RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia. - CNRS - Centre national de la recherche scientifique Accéder directement au contenu
Article Dans Une Revue Proceedings of the National Academy of Sciences of the United States of America Année : 2006

RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia.

Martine Schmitt
Jean-Paul Laulin
  • Fonction : Auteur
Emilie Laboureyras
  • Fonction : Auteur
Jack H Jhamandas
  • Fonction : Auteur
David Mactavish
  • Fonction : Auteur
Catherine Mollereau
Patrick Laurent
  • Fonction : Auteur
Marc Parmentier
  • Fonction : Auteur
Jean-Jacques Bourguignon
  • Fonction : Auteur
Guy Simonnet
  • Fonction : Auteur

Résumé

Neuropeptide FF (NPFF) has been proposed to play a role in pain modulation, opioid tolerance, and several other physiological processes. However, pharmacological agents that would help define physiological roles for this peptide are still missing. Here we report the discovery of a potent and selective NPFF receptor antagonist, RF9, that can be administered systemically. This compound does not show any effects by itself but can block efficiently the increase in blood pressure and heart rate evoked by NPFF. When chronically coinjected with heroin, RF9 completely blocks the delayed and long-lasting paradoxical opioid-induced hyperalgesia and prevents the development of associated tolerance. Our data indicate that NPFF receptors are part of a bona fide antiopioid system and that selective antagonists of these receptors could represent useful therapeutic agents for improving the efficacy of opioids in chronic pain treatment.

Dates et versions

hal-00188146 , version 1 (15-11-2007)

Identifiants

Citer

Frédéric Simonin, Martine Schmitt, Jean-Paul Laulin, Emilie Laboureyras, Jack H Jhamandas, et al.. RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia.. Proceedings of the National Academy of Sciences of the United States of America, 2006, 103 (2), pp.466-71. ⟨10.1073/pnas.0502090103⟩. ⟨hal-00188146⟩
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