Radiolabeling, Chemical and Biological Evaluation of Some Drugs for Nuclear Medicine Applications

Abstract

This study aims to develop potential radiopharmaceuticals for non-invasive cardiac imaging by exploiting the advantages of drugs that can act on the heart. Lidocaine hydrochloride, Verapamil hydrochloride and Epinephrine were successfully labeled with radioactive iodine (125I) using Chloramine-T via an electrophilic substitution reaction.125I-Lidocaine, 125I-Verapamil, and 125I-Epinphrine gave maximum labeling yields of 93.2 % ± 0.1, 95.4 % ± 0.4 and 96% ± 0.8, respectively. Biodistribution studies showed that the maximum uptake of radioidonated Lidocaine, Verapamil of mice was 19.8 % and 18.3 %, respectively, at 60 min post injection while the maximum uptake of radioidonated Epinephrine was 18.6% at 180 min post injection.