| Project/Area Number |
23590133
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Kitasato University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
NAGASE Hiroshi 筑波大学, 国際統合睡眠医科学研究機構, 教授 (70383651)
UEZONO Yasuhito 独立行政法人国立がん研究センター, 研究所, 部長 (20213340)
HIRAYAMA Shigeto 北里大学, 薬学部, 助教 (40565842)
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| Project Period (FY) |
2011 – 2013
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| Project Status |
Completed (Fiscal Year 2013)
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| Budget Amount *help |
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2013: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2012: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2011: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Keywords | 医薬分子設計 / 受容体ダイマー / オピオイド / κ作動薬 / ファーマコフォー |
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| Research Abstract |
On the basis of our 3D pharmacophore model of kappa agonists, compounds belonging to the binding mode 1, 3, or 4 were synthesized and their binding affinities and agonistic activities for the opioid receptors were evaluated. The test compounds showed selective binding abilities and agonistic activities for the kappa receptor although the strengths of bindings and activities depended on the structures. The binding modes of the compounds were not observed to affect the impedance patterns detected by CellKey SystemTM which was used in the functional assays.
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