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Type: Artigo de periódico
Title: Effect Of A Nanostructured Dendrimer-naloxonazine Complex On Endogenous Opioid Peptides μ 1 Receptor-mediated Post-ictal Antinociception
Author: Felippotti T.T.
Ribeiro do Carmo D.
Paim L.L.
Stradiotto N.R.
Bicalho U.D.O.
Parada C.A.
Grillo R.
Fraceto L.F.
Coimbra N.C.
Abstract: The aim of this study was to investigate the capacity of the host dendrimer DAB-Am-16 as a drug carrier to reduce the time required for the encapsulated naloxonaxine to establish an irreversible covalent bond with μ 1-opioid receptor (resulting in a pharmacologically selective effect). The efficacy of dendrimer-naloxonazine nanocomplex (DNC) was studied in antinociception induced by convulsions elicited by intraperitoneal (IP) administration of pentylenetetrazole, and analgesia was measured by the tail-flick test. We found that animals showed increased tail-flick latencies following convulsions. Furthermore, acute pre-treatment (10 minutes) with DNC, but not with naloxonazine alone, antagonized post-ictal analgesia in comparison with control pre-treatment. However, naloxonazine treatment 24 hours before PTZ decreased post-ictal antinociception, but DNC failed to antagonize tonic-clonic seizure-induced analgesia. In addition, according to Racine's index of seizure severity, naloxonazine, DAB-Am-16 dendrimer or DNC did not influence seizure severity when administered either 10 minutes or 24 hours before PTZ. From the Clinical Editor: This study characterizes the effect of a dendrimer-naloxonazine complex on μ1 receptor-mediated post-ictal antinociception in an animal model of seizure disorder. © 2011 Elsevier Inc.
Rights: fechado
Identifier DOI: 10.1016/j.nano.2011.02.005
Date Issue: 2011
Appears in Collections:Unicamp - Artigos e Outros Documentos

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