High-efficacy 5-HT1A receptor activation causes a curative-like action on allodynia in rats with spinal cord injury.
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.
Centre de Recherche Pierre Fabre, 17 Avenue Jean Moulin, 81100 Castres, France. francis.colpaert@pierre-fabre.com
Francis C
FC
Colpaert
Wei-Ping
WP
Wu
Jing-Xia
JX
Hao
Isabelle
I
Royer
François
F
Sautel
Zsuzsanna
Z
Wiesenfeld-Hallin
Xiao-Jun
XJ
Xu
D000700:Analgesics / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D003080:Cold Temperature; D005260:Female; D007262:Infusions, Intravenous; D010146:Pain / Q000188:drug therapy* / Q000209:etiology; D010147:Pain Measurement; D017288:Pain Threshold; D010880:Piperidines / Q000494:pharmacology / Q000627:therapeutic use*; D011725:Pyridines / Q000494:pharmacology / Q000627:therapeutic use*; D051381:Rats; D017207:Rats, Sprague-Dawley; D058825:Serotonin 5-HT1 Receptor Agonists; D013119:Spinal Cord Injuries / Q000150:complications*; D014110:Touch; D014828:Vocalization, Animal / Q000187:drug effects
D000700:Analgesics; D010880:Piperidines; D011725:Pyridines; D058825:Serotonin 5-HT1 Receptor Agonists; C473959:befiradol