2010 Fiscal Year Final Research Report
Development of Novel Ligands for Glutamate Receptors Using Natural Neurotoxins as the Structural Motif
| Project/Area Number |
19201045
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| Research Category |
Grant-in-Aid for Scientific Research (A)
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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 | Osaka City University |
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Principal Investigator |
OHFUNE Yasufumi Osaka City University, 大学院・理学研究科, 教授 (20142078)
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| Co-Investigator(Kenkyū-buntansha) |
SHINADA Tetsuro 大阪市立大学, 大学院・理学研究科, 教授 (30271513)
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| Project Period (FY) |
2008 – 2010
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| Keywords | グルタミン酸受容体 / カイトセファリン / アンタゴニスト / 全合成 / 構造活性相関 / エステル交換反応 / α,β-デヒドロアミノ酸 / カイニン酸 |
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| Research Abstract |
Kaitocephalin has attracted much attention due to its potent antagonist activity to glutamate receptors in mammalian CNS, and is expected to be a potent candidate as a tool to investigate the function of glutamate receptors as well as a leadto develop neuroprotecting agent. In this study, we have achieved the highly efficient total synthesis of kaitocephalin which was accompanied by the development of new synthetic methods. We also performed the synthesis of its derivatives, structurally simplifiedanalogs, and other neuroactive amino acids, whose SAR studies revealed that kaitocephalin and some of its derivatives exhibited potent binding activities to NMDA receptors.
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