| Project/Area Number |
17591309
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Radiation science
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| Research Institution | National Institute of Radiological Sciences (2006)
Research institute for Brain and Blood Vesseis Akita (2005) |
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Principal Investigator |
TAKAHASHI Kazuhiro National Institute of Radiological Sciences, Molecular Imaging Center, Senior Researcher, 分子イメージング研究センター, 主任研究員 (20370257)
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| Project Period (FY) |
2005 – 2006
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| Project Status |
Completed (Fiscal Year 2006)
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| Budget Amount *help |
¥1,900,000 (Direct Cost: ¥1,900,000)
Fiscal Year 2006: ¥700,000 (Direct Cost: ¥700,000)
Fiscal Year 2005: ¥1,200,000 (Direct Cost: ¥1,200,000)
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| Keywords | bio-molecule / cancer / radiology / molecular Probe / radio-labeling / apoptosis / PET / molecular imaging / 脳・神経 |
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| Research Abstract |
For studying intracellular apoptotic system in the human brain, It is well known that Bcl-xL plays an important role in apoptosis signal cascade. BH3I-2' was reported to be a Bcl-xL inhibitor, which bound to BH3 domain in Bcl-xL. We attempted to synthesize [18F]FBH3I-2' with expectation that it could be used for measuring Bcl-xL in the living tissue by PET. We carried out the labeling of [18F]FBH3I-2' and a preliminary study of biodistribution in rats.
Fluorination of the trimethylammonium sault of BH3I-2' with [18F]trtrabutylammonium fluoride (TBAF). was carried out in DMSO at 130°C for 10 min. The product was purified using a preparative reversed phase HPLC system After evaporation of solvent, the residue was dissolve saline and filtered through a 0.22 □m sterile filter. The radiochemical yield was 50 % based on [18F] TBAF and the radiochemical purity was better than 99 % The over all time of synthesis including purification and sterilization was 60 min after EOB.
Tissue distribution of [18F]FBH3I-2' was studied in 4 male Sprague-Dawley rats. Liver and kidney show high uptakes of [18F]FBH3I-2', which should mean fast metabolism and fast excretion of this tracer. Brain uptake was much lower than that in blood. Tissue distribution of [18F]FBH3I-2' was also studied in tumor bearing mice dynamically with Positron planer imaging system (Hamamatsu Photonics). The uptake in tumor region was increasingly higher with time after injection. These results suggest that [18F]FBH3I-2'could not suitale for imaging Bcl-xL It is expected that more permiable derivatives of [18F]FBH3I-2' would be useful for imaging Bcl-xL in the living tissues with PET.
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