%0 Journal Article
%A Bier, Dirk
%A Holschbach, Marcus
%A Wedekind, Franziska
%A Sihver, Wiebke
%A Drewes, Birte
%A Schulze, Annette
%A Neumaier, Felix
%A Neumaier, Bernd
%A Bauer, Andreas
%T Preparation of 5-[131I]iodotubercidin for the detection of adenosine kinase
%J Journal of radioanalytical and nuclear chemistry
%V 326
%N 3
%@ 1588-2780
%C Dordrecht [u.a.]
%I Springer Science + Business Media B.V.
%M FZJ-2021-00234
%P 1691 - 1697
%D 2020
%X 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.
%F PUB:(DE-HGF)16
%9 Journal Article
%U <Go to ISI:>//WOS:000584877900006
%R 10.1007/s10967-020-07465-2
%U https://juser.fz-juelich.de/record/889345