Mesalamine was labelled with technetium-99m ( 99m Tc) 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 PPARc 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 99m Tc-mesalamine as a radiotracer for ulcerative colitis.
Discovery of
99m
Tc-labeled imidazole derivatives as a potential radiotracer for hypoxic tumor imaging is considered to be of great interest because of non-invasive detection capabilities. 2-Mercaptobenzimidazole (2-MBI) was successfully synthesized, characterized and radiolabeled with [
99m
Tc (CO)
3
(H
2
O)
3
]
+
intermediate to form
99m
Tc-2-MBI complex with radiochemical purity of ≥95% yield as observed by instant-thin layer chromatography (ITLC) and radio-high performance liquid chromatography (radio-HPLC). The
99m
Tc-2-MBI complex was observed to be stable in saline and serum with no noticeable decomposition at room temperature and 37 °C, respectively, over a time period of 24 h. Biodistribution results in Balb/c mice bearing S180 tumor show that
99m
Tc-2-MBI highly internalized in tumor tissue, also possess preferably high tumor/muscle and tumor/blood ratios 4.14 ± 0.77 and 3.91 ± 0.63, respectively at 24 h incubation. Scintigraphic imaging study shows
99m
Tc-2-MBI is visibly accumulated in hypoxic tumor tissue, suggesting it would be a promising radiotracer for early stage diagnosis of tumor hypoxia.
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