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Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold

Mstislav Igorevich Lavrov 1, 2
Mstislav Igorevich Lavrov
, 
Dmitry Sergeevich Karlov 1, 2
Dmitry Sergeevich Karlov
, 
Vladimir Alexandrovich Palyulin 1, 2
Vladimir Alexandrovich Palyulin
, 
Vladimir Viktorovich Grigoriev 2
Vladimir Viktorovich Grigoriev
, 
Vladimir Lollievich Zamoyski 2
Vladimir Lollievich Zamoyski
, 
Galina Èduardovna Brkich 3
Galina Èduardovna Brkich
, 
Natalia Valer'evna Pyatigorskaya 3
Natalia Valer'evna Pyatigorskaya
, 
Maxim Èduardovich Zapolskiy 4
Maxim Èduardovich Zapolskiy
10.1016/j.mencom.2018.05.028
Published 2018-04-27
Communication , Volume 28, Issue 3, 311-313
18
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Lavrov M. I. et al. Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold // Mendeleev Communications. 2018. Vol. 28. No. 3. pp. 311-313.
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Lavrov M. I., Karlov D. S., Palyulin V. A., Grigoriev V. V., Zamoyski V. L., Brkich G. È., Pyatigorskaya N. V., Zapolskiy M. È. Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold // Mendeleev Communications. 2018. Vol. 28. No. 3. pp. 311-313.
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TY - JOUR
DO - 10.1016/j.mencom.2018.05.028
UR - https://mendcomm.colab.ws/publications/10.1016/j.mencom.2018.05.028
TI - Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold
T2 - Mendeleev Communications
AU - Lavrov, Mstislav Igorevich
AU - Karlov, Dmitry Sergeevich
AU - Palyulin, Vladimir Alexandrovich
AU - Grigoriev, Vladimir Viktorovich
AU - Zamoyski, Vladimir Lollievich
AU - Brkich, Galina Èduardovna
AU - Pyatigorskaya, Natalia Valer'evna
AU - Zapolskiy, Maxim Èduardovich
PY - 2018
DA - 2018/04/27
PB - Mendeleev Communications
SP - 311-313
IS - 3
VL - 28
ER -
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@article{2018_Lavrov,
author = {Mstislav Igorevich Lavrov and Dmitry Sergeevich Karlov and Vladimir Alexandrovich Palyulin and Vladimir Viktorovich Grigoriev and Vladimir Lollievich Zamoyski and Galina Èduardovna Brkich and Natalia Valer'evna Pyatigorskaya and Maxim Èduardovich Zapolskiy},
title = {Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold},
journal = {Mendeleev Communications},
year = {2018},
volume = {28},
publisher = {Mendeleev Communications},
month = {Apr},
url = {https://mendcomm.colab.ws/publications/10.1016/j.mencom.2018.05.028},
number = {3},
pages = {311--313},
doi = {10.1016/j.mencom.2018.05.028}
}
MLA
Cite this
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Lavrov, Mstislav Igorevich, et al. “Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold.” Mendeleev Communications, vol. 28, no. 3, Apr. 2018, pp. 311-313. https://mendcomm.colab.ws/publications/10.1016/j.mencom.2018.05.028.

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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