Universität zu Köln

Bier, Dirk ORCID: 0000-0001-9231-4303, Holschbach, Marcus, Wedekind, Franziska, Sihver, Wiebke, Drewes, Birte, Schulze, Annette, Neumaier, Felix, Neumaier, Bernd and Bauer, Andreas (2020). Preparation of 5-[I-131]iodotubercidin for the detection of adenosine kinase. J. Radioanal. Nucl. Chem., 326 (3). S. 1691 - 1698. DORDRECHT: SPRINGER. ISSN 1588-2780

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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 I-131, we prepared no-carrier-added 5-[I-131]iodotubercidin (5-[I-131]IT) in a radiochemical yield of 61 +/- 13% and with a radiochemical purity of > 99% (molar activity = 10-40 GBq/mu mol). In vitro competition and saturation experiments demonstrated specific binding of 5-[I-131]IT in rodent brain slices (K-D similar to 31 nM), but ex vivo autoradiography revealed its accumulation in cerebral vessels. We conclude that 5-[I-131]IT could be a useful tool for the detection and quantification of AK in in vitro studies.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Bier, Dirk UNSPECIFIED orcid.org/0000-0001-9231-4303 UNSPECIFIED Holschbach, Marcus UNSPECIFIED UNSPECIFIED UNSPECIFIED Wedekind, Franziska UNSPECIFIED UNSPECIFIED UNSPECIFIED Sihver, Wiebke UNSPECIFIED UNSPECIFIED UNSPECIFIED Drewes, Birte UNSPECIFIED UNSPECIFIED UNSPECIFIED Schulze, Annette UNSPECIFIED UNSPECIFIED UNSPECIFIED Neumaier, Felix UNSPECIFIED UNSPECIFIED UNSPECIFIED Neumaier, Bernd UNSPECIFIED UNSPECIFIED UNSPECIFIED Bauer, Andreas UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-314074
DOI:	10.1007/s10967-020-07465-2
Journal or Publication Title:	J. Radioanal. Nucl. Chem.
Volume:	326
Number:	3
Page Range:	S. 1691 - 1698
Date:	2020
Publisher:	SPRINGER
Place of Publication:	DORDRECHT
ISSN:	1588-2780
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language SPINAL-CORD; INHIBITION; RELEASE; DEAMINASE; RAT; ANALOGS; BRAIN Multiple languages Chemistry, Analytical; Chemistry, Inorganic & Nuclear; Nuclear Science & Technology Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/31407