Modelling of the blood plasma species of biguanide derivatives exhibiting potential as diagnostic radiopharmaceuticals
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Date
Authors
Wagener, Judith Marie
Dithebe, Midred K.
Mogano, Daniel
Cukrowski, Ignacy
Zeevaart, Jan Rijn
Journal Title
Journal ISSN
Volume Title
Publisher
South African Chemical Institute
Abstract
99mTc-DMSA (DMSA=dimercaptosuccinic acid), the gold standard for static renal imaging, has a long uptake time, which is a limiting factor in diagnostic procedures and also leads to a relatively high radiation dose to patients. The ligands dimethyl biguanide (DMBG), biuret (BIU), 2-imino-4-thiobiuret (ITB) and carboxy-biguanide (CBIG) have nitrogen donor atoms, which are able to complex transition elements. The formation constants needed in order to establish a blood plasma model for these ligands were determined by potentiometry and the results are reported herein. Based on blood plasma modelling, it was shown that the ligands had selectivity for 99mTc over blood plasma metal ions at physiological pH and it was therefore hypothesized that the Tc-ligand complex would survive in blood plasma. Furthermore, no or few side effects related to the mobilization of blood plasma metal ions by these ligands are expected, once the radiopharmaceutical has been administered. It is also expected that these ligands should clear rapidly from the blood plasma.
Description
Keywords
Biguanides, Kidney agents, Stability formation constants, Blood plasma speciation, CBIG, DMBG, BIU, ITB
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Citation
Wagener, JM, Dithebe, MK, Mogano, D, Cukrowski, I & Zeevaart, JR 2008, 'Modelling of the blood plasma species of biguanide derivatives exhibiting potential as diagnostic radiopharmaceuticals', South African Journal of Chemistry, vol. 61, pp. 82-92. [http://journals.sabinet.co.za/sajchem/]