| Project/Area Number |
15500278
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Neurochemistry/Neuropharmacology
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| Research Institution | National Institute of Advanced Industrial Science and Technology |
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Principal Investigator |
SHIGERI Yasushi National Institute of Advanced Industrial Science and Technology, Research institute for cell engineering, Senior Researcher, セルエンジニアリング研究部門, 主任研究員 (90357187)
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| Co-Investigator(Kenkyū-buntansha) |
SHIMAMOTO Keiko Suntory, Institute for Bioorganic Research, Senior Researcher, 主任研究員 (70235638)
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| Project Period (FY) |
2003 – 2005
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| Project Status |
Completed (Fiscal Year 2005)
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| Budget Amount *help |
¥3,600,000 (Direct Cost: ¥3,600,000)
Fiscal Year 2005: ¥700,000 (Direct Cost: ¥700,000)
Fiscal Year 2004: ¥1,400,000 (Direct Cost: ¥1,400,000)
Fiscal Year 2003: ¥1,500,000 (Direct Cost: ¥1,500,000)
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| Keywords | glutamic acid / glutamate transporter / blocker / EAATs / DL-TBOA / TFB-TBOA / neutral amino acid / ASCT / グルタミン酸トランスポータ / グルタミン酸トランスポーター / 海綿抽出物ライブラリー / アミノ酸アナログライブラリー |
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| Research Abstract |
L-Glutamate is the major excitatory neurotransmitter. Termination of glutamate function is mainly achieved by glutamate transporters (EAATs1-5). To identify the physiological roles of EAATs, selective inhibitors are strongly required. We developed the binding assay system to characterize inhibitors for all subtypes of EAATs. We synthesized a tritium derivative of (2S,3S)-3-{3-[4-ethylbenzoylamino]benzyloxy}aspartate ([^3H]ETB-TBOA). As expected, [^3H]ETB-TBOA showed significant specific binding to EAATs. The binding was Na^+-dependent and was displaced by known substrates and blockers. The rank order of the inhibition by these compounds was well consistent with the reported results in the uptake assay. Thus, the binding assay using [^3H]ETB-TBOA would be useful to screening novel inhibitors for all subtypes of EAATs.
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