Published December 2020 | Version v1
Journal article Metadata-only

Preparation of 5-[131I]iodotubercidin for the detection of adenosine kinase

Creators

  • 1. Institute of Neuroscience and Medicine, Nuclear Chemistry (INM-5), Forschungszentrum Juelich GmbH, Juelich (Germany)
  • 2. Forschungszentrum Juelich GmbH, Juelich (Germany). Molecular Organization of the Brain (INM-2)
  • 3. Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf, Dresden (Germany)
  • 4. University of Cologne, Cologne (Germany). Institute of Radiochemistry and Experimental Molecular Imaging, Faculty of Medicine and University Hospital Cologne
  • 5. Molecular Organization of the Brain (INM-2), Forschungszentrum Juelich GmbH, Juelich (Germany)

Description

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. (author)

Additional details

Publishing Information

Journal Title
Journal of Radioanalytical and Nuclear Chemistry
Journal Volume
326
Journal Issue
3
Journal Page Range
p. 1691-1697
ISSN
0236-5731
CODEN
JRNCDM

INIS

Country of Publication
Hungary
Country of Input or Organization
Hungary
INIS RN
52024436
Subject category
S60: APPLIED LIFE SCIENCES;
Descriptors DEI
ADENOSINE; ANTIBIOTICS; AUTORADIOGRAPHY; ENZYME INHIBITORS; IN VITRO; IODINATION; NUCLEOSIDES; PHOSPHOTRANSFERASES
Descriptors DEC
ANTI-INFECTIVE AGENTS; CHEMICAL REACTIONS; DRUGS; ENZYMES; HALOGENATION; NUCLEOSIDES; NUCLEOTIDES; ORGANIC COMPOUNDS; PHOSPHORUS-GROUP TRANSFERASES; PROTEINS; RIBOSIDES; TRANSFERASES

Optional Information

Notes
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