Document Detail


Structure dependence of long-chain [18F]fluorothia fatty acids as myocardial fatty acid oxidation probes.
MedLine Citation:
PMID:  23153307     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In vivo imaging of regional fatty acid oxidation (FAO) rates would have considerable potential for evaluation of mammalian diseases. We have synthesized and evaluated 18F-labeled thia fatty acid analogues as metabolically trapped FAO probes to understand the effect of chain length, degree of unsaturation, and placement of the thia substituent on myocardial uptake and retention. 18-[18F]Fluoro-4-thia-(9Z)-octadec-9-enoic acid (3) showed excellent heart/background radioactivity concentration ratios along with highest retention in heart and liver. Pretreatment of rats with the CPT-1 inhibitor, POCA, caused >80% reduction in myocardial uptake of 16-[18F]fluoro-4-thiahexadecanoic acid (2) and 3, indicating high specificity for FAO. In contrast, 18-[18F]fluoro-4-thiaoctadecanoic acid (4) showed dramatically reduced myocardial uptake and blunted response to POCA. 18-[18F]Fluoro-6-thiaoctadecanoic acid (5) showed moderate myocardial uptake and no sensitivity of myocardial uptake to POCA. The results demonstrate relationships between structures of 18F-labeled thia fatty acid and uptake and their utility as FAO probes in various tissues.
Authors:
Mukesh K Pandey; Anthony P Belanger; Shuyan Wang; Timothy R DeGrado
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2012-11-27
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  55     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2012 Dec 
Date Detail:
Created Date:  2012-12-13     Completed Date:  2013-02-26     Revised Date:  2013-07-11    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  10674-84     Citation Subset:  IM    
Affiliation:
Department of Radiology, Mayo Clinic, 200 First Street SW, Rochester, Minnesota 55905, United States.
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MeSH Terms
Descriptor/Qualifier:
Animals
Fatty Acids / chemistry,  metabolism*
Fluorine Radioisotopes / chemistry*
Molecular Probes*
Molecular Structure
Oxidation-Reduction
Positron-Emission Tomography
Rats
Rats, Sprague-Dawley
Grant Support
ID/Acronym/Agency:
R01 CA108620/CA/NCI NIH HHS; R01 CA108620/CA/NCI NIH HHS; R01 HL-63371/HL/NHLBI NIH HHS; R01 HL063371/HL/NHLBI NIH HHS
Chemical
Reg. No./Substance:
0/Fatty Acids; 0/Fluorine Radioisotopes; 0/Molecular Probes
Comments/Corrections

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