Effect of a nanostructured dendrimer-naloxonazine complex on endogenous opioid peptides μ1 receptor-mediated post-ictal antinociception.

Autor: Felippotti TT; Laboratory of Neuroanatomy & Neuropsychobiology, Department of Pharmacology, Ribeirão Preto School of Medicine of University of São Paulo, Ribeirão Preto (SP), Brazil., do Carmo DR, Paim LL, Stradiotto NR, Bicalho Ude O, Parada CA, Grillo R, Fraceto LF, Coimbra NC
Jazyk: angličtina
Zdroj: Nanomedicine : nanotechnology, biology, and medicine [Nanomedicine] 2011 Dec; Vol. 7 (6), pp. 871-80. Date of Electronic Publication: 2011 Mar 17.
DOI: 10.1016/j.nano.2011.02.005
Abstrakt: 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.
(Copyright © 2011 Elsevier Inc. All rights reserved.)
Databáze: MEDLINE
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