Radioiodinated Azilsartan as a New Highly Selective Radiotracer for Myocardial Perfusion Imaging

Abstract

Azilsartan (AZ) was labeled with 131I using Chloramine-T as oxidizing agent. Factors affecting the labeling efficiency were systematically studied, and optimum conditions were found: oxidizing agent amount 100 μg, substrate amount 100 μg, pH 6, reaction time 30 min, and ambient temperature. Biodistribution studies showed that [131I]iodoAZ is concentrated in heart at 5 min post-injection to give high uptake of 29.0 ± 0.6% injected dose/g organ. Thus, iodoAZ shows promise as a radiotracer for heart imaging.