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Development of an 111In-Labeled Dihydropyridine Complex for L-Type Calcium Channel Imaging Publisher



Firouzyar T1 ; Jalilian AR2 ; Shafieeardestani M1 ; Aboudzadeh MR2 ; Fazaeli Y2 ; Bolourinovin F2 ; Mirzaii M2 ; Khalaj A1
Authors
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Authors Affiliations
  1. 1. Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), P. O. Box 14395-836, Tehran, Iran

Source: Journal of Radioanalytical and Nuclear Chemistry Published:2015


Abstract

[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. © 2014, Akademiai Kiado, Budapest, Hungary.