Mendeleev Communications
,  volume 28 ,  issue 3 ,  pages 311-313

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

Mstislav I. Lavrov 1, 2
, 
Dmitry S Karlov 1, 2
, 
V. A. Palyulin 1, 2
, 
Vladimir V. Grigoriev 3
, 
Vladimir L Zamoyski 3
, 
Galina E Brkich 4
, 
Natalia V Pyatigorskaya 4
, 
Maxim E Zapolskiy 5
1
 
2
 
3
 
4
 
5
 
QM PHARMA LLC, Skolkovo Innovation Center, 143026 Moscow, Russian Federation | 
Publication type: Journal Article
Publication date: 2018-05-26
scimago Q3
wos Q3
SJR: 0.305
CiteScore: 3.0
Impact factor: 1.7
ISSN: 09599436, 1364551X
General Chemistry
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).
Found 
Found 
2 citations
Vasilenko Dmitry
🥼 🤝
PhD in Chemistry
34 publications,  293 citations
h-index: 10
Lomonosov Moscow State University
Lomonosov Moscow State University
Research interests
Medicinal Chemistry
Organic Chemistry
1 citation
Vatsadze Sergey
DSc in Chemistry, professor, professor of the Russian Academy of Sciences 
170 publications,  2 118 citations,  9 reviews
h-index: 20
N.D. Zelinsky Institute of Organic Chemistry of the Russian Academy of Sciences
N.D. Zelinsky Institute of Organic Chemistry of the Russian Academy of Sciences
Research interests
Supramolecular chemistry
1 citation
Medved’ko Aleksei
🥼 🤝
PhD in Chemistry
62 publications,  737 citations,  8 reviews
h-index: 14
N.D. Zelinsky Institute of Organic Chemistry of the Russian Academy of Sciences
N.D. Zelinsky Institute of Organic Chemistry of the Russian Academy of Sciences
Photochemistry Center
Photochemistry Center
1 citation
Sadovnikov Kirill
PhD in Chemistry
17 publications,  98 citations
h-index: 7
A.V. Topchiev Institute of Petrochemical Synthesis RAS
A.V. Topchiev Institute of Petrochemical Synthesis RAS
Research interests
Medicinal Chemistry
Organic Chemistry
Polymer science

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GOST |
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GOST Copy
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.
GOST all authors (up to 50) Copy
Lavrov M. I., Karlov D. S., Palyulin V. A., Grigoriev V. V., Zamoyski V. L., Brkich G. E., Pyatigorskaya N. V., Zapolskiy M. E. Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold // Mendeleev Communications. 2018. Vol. 28. No. 3. pp. 311-313.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.mencom.2018.05.028
UR - https://doi.org/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 I.
AU - Karlov, Dmitry S
AU - Palyulin, V. A.
AU - Grigoriev, Vladimir V.
AU - Zamoyski, Vladimir L
AU - Brkich, Galina E
AU - Pyatigorskaya, Natalia V
AU - Zapolskiy, Maxim E
PY - 2018
DA - 2018/05/26
PB - OOO Zhurnal "Mendeleevskie Soobshcheniya"
SP - 311-313
IS - 3
VL - 28
SN - 0959-9436
SN - 1364-551X
ER -
BibTex |
Cite this
BibTex (up to 50 authors) Copy
@article{2018_Lavrov,
author = {Mstislav I. Lavrov and Dmitry S Karlov and V. A. Palyulin and Vladimir V. Grigoriev and Vladimir L Zamoyski and Galina E Brkich and Natalia V Pyatigorskaya and Maxim E Zapolskiy},
title = {Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold},
journal = {Mendeleev Communications},
year = {2018},
volume = {28},
publisher = {OOO Zhurnal "Mendeleevskie Soobshcheniya"},
month = {may},
url = {https://doi.org/10.1016/j.mencom.2018.05.028},
number = {3},
pages = {311--313},
doi = {10.1016/j.mencom.2018.05.028}
}
MLA
Cite this
MLA Copy
Lavrov, Mstislav I., et al. “Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold.” Mendeleev Communications, vol. 28, no. 3, May. 2018, pp. 311-313. https://doi.org/10.1016/j.mencom.2018.05.028.