A Promising Dual-functional Neuroprotective Derivative of Memantine
Journal Title: Journal of Pharmaceutical and Biomedical Sciences - Year 2016, Vol 6, Issue 6
Abstract
Background Memantine, an open-channel, uncompetitive blocker of NMDA receptors, is a major treatment for moderate-to-severe Alzheimer’s disease. The NMDA receptor activity can also be inhibited allosterically by S-nitrosylation of Cys residues, a redox-mediated chemical reaction. Aim To enhance the inhibitory effect of memantine on NMDA receptors and its neuroprotective effect. Settings and Design In this study, we designed and synthesized a memantine nitrate compound (MN-2, also known as YQW-035), with the potential for both allosteric and direct uncompetitive blockade. Then, the protective effects of MN-2 were evaluated both in vitro and in vivo. Results and Conclusions Biological evaluations demonstrated that MN-2 showed a stronger protective effect in cultured neuronal cells and in a rat transient stroke model compared with memantine. The mechanism underlying the action of MN-2 may be attributed to its dual inhibition of NMDA receptors. These results suggested MN-2 has promising potential for treatment of various neurological disorders characterized by overstimulation of NMDA receptors.
Authors and Affiliations
Yewei Sun, Baojian Guo, Zheng Liu, Gaoxiao Zhang, Zaijun Zhang, Lipeng Xu, Yuqiang Wang
Keywords
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