Partenaires

CNRS
Logo tutelle Logo tutelle


Rechercher

Sur ce site

Sur le Web du CNRS


Accueil du site > Teams > Organic & Medicinal chemistry > CESMA - Design and Synthesis of Analgesic Molecules > Project TREK

Project TREK

by Sylvie Ducki - 23 March 2012

All the versions of this article: English , français

Description of project

Potassium channels TREK-1 were identified as an important target in the perception of the pain. [Alloui 2006, Noel 2009] Indeed, they showed that the treatment of TREK-KO animals with analgesics of reference did not produce any analgesic effect whereas the activation of this channel led to an analgesic effect, thus validating the therapeutic target. A screening of molecules known as activators of TREK-1 was carried out by our team and allowed us to identify a lead molecule, able to activate TREK-1 channels (shown by electrophysiology) and having an analgesic effect in vivo (test of the acetic acid). Analogues of this lead were conceived then synthesized in order to identify the pharmacophore of the lead. These molecules were the subject of a pharmacological evaluation and a molecule emerged with a promising pharmacological activity.

Publication

Ducki, S. ; Rodrigues, N. ; Bennis, K. ; Eschalier, A. « Composés anti-Douleur », FR1162564, French patent deposited on December 30, 2011.

Grants

Bourse Innovation du Conseil Régional d’Auvergne / FEDER (2009-2011) Bourse Novartis (2011) Bourse MESR (2011-2014)

Academic and industrial collaborations

Dr Jérôme Busserolles et Pr Alain Eschalier - Equipe « Pharmacologie fondamentale et clinique de la Douleur » de l’Institut NeurolDol (UMR1107) à l’Université d’Auvergne, Clermont-Ferrand. Dr Florian LESAGE – Equipe « Physiologie moléculaire et physiopathologie des canaux ioniques » de l’Institut de Pharmacologie Moléculaire et Cellulaire (UMR7275) à Valbonne Sophia Antipolis. Dr François Caussade – ANS Biotech, Clermont-Ferrand.