新型认知增强剂DM232 (Unifiram)和DM235 (Sunifiram)的药理特性

M. N. Romanelli, N. Galeotti, C. Ghelardini, D. Manetti, E. Martini, F. Gualtieri
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引用次数: 17

摘要

DM232 (unifiram)和DM235 (sunfiram)是有效的认知增强剂,其效力比吡拉西坦强4个数量级。这些化合物,虽然在结合研究中没有显示出对最重要的中枢受体或通道的亲和力,但能够防止由几种神经传递系统的调节引起的健忘症。这些化合物能够增加大鼠大脑皮层乙酰胆碱的释放,并且就unifiram而言,可以增加大鼠海马切片中fEPSP的振幅。在海马体切片上进行的体外实验也支持AMPA受体在unifiram和sununifiram的认知增强特性中发挥作用的假设。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Pharmacological Characterization of DM232 (Unifiram) and DM235 (Sunifiram), New Potent Cognition Enhancers

DM232 (unifiram) and DM235 (sunifiram) are potent cognition-enhancers, which are four order of magnitude more potent than piracetam. These compounds, although not showing affinity in binding studies for the most important central receptors or channels, are able to prevent amnesia induced by modulation of several neurotransmission systems. These compounds are able to increase the release of acetylcholine from rat cerebral cortex, and, as far as unifiram is concerned, to increase the amplitude of fEPSP in rat hippocampal slices. In vitro experiments, performed on hippocampal slices, also supported the hypothesis of a role of the AMPA receptors for the cognition-enhancing properties of unifiram and sunifiram.

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