Development of an 111In-labeled dihydropyridine complex for L-type calcium channel imaging
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[111In]-DTPA-Amlodipine complex ([111In]-DTPA-AMLO) was prepared starting high purity [111In]indium chloride and conjugated DTPA-AMLO in 30 min at room temperature in acetate buffer in high radiochemical purity (>99 %, RTLC/HPLC; specific activity: 8–10 GBq/mmol). The log P, stability, biodistribution studies and imaging studies in untreated and amlodipine-pretreated rats were determined. The tracer is mostly washed out through kidneys as expected for a dihydropyridine compound. Blocking studies demonstrated high specific binding of the tracer in calcium channel-rich organs including intestine, heart and colon. SPECT images fully supported above results in normal and treated rats.
Keywords111In Dihydropyridines Amlodipine Radiolabeling Biodistribution Blocking studies SPECT
Authors wish to thank Ms F. Bolourinovin for chromatography experiments. This study has been funded and supported by Tehran University of Medical Sciences, Tehran, Iran; Grant No. 18308.
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