Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold
Mendeleev Communications(2018)
Abstract
Molecular modeling, synthesis, and activity evaluation of a novel positive allosteric modulator of the AMPA receptor, 6-[4-methoxy-3-(1H-pyrazol-1-ylmethyl)benzyl]-1,11-dimethyl-3,6,9-triazatricyclo[7.3.1.13,11]tetradecane-4,8,12-trione, are presented. The main point of the design was to fill the interdomain cavity of GluA2 ligand binding domains based on the cyclothiazide binding mode. Electrophysiological studies showed high potentiation of the kainate-induced currents (pECmax∼12).
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Key words
novel positive allosteric modulator,tricyclic scaffold,ampa-receptors
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