Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold
Lavrov M. I., Karlov D. S., Palyulin V. A., Grigoriev V. V., Zamoyski V. L., Brkich G. E`., Pyatigorskaya N. V., Zapolskiy M. E.
Mendeleev Communications
Vol.28, Issue3, P. 311-313
Опубликовано: 2018
Тип ресурса: Статья
DOI:10.1016/j.mencom.2018.05.028
Аннотация:
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). © 2018
Язык текста: Английский
ISSN: 1364-551X
Lavrov M. I.
Karlov D. S.
Palyulin V. A.
Grigoriev V. V.
Zamoyski V. L.
Brkich G. E`. Galina E`duardovna 1967-
Pyatigorskaya N. V. Natal`ya Valeryevna 1965-
Zapolskiy M. E.
Лавров М. И.
Карлов Д. С.
Палюлин В. А.
Григориев В. В.
Замоyски В. Л.
Бркич Г. Э. Галина Эдуардовна 1967-
Пятигорская Н. В. Наталья Валерьевна 1965-
Заполскиy М. Е.
Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold
Текст визуальный непосредственный
Mendeleev Communications
Elsevier Science Publisher B.V.
Vol.28, Issue3 P. 311-313
2018
Статья
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). © 2018