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Pharmacological and Electrophysiological Characterization of Novel NMDA Receptor Antagonists.

ABSTRACT: 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.

SUBMITTER: Leiva R

PROVIDER: S-EPMC6249113 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature

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Pharmacological and Electrophysiological Characterization of Novel NMDA Receptor Antagonists.

Leiva Rosana R Phillips Matthew B MB Turcu Andreea L AL Gratacòs-Batlle Esther E León-García Lara L Sureda Francesc X FX Soto David D Johnson Jon W JW Vázquez Santiago S

ACS chemical neuroscience 20180601 11

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. ...[more]

PMID: 29767953

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