Radioiodination of olmesartan medoxomil and biological evaluation of the product as a tracer for cardiac imaging

Abstract

Abstract The present study is oriented to synthesis of radioiodinated olmesartan medoxomil (OM) for potential cardiac imaging. Olmesartan medoxomil has been labeled with [125/131I] using chloramine-T (Ch-T) as an oxidizing agent. The key effective factors such as amount of oxidizing agent, amount of substrate, pH, reaction temperature and reaction time, have been systematically studied to get high radiochemical yield of the [125I]olmesartan medoxomil reaching values of 98.5%. The labeled compound was separated and purified using thin layer chromatography (TLC), paper electrophoresis and high performance liquid chromatography (HPLC). The biological distribution indicates the suitability of [125I]olmesartan medoxomil as a novel tracer to image heart with high heart/blood ratio within 30 min which was detected by gamma camera.