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Updated: Jun 26, 2026

A High-throughput Calcium-flux Assay to Study NMDA-receptors with Sensitivity to Glycine/D-serine and Glutamate
Published on: July 10, 2018
Development of 3-substituted-1H-indole derivatives as NR2B/NMDA receptor antagonists
Rosaria Gitto1, Laura De Luca, Stefania Ferro
1Dipartimento Farmaco-Chimico, Università di Messina, Messina, Italy. rgitto@pharma.unime.it
Abstract:
A combined ligand-based and structure-based approach has previously allowed us to identify NR2B/NMDA receptor antagonists containing indole scaffold. In order to further explore the main structure activity relationships of this class of derivatives we herein report the design, synthesis and biological evaluation of new analogues. Some derivatives demonstrated to produce significant anticonvulsant properties and NMDA antagonism. The most active of them (3d) showed NR2B binding affinity equipotent to that of ifenprodil. These results were also corroborated by computational studies.
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