Basic investigation on radionuclide therapy with auger electron by using Br-77 labeled MBBG
Project/Area Number |
23791464
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Research Category |
Grant-in-Aid for Young Scientists (B)
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Allocation Type | Multi-year Fund |
Research Field |
Radiation science
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Research Institution | Japan Atomic Energy Agency |
Principal Investigator |
WATANABE Shigeki 独立行政法人日本原子力研究開発機構, 量子ビーム応用研究部門, 研究員 (10450305)
|
Co-Investigator(Renkei-kenkyūsha) |
HANAOKA Hirofumi 千葉大学, 大学院・薬学研究府, 助教 (50361390)
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Project Period (FY) |
2011 – 2012
|
Project Status |
Completed (Fiscal Year 2012)
|
Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2012: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
Fiscal Year 2011: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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Keywords | 核医学(PET を含む) / Br-77 / オージェ電子 / 内用放射線治療 / 褐色細胞腫 / RI内用療法 |
Research Abstract |
β-emitting radiopharmaceutical, I-131 labeled m-iodobenzylguanidine (I-131 MIBG) has been used for radionuclide therapy of malignant pheochromocytoma. Therapeutic effect of this approach is however less than expected. As auger electron possesses higher toxicity against tumor cells than β-emitting radionuclide therapy, we challenged to reveal efficacy of auger electron by using auger emitting radionuclide Br-77 labeled m-bromobenzylguanidne. First of all, we tried to prepare Br-77 labeled MBBG via boron-bromine exchange reaction which is expected to obtain enough amount of radioactivity to radionuclide therapy. Although desired boronate compound, 3-Pinacolateboryl-benzyl(N,N’,N’’-triBoc)guanidine, was synthesized, following radiobromination was not proceeded at all. We then successfully synthesized Br-77 labeled MBBG by iodine-bromine exchange reaction which is conventional route of MBBG synthesis. We conducted cellular uptake studies, and the results showed that MBBG was taken up into PC-12 cells at 3 hours after incubation. However, we don’t revealed localization of Br-77 MBBG in PC-12 cells.
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Report
(3 results)
Research Products
(6 results)