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Updated: May 4, 2026

A High-throughput Calcium-flux Assay to Study NMDA-receptors with Sensitivity to Glycine/D-serine and Glutamate
Published on: July 10, 2018
Structure-activity relationships of N-substituted 4-(trifluoromethoxy)benzamidines with affinity for
Corinne Beinat1, Samuel D Banister2, Jane Hoban1
1School of Chemistry, The University of Sydney, NSW 2006, Australia.
Abstract:
GluN2B subtype-selective NMDA antagonists represent promising therapeutic targets for the symptomatic treatment of multiple CNS pathologies. A series of N-benzyl substituted benzamidines were synthesised and the benzyl ring was further replaced with various polycyclic moieties. Compounds were evaluated for activity at GluN2B containing NMDA receptors where analogues 9, 12, 16 and 18 were the most potent of the series, replacement of the benzyl ring with polycycles resulted in a complete loss of activity.
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