| Evaluation of (4-[(18)F]Fluorophenyl)triphenylphosphonium Ion. A Potential Myocardial Blood Flow Agent for PET. | |
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MedLine Citation:
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PMID: 20563755 Owner: NLM Status: In-Data-Review |
Abstract/OtherAbstract:
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PURPOSE: The lipophilic cationic compound, (4-[(18)F]fluorophenyl)triphenylphosphonium ion ((18)F-FTPP) was synthesized and evaluated as a potential positron emission tomography (PET) myocardial perfusion agent. PROCEDURE: (18)F-FTPP was prepared from (4-nitrophenyl)triphenylphosphonium nitrate and ammonium [(18)F]fluoride by nucleophilic aromatic substitution and was purified by high performance liquid chromatography before use. Biodistribution studies were performed in rats at 5, 30, 60 min (five rats per time point). Three rats were evaluated by microPET imaging after injection of (18)F-FTPP. In addition, microPET imaging in rabbits (three) was performed before and after occlusion of the left anterior descending (LAD) artery with (13)NH(3) (111 MBq) and (18)F-FTPP (74 MBq). RESULTS: Biodistribution data in rats showed rapid blood clearance and high levels of accumulation in the heart; 75:1 heart-to-blood ratio at 30 min. Uptake of radioactivity in the heart was 1.64% ID/G, 1.51% ID/g, and 1.57% ID/g at 5, 30, and 60 min. At 5, 30, and 60 min, lung activity was 0.69% ID/g, 0.03% ID/g, and 0.38% ID/g, and liver uptake was 0.34% ID/g, 0.18% ID/g, and 0.17% ID/g. Heart-to-lung ratios at 5, 30, and 60 min were 2, 5, and 4. Bone accumulation was minimal. MicroPET imaging in both rats and rabbits after injection of (18)F-FTPP demonstrated an initial spike of activity in the myocardium corresponding to blood flow followed by a plateau after 1 min. Region of interest analysis of microPET images of normal and LAD-occluded rabbits with (13)NH(3) and (18)F-FTPP indicated similar distributions of the two tracers in both normal and altered blood flow regions. CONCLUSION: The excellent heart-to-blood ratio of (18)F-FTPP and its correlation with (13)NH(3) distribution in normal and LAD-occluded rabbits suggest that this radiopharmaceutical may have potential as a PET agent for characterizing mitochondrial damage and/or myocardial blood flow. |
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Authors:
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Timothy M Shoup; David R Elmaleh; Anna-Liisa Brownell; Aijun Zhu; J Luis Guerrero; Alan J Fischman |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging Volume: 13 ISSN: 1860-2002 ISO Abbreviation: Mol Imaging Biol Publication Date: 2011 Jun |
Date Detail:
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Created Date: 2011-05-05 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101125610 Medline TA: Mol Imaging Biol Country: United States |
Other Details:
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Languages: eng Pagination: 511-7 Citation Subset: IM |
Affiliation:
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Department of Radiology, Massachusetts General Hospital, Edwards Building B015, 55 Fruit Street, Boston, MA, 02114, USA, tshoup@partners.org. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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