2016 Fiscal Year Final Research Report
Studies on the synthesis of SPECT probe to elucidate the in vivo dynamics of natural opioids
| 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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| Keywords | SPECT / オピオイド / アルカロイド / 全合成 / Mitragyna |
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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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| Free Research Field |
天然物化学
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