Dual, Hyperalgesic, and Analgesic Effects of the High-Efficacy 5-Hydroxytryptamine 1A (5-HT1A) Agonist F 13640 [(3-Chloro-4-fluoro-phenyl)-[4-fluoro-4-{[(5-methyl-pyridin-2-ylmethyl)-amino]-methyl}piperidin-1-yl]methanone, Fumaric Acid Salt]: Relationship with 5-HT1A Receptor Occupancy and Kinetic P

@article{Bardin2005DualHA,
  title={Dual, Hyperalgesic, and Analgesic Effects of the High-Efficacy 5-Hydroxytryptamine 1A (5-HT1A) Agonist F 13640 [(3-Chloro-4-fluoro-phenyl)-[4-fluoro-4-\{[(5-methyl-pyridin-2-ylmethyl)-amino]-methyl\}piperidin-1-yl]methanone, Fumaric Acid Salt]: Relationship with 5-HT1A Receptor Occupancy and Kinetic P},
  author={Laurent Bardin and Marie Bernadette Assi{\'e} and Martine P{\'e}lissou and Isabelle Royer-Urios and Adrian Newman-Tancredi and J P Ribet and François Sautel and Wouter Koek and F. C. Colpaert},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2005},
  volume={312},
  pages={1034 - 1042}
}
  • L. BardinM. Assié F. Colpaert
  • Published 1 March 2005
  • Biology, Chemistry, Medicine
  • Journal of Pharmacology and Experimental Therapeutics
The aim of the present study was to establish the relationship between the plasma and brain concentration-time profiles of F 13640 [(3-chloro-4-fluoro-phenyl)-[4-fluoro-4-{[(5-methyl-pyridin-2-ylmethyl)-amino]-methyl}piperidin-1-yl]methanone, fumaric acid salt] after acute administration and both its hyper- and hypoanalgesic effects in rats. The maximal plasma concentration (Cmax) of F 13640 after i.p. administration of 0.63 mg/kg was obtained at 15 min and decreased to half its maximal value… 

Figures and Tables from this paper

[3H]-F13640, a novel, selective and high-efficacy serotonin 5-HT1A receptor agonist radioligand

3H]-F13640 is a potent agonist radioligand at 5-HT1A receptors and may be a useful tool in pharmacological studies at native and recombinant 5- HT1A receptor receptors.

5-HT1A Receptor Agonist Befiradol Reduces Fentanyl-induced Respiratory Depression, Analgesia, and Sedation in Rats

The reversal of opioid-induced respiratory depression and sedation by befiradol in adult rats was robust, whereas involved mechanisms are unclear, however, there were adverse concomitant decreases in fentanyl-induced analgesia and altered baseline ventilation, nociception, and behavior.

The Counteraction of Opioid-Induced Ventilatory Depression by the Serotonin 1A-Agonist 8-OH-DPAT Does Not Antagonize Antinociception in Rats In Situ and In Vivo

5-HT1A-R-agonist 8-OH-DPAT activates spontaneous breathing without diminishing opioid-induced antinociception in rats.

Effect of buspirone on thermal sensory and pain thresholds in human volunteers

The negative results of the present study do not rule out a possible analgesic effect of more specific 5-HT1A receptor agonists, as it is only a partial agonist at the 5- HT1A receptors and also acts on other receptor types.

References

SHOWING 1-10 OF 50 REFERENCES

Continuous Administration of the 5-Hydroxytryptamine1A Agonist (3-Chloro-4-fluoro-phenyl)-[4-fluoro-4-{[(5-methyl-pyridin-2-ylmethyl) -amino]-methyl}piperidin-1-yl]-methadone (F 13640) Attenuates Allodynia-Like Behavior in a Rat Model of Trigeminal Neuropathic Pain

The data presented here suggest that F 13640 may perhaps offer a lasting treatment of trigeminal neuralgia and are consistent with a theory of nociceptive signal transduction, as well as with previous data, in demonstrating the neuroadaptive mechanisms of inverse tolerance and cooperation.

Tolerance and inverse tolerance to the hyperalgesic and analgesic actions, respectively, of the novel analgesic, F 13640.

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

Selective activation of 5HT1A receptors induces lower lip retraction in the rat

Effects of the putative 5-HT1A receptor agonist 8-OH-2-(di-n-propylamino)tetralin on nociceptive sensitivity in mice