2013 Fiscal Year Final Research Report
Synthesis of highly selective and potent delta opioid receptor agonists
| Project/Area Number |
23790139
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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 | Kitasato University |
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Principal Investigator |
NEMOTO TORU 北里大学, 薬学部, 助教 (40458766)
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| Project Period (FY) |
2011 – 2013
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| Keywords | 医薬品化学 |
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| 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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