Positive and negative AMPA receptor modulators based on tricyclic bispidine derivative: Minor structural change inverts the type of activity
Mstislav I. Lavrov
1
,
Polina N Veremeeva
1
,
Elena N Golubeva
1
,
Vladimir L Zamoyski
2
,
Vladimir V. Grigoriev
1, 2
,
Publication type: Journal Article
Publication date: 2022-05-27
scimago Q3
wos Q3
SJR: 0.305
CiteScore: 3.0
Impact factor: 1.7
ISSN: 09599436, 1364551X
General Chemistry
Abstract
Two new potent AMPA receptor allosteric modulators, 6-(1,3-benzodioxol-5-yl)-1,11-dimethyl-3,6,9-triazatri-cyclo[7.3.1.1 3,11 ]tetradecane-4,8,12-trione and -4,8-dione were synthesized from 1,3-benzodioxol-5-amine and the corresponding 3,7-dichloroacetyl-3,7-diazabicyclo[3.3.1]-nonanes. In a wide concentration range (10 −12 –10 −7 m), the 12-oxo derivative acts as a positive modulator causing the potentiation of the kainate-induced AMPA receptor currents with maximum potentiation at 1 nm (62%) while its analogue without a ketone group has significant (up to 40%) negative modulator effect. Their tentative mechanisms of action were analyzed by means of molecular modelling
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12
Total citations:
12
Citations from 2025:
3
(25%)
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Lavrov M. I. et al. Positive and negative AMPA receptor modulators based on tricyclic bispidine derivative: Minor structural change inverts the type of activity // Mendeleev Communications. 2022. Vol. 32. No. 3. pp. 360-363.
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Lavrov M. I., Veremeeva P. N., Golubeva E. N., Radchenko E. V., Zamoyski V. L., Grigoriev V. V., Palyulin V. A. Positive and negative AMPA receptor modulators based on tricyclic bispidine derivative: Minor structural change inverts the type of activity // Mendeleev Communications. 2022. Vol. 32. No. 3. pp. 360-363.
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RIS
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TY - JOUR
DO - 10.1016/j.mencom.2022.05.023
UR - https://doi.org/10.1016/j.mencom.2022.05.023
TI - Positive and negative AMPA receptor modulators based on tricyclic bispidine derivative: Minor structural change inverts the type of activity
T2 - Mendeleev Communications
AU - Lavrov, Mstislav I.
AU - Veremeeva, Polina N
AU - Golubeva, Elena N
AU - Radchenko, Eugene V.
AU - Zamoyski, Vladimir L
AU - Grigoriev, Vladimir V.
AU - Palyulin, V. A.
PY - 2022
DA - 2022/05/27
PB - OOO Zhurnal "Mendeleevskie Soobshcheniya"
SP - 360-363
IS - 3
VL - 32
SN - 0959-9436
SN - 1364-551X
ER -
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BibTex (up to 50 authors)
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@article{2022_Lavrov,
author = {Mstislav I. Lavrov and Polina N Veremeeva and Elena N Golubeva and Eugene V. Radchenko and Vladimir L Zamoyski and Vladimir V. Grigoriev and V. A. Palyulin},
title = {Positive and negative AMPA receptor modulators based on tricyclic bispidine derivative: Minor structural change inverts the type of activity},
journal = {Mendeleev Communications},
year = {2022},
volume = {32},
publisher = {OOO Zhurnal "Mendeleevskie Soobshcheniya"},
month = {may},
url = {https://doi.org/10.1016/j.mencom.2022.05.023},
number = {3},
pages = {360--363},
doi = {10.1016/j.mencom.2022.05.023}
}
Cite this
MLA
Copy
Lavrov, Mstislav I., et al. “Positive and negative AMPA receptor modulators based on tricyclic bispidine derivative: Minor structural change inverts the type of activity.” Mendeleev Communications, vol. 32, no. 3, May. 2022, pp. 360-363. https://doi.org/10.1016/j.mencom.2022.05.023.
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