Synthesis of highly selective and potent delta opioid receptor agonists
Project/Area Number |
23790139
|
Research Category |
Grant-in-Aid for Young Scientists (B)
|
Allocation Type | Multi-year Fund |
Research Field |
Drug development chemistry
|
Research Institution | Kitasato University |
Principal Investigator |
NEMOTO TORU 北里大学, 薬学部, 助教 (40458766)
|
Project Period (FY) |
2011 – 2013
|
Project Status |
Completed (Fiscal Year 2013)
|
Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2012: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2011: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
|
Keywords | 医薬品化学 / 医薬分子設計 / オピオイド / δ受容体 / 作動薬 / 生物活性物質 |
Research Abstract |
We investigated the structure activity relationship for the delta opioid agonist KNT-127 which showed high affinity and selectivity for the delta receptor and the potent analgesic effect (s.c.), to obtain more selective and more potent agonists for the delta receptor. The various KNT-127 derivatives were synthesized and evaluated the opioid receptor binding ability and the agonistic activity. As a result, some compounds showed more selective agonistic activity in in vitro for the delta receptor than KNT-127. Especially, the compound with a 17-(3-ethoxypropyl) group showed the best selectivity and potent agonistic activity for the delta receptor.
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Report
(4 results)
Research Products
(25 results)