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

Nadezhda Sergeevna Temnyakova 1
Nadezhda Sergeevna Temnyakova
Dmitry Alekseevich Vasilenko 1
Dmitry Alekseevich Vasilenko
Mstislav Igorevich Lavrov 1, 2
Mstislav Igorevich Lavrov
Dmitry Sergeevich Karlov 1
Dmitry Sergeevich Karlov
Vladimir Lollievich Zamoyski 2
Vladimir Lollievich Zamoyski
Vladimir Viktorovich Grigoriev 1, 2
Vladimir Viktorovich Grigoriev
Elena Borisovna Averina 1, 2
Elena Borisovna Averina
Vladimir Alexandrovich Palyulin 1, 2
Vladimir Alexandrovich Palyulin
Published 2021-03-03
CommunicationVolume 31, Issue 2, 216-218
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Temnyakova N. S. et al. Novel bivalent positive allosteric AMPA receptor modulator of bis-amide series // Mendeleev Communications. 2021. Vol. 31. No. 2. pp. 216-218.
GOST all authors (up to 50) Copy
Temnyakova N. S., Vasilenko D. A., Lavrov M. I., Karlov D. S., Grishin Y. K., Zamoyski V. L., Grigoriev V. V., Averina E. B., Palyulin V. A. Novel bivalent positive allosteric AMPA receptor modulator of bis-amide series // Mendeleev Communications. 2021. Vol. 31. No. 2. pp. 216-218.
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TY - JOUR
DO - 10.1016/j.mencom.2021.03.023
UR - https://mendcomm.colab.ws/publications/10.1016/j.mencom.2021.03.023
TI - Novel bivalent positive allosteric AMPA receptor modulator of bis-amide series
T2 - Mendeleev Communications
AU - Temnyakova, Nadezhda Sergeevna
AU - Vasilenko, Dmitry Alekseevich
AU - Lavrov, Mstislav Igorevich
AU - Karlov, Dmitry Sergeevich
AU - Grishin, Yuri Konstantinovich
AU - Zamoyski, Vladimir Lollievich
AU - Grigoriev, Vladimir Viktorovich
AU - Averina, Elena Borisovna
AU - Palyulin, Vladimir Alexandrovich
PY - 2021
DA - 2021/03/03
PB - Mendeleev Communications
SP - 216-218
IS - 2
VL - 31
ER -
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@article{2021_Temnyakova,
author = {Nadezhda Sergeevna Temnyakova and Dmitry Alekseevich Vasilenko and Mstislav Igorevich Lavrov and Dmitry Sergeevich Karlov and Yuri Konstantinovich Grishin and Vladimir Lollievich Zamoyski and Vladimir Viktorovich Grigoriev and Elena Borisovna Averina and Vladimir Alexandrovich Palyulin},
title = {Novel bivalent positive allosteric AMPA receptor modulator of bis-amide series},
journal = {Mendeleev Communications},
year = {2021},
volume = {31},
publisher = {Mendeleev Communications},
month = {Mar},
url = {https://mendcomm.colab.ws/publications/10.1016/j.mencom.2021.03.023},
number = {2},
pages = {216--218},
doi = {10.1016/j.mencom.2021.03.023}
}
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Temnyakova, Nadezhda Sergeevna, et al. “Novel bivalent positive allosteric AMPA receptor modulator of bis-amide series.” Mendeleev Communications, vol. 31, no. 2, Mar. 2021, pp. 216-218. https://mendcomm.colab.ws/publications/10.1016/j.mencom.2021.03.023.

Keywords

AMPA receptor
carboxamides
patch clamp
positive allosteric modulator
Purkinje neurons

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.

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