Abstract—This review presents the results of consistent scientific studies of a new class of positive allosteric modulators of AMPA receptors from the class of 3,7-diazabicyclo[3.3.1]nonane derivatives, starting from the theoretical prediction of the structures of the compounds, their synthesis, and study of their effect on the currents of AMPA receptors as evidence of assigning them to the PAM class by studying their activity and effectiveness in behavioral experiments that simulate both various acute impairments of memory and cognitive functions and in chronic experiments that simulate the pathology of Alzheimer’s disease, and by studying their molecular mechanism of interaction with the AMPA receptor using 3D computer modeling, radioligand studies of labeled compound 5 with fractions of synaptic membranes of the hippocampus in order to determine the binding sites of this PAM in the brain of rats. All of the above characterizes new compounds of this class as the most active among known PAMs that have a pronounced cognitive-stimulating effect in both normal animals and in various models of pathological memory disorder, which indicates their great therapeutic potential.

摘要—本综述从化合物结构的理论预测出发，介绍了 3,7-二氮杂双环[3.3.1]壬烷衍生物类新型 AMPA 受体正变构调节剂的一致科学研究结果，它们的合成，并研究它们对 AMPA 受体电流的影响，作为将它们分配到 PAM 类的证据，通过在模拟各种急性记忆和认知功能损伤的行为实验以及模拟记忆和认知功能的慢性实验中研究它们的活性和有效性阿尔茨海默病的病理学，并通过使用 3D 计算机建模研究其与 AMPA 受体相互作用的分子机制，对标记化合物5进行放射性配体研究与海马体突触膜的片段一起，以确定该 PAM 在大鼠大脑中的结合位点。所有上述特征都表明此类新化合物是已知 PAM 中最活跃的，在正常动物和各种病理性记忆障碍模型中具有显着的认知刺激作用，这表明它们具有巨大的治疗潜力。