Design and synthesis of kainoid-type molecular probes for elucidation of the mechanism of allodynia induction

2014 Fiscal Year Final Research Report

• Project/Area Number: 24310154
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Partial Multi-year Fund
• Section: 一般
• Research Field: Living organism molecular science
• 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)
• Project Period (FY): 2012-04-01 – 2015-03-31
• 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

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.

Free Research Field

生物有機化学