Journal of Radioanalytical and Nuclear Chemistry
Volume/Issue:
Volume 283: Issue 1
99mTc-labelled biguanide derivatives: chemical speciation modelling thereof and evaluation in vervets
Authors:
Jan Zeevaart NECSA Department of Radiochemistry PO Box 582 Pretoria 0001 South Africa

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Judith Wagener NECSA Department of Radiochemistry PO Box 582 Pretoria 0001 South Africa

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Maria Neves Instituto Tecnologico Nuclear 2686-953 Sacavem Portugal

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Maria Costa Instituto Nacional de Engenharia, Tecnologia e Inovação, I.P. 1649-038 Lisbon Portugal

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Cristina Rodrigues Instituto Nacional de Engenharia, Tecnologia e Inovação, I.P. 1649-038 Lisbon Portugal

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Mildred Dithebe North West University, Mafikeng Campus CARST Mmabatho 2735 South Africa

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Elmaré Kilian University of Pretoria UPBRC, Onderstepoort Pretoria 0002 South Africa

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Ignacy Cukrowski University of Pretoria Department of Chemistry Pretoria 0002 South Africa

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Pages:
123–131
Online Publication Date:
06 Jul 2009
Publication Date:
01 Jan 2010
Article Category:
Research Article
DOI:
https://doi.org/10.1007/s10967-009-0131-6
Keywords:
Biguanides; Blood plasma speciation; Kidney agents
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Abstract  

99mTc-DMSA (dimercaptosuccinic acid) is known to be a safe and effective agent for static renal imaging. However, it has a long uptake time which is a limiting factor in diagnostic procedures and also leads to a relatively high radiation dose being administered to patients. There is a constant search for possible new renal imaging agents with a good resolution, kidney/liver contrast and low radiation dose to all organs. A series of biguanide derivatives (potential as non-insulin-dependent diabetes mellitus agents) labelled with 99mTc were investigated as potential alternative kidney-imaging agents on theoretical grounds (in silico) and their biodistribution (in vivo) verified in a limited number of animal experiments. Such a dual approach has the benefit that it reduces the number of animal experiments needed to evaluate a potential radiopharmaceutical. The blood plasma model shows little or no complexation of the biguanide type ligands by the metal ions in blood plasma. It was therefore expected that these ligands will clear rapidly through the kidneys and liver (increased lipophilicity). These predictions were verified by studies on single vervets comparing them with 99mTc-DMSA as gold standard. All the biguanide derivatives labelled with 99mTc show liver, kidney and gallbladder uptake in vervets. It was shown that the agent 99mTc-CBIG (carboxylbiguanide) has a very fast kidney clearance, which will reduce the dose to organs (as experienced for 99mTc-DMSA), although it’s potential as a kidney agent is limited by its gallbladder uptake.

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Cover Journal of Radioanalytical and Nuclear Chemistry
Journal of Radioanalytical and Nuclear Chemistry
Print ISSN:
0236-5731
Online ISSN:
1588-2780

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Journal of Radionalytical and Nuclear Chemistry
Language English
Size A4
Year of
Foundation		 1968
Volumes
per Year		 1
Issues
per Year		 12
Founder Akadémiai Kiadó
Founder's
Address		 H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher Akadémiai Kiadó
Springer Nature Switzerland AG
Publisher's
Address		 H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible
Publisher		 Chief Executive Officer, Akadémiai Kiadó
ISSN 0236-5731 (Print)
ISSN 1588-2780 (Online)

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