Journal Article

FZJ-2021-00234

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Preparation of 5-[131I]iodotubercidin for the detection of adenosine kinase

Bier, D. (Corresponding author)FZJ* ; Holschbach, M.FZJ* ; Wedekind, F.FZJ* ; Sihver, W. ; Drewes, B.FZJ* ; Schulze, A.FZJ* ; Neumaier, F.FZJ* ; Neumaier, B.FZJ* ; Bauer, A.FZJ*

2020
Springer Science + Business Media B.V. Dordrecht [u.a.]

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Please use a persistent id in citations: http://hdl.handle.net/2128/27196  doi:10.1007/s10967-020-07465-2

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.

Keyword(s): Chemistry (2nd) ; Medicine (2nd)

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Contributing Institute(s):

1. Nuklearchemie (INM-5)
2. Molekulare Organisation des Gehirns (INM-2)

Research Program(s):

1. 573 - Neuroimaging (POF3-573) (POF3-573)

Appears in the scientific report 2021

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Database coverage:
; ; Clarivate Analytics Master Journal List ; Current Contents - Physical, Chemical and Earth Sciences ; DEAL Springer ; Ebsco Academic Search ; Essential Science Indicators ; IF < 5 ; JCR ; Nationallizenz ; SCOPUS ; Science Citation Index Expanded ; Web of Science Core Collection

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