Douleur - page 19 - Publications Scientifiques

Dernière publication 30/11/2002

Large-amplitude 5-HT1A receptor activation- a new mechanism of profound- central

We report the discovery of F 13640 and evidence suggesting this agent to produce powerful, broad-spectrum analgesia by novel molecular and...

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    [title] => Large-amplitude 5-HT1A receptor activation- a new mechanism of profound- central
    [paragraph] => Large-amplitude 5-HT1A receptor activation: a new mechanism of profound, central analgesia.
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Authors
F.C. Colpaert, J.P. Tarayre, W. Koek, P.J. Pauwels, L. Bardin et al.

 Lab
Centre de Recherche Pierre Fabre, Castres, France ; Karolinska Institutet, Huddinge, Sweden.
Journal
Neuropharmacology
Abstract
We report the discovery of F 13640 and evidence suggesting this agent to produce powerful, broad-spectrum analgesia by novel molecular and neuroadaptative mechanisms. F 13640 stimulates G__ protein coupling to 5-HT1A receptors to an extent unprecedented by selective, non-native 5-HT1A ligands. Fifteen minutes after its injection in normal rats, F 13640 (0.01–2.5 mg/kg) decreases the vocalization threshold to paw pressure; 15 min upon injection in rats that are exposed to formalin-induced tonic nociception, F 13640 inhibits pain behavior. The initial hyperalgesia induced by 0.63 mg/kg F 13640 was followed, 8 hrs later, by paradoxical hypo-algesia; 5 mg/kg of morphine produces the opposite effects (i.e., hypo-algesia followed by hyper-algesia). Repeated F 13640 injections cause an increase in the basal vocalization threshold and a reduction of F 13640-produced hyperalgesia; in these conditions, morphine causes basal hyperalgesia and antinociceptive tolerance. Continuous two-week infusion of F 13640 (0.63 mg/day) exerts little effect on the threshold in normal rats, but markedly reduces analgesic self-administration in arthritic rats. F 13640 infusion also decreases allodynic responses to tactile and thermal stimulations in rats sustaining spinal cord or sciatic nerve injury. In these models of chronic nociceptive and neuropathic pain, the analgesia afforded by F 13640 consistently surpasses that of morphine (5 mg/day), imipramine (2.5 mg/day), ketamine (20 mg/day) and gabapentin (10 mg/day). Very-high-efficacy 5-HT1A receptor activation constitutes a novel mechanism of central analgesia that grows rather than decays with chronicity, that is amplified by nociceptive stimulation, and that may uniquely relieve persistent nociceptive and neuropathic pains.
BIOSEB Instruments Used
Electronic Von Frey 4 (BIO-EVF4),Electronic Von Frey 5 with embedded camera (BIO-EVF5)
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Une solution rapide pour déterminer le seuil de sensibilité à la douleur mécanique chez les rongeurs (rats et souris). Maintenant en version sans-fil, pour être libéré des câbles!

Cet instrument électronique précis et simple d'utilisation est le test de référence pour vos recherches en analgésie, nociception, neuropathies et douleurs post-opératoires

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L'EVF5 intègre une caméra embarquée au niveau de la zone de stimulation et fonctionne avec un nouveau logiciel dédié révolutionnaire

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