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Updated: Jun 23, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Combined strategies for the discovery of ionotropic glutamate receptor antagonists
Alba Chimirri1, Laura De Luca, Stefania Ferro
1Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy. chimirri@pharma.unime.it
Abstract:
New glutamate receptor ligands: This review describes the discovery of rationally designed AMPA and NMDA receptor antagonists, some of which have been proven to be highly potent anticonvulsant and neuroprotective agents.This review summarizes the results of our research group engaged in the development of new glutamate receptor ligands. Chemical and biological studies of several active molecules have been carried out. In particular, extensive work has addressed the identification of antagonists of AMPA and NMDA receptor subtypes using a combination of computational strategies. Innovative synthetic pathways have been used and small libraries of new molecules prepared. In vitro and in vivo tests were performed, and some compounds proved to be highly potent anticonvulsant and neuroprotective agents.
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