Synthesis and biodistribution studies of 99m Tc labeled fatty acid derivatives prepared via "Click approach" for potential use in cardiac imaging

Journal of Labelled Compounds & Radiopharmaceuticals
Soumen DasAshutosh Dash

Abstract

123 I-Iodophenylpentadecanoic acid (IPPA) is a metabolic agent used in nuclear medicine for diagnosis of myocardial defects. Efforts are underway worldwide to develop a 99m Tc substitute of the above radiopharmaceutical for the aforementioned application. Herein, we report synthesis and biodistribution studies of 99m Tc labeled fatty acids (8, 11, and 15 carbons) obtained via "click chemistry" for its potential use in myocardial imaging. ω-Bromo fatty acids (8C/11C/15C) were synthetically modified at bromo terminal to introduce a heterocyclic triazole with glycine sidearm in a five step procedure. Modified fatty acids were subsequently radiolabeled with preformed [99m Tc(CO)3 ]+ synthon to yield the desired fatty acid complexes which were evaluated in Swiss mice. All the radiolabeled complexes were obtained with radiochemical purities >80%, as characterized by HPLC. Biodistribution studies of all three complexes in Swiss mice showed myocardial uptake of ~6-9% ID/g at 2 minutes post-injection, close to* I-IPPA (~9% ID/g). Complexes exhibited significant retention in the myocardium up to 30 minutes (~1% ID/g) but were lower to the standard agent (~7% ID/g). Similar uptake of activity in myocardium for the newly synthesized comple...Continue Reading

References

Mar 18, 2004·Bioconjugate Chemistry·Yasuhiro MagataHideo Saji
Nov 23, 2006·Journal of the American Chemical Society·Thomas L MindtRoger Schibli
Dec 13, 2006·Current Opinion in Biotechnology·Keiichiro Yoshinaga, Nagara Tamaki
Feb 3, 2007·Journal of Medicinal Chemistry·Tomoya UeharaYasushi Arano
Jun 30, 2007·Journal of Nuclear Cardiology : Official Publication of the American Society of Nuclear Cardiology·Christopher J PastoreJames E Udelson
Aug 15, 2008·Bioorganic & Medicinal Chemistry·Anupam MathurMeera Venkatesh
Jan 13, 2010·Dalton Transactions : an International Journal of Inorganic Chemistry·Harriet StruthersRoger Schibli
Jan 17, 2013·Dalton Transactions : an International Journal of Inorganic Chemistry·Huahui ZengHuabei Zhang

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Citations

Oct 9, 2019·Biomolecules·Ravi Kumar Akula, Yong-Uk Kwon

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