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Cyclen-containing phosphonic acids as components of osteotropic 68Ga radiopharmaceuticals

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Abstract

The known methods of preparation of cyclen-containing phosphonic acids, promising components of radiopharmaceuticals, have been improved, and new approaches have been developed. Application of 31Р and 13С NMR spectroscopy for initial screening of complex formation between cyclen-containing phosphonic acids and Ga3+ in D2O has been demonstrated. The conditions of 68Ga complex formation with cyclencontaining phosphonic acids and estimation of their radiochemical yield in water by means of thin-layer chromatography have been elaborated. A correlation between the NMR and TLC data has been found. Biological distribution of the selected 68Ga radiopharmaceuticals has been determined in vivo from the positron emission tomography data. The obtained standardized uptake values point at the osteotropicity of the 68Ga compounds.

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Authors and Affiliations

  1. Frumkin Institute of Physical Chemistry and Electrochemistry, Russian Academy of Sciences, Leninskii pr. 31/4, Moscow, 119071, Russia

    G. S. Tsebrikova, V. E. Baulin, I. P. Kalashnikova & A. Yu. Tsivadze

  2. Institute of Physiologically Active Compounds, Russian Academy of Sciences, Chernogolovka, Moscow oblast, Russia

    V. E. Baulin, I. P. Kalashnikova, V. V. Ragulin & V. O. Zavel’skii

  3. Burnazyan Federal Medical Biophysical Center, Federal Medical Biological Agency of Russia, Moscow, Russia

    A. Ya. Maruk, A. S. Lunev, O. E. Klement’eva & G. E. Kodina

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  1. G. S. Tsebrikova
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Correspondence to G. S. Tsebrikova.

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Original Russian Text © G.S. Tsebrikova, V.E. Baulin, I.P. Kalashnikova, V.V. Ragulin, V.O. Zavel’skii, A.Ya. Maruk, A.S. Lunev, O.E. Klement’eva, G.E. Kodina, A.Yu. Tsivadze, 2015, published in Zhurnal Obshchei Khimii, 2015, Vol. 85, No. 9, pp. 1490–1498.

To the 85th Anniversary of birthday of late Yu.G. Gololobov

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Tsebrikova, G.S., Baulin, V.E., Kalashnikova, I.P. et al. Cyclen-containing phosphonic acids as components of osteotropic 68Ga radiopharmaceuticals. Russ J Gen Chem 85, 2071–2079 (2015). https://doi.org/10.1134/S1070363215090091

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  • DOI: https://doi.org/10.1134/S1070363215090091

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