
2014-03-05T16:55:58Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10451/10689
url http://hdl.handle.net/10451/10689
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Amino Acids (2013) 45:171–178
0939-4451
http://dx.doi.org/10.1007/s00726-013-1484-2
dc.rights.driver.fl_str_mv metadata only access
info:eu-repo/semantics/openAccess
rights_invalid_str_mv metadata only access
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Springer
publisher.none.fl_str_mv Springer
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
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repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv
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