Imaging hypoxia in vivo by controlling the electrochemistry of copper radionuclide complexes

Blower, P.J. and Went, M.J. and Martin, K.E. and Smith, G.E. (2007) Imaging hypoxia in vivo by controlling the electrochemistry of copper radionuclide complexes. Journal of Labelled Compounds & Radiopharmaceuticals, 50 (5-6). pp. 354-359. ISSN 0362-4803. (Access to this publication is restricted)

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Abstract

Tissue hypoxia is a feature of cancer, heart disease and stroke, and imaging it may become clinically important. Copper-ATSM (ATSMH(2) = 2,3-butanedione bis(N-methyl)thiosemicarb-azone), labelled With (CU)-C-60, (CU)-C-62 or (CU)-C-64, is selectively taken up in hypoxic cells in vitro and in vivo by a bioreductive mechanism, and is a prototype hypoxia. imaging agent amenable to improvement. In vitro studies with several differently alkylated analogues of CuATSM show that hypoxia. selectivity is a general property of complexes with two alkyl groups at the diketone backbone, offering a range of pharmacokinetic proper-ties while retaining hypoxia. selectivity. This pharmacokinetic control affords a route to development of second-generation hypoxia imaging agents With optimized properties for different clinical applications. Combinatorial synthesis of these analogues, including asymmetric ones, is possible by combining several diketones with several thiosemicarbazides and separating the products chromatographically.

Item Type: Article
Uncontrolled keywords: copper; hypoxia; PET; imaging
Subjects: Q Science > QD Chemistry
Divisions: Faculties > Science Technology and Medical Studies > School of Biosciences
Faculties > Science Technology and Medical Studies > School of Physical Sciences
Depositing User: Stephen Holland
Date Deposited: 19 Dec 2007 19:24
Last Modified: 05 Sep 2011 23:25
Resource URI: http://kar.kent.ac.uk/id/eprint/2025 (The current URI for this page, for reference purposes)
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