| Project/Area Number |
26670042
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Natural medicines
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| Research Institution | Chiba University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
HORIE SHUNJI 城西国際大学, 薬学部, 教授 (50209285)
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| Project Period (FY) |
2014-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2016: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2015: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2014: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
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| Keywords | SPECT / オピオイド / アルカロイド / 全合成 / Mitragyna / 標識化合物 |
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| Outline of Final Research Achievements |
Based on a natural analgesic indole alkaloid, 7-hydroxymitragynine, we planned the creation of a radioactive iodine-labeled compound that binds to the brain opioid receptor, which will be utilized in SPECT and in vivo imaging studies.
As an iodine-containing derivative for SPECT, compounds having iodine on the acrylate side chain in MGM-15 were synthesized and the agonistic activity was evaluated by in vitro experiment. As a result, it was found that the meta-iodobenzyloxy derivative had the same degree of activity as morphine, and then the activity was evaluated by the Tail flick method in vivo (mouse). But, it did not show effective analgesic activity. Therefore, a novel derivative possessing an iodoalkene at position 20 of MGM-15 was designed. The total synthesis was attempted by two routes. At the present time, asymmetric synthesis of a precursor of the target molecule was completed.
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