Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffoldстатьяКраткое сообщение
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Дата последнего поиска статьи во внешних источниках: 30 августа 2018 г.
Аннотация: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).