Development of 11C-Labeled ω-sulfhydryl fatty acid tracer for myocardial imaging with PET

Development of 11C-Labeled ω-sulfhydryl fatty acid tracer for myocardial imaging with PET [11C]-S-methyl-16-thiopalmitic acid (a) was developed with excellent heart-to-background uptake ratios and higher retention in heart. Myocardial uptake and metabolism of the tracer is markedly higher CPT I dependent. When compared to [11C]-S-methyl-14-thiomyristic acid (b), [11C]-S-methyl-12-thiododecanoic acid (c) and [11C]-palmitate, a showed an early high uptake and a significantly slower late clearance in heart and a prolonged myocardial elimination half-life (30 min). Analysis of heart tissue and urine samples showed that a was metabolized via beta-oxidation in myocardium. Small animal PET images of the accumulation of a in the rat myocardium were clearly superior to [11C]-palmitate. These initial studies suggest that a could be a potentially useful clinical PET tracer to assess myocardial fatty acid metabolism. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png European Journal of Medicinal Chemistry Elsevier

Development of 11C-Labeled ω-sulfhydryl fatty acid tracer for myocardial imaging with PET

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Publisher
Elsevier
Copyright
Copyright © 2017 Elsevier Masson SAS
ISSN
0223-5234
eISSN
1768-3254
D.O.I.
10.1016/j.ejmech.2017.10.062
Publisher site
See Article on Publisher Site

Abstract

[11C]-S-methyl-16-thiopalmitic acid (a) was developed with excellent heart-to-background uptake ratios and higher retention in heart. Myocardial uptake and metabolism of the tracer is markedly higher CPT I dependent. When compared to [11C]-S-methyl-14-thiomyristic acid (b), [11C]-S-methyl-12-thiododecanoic acid (c) and [11C]-palmitate, a showed an early high uptake and a significantly slower late clearance in heart and a prolonged myocardial elimination half-life (30 min). Analysis of heart tissue and urine samples showed that a was metabolized via beta-oxidation in myocardium. Small animal PET images of the accumulation of a in the rat myocardium were clearly superior to [11C]-palmitate. These initial studies suggest that a could be a potentially useful clinical PET tracer to assess myocardial fatty acid metabolism.

Journal

European Journal of Medicinal ChemistryElsevier

Published: Jan 1, 2018

References

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