In silico study and preclinical evaluation of radioiodinated procaterol as a potential scintigraphic agent for lung imaging

Abstract

PROCATEROL has been labeled using [125/131I] with chloramine-T (Ch-T) as oxidizing agent which can be used for lung imaging instead of the commercially available complex (Macro-aggregated albumin complex,99mTc-MAA) which is called blood-derived product. In addition, a comparison between a new radiotracer and other radiotracers such as 99mTc-DHPM,99mTc(CO)5I , 125/123I-IPMPD, 125I-fenoterol ,125I-reproterol, 125I-levalbuterol, 99mTc-levosalbutamol and 99mTc-tricarbonyl levosalbutamol is conducted. Factors such as the amount of oxidizing agent(100 μg), amount of substrate (100 μg), pH of reaction mixture (4), ambient temperature and reaction time (15min), have been systematically studied to optimize the iodination. Additionally, the in-vitro stability of radioiodinated procaterol was studied in two different media , namely, saline and serum up to 72 hours that indicates its stability upto 12hr. The labeled compound was separated and purified using thin layer chromatography (TLC), paper electrophoreses and high performance liquid chromatography (HPLC). Biodistribution studies indicated the suitability of radioiodinated procaterol as a novel tracer for lungs imaging. Radioiodinated procaterol could be considered a new radiotracer for lung imaging.