Novel bivalent positive allosteric AMPA receptor modulator of bis-amide series

Nadezhda S. Temnyakova,Dmitry A. Vasilenko,Mstislav I. Lavrov,Dmitry S. Karlov,Yuri K. Grishin,Vladimir L. Zamoyski,Vladimir V. Grigoriev,Elena B. Averina,Vladimir A. Palyulin

Mendeleev Communications（2021）

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摘要

A series of bis-amides of bis(aminoalkyl)benzenes and diaminoalkanes were synthesized. Positive modulation of kainate-induced transmembrane currents was registered on Purkinje neurons for isobutyric acid derivative with 1,4-bis(aminomethyl)benzene linker (40% potentiation at 1nm). This compound also demonstrated a neuroprotective effect at 0.1nm in an oxidative stress model in HT-22 cells when applied 24h before H2O2.

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关键词

AMPA receptor,positive allosteric modulator,patch clamp,Purkinje neurons,carboxamides

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