Publications

Latest publication 12/01/2011

Effect of potent endomorphin degradation blockers on analgesic and antidepressan

The biological effects of endomorphins (EMs) are short-lasting due to their rapid degradation by endogenous enzymes. Competing enzymatic...

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    [title] => Effect of potent endomorphin degradation blockers on analgesic and antidepressan
    [paragraph] => Effect of potent endomorphin degradation blockers on analgesic and antidepressant-like responses in mice. 
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Authors
A. Cravezic, J. Fichna, K. Gach, A. Wyrebska, R. Perlikowska et al. 

 Lab
University of Rouen, Institut Fédératif de Recherches Multidisciplinaires sur les Peptides, IFRMP23, Mont-Saint-Aignan, France.
Journal
Neuropharmacology
Abstract
The biological effects of endomorphins (EMs) are short-lasting due to their rapid degradation by endogenous enzymes. Competing enzymatic degradation is an approach to prolong EM bioavailability. In the present study, a series of tetra- and tripeptides of similar to EMs structure was synthesized and tested in vitro and in vivo for their ability to inhibit degradation of EMs. The obtained results indicated that, among the series of analogs, the tetrapeptide Tyr-Pro-d-ClPhe-Phe-NH(2) and the tripeptide Tyr-Pro-Ala-NH(2), which did not bind to the _-opioid receptors, were potent inhibitors of EM catabolism in rat brain homogenate. In vivo, these two peptides significantly prolonged the analgesic and antidepressant-like effects, induced by exogenous EMs, by blocking EM degrading enzymes. These new potent inhibitors may therefore increase the level and the half life of endogenous EMs and could be used in a new therapeutic strategy against pain and mood disorders, based on increasing of EM bioavailability.
BIOSEB Instruments Used
Forced Swimming Test: New FST DUAL SENSOR (BIO-FST-DSM)
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Combining a double input from vibrations and video,
 the TYC (Train-Your-Computer) algorithm compares both inputs to determine the animal's behavior in real time, making results completely operator-independent.

Experiment manager, analysis module, replay possibilities and the TYC algorithm are some of the features that make FST DUAL SENSOR a very innovative and easy to use instrument for both mice or rats studies (up to 4 animals can be tested at a time), based on the famous Porsolt Test, or "behavioral despair" test

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