Investigation on allosteric modulators of Metabotropic Glutamate Receptor 5: studies and structure-activity relationships on mGlu5 ligands in Recordati
Il 19/01/2018 ore 14.30 - 15.30
Sala Conferenze CNR, via P. Castellino, 111 - 80131 Napoli
Dr Davide Graziani, from Drug Discovery, Recordati S.p.A. in Milano, will give a seminar on methods and compounds for the treatment and/or prevention of neurological and psychiatric disorders.
The mGlu5 receptor is a G protein-coupled receptor highly expressed in the central nervous system that has received particular attention as putative therapy of neurological disorders: anxiety, chronic pain, schizophrenia, Parkinson’s disease, levodopa induced dyskinesia, epilepsy and Fragile X syndrome.
A number of derivatives of prop-2-ynylidenecycloalkylamine, were synthesized as novel, potent and selective negative allosteric modulators of metabotropic glutamate receptor 5. Structure activity relationship, modulation of solubility, minimization of cytochrome interaction and metabolic stability of the newly synthesized classes of compounds was deeply evaluated in order to select the most suitable preclinical candidate. In silico and experimental analysis on the investigated series of compounds were performed to rationalize ligand protein interactions.
Organizzato da:
Ibp, Cnr
Referente organizzativo:
Andrea Beccari
Cnr - Istituto di biochimica delle proteine
Via P. castellino, 111 - 80131 Napoli
a.beccari@ibp.cnr.it
Modalità di accesso: ingresso libero