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Pharmacological and Electrophysiological Characterization of Novel NMDA Receptor Antagonists

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journal contribution
posted on 16.05.2018, 00:00 by Rosana Leiva, Matthew B. Phillips, Andreea L. Turcu, Esther Gratacòs-Batlle, Lara León-García, Francesc X. Sureda, David Soto, Jon W. Johnson, Santiago Vázquez
This work reports the synthesis and pharmacological and electrophysiological evaluation of new N-methyl-d-aspartic acid receptor (NMDAR) channel blocking antagonists featuring polycyclic scaffolds. Changes in the chemical structure modulate the potency and voltage dependence of inhibition. Two of the new antagonists display properties comparable to those of memantine, a clinically approved NMDAR antagonist.