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XB-ART-54675
Bioorg Med Chem 2018 Feb 01;263:603-608. doi: 10.1016/j.bmc.2017.12.021.
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Design, synthesis, and evaluation of polyamine-memantine hybrids as NMDA channel blockers.

Kumamoto T , Nakajima M , Uga R , Ihayazaka N , Kashihara H , Katakawa K , Ishikawa T , Saiki R , Nishimura K , Igarashi K .


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N-Methyl-d-aspartate (NMDA) receptors have been implicated in learning and memory, and may also play a central role in various conditions leading to neuronal degradation. NMDA receptor antagonists could therefore be of therapeutic benefit for a number of neurological disorders. We have designed hybrid compounds of polyamines and memantine, both of which function as NMDA channel blockers. The triamine derivative with a guanidine moiety showed more potent antagonistic activity than memantine.

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