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
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.
Cite this paper
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