Author/Authors :
Stephan Schann، نويسنده , , Christel Menet، نويسنده , , Paul Arvault، نويسنده , , Geraldine Mercier، نويسنده , , Mélanie Frauli، نويسنده , , Stanislas Mayer، نويسنده , , Nadia Hubert، نويسنده , , Nicolas Triballeau، نويسنده , , Hugues-Olivier Bertrand، نويسنده , , Francine Acher، نويسنده , , Pascal Neuville، نويسنده ,
Abstract :
A new family of mGlu receptor orthosteric ligands called APTCs was designed and synthesized using a parallel chemistry approach. Amongst 65 molecules tested on mGlu4, mGlu6 and mGlu8 subtypes, (2S,4S)-4-amino-1-[(E)-3-carboxyacryloyl]pyrrolidine-2,4-dicarboxylic acid (8a06—FP0429) has been shown to be a full mGlu4 agonist and a partial mGlu8 agonist. In addition, 8a06 was shown to be selective versus group I and II mGlu subtypes. A possible explanation for this efficacy difference is proposed by docking experiment performed with molecular model of the receptor.
