In vivo evaluation of 11C-labeled 2-arylpropionic acid as a PET probe for COXs in neuroinflammation
| Project/Area Number |
22790517
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Applied pharmacology
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| Research Institution | The Institute of Physical and Chemical Research |
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Principal Investigator |
SHUKURI Miho 独立行政法人理化学研究所, 分子プローブ機能評価研究チーム, 研究員 (20525571)
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| Project Period (FY) |
2010 – 2011
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| Project Status |
Completed (Fiscal Year 2011)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2011: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2010: ¥2,860,000 (Direct Cost: ¥2,200,000、Indirect Cost: ¥660,000)
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| Keywords | シクロオキシゲナーゼ / 非ステロイド性抗炎症薬 / PET / 脳炎症 / ミクログリア / 神経変性疾患 / LPS / アラキドン酸カスケード / 脳内炎症 |
|---|
| Research Abstract |
In order to develop the imaging agent for the in vivo monitoring of COXs activity and/or expression, a series of 2-arylpropionic acid derivatives of NSAIDs were labeled with 11C. Among them, we found that^<11> C-labeled ketoprofen-methyl ester(KTP-Me), its acid form rather specific to COX-1, showed superior sensitivity to inflammation of rat brain. In addition, our results suggest that^<11> C-KTP-Me recognize the changes of COX-1 expression in brain, and provide new evidence for the specific imaging of microglial activation. PET study in monkeys also showed the high accumulation of^<11> C-KTP-Me in neuroinflammatory area. The safety, biodistribution and kinetics of^<11> C-KTP-Me in both rats and monkeys indicate that it should be acceptable for the use of study in human.
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Report
(3 results)
Research Products
(27 results)
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[Presentation] A novel PET probe, 11C-ketoprofen-methyl ester, targeting cyclooxygenase-1 in the brain2011
Author(s)
Miho Shukuri, Misato Takashima-Hirano, Keiko Tokuda, Kiyoshi Matsumura, Miki Goto, Hisashi Doi, Masaaki Suzuki, Yasuyoshi Watanabe & Hirotaka Onoe
Organizer
2011 SNM Annual Meeting
Place of Presentation
San Antonio, Texas
Related Report
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