Document Detail


Synthesis and evaluation of 15-(4-(2-[¹⁸F]Fluoroethoxy)phenyl)pentadecanoic acid: a potential PET tracer for studying myocardial fatty acid metabolism.
MedLine Citation:
PMID:  21070001     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Zhude Tu; Shihong Li; Terry L Sharp; Pilar Herrero; Carmen S Dence; Robert J Gropler; Robert H Mach
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural     Date:  2010-11-11
Journal Detail:
Title:  Bioconjugate chemistry     Volume:  21     ISSN:  1520-4812     ISO Abbreviation:  Bioconjug. Chem.     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2011-04-12     Completed Date:  2011-08-04     Revised Date:  2014-09-08    
Medline Journal Info:
Nlm Unique ID:  9010319     Medline TA:  Bioconjug Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2313-9     Citation Subset:  IM    
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Descriptor/Qualifier:
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:
HL69100/HL/NHLBI NIH HHS; P30 DK056341/DK/NIDDK NIH HHS; P30 DK056341-10/DK/NIDDK NIH HHS; R01 HL069100-05/HL/NHLBI NIH HHS
Chemical
Reg. No./Substance:
0/Carbon Isotopes; 0/Ethyl Ethers; 0/Fatty Acids; 0/Fluorine Radioisotopes; 0/Radiopharmaceuticals; 2V16EO95H1/Palmitic Acid; CCW02D961F/pentadecanoic acid
Comments/Corrections

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


Previous Document:  Radiosynthesis and Biodistribution of a Prosthetic Group ((18)F-FENMA) Conjugated to Cyclic RGD Pept...
Next Document:  Synthesis of Triple-Stranded Complexes Using Bis(dipyrromethene) Ligands.