| 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)
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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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