Novel Positive Allosteric Modulators of AMPA Receptors Based on 3,7-Diazabicyclo[3.3.1]nonane Scaffold
Mstislav I. Lavrov
1, 2
,
Dmitry S Karlov
1, 3
,
Tatiana A. Voronina
4
,
Vladimir V. Grigoriev
2
,
S. O. Bachurin
2
,
V. A. Palyulin
1, 2
Publication type: Journal Article
Publication date: 2019-09-12
scimago Q1
wos Q1
SJR: 1.397
CiteScore: 8.4
Impact factor: 4.3
ISSN: 08937648, 15591182
PubMed ID:
31515692
Neurology
Cellular and Molecular Neuroscience
Neuroscience (miscellaneous)
Abstract
A series of new positive allosteric modulators (PAMs) of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors based on 3,7-diazabicyclo[3.3.1]nonane scaffold have been designed, synthesized, and analyzed. In electrophysiological patch clamp studies, several compounds have demonstrated a sub-nanomolar potency. Compound 4 in in vivo tests showed anti-amnestic properties in the scopolamine-induced model of amnesia in the step-through passive avoidance or maximal electroshock experiments in rats at 0.01 mg/kg showing a significant “dose-response” advantage over memantine. Based on the analysis of the flexible docking results of PAMs, the cyclothiazide-like mechanism of binding mode was suggested as the major site for the interaction with AMPA receptors.
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Total citations:
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Citations from 2025:
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(13.04%)
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GOST
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Lavrov M. I. et al. Novel Positive Allosteric Modulators of AMPA Receptors Based on 3,7-Diazabicyclo[3.3.1]nonane Scaffold // Molecular Neurobiology. 2019. Vol. 57. No. 1. pp. 191-199.
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Lavrov M. I., Karlov D. S., Voronina T. A., Grigoriev V. V., Ustyugov A. A., Bachurin S. O., Palyulin V. A. Novel Positive Allosteric Modulators of AMPA Receptors Based on 3,7-Diazabicyclo[3.3.1]nonane Scaffold // Molecular Neurobiology. 2019. Vol. 57. No. 1. pp. 191-199.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1007/s12035-019-01768-6
UR - https://doi.org/10.1007/s12035-019-01768-6
TI - Novel Positive Allosteric Modulators of AMPA Receptors Based on 3,7-Diazabicyclo[3.3.1]nonane Scaffold
T2 - Molecular Neurobiology
AU - Lavrov, Mstislav I.
AU - Karlov, Dmitry S
AU - Voronina, Tatiana A.
AU - Grigoriev, Vladimir V.
AU - Ustyugov, Aleksey A.
AU - Bachurin, S. O.
AU - Palyulin, V. A.
PY - 2019
DA - 2019/09/12
PB - Springer Nature
SP - 191-199
IS - 1
VL - 57
PMID - 31515692
SN - 0893-7648
SN - 1559-1182
ER -
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BibTex (up to 50 authors)
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@article{2019_Lavrov,
author = {Mstislav I. Lavrov and Dmitry S Karlov and Tatiana A. Voronina and Vladimir V. Grigoriev and Aleksey A. Ustyugov and S. O. Bachurin and V. A. Palyulin},
title = {Novel Positive Allosteric Modulators of AMPA Receptors Based on 3,7-Diazabicyclo[3.3.1]nonane Scaffold},
journal = {Molecular Neurobiology},
year = {2019},
volume = {57},
publisher = {Springer Nature},
month = {sep},
url = {https://doi.org/10.1007/s12035-019-01768-6},
number = {1},
pages = {191--199},
doi = {10.1007/s12035-019-01768-6}
}
Cite this
MLA
Copy
Lavrov, Mstislav I., et al. “Novel Positive Allosteric Modulators of AMPA Receptors Based on 3,7-Diazabicyclo[3.3.1]nonane Scaffold.” Molecular Neurobiology, vol. 57, no. 1, Sep. 2019, pp. 191-199. https://doi.org/10.1007/s12035-019-01768-6.
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