Otro
Effect of a nanostructured dendrimer-naloxonazine complex on endogenous opioid peptides mu(1) receptor-mediated post-ictal antinociception
Registro en:
Nanomedicine-nanotechnology Biology and Medicine. Amsterdam: Elsevier B.V., v. 7, n. 6, p. 871-880, 2011.
1549-9634
10.1016/j.nano.2011.02.005
WOS:000297699900023
Autor
Felippotti, Tatiana Tocchini
do Carmo, Devaney Ribeiro
Paim, Leonardo Lataro
Stradiotto, Nelson Ramos
Bicalho, Urquisa de Oliveira
Parada, Carlos Amilcar
Grillo, Renato
Fraceto, Leonardo Fernandes
Coimbra, Norberto Cysne
Resumen
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. 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)