Home > Publications database > Preparation of 5-[131I]iodotubercidin for the detection of adenosine kinase > print

001     889345
005     20230111074311.0
024 7 _ |a 10.1007/s10967-020-07465-2
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024 7 _ |a 0134-0719
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024 7 _ |a 1417-2097
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024 7 _ |a 1588-2780
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024 7 _ |a 2064-2857
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024 7 _ |a 2128/27196
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100 1 _ |a Bier, Dirk
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245 _ _ |a Preparation of 5-[131I]iodotubercidin for the detection of adenosine kinase
260 _ _ |a Dordrecht [u.a.]
|c 2020
|b Springer Science + Business Media B.V.
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520 _ _ |a 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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700 1 _ |a Holschbach, Marcus
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700 1 _ |a Wedekind, Franziska
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700 1 _ |a Sihver, Wiebke
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700 1 _ |a Drewes, Birte
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700 1 _ |a Schulze, Annette
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700 1 _ |a Neumaier, Felix
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700 1 _ |a Neumaier, Bernd
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700 1 _ |a Bauer, Andreas
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773 _ _ |a 10.1007/s10967-020-07465-2
|g Vol. 326, no. 3, p. 1691 - 1697
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|p 1691 - 1697
|t Journal of radioanalytical and nuclear chemistry
|v 326
|y 2020
|x 1588-2780
856 4 _ |u https://juser.fz-juelich.de/record/889345/files/Bier2020_Article_PreparationOf5-%5B131I%5Diodotuber.pdf
856 4 _ |y Published on 2020-10-29. Available in OpenAccess from 2021-10-29.
|u https://juser.fz-juelich.de/record/889345/files/JRNC_Manuscript_Iodotubercidin_r1b.pdf
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