99mTc-Mesalamine as potential agent for diagnosis and monitoring of ulcerative colitis: labelling, characterisation and biological evaluation
Mesalamine was labelled with technetium-99m (99mTc) in high radiolabelling yield (~98.4 %), in vitro stability (~4 h) and in serum persistence (~24 h). Optimum labelling conditions were investigated. The structure of the complex was confirmed using in silico analysis. Molecular docking was performed to evaluate the complex binding to its biochemical target, the PPARγ receptor. Biodistribution and clearance studies were performed in normal and ulcerative colitis models in mice. The tracer’s localization was highest (~65.2 %) in microbial model compared to chemical model (~42.4 %) and normal mice (~22.1 %) at 60 min post injection. All data supported the usefulness of 99mTc-mesalamine as a radiotracer for ulcerative colitis.
KeywordsMesalamine 99mTc-Mesalamine complex Ulcerative colitis Diagnosis Biological evaluation PPARγ receptor
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