N. S. Temnyakova, D. A. Vasilenko, M. I. Lavrov, D. S. Karlov, Yu. K. Grishin, V. L. Zamoyski, V. V. Grigoriev, E. B. Averina, V. A. Palyulin, “Novel bivalent positive allosteric AMPA receptor modulator of bis-amide series”, Mendeleev Commun., 2021, Volume 31, Issue 2,Pages <nobr>216

This article is cited in 8 papers

Communications

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

N. S. Temnyakova^a, D. A. Vasilenko^a, M. I. Lavrov^ab, D. S. Karlov^a, Yu. K. Grishin^a, V. L. Zamoyski^b, V. V. Grigoriev^ab, E. B. Averina^ab, V. A. Palyulin^ab

^a Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow, Russian Federation
^b Institute of Physiologically Active Compounds, Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow Region, Russian Federation

Abstract: 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.

Keywords: AMPA receptor, positive allosteric modulator, patch clamp, Purkinje neurons, carboxamides.

Language: English

DOI: 10.1016/j.mencom.2021.03.023

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