AbstractThe present study is oriented to synthesis of radioiodinated olmesartan medoxomil (OM) for potential cardiac imaging. Olmesartan medoxomil has been labeled with [125/131I] using chloramine-T (Ch-T) as an oxidizing agent. The key effective factors such as amount of oxidizing agent, amount of substrate, pH, reaction temperature and reaction time, have been systematically studied to get high radiochemical yield of the [125I]olmesartan medoxomil reaching values of 98.5%. The labeled compound was separated and purified using thin layer chromatography (TLC), paper electrophoresis and high performance liquid chromatography (HPLC). The biological distribution indicates the suitability of [125I]olmesartan medoxomil as a novel tracer to image heart with high heart/blood ratio within 30 min which was detected by gamma camera.
One of the most famous techniques for stomach ulcer imaging is the nuclear imaging technique. We aim to focus on the synthesis of 125I-cimetidine (125I-cim) as an agent for peptic ulcer imaging. Cimetidine was labeled with Iodine-125 using a different oxidizing agent (Ch-T, NBS). All factors affecting the labeling yield were optimized. The radiochemical yield of 125I-cim was 98 ± 0.22% at optimum conditions. In vitro stability, in vivo biodistribution of 125I-cimetidine was studied in three groups: control group, pretreated group, and ulcer bearing group. In vivo biodistribution studies of 125I-cim revealed high uptake in the stomach ulcer, reaching about 75.4 ± 1.2% ID/g at 15 min post-injection, than pretreated groups compared to the control. The results showed the suitability of using 125I-cimetidine for stomach ulcer imaging.
The imaging of organs is very important in the field of diagnosis especially in case of liver diseases. In the present work, carnosine was successfully labeled with iodine-131 at room temperature in acidic medium using chloramine-T (Ch-T) as moderate oxidizing agent. The parameters affecting labeling of carnosine such as amount of oxidizing agent, amount of substrate, pH value of the reaction mixture, reaction temperature and reaction time, were investigated. The best conditions for formation of 131I-carnosine (131I-CAR) complex were 40 μg of chloramine-T (Ch-T), 75 μg of carnosine, pH 4 and 45 min reaction time at room temperature. The radiochemical yield for 131I-CAR complex was (91 ± 0.11) % at optimum conditions and the labeled complex was stable for 2 h after labeling process. Biodistribution study was achieved using three groups of rats (normal, treated by inactive carnosine and hepatotoxicity rats induced by CCl4). Hepatotoxicity of liver was evaluated using different biochemical markers such as ALT, AST and ALK.P. The 131I-CAR complex showed selective bio-localization in stomach and liver and its selectivity increases in acquired hepatotoxicity. The biological distribution indicates that the suitability of 131I-CAR as a potential hepatotoxicity imaging to detect hepatitis and medical prognosis.
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