Preparation of radioiodo-metoprolol and its biological evaluation as a possible cardiac imaging agent1
125I-Metoprolol was prepared by electrophilic substitution reaction in the presence of Chloramine-T (CAT) as an oxidizing agent. The reaction conditions were optimized. The radiochemical yield of 125I-metoprolol exceeding 90% was attained in 10 min at ambient temperature (25 ± 1°C). The radiochemical yield and purity of the labeled product were evaluated by electrophoresis, thin-layer chromatography (TLC), and high-performance liquid chromatography (HPLC). Biodistribution studies of 125I-iodometoprolol were carried out in normal Albino Swiss mice. The results indicate the possibility of using [125I]- iodometoprolol for myocardial imaging. Pleiades Publishing, Inc., 2010.