| Budget Amount *help |
¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2014: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2013: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2012: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Outline of Final Research Achievements |
The aim of this study was to develop a PET probe for measuring the activity of multidrug resistance-associated protein 4 (MRP4) in the brain. Several hippuric acid ester derivatives labeled with C-11 were synthesized and benzyl hippurate labeled with C-11 showed favorable hydrolysis rate and uptake properties in the brain of mice. Further evaluation using transporter knockout mice revealed that this compound was specifically hydrolyzed to form hippuric acid labeled with C-11 in vivo after the intravenous administration and the radioactive metabolite was retained in the brain and heart of Oat3 knockout mice and Mrp4 knockout mice, respectively, compared with control mice. Therefore, benzyl hippurate labeled with C-11 could be used as a probe for measuring the activities of OAT3 and MRP4 in mouse brain and heart, respectively.
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