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dc.contributor.author
Higgs, Josefina
dc.contributor.author
Wasowski, Cristina Lucia N.
dc.contributor.author
Loscalzo, Leonardo Martin
dc.contributor.author
Marder, Nora Mariel
dc.date.available
2016-02-29T18:57:22Z
dc.date.issued
2013-05
dc.identifier.citation
Higgs, Josefina; Wasowski, Cristina Lucia N.; Loscalzo, Leonardo Martin; Marder, Nora Mariel; In vitro binding affinities of a series of flavonoids for mu-opioid receptors. Antinociceptive effect of the synthetic flavonoid 3,3-dibromoflavanone in mice; Elsevier; Neuropharmacology; 72; 5-2013; 9-19
dc.identifier.issn
0028-3908
dc.identifier.uri
http://hdl.handle.net/11336/4526
dc.description.abstract
The pharmacotherapy for the treatment of pain is an active area of investigation. There are effective drugs to treat this problem, but there is also a need to find alternative treatments free of undesirable side effects. In the present work the capacity of a series of flavonoids to bind to the m opioid receptor was evaluated. The most active compound, 3,3-dibromoflavanone (31), a synthetic flavonoid, presented a significant inhibition of the binding of the selective m opioid ligand [3 H]DAMGO, with a Ki of 0.846 0.263 mM. Flavanone 31 was further synthesized using a simple and cheap procedure with good yield. Its in vivo effects in mice, after acute treatments, were studied using antinociceptive and behavioral assays. It showed no sedative, anxiolytic, motor incoordination effects or inhibition of the gastrointestinal transit in mice at the doses tested. It evidenced antinociceptive activity on the acetic acid-induced nociception, hot plate and formalin tests (at 10 mg/kg and 30 mg/kg). The results showed that the 5-HT2 receptor and the adrenoceptors seem unlikely to be involved in its antinociceptive effects. Naltrexone, a nonselective opioid receptors antagonist, totally blocked compound 31 antinociceptive effects on the hot plate test, but naltrindole (d opioid antagonist) and nor-binaltorphimine (k opioid antagonist) did not. These findings demonstrated that 3,3-dibromoflavanone (31), at doses that did not interfere with the motor performance, exerted clear dose dependent antinociception when assessed in the chemical and thermal models of nociception in mice and it seems that its action is related to the activation of the m opioid receptor.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Elsevier
dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
3,3-Dibromoflavanone
dc.subject
Natural And Synthetic flavonoids
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Opioid Receptors
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Acute Treatment
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Antinociceptive Effects
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Farmacología y Farmacia
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Medicina Básica
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CIENCIAS MÉDICAS Y DE LA SALUD
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Neurología Clínica
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Medicina Clínica
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CIENCIAS MÉDICAS Y DE LA SALUD
dc.title
In vitro binding affinities of a series of flavonoids for mu-opioid receptors. Antinociceptive effect of the synthetic flavonoid 3,3-dibromoflavanone in mice
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2016-03-30 10:35:44.97925-03
dc.journal.volume
72
dc.journal.pagination
9-19
dc.journal.pais
Estados Unidos
dc.journal.ciudad
Amsterdam
dc.description.fil
Fil: Higgs, Josefina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Fisicoquímica Biológicas; Argentina
dc.description.fil
Fil: Wasowski, Cristina Lucia N.. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Fisicoquímica Biológicas; Argentina
dc.description.fil
Fil: Loscalzo, Leonardo Martin. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Fisicoquímica Biológicas; Argentina
dc.description.fil
Fil: Marder, Nora Mariel. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Fisicoquímica Biológicas; Argentina
dc.journal.title
Neuropharmacology
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0028390813001664
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info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.neuropharm.2013.04.020
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info:eu-repo/semantics/altIdentifier/issn/0028-3908