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Development of an 111In-labeled dihydropyridine complex for L-type calcium channel imaging

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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.

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Acknowledgments

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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Authors and Affiliations

  1. Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

    T. Firouzyar, M. Shafiee-Ardestani & A. Khalaj

  2. Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), P. O. Box 14395-836, Tehran, Iran

    A. R. Jalilian, M. R. Aboudzadeh, Y. Fazaeli, F. Bolourinovin & M. Mirzaii

Authors
  1. T. Firouzyar
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  2. A. R. Jalilian
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  3. M. Shafiee-Ardestani
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  4. M. R. Aboudzadeh
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  5. Y. Fazaeli
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  6. F. Bolourinovin
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  7. M. Mirzaii
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  8. A. Khalaj
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Correspondence to A. R. Jalilian.

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Firouzyar, T., Jalilian, A.R., Shafiee-Ardestani, M. et al. Development of an 111In-labeled dihydropyridine complex for L-type calcium channel imaging. J Radioanal Nucl Chem 303, 2361–2369 (2015). https://doi.org/10.1007/s10967-014-3656-2

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  • DOI: https://doi.org/10.1007/s10967-014-3656-2

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