Antinociceptive and anti-allodynic effects of oral PL37, a complete inhibitor of enkephalin-catabolizing enzymes, in a rat model of peripheral neuropathic pain induced by vincristine

Thibault, Karine; Bonnard, Elisabeth; Dubacq, Sophie; Claude, F; Bernard, Roques; Bernard, Calvino

doi:10.1016/j.ejphar.2008.10.004

Cited by 41 publications

(34 citation statements)

References 30 publications

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“…Except in one study, 57 only static stimuli were applied, whereas dynamic stimuli could give us further information regarding physiopathology of this kind of neuropathic pain. Very few studies carried out a motor performance assessment in animals to evaluate the real feasibility of sensory behavioral tests.…”

Section: Resultsmentioning

confidence: 99%

“…55 Finally, concerning the opioid system, administration of a complete inhibitor of enkephalincatabolizing enzymes (PL37) also induced an antinociceptive and anti-allodynic effect, but were not effective on cold allodynia. 57 More recently, to investigate if blood flow reduction is involved in this neuropathy, Gauchan et al 58 assessed the effect of limaprost, a prostaglandin E1 analog, on mechanical allodynia without effectiveness.…”

Section: Treatment Strategiesmentioning

confidence: 99%

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Animal Models of Chemotherapy-Evoked Painful Peripheral Neuropathies

et al. 2009

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Summary:This review examines recent preclinical research on toxic peripheral neuropathy and potential therapeutic developments. Chemotherapy-induced peripheral neurotoxicity is a major clinical problem because it represents the dose-limiting side effects of a significant number of antineoplastic drugs. Patients are unable to complete full or optimal treatment schedules. The incidence of chemotherapy-induced peripheral neuropathy varies depending on the drugs and schedules used, and this can be quite high, particularly when neurophysiological methods are used to make a diagnosis. However, even when chemotherapy-induced peripheral neuropathy is not a doselimiting side effect, its onset may severely affect the quality of life of cancer patients and cause chronic discomfort. As such, improved understanding of the pathophysiology of chemotherapy-induced neurotoxicity need for animal models is clinically relevant and will assist in the development of future neuroprotective strategies and also in the design of novel chemotherapies with improved toxicity profiles. In this review, the features of animal models of chemotherapy-induced painful neuropathy developed for 20 years, due to the administration of the most widely used drugs, such as platinum drugs, taxanes, and vinca alkaloids, will be discussed. In a second part, data available on neuroprotectants and treatment strategies, evaluated using these previous animal models in the attempt to prevent neuropathic pain, will be summarized.

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Section: Resultsmentioning

confidence: 99%

Section: Treatment Strategiesmentioning

confidence: 99%

Animal Models of Chemotherapy-Evoked Painful Peripheral Neuropathies

et al. 2009

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“…The stimulus was applied five times with a 5 s interval and the numbers of withdrawals were noted (between 0 and 5). The same procedure was repeated twice, with a gap of five minutes and the total number of withdrawals (in three tests) were added to obtain a single cumulative score of mechanical dynamic allodynia with a minimum value of 0 and maximum of 15 (Thibault et al, 2008;Weissman-Fogel et al, 2008).…”

Section: Mechanical Dynamic Allodynia (Paint-brush Test)mentioning

confidence: 99%

Dose-related neuropathic and anti-neuropathic effects of simvastatin in vincristine-induced neuropathic pain in rats

Bhalla

Singh

Jaggi

2015

Food and Chemical Toxicology

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“…Le Debio 0827 est également actif PO dans le modèle du rat diabétique où son action à 50 mg/kg est du même ordre que celui de la gabapentine (100 mg/kg, IP), mais avec une durée d'action plus longue (résultats non publiés). Enfin, dans les douleurs neuropathiques induites par administration de vincristine, il diminue très sensiblement la contribution mécanique statique (test de von Frey) et dynamique (test du pinceau) [23]. Dans tous ces tests, la contribution péri-phérique est dominante, démontrant que le PL37 après passage de la barrière intestinale diffuse rapidement au niveau des nocicepteurs et exerce son inhibition de la NEP et de l'APN après rupture du pont disulfure.…”

Section: Debio 0827 Et Douleur Neurophatiqueunclassified

Potentiation of the control of pain by endogenous enkephalins through inhibition of their enzymatic inactivation, a new approach towards physiological analgesics

Roques

2009

Douleur analg

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Les inhibiteurs mixtes des deux enzymes d'inactivation des enképhalines endogènes, tels que le Debio 0827, augmentent leur concentration synaptique. Actifs par voie systémique et orale sur les douleurs aiguës, inflammatoires ou neuropathiques, ils sont dépourvus des effets secondaires de la morphine, y compris la tolérance, et représentent une avancée vers le développement d'analgésiques physiologiques. Le Debio 0827 est désormais en essai clinique (phase I). Mots clés Enképhalines · Métallopeptidases · Inhibiteurs mixtes · Analgésie physiologique · Douleur neuropathiqueAbstract Dual inhibitors of the two peptidases (neprilysine and aminopeptidase-N) involved in enkephalins inactivation as Debio 0827 led to an increase in their synaptic concentration. These inhibitors are active by systemic and oral route on nociceptive inflammatory and neuropathic pain in rodents. They are devoid of morphine side effects including tolerance and appear as a new approach towards physiological analgesics. Debio 0827 is now in clinical trial (phase I).

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Antinociceptive and anti-allodynic effects of oral PL37, a complete inhibitor of enkephalin-catabolizing enzymes, in a rat model of peripheral neuropathic pain induced by vincristine

Cited by 41 publications

References 30 publications

Animal Models of Chemotherapy-Evoked Painful Peripheral Neuropathies

Animal Models of Chemotherapy-Evoked Painful Peripheral Neuropathies

Dose-related neuropathic and anti-neuropathic effects of simvastatin in vincristine-induced neuropathic pain in rats

Potentiation of the control of pain by endogenous enkephalins through inhibition of their enzymatic inactivation, a new approach towards physiological analgesics

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