TY  - JOUR
AU  - Bier, Dirk
AU  - Holschbach, Marcus
AU  - Wedekind, Franziska
AU  - Sihver, Wiebke
AU  - Drewes, Birte
AU  - Schulze, Annette
AU  - Neumaier, Felix
AU  - Neumaier, Bernd
AU  - Bauer, Andreas
TI  - Preparation of 5-[131I]iodotubercidin for the detection of adenosine kinase
JO  - Journal of radioanalytical and nuclear chemistry
VL  - 326
IS  - 3
SN  - 1588-2780
CY  - Dordrecht [u.a.]
PB  - Springer Science + Business Media B.V.
M1  - FZJ-2021-00234
SP  - 1691 - 1697
PY  - 2020
AB  - 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.
LB  - PUB:(DE-HGF)16
UR  - <Go to ISI:>//WOS:000584877900006
DO  - DOI:10.1007/s10967-020-07465-2
UR  - https://juser.fz-juelich.de/record/889345
ER  -