2016 Fiscal Year Final Research Report
Clarification of the optimal orientation and length of the side chain in opioid kappa receptor ligands and its application
| Project/Area Number |
26860076
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | University of Tsukuba |
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Principal Investigator |
YAMAMOTO Naoshi 筑波大学, 国際統合睡眠医科学研究機構, 助教 (80580216)
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| Project Period (FY) |
2014-04-01 – 2017-03-31
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| Keywords | κ受容体作動薬 |
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| Outline of Final Research Achievements |
The synthetic route for the 4,5-epoxymorphinan derivatives with a bicycle[2.2.2]octane skeleton from naltrexone hydrochloride was established. The F-ring contained 4,5-epoxymorphinan derivatives with the side chain characterized by an orientation and a length were prepared and assayed for the affinity for opioid receptors. As a result, the derivative with a benzyl amide side chain oriented in the same plane of the F-ring showed potent activity and high selectivity for opioid kappa receptor.
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| Free Research Field |
創薬化学
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