Development of selective modulators for synaptic receptors in the central nervous system

2016 Fiscal Year Final Research Report

• Project/Area Number: 26282216
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Partial Multi-year Fund
• Section: 一般
• Research Field: Chemical biology
• Research Institution: Yokohama City University
• Principal Investigator: Oikawa Masato 横浜市立大学, 生命ナノシステム科学研究科, 教授 (70273571)
• Co-Investigator(Kenkyū-buntansha): 酒井 隆一 北海道大学, 水産科学研究科(研究院), 教授 (20265721)
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: AMPA型受容体 / 多様性指向型有機合成 / モジュレーター / 神経科学 / 作用標的

Outline of Final Research Achievements

Ionotropic glutamate receptors (iGluR) play a central role in the excitatory neurotransmission in the central nervous system. In the present study, we have studied synthesis and evaluation of the inhibitory nature of the analogs of our original ligand IKM-159, to develop novel compound that would be used for therapeutic treatment of neuronal disorders.
We first developed synthetic route for diverse analogs of IKM-159, and we identified IKM-154 acts as an excitatory agent in vivo. Like the inhibitory IKM-159, the excitatory IKM-154 is supposed to be also a ligand for AMPA receptor which is one of the subtype protein of iGluR. With IKM-154 and IKM-159 in hand, it is now possible to explore the detailed biological function and the macinery of AMPA receptor, by selective activation and inactivation.

Free Research Field

ケミカルバイオロジー