| Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2011: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2010: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2009: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
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| Research Abstract |
Development of novel ligands, that specifically interact with receptors located at synapses of mammalian nervous system, is important to understand and control complex brain functions at a molecular level. We had synthetically developed IKM-159 as a specific AMPA receptor antagonist, and in the present study, the structure-activity relationships have been extensively studied. As a result, we found that(2R)-IKM159 is neuronally active, whereas the(2S)-isomer is inactive. Furthermore, the interactions with GluA2 subunit have been clarified by X-ray crystallography of(2R)-IKM159 in complex with GluA2 dimer.
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