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Effect of a nanostructured dendrimer-naloxonazine complex on endogenous opioid peptides mu(1) receptor-mediated post-ictal antinociception
  • Universidade de São Paulo (USP)
  • Universidade Estadual Paulista (UNESP)
  • Universidade Estadual de Campinas (UNICAMP)
  • Inst Neurosci & Behav INeC
  • Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
  • Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
  • Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
  • Technician scholarships: Bolsas de Apoio Tecnico
  • Ciencias da Vida
Sponsorship Process Number: 
  • FAPESP: 03/12882-6
  • FAPESP: 07/01174-1
  • FAPESP: 09/00668-6
  • FAPESP: 03/09129-4
  • FAPESP: 02/01497-1
  • CNPq: 23038.027801/2009-37
  • CNPq: 474425/2008-8
  • CNPq: 301905/2010-0
  • Ciencias da Vida: 501858/2005-9
  • Ciencias da Vida: 500896/2008-9
  • Ciencias da Vida: 505461/2010-2
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 mu(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 mu(1) receptor-mediated post-ictal antinociception in an animal model of seizure disorder. (C) 2011 Elsevier B.V. All rights reserved.
Issue Date: 
Nanomedicine-nanotechnology Biology and Medicine. Amsterdam: Elsevier B.V., v. 7, n. 6, p. 871-880, 2011.
Time Duration: 
Elsevier B.V.
  • DAB-Am-16 Dendrimer
  • GABA-A receptor
  • mu(1)-opioid receptor
  • Post-ictal analgesia
  • nanostructured materials
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Appears in Collections:Artigos, TCCs, Teses e Dissertações da Unesp

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