| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2016: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
|
|---|
| Outline of Final Research Achievements |
The aim of this study is to find suitable radioligands for PET studies which are targeted COX-2 in brain. Nimesulide derivatives are selected as a ligand expecting brain uptake.
We synthesized six isomeric methoxy-/iodo- analogs of nimesulide, and evaluated for potential as radioligands for brain COX-2 imaging. All synthesized compounds were shown suitable parameters for favorable brain penetration, and three compounds were found as potent and selective COX-2 inhibitors. Furthermore, three isomeric methoxy analogs of nimesulide have been 14C-radiolabeled. Future studies will aim to develop radiolabeled forms of this nimesulide analog for further in vivo evaluation.
|
