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Design,synthesis, and evaluation of polyamine-memantine hybrids as NMDA channel blockers |
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| Authors: | Takuya Kumamoto Marie Nakajima Reina Uga Naoko Ihayazaka Haruna Kashihara Kazuaki Katakawa Tsutomu Ishikawa Ryotaro Saiki Kazuhiro Nishimura Kazuei Igarashi |
| Affiliation: | 1. Graduate School of Biomedical & Health Sciences, Hiroshima University, 1-2-3 Kasumi, Minami-ku, Hiroshima 732-8553, Japan;2. Research Institute of Pharmaceutical Sciences, Musashino University, 1-1-20 Shinmachi, Nishitokyo 202-8585, Japan;3. Graduate School of Pharmaceutical Sciences, Chiba University, 1-8-1 Inohana, Chuo-ku, Chiba 260-8675, Japan;4. Amine Pharma Research Institute, Innovation Plaza at Chiba University, 1-8-15 Inohana, Chuo-ku, Chiba 260-8675, Japan |
| Abstract: | 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. |
| Keywords: | Polyamine NMDA channel blocker Alzheimer’s disease Memantine Guanidine |
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