Clarification of the optimal orientation and length of the side chain in opioid kappa receptor ligands and its application
| Project/Area Number |
26860076
|
|---|
| Research Category |
Grant-in-Aid for Young Scientists (B)
|
| Allocation Type | Multi-year Fund |
|---|
| Research Field |
Drug development chemistry
|
|---|
| Research Institution | University of Tsukuba |
|---|
Principal Investigator |
YAMAMOTO Naoshi 筑波大学, 国際統合睡眠医科学研究機構, 助教 (80580216)
|
|---|
| Project Period (FY) |
2014-04-01 – 2017-03-31
|
| Project Status |
Completed (Fiscal Year 2016)
|
| Budget Amount *help |
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2016: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2015: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2014: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
|
|---|
| Keywords | κ受容体作動薬 / オピオイド / モルヒナン |
|---|
| 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.
|
Report
(4 results)
Research Products
(11 results)
