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Preparation of 5-[131I]iodotubercidin for the detection of adenosine kinase

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Abstract

5-Iodotubercidin is a prototype adenosine kinase (AK) inhibitor with potent anti-seizure activity in rodent epilepsy models. Using the chloramine-T method for radioiodination of tubercidin with 131I, we prepared no-carrier-added 5-[131I]iodotubercidin (5-[131I]IT) in a radiochemical yield of 61 ± 13% and with a radiochemical purity of > 99% (molar activity = 10–40 GBq/µmol). In vitro competition and saturation experiments demonstrated specific binding of 5-[131I]IT in rodent brain slices (KD ~ 31 nM), but ex vivo autoradiography revealed its accumulation in cerebral vessels. We conclude that 5-[131I]IT could be a useful tool for the detection and quantification of AK in in vitro studies.

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Authors and Affiliations

  1. Institute of Neuroscience and Medicine, Nuclear Chemistry (INM-5), Forschungszentrum Jülich GmbH, Jülich, Germany

    Dirk Bier, Marcus Holschbach, Birte Drewes, Annette Schulze, Felix Neumaier & Bernd Neumaier

  2. Molecular Organization of the Brain (INM-2), Forschungszentrum Jülich GmbH, Wilhelm-Johnen-Straße, 52428, Jülich, Germany

    Franziska Wedekind & Andreas Bauer

  3. Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Bautzner Landstraße 400, 01328, Dresden, Germany

    Wiebke Sihver

  4. Institute of Radiochemistry and Experimental Molecular Imaging, Faculty of Medicine and University Hospital Cologne, University of Cologne, 50937, Cologne, Germany

    Felix Neumaier & Bernd Neumaier

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  1. Dirk Bier
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Bier, D., Holschbach, M., Wedekind, F. et al. Preparation of 5-[131I]iodotubercidin for the detection of adenosine kinase. J Radioanal Nucl Chem 326, 1691–1697 (2020). https://doi.org/10.1007/s10967-020-07465-2

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