2009 Fiscal Year Final Research Report
Search, asymmetric synthesis, and medicinal chemistry study on the plant alkaloids that regulate the brain nervous system.
| Project/Area Number |
19310137
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Living organism molecular science
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| Research Institution | Chiba University |
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Principal Investigator |
TAKAYAMA Hiromitsu Chiba University, 大学院・薬学研究院, 教授 (90171561)
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| Co-Investigator(Kenkyū-buntansha) |
HORIE Shunji 城西国際大学, 薬学部, 教授 (50209285)
KITAJIMA Mariko 千葉大学, 大学院・薬学研究院, 准教授 (60195261)
KOGURE Noriyuki 千葉大学, 大学院・薬学研究院, 助教 (80396689)
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| Project Period (FY) |
2007 – 2009
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| Keywords | 鎮痛薬 / 脳機能改善薬 / アルカロイド / 成分探索 / 不斉全合成 / 構造活性相関 |
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| Research Abstract |
In order to find new biologically active compounds that act on the brain nervous systems, we have investigated plant alkaloids. As a result, several new alkaloids having opioid agonistic activity or acetylcholine-esterase inhibitory activity were found. Their asymmetric total syntheses were also achieved. Further, based on those natural products, we have developed potent channel blocker on NMDA receptors, which would be a seed molecule for dementia medicine, as well as novel and quite potent opioid agonist, which would be a lead compound for new analgesic.
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[Journal Article] MGM-9 [(E)-Methyl 2-(3-ethyl-7a, 12a-(epoxyethanoxy)-9-fluoro-1,2,3,4,6,7,12,12b-octahydro-8-methoxyindolo [2,3-a] quinolizin-2-yl)-3-methoxyacrylate], a Derivative of the Indole Alkaloid Mitragynine : A Novel Dual-acting μ-and κ-Opioid Agonist with Potent Antinociceptive and Weak Rewarding Effects in Mice2008
Author(s)
K. Matsumoto, H. Takayama, M. Narita, A. Nakamura, M. Suzuki, T. Suzuki, T. Murayama, S. Wongseripipatana, K. Misawa, M. Kitajima, K. Tashima, S. Horie
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Journal Title
Neuropharmacology 55
Pages: 154-165
Peer Reviewed
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