Bivalent AMPA receptor positive allosteric modulators of the bis(pyrimidine) series

Bivalent AMPA receptor positive allosteric modulators of the bis(pyrimidine) series

The first example of a novel class of AMPA receptor positive allosteric modulators of the bis(pyrimidine) series having a hydroquinone linker has been obtained and showed a potency to increase kainate-induced currents at subnanomolar concentrations. Bis(tetrahydroquinazolines) potentiate kainate-ind...

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Veröffentlicht in:MedChemComm 2019-09, Vol.1 (9), p.1615-1619
Hauptverfasser: Nazarova, Anna A, Sedenkova, Kseniya N, Karlov, Dmitry S, Lavrov, Mstislav I, Grishin, Yuri K, Kuznetsova, Tamara S, Zamoyski, Vladimir L, Grigoriev, Vladimir V, Averina, Elena B, Palyulin, Vladimir A
Format: Artikel
Sprache:eng
Schlagworte:
Allosteric properties
Chemistry
Docking
Hydroquinone
Modulators
NMR
Nuclear magnetic resonance
α-Amino-3-hydroxy-5-methyl-4-isoxazole propionic acid
α-Amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptors
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Beschreibung
Zusammenfassung:The first example of a novel class of AMPA receptor positive allosteric modulators of the bis(pyrimidine) series having a hydroquinone linker has been obtained and showed a potency to increase kainate-induced currents at subnanomolar concentrations. Bis(tetrahydroquinazolines) potentiate kainate-induced currents at 10 −12 -10 −8 M.
ISSN:2040-2503
2040-2511
2040-2511
DOI:10.1039/c9md00262f