| Synthesis and evaluation of 15-(4-(2-[¹⁸F]Fluoroethoxy)phenyl)pentadecanoic acid: a potential PET tracer for studying myocardial fatty acid metabolism. | |
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MedLine Citation:
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PMID: 21070001 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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15-(4-(2-[¹⁸F]fluoroethoxy)phenyl)pentadecanoic acid ([¹⁸F]7) was synthesized as a PET probe for assessing myocardial fatty acid metabolism. The radiosynthesis of [¹⁸F]7 was accomplished using a two-step reaction, starting with the corresponding tosylate ester, methyl 15-(4-(2-(tosyloxy)ethoxy)phenyl)pentadecanoate (5), and gave the radiolabeled fatty acid, [¹⁸F]7 in a radiolabeling yield of 55-60% and a specific activity of >2000 Ci/mmol (decay corrected to EOB). The biological evaluation of [¹⁸F]7 in rats displayed high uptake in heart (1.94%ID/g at 5 min), which was higher than the uptake (%ID/g) in blood, lung, muscle, pancreas, and brain. MicroPET studies of [¹⁸F]7 in Sprague-Dawley rats demonstrated excellent images of the myocardium when compared with [¹¹C]palmitate images in the same animal. Moreover, the tracer kinetics of [¹⁸F]7 paralleled those seen with [¹¹C]palmitate, with an early peak followed by biphasic washout. When compared to [¹¹C]palmitate, [¹⁸F]7 exhibited a slower early clearance (0.17 ± 0.01 vs 0.30 ± 0.02, P < 0.0001) and a significantly higher late clearance (0.0030 ± 0.0005 vs 0.0006 ± 0.00013, P < 0.01). These initial studies suggest that [¹⁸F]7 could be a potentially useful clinical PET tracer to assess abnormal myocardial fatty acid metabolism. |
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Authors:
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Zhude Tu; Shihong Li; Terry L Sharp; Pilar Herrero; Carmen S Dence; Robert J Gropler; Robert H Mach |
Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural Date: 2010-11-11 |
Journal Detail:
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Title: Bioconjugate chemistry Volume: 21 ISSN: 1520-4812 ISO Abbreviation: Bioconjug. Chem. Publication Date: 2010 Dec |
Date Detail:
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Created Date: 2011-04-12 Completed Date: 2011-08-04 Revised Date: 2012-02-03 |
Medline Journal Info:
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Nlm Unique ID: 9010319 Medline TA: Bioconjug Chem Country: United States |
Other Details:
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Languages: eng Pagination: 2313-9 Citation Subset: IM |
Affiliation:
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Division of Radiological Sciences, Washington University School of Medicine, St. Louis, Missouri 63110, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Carbon Isotopes / chemistry, metabolism Ethyl Ethers / chemistry, metabolism Fatty Acids / chemistry, metabolism*, pharmacokinetics Fluorine Radioisotopes / chemistry, pharmacokinetics* Isotope Labeling / methods Lipid Metabolism Male Myocardium / metabolism* Organ Specificity Palmitic Acid / chemistry, metabolism Positron-Emission Tomography / methods* Radiopharmaceuticals / chemical synthesis, pharmacokinetics* Rats Rats, Sprague-Dawley Tissue Distribution |
| Grant Support | |
ID/Acronym/Agency:
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HL69100/HL/NHLBI NIH HHS; P30 DK056341-10/DK/NIDDK NIH HHS; R01 HL069100-05/HL/NHLBI NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Carbon Isotopes; 0/Ethyl Ethers; 0/Fatty Acids; 0/Fluorine Radioisotopes; 0/Radiopharmaceuticals; 0/pentadecanoic acid; 57-10-3/Palmitic Acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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