Abstract

Nitrofurantoin (NF) was labeled with iodine-125 via electrophilic substitution reaction. Some factors affecting the radiochemical yield of 125I-NF, such as NF concentration, chloramine-T (CAT) concentration, pH of the reaction mixture, reaction time, temperature, and reaction medium, were studied. The maximum yield of 125I-NF (90%) was obtained by using 3.7 MBq of Na125I, 1 mM CAT, 1 mM NF in DMF, at pH 2 and 60 °C within 5 min. The specific activity of 125I-NF reaches 33.3 MBq/0.2 mmol, and the 125I-NF was completely separated and purified by means of high pressure liquid chromatography. The biological distribution in normal mice indicates the suitability of radioiodinated NF for urinary tract imaging. Copyright © 2012 John Wiley & Sons, Ltd.

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