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Inhibition of neuropeptide FF (NPFF)-induced hypothermia and anti-morphine analgesia by RF9, a new selective NPFF receptors antagonist.

Abstract
Neuropeptide FF (NPFF) belongs to a neuropeptide family including two precursors (pro-NPFF A and pro-NPFF B) and two receptors (NPFF1 and NPFF2). Very recently, the novel compound RF9 was reported as the truly selective antagonist on NPFF receptors. The present study examined the effects of RF9 on the hypothermia and anti-morphine action induced by NPFF in mice. (1) RF9 injected into the third ventricle was devoid of any residual agonist activity, but it completely antagonized the hypothermic effects of NPFF (30 or 45 nmol) after cerebral administration in mice; (2) RF9 did not alter the tail-flick latency and morphine analgesia in nociceptive test, however, co-administration of RF9 prevented the anti-morphine action of intracerebroventricularly applied NPFF (10 nmol, i.c.v.) in the mouse tail-flick assay. Collectively, our data indicate that RF9, behaving as a truly pure NPFF receptors antagonist, prevents NPFF-induced drops of the body temperature and morphine analgesia in mice. In addition, it further confirms that the hypothermia and anti-morphine action of NPFF are mediated directly by NPFF receptors.
AuthorsQuan Fang, Yi-Qing Wang, Feng He, Jia Guo, Jia Guo, Qiang Chen, Rui Wang
JournalRegulatory peptides (Regul Pept) Vol. 147 Issue 1-3 Pg. 45-51 (Apr 10 2008) ISSN: 0167-0115 [Print] Netherlands
PMID18276024 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Analgesics, Opioid
  • Dipeptides
  • Narcotic Antagonists
  • Oligopeptides
  • Receptors, Neuropeptide
  • adamantylcarbonyl-arginyl-phenylalaninamide
  • neuropeptide FF receptor
  • Morphine
  • phenylalanyl-leucyl-phenylalanyl-glutaminyl-prolyl-glutaminyl-arginyl-phenylalaninamide
  • Adamantane
Topics
  • Adamantane (analogs & derivatives, pharmacology)
  • Analgesics, Opioid (antagonists & inhibitors)
  • Animals
  • Body Temperature (drug effects)
  • Dipeptides (pharmacology)
  • Hypothermia (chemically induced, metabolism)
  • Male
  • Mice
  • Morphine (antagonists & inhibitors)
  • Narcotic Antagonists (pharmacology)
  • Oligopeptides (antagonists & inhibitors)
  • Pain Measurement
  • Receptors, Neuropeptide (antagonists & inhibitors)

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