Development of automatic synthesis of an androgen receptor imaging tracer for positron emission tomography
| Project/Area Number |
22791182
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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 |
Radiation science
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| Research Institution | University of Fukui |
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Principal Investigator |
MORI Tetsuya 福井大学, 高エネルギー医学研究センター, 助教 (40397287)
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| Research Collaborator |
KIYONO Yasushi 福井大学, 高エネルギー医学研究センター, 教授 (50305603)
OKAZAWA Hidehiko 福井大学, 高エネルギー医学研究センター, 教授 (50360813)
FUJIBAYASHI Yasuhisa 放射線医学総合研究所, 分子イメージング研究センター, センター長 (50165411)
WELCH M. J. Washington University in St. Louis, Department of Biomedical Engineering, Professor
KATZENELLENBOG J. A. University of Illinois, Department of Chemistry, Professor
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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 |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2011: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2010: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | 放射性診断薬 / PET / 薬剤開発 / アンドロゲンレセプター / 薬学 / PET薬剤 / 画像診断 / 前立腺がん |
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| Research Abstract |
Androgen receptor(AR) expression is an important factor to predict tumor responsiveness to hormonal therapy in prostate cancer. 16β-[^<18> F] fluoro-5α-dihydrotestosterone([^<18> F] FDHT) is a candidate for AR imaging PET radiopharmaceutical, however, the reported method was difficult to adopt an automatic modules because of the complex reaction conditions. In this study, we developed an automatic synthesis method for[^<18> F] FDHT using a plastic cassette-type automatic PET radiopharmaceutical synthesizer. We chose a TRACERlab MXFDG(GE) as the module for[^<18> F] FDHT synthesis because it has the flexibility programming and accepts modification to the cassette layout in aseptic condition. Optimum labeling condition was investigated by changing several factors(amount of precursor and NaBH_4, temperature and time of labeling, reduction and hydrolysis etc.) and the optimized condition is as follows : 1, 2 or 4 mg of 16τ-[[(trifluoromethyl) sulfonyl] oxy]-3, 3-(ethylenedioxy) and rostan-1
… More
7-one in abs. acetonitrile was heated at 125℃for 10 min with dried[^<18> F] fluoride. The resultant solution was evaporated, and then reduced with NaBH_4 in ethanol at room temperature. The hydrolysis with 0. 1N HCl was carried out for 15 min. Then the preparative HPLC was performed using a Cosmosil 5C_<18>-AR-2, 20 mmI. D. x 250 mm, Nacalai Tesque, 50% acetonitrile/water, 8. 0 ml/min, 210 nm) was performed. The desired radioactive fraction was collected to a round-bottom flask containing sodium ascorbate as a radical scavenger. The solvent was removed in vacuo and the residue was dissolved in 10 ml of saline, and then passed through a sterile 0. 22μm filter to a pyrogen-free vial. The reduction using NaBH_4 was completed in 5 min. The hydrolysis was inadequacy at RT in 15 min but it was accomplished at 85℃. The radiochemical yield in the final product was 13. 4±4. 4%(n 7). The total synthesis time including the preparative HPLC and the preparation process for an injection was less than 100 min. The quality control including acute toxicity test using mouse was confirmed that the final product was high quality and adapted for clinical research. Less
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Report
(3 results)
Research Products
(3 results)
