Design and synthesis of kainoid-type molecular probes for elucidation of the mechanism of allodynia induction
Project/Area Number |
24310154
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Research Category |
Grant-in-Aid for Scientific Research (B)
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Allocation Type | Partial Multi-year Fund |
Section | 一般 |
Research Field |
Living organism molecular science
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Research Institution | Gifu University |
Principal Investigator |
FURUTA Kyoji 岐阜大学, 医学(系)研究科(研究院), 准教授 (40173538)
|
Co-Investigator(Renkei-kenkyūsha) |
MINAMI Toshiaki 大阪医科大学, 医学研究科, 教授 (00257841)
DOI Hisashi 理化学研究所, ライフサイエンス技術基盤研究センター, チームリーダー (00421818)
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Project Period (FY) |
2012-04-01 – 2015-03-31
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Project Status |
Completed (Fiscal Year 2014)
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Budget Amount *help |
¥19,500,000 (Direct Cost: ¥15,000,000、Indirect Cost: ¥4,500,000)
Fiscal Year 2014: ¥6,110,000 (Direct Cost: ¥4,700,000、Indirect Cost: ¥1,410,000)
Fiscal Year 2013: ¥6,110,000 (Direct Cost: ¥4,700,000、Indirect Cost: ¥1,410,000)
Fiscal Year 2012: ¥7,280,000 (Direct Cost: ¥5,600,000、Indirect Cost: ¥1,680,000)
|
Keywords | アロディニア / 神経障害性疼痛 / アクロメリン酸 / カイノイド / 分子プローブ / グルタミン酸受容体 / 受容体 / カイニン酸 |
Outline of Final Research Achievements |
Several kainoid-type analogs were designed and synthesized for the purpose of identifying a novel receptor involved in the induction and maintenance of allodynia, a major symptom of neuropathic pain. Efficient synthetic methods to selectively modify the individual substituents attached to the pyrrolidine-ring skeleton of kainoids were established, making it possible to easily prepare kainoid analogs with a variety of substituents. Evaluation of the synthetic kainoids for allodynia-inducing/suppressing activity and binding affinity for glutamate receptors specified some promising analogs as biochemical tools. The existence of a novel activation mechanism of kainate receptor was also suggested.
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Report
(4 results)
Research Products
(2 results)
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[Journal Article] The action site of the synthetic kainoid (2S,3R,4R)-3-carboxymethyl-4-(4-methylp henylthio) pyrrolidine-2-carboxylic acid (PSPA-4), an analogue of Japanese mushroom poison acromelic acid, for allodynia (tactile pain)2012
Author(s)
Miyazaki S, Minami T, Mizuma H, Kanazawa, M, Doi H, Matsumura S, Lu J, Onoe H, Furuta K, Suzuki M and Ito S
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Journal Title
Eur J Pharmacol
Volume: (in press)
Issue: 1-3
Pages: 120-127
DOI
Related Report
Peer Reviewed
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