Abstract
A labeled norepinephrine analogue was prepared by bromination of norepinephrine with subsequent debromination with tritium or deuterium gas. The yield of tritiated norepinephrine was 10–20% with a molar radioactivity of 27 Ci/mmol. The biological activity of tritiated norepinephrine was evaluated by analyzing its specific capture by noradrenergic neutrons in thick sections of the brainstem and midbrain of Wistar rats, and in a suspension of cells of pheochromocytoma PC12 expressing the membrane transporter of norepinephrine. It is shown that tritium-labeled norepinephrine synthesized by the proposed method does not differ in biological activity from the natural norepinephrine.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Voges, R., Heys, J.R., and Moenius, Th., Preparation of Compounds Labeled with Tritium and Carbon-14, Chichester: Wiley, 2009.
Shevchenko, V.P., Nagaev, I.Yu., Shevchenko, K.V., and Myasoedov, N.F., Izotopy v meditsine: Sintez mechennykh tritiem biologicheski aktivnykh soedinenii dlya issledovaniya aktual’nykh problem biologii i meditsiny (Isotopes in Medicine: Synthesis of Tritiated Biologically Active Compounds for Study of Important Problems of Biology and Medicine), Moscow: Fizmatlit, 2005, vol. 2, pp. 484–538.
Shevchenko, V.P., Nagaev, I.Yu., and Myasoedov, N.F., J. Label. Comp. Radiopharm., 2010, vol. 53, nos. 11–12, pp. 693–703.
Shevchenko, V.P., Myasoedov, N.F., Nagaev, I.Yu., Shevchenko, K.V., Badun, G.A., Chernysheva, M.G., and Fedoseev, V.M., RF Patent 2422436, 27.06.2011, Byul., No. 18, 2011.
Shevchenko, V.P., Nagaev, I.Yu., and Myasoedov, N.F., RF Patent 2620190, 23.05.2017, Byul., No. 15, 2017.
Saraswat, L.D., Kenny, J.M., Davis, Sh.K., and Justice, J.B., J. Label. Comp. Radiopharm., 1980, vol. 18, no. 10, pp. 1507–1516.
Sinhababu, A.K. and Borchardt, R.T., J. Label. Comp. Radiopharm., 1984, vol. 22, no. 8, pp. 767–774.
Shevchenko, V.P., Nagaev, I.Yu., Shevchenko, K.V., Chernysheva, M.G., Badun, G.A., Fedoseev, V.M., and Myasoedov, N.F., Radiokhimiya, 2011, vol. 53, no. 3, pp. 285–288.
Schwetlik, K., Organikum: Organisch-chemisches Grundpraktikum, Berlin: VEB Deutscher Verlag der Wissenschaften, 1977. Translated under the title Praktikum po organicheskoi khimii, Moscow: Mir, 1979.
Mingazov, E.R., Khakimova, G.R., Kozina, E.A., Medvedev, A.E., Buneeva, O.A., Bazyan, A.S., and Ugrumov, M.V., Mol. Neurobiol., 2017. doi 10.1007/s12035-017-0559-6
Khakimova, G.R., Kozina, E.A., Sapronova, A.Ya., and Ugryumov, M.V., Dokl. Biol. Sci., 2010, vol. 435, part 1, pp. 381–383.
Zhu, M.Y. and Ordway, G.A., J. Neurochem., 1997, vol. 68, no. 1, pp. 134–141.
Author information
Authors and Affiliations
Corresponding author
Additional information
Original Russian Text © V.P. Shevchenko, I.Yu. Nagaev, T.S. Pronina, K.V. Shevchenko, A.R. Murtazina, S.A. Surkov, M.V. Ugryumov, N.F. Myasoedov, 2018, published in Doklady Akademii Nauk, 2018, Vol. 480, No. 5, pp. 551–554.
Rights and permissions
About this article
Cite this article
Shevchenko, V.P., Nagaev, I.Y., Pronina, T.S. et al. Synthesis of Deuterium- or Tritium-Labeled Norepinephrine and Evaluation of Its Biological Activity. Dokl Chem 480, 117–120 (2018). https://doi.org/10.1134/S001250081806006X
Received:
Published:
Issue Date:
DOI: https://doi.org/10.1134/S001250081806006X