Abstract
A procedure for radioiodination of valsartan with iodine-125 is carried out via an electrophilic substitution of hydrogen atom with the iodonium cation I+. All reaction parameters were studied to optimize the labeling conditions of valsartan and to obtain a maximum radiochemical yield (RCY) of the 125I-Valsartan [125I-Val]. By using 3.7 MBq of Na125I, 50 μg of valsartan (0.2 mM) as substrate, 25 μg of Iodogen (0.15 mM) as oxidizing agent in ethanol at room temperature for 30 min, the radiochemical yield of 125I-Val was 98.6% The radiochemical yield was determined by electrophoresis using cellulose acetate moistened with 0.02 M phosphate buffer pH 7. The labeled compound was separated and purified by means of high-pressure liquid chromatography (HPLC). The biological distribution in normal mice indicates the suitability of radioiodinated valsartan to image any cardiovascular disorders.
Highlights
Myocardial assessment continues to be an issue in patients with coronary artery disease and left ventricular dysfunction
The data indicated that valsartan amount has no significant effect on the radiochemical yield (RCY) of 125I-Val
The RCY was not affected by increasing the amount of valsartan higher than (50 μg) (0.2 mM)
Summary
Myocardial assessment continues to be an issue in patients with coronary artery disease and left ventricular dysfunction. Nuclear imaging has long played an important role in this field. Positron emission tomography (PET) imaging using 18F-fluorodeoxyglucose is regarded as the metabolic gold standard of tissue viability [1,2], which has been supported by a wide clinical experience. Viability assessment using single photon emission computed tomography (SPECT) techniques has gained more wide-spread clinical acceptance than PET, because it is more widely available at lower cost. Technical advances in SPECT technology such as gated-SPECT further improve the diagnostic accuracy of the test. Further efforts are necessary to improve the diagnostic performance of nuclear imaging as reliable viability test [3]
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