1. Pharmacological and Electrophysiological Characterization of Novel NMDA Receptor Antagonists.
- Author
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Leiva R, Phillips MB, Turcu AL, Gratacòs-Batlle E, León-García L, Sureda FX, Soto D, Johnson JW, and Vázquez S
- Subjects
- Amines chemical synthesis, Amines pharmacology, Animals, Cerebellum cytology, Excitatory Amino Acid Antagonists pharmacology, Inhibitory Concentration 50, Memantine pharmacology, Patch-Clamp Techniques, Polycyclic Compounds pharmacology, Rats, Structure-Activity Relationship, Excitatory Amino Acid Antagonists chemical synthesis, Neurons drug effects, Polycyclic Compounds chemical synthesis, Receptors, N-Methyl-D-Aspartate antagonists & inhibitors
- 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.
- Published
- 2018
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