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High-efficacy 5-HT1A receptor activation causes a curative-like action on allodynia in rats with spinal cord injury.

Abstract
The selective, high-efficacy 5-HT(1A) receptor agonist, (3-chloro-4-fluoro-phenyl)-[4-fluoro-4-[[(5-methyl-pyridin-2-ylmethyl)-amino]-methyl]piperidin-1-yl]-methanone (F 13640) has been reported to produce long-term analgesia in rodent models of chronic nociceptive and neuropathic pain; it also preempts allodynia following spinal cord injury. Here, rats underwent spinal cord injury, fully developed allodynia, and were infused with saline or 0.63 mg/day of F 13640 for 56 days. Infusion was then discontinued, and further assessments of allodynia (vocalization threshold to von Frey filament stimulation, responses to brush and cold) were conducted for another 70 days. F 13640-induced analgesia persisted during this post-treatment period. The data offer initial evidence that high-efficacy 5-HT(1A) receptor activation produces an unprecedented curative-like action on pathological pain.
AuthorsFrancis C Colpaert, Wei-Ping Wu, Jing-Xia Hao, Isabelle Royer, François Sautel, Zsuzsanna Wiesenfeld-Hallin, Xiao-Jun Xu
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 497 Issue 1 Pg. 29-33 (Aug 16 2004) ISSN: 0014-2999 [Print] Netherlands
PMID15321732 (Publication Type: Journal Article)
Chemical References
  • Analgesics
  • F 13640
  • Piperidines
  • Pyridines
  • Serotonin 5-HT1 Receptor Agonists
Topics
  • Analgesics (pharmacology, therapeutic use)
  • Animals
  • Behavior, Animal (drug effects)
  • Cold Temperature
  • Female
  • Infusions, Intravenous
  • Pain (drug therapy, etiology)
  • Pain Measurement
  • Pain Threshold
  • Piperidines (pharmacology, therapeutic use)
  • Pyridines (pharmacology, therapeutic use)
  • Rats
  • Rats, Sprague-Dawley
  • Serotonin 5-HT1 Receptor Agonists
  • Spinal Cord Injuries (complications)
  • Touch
  • Vocalization, Animal (drug effects)

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