Side-effects of analgesic kyotorphin derivatives: advantages over clinical opioid drugs
dc.contributor.author
dc.date.accessioned
2015-03-23T11:55:07Z
dc.date.available
2015-03-23T11:55:07Z
dc.date.issued
2013-07-01
dc.identifier.issn
0939-4451
dc.identifier.uri
dc.description.abstract
The 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-NH 2 as advantageous alternatives over current opioids
dc.format.mimetype
application/pdf
dc.language.iso
eng
dc.publisher
Springer Verlag
dc.relation.isformatof
Reproducció digital del document publicat a: http://dx.doi.org/10.1007/s00726-013-1484-2
dc.relation.ispartof
© Amino Acids, 2013, vol. 45, p. 171-178
dc.relation.ispartofseries
Articles publicats (D-Q)
dc.rights
Tots els drets reservats
dc.subject
dc.title
Side-effects of analgesic kyotorphin derivatives: advantages over clinical opioid drugs
dc.type
info:eu-repo/semantics/article
dc.rights.accessRights
info:eu-repo/semantics/embargoedAccess
dc.embargo.terms
Cap
dc.date.embargoEndDate
info:eu-repo/date/embargoEnd/2026-01-01
dc.relation.projectID
info:eu-repo/grantAgreement/EC/FP7/230654/EU/Selected peptides as drug candidates directed to pain and neurodegeneration/PEP2BRAIN
dc.type.version
info:eu-repo/semantics/publishedVersion
dc.identifier.doi
dc.relation.FundingProgramme
dc.relation.ProjectAcronym
dc.identifier.eissn
1438-2199