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Chemical and biological evaluation of technetium (I) Tricarbonyl complexes with EHIDA and DPD
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Abstract
MATERIAL AND METHODS: DPD and EHIDA were synthesised and prepared in kit form in INS “Vinca”. A carbonyl labelling agent IsolinkTM (Mallinckrodt Medical B.V.) and a carbonyl precursor (NCRS Demokritos) were applied. The samples of each compound were added to a vial containing 99mTc-carbonyl precursor, in which original pH (10÷11) was neutralised to a pH of around 5.5 or 7.5, the same one as the pH of the investigated compounds. After heating, the reaction products were analysed by HPLC equipped with UV and g-detector, with TEAP 0.05 M, methanol and water as solvent. The biological evaluation of 99m99mTc(I)-coordinated compounds, as well as 99mTc-DPD and 99mTc-EHIDA complexes, involved a bio distribution examination on Wistar rats.
RESULTS: The results have shown that hydrophilic organometallic [99mTc(CO)3(H2O)3]+ precursor facilitates the formation of Tc (I) complexes with these ligands, based on the tricarbonyltechnetium (I) core. The changes in structure of DPD and EHIDA labelled molecules influenced biological behaviour: 99Tc(CO)3 -DPD did not accumulate in bone (< 1% of the complex was found in the femur), while 99Tc(CO)3 - EHIDA has shown slower billiary excretion and faster filtration through the kidneys.
DISCUSSION: The results of the labelling of DPD and EHIDA with [99mTc(CO)3(H2O)3]+ and their chemical and biological behaviour, in comparison with the same one for 99mTc-DPD and 99mTc-EHIDA, confirmed that different oxidation states of technetium make the formation of a variety of complexes with quite different behaviour possible.
Abstract
MATERIAL AND METHODS: DPD and EHIDA were synthesised and prepared in kit form in INS “Vinca”. A carbonyl labelling agent IsolinkTM (Mallinckrodt Medical B.V.) and a carbonyl precursor (NCRS Demokritos) were applied. The samples of each compound were added to a vial containing 99mTc-carbonyl precursor, in which original pH (10÷11) was neutralised to a pH of around 5.5 or 7.5, the same one as the pH of the investigated compounds. After heating, the reaction products were analysed by HPLC equipped with UV and g-detector, with TEAP 0.05 M, methanol and water as solvent. The biological evaluation of 99m99mTc(I)-coordinated compounds, as well as 99mTc-DPD and 99mTc-EHIDA complexes, involved a bio distribution examination on Wistar rats.
RESULTS: The results have shown that hydrophilic organometallic [99mTc(CO)3(H2O)3]+ precursor facilitates the formation of Tc (I) complexes with these ligands, based on the tricarbonyltechnetium (I) core. The changes in structure of DPD and EHIDA labelled molecules influenced biological behaviour: 99Tc(CO)3 -DPD did not accumulate in bone (< 1% of the complex was found in the femur), while 99Tc(CO)3 - EHIDA has shown slower billiary excretion and faster filtration through the kidneys.
DISCUSSION: The results of the labelling of DPD and EHIDA with [99mTc(CO)3(H2O)3]+ and their chemical and biological behaviour, in comparison with the same one for 99mTc-DPD and 99mTc-EHIDA, confirmed that different oxidation states of technetium make the formation of a variety of complexes with quite different behaviour possible.
Keywords
Technetium-99m; [99mTc(CO)3(H2O)3]+; labelling; EHIDA; DPD
Title
Chemical and biological evaluation of technetium (I) Tricarbonyl complexes with EHIDA and DPD
Journal
Issue
Pages
1-5
Published online
2004-01-22
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703
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1704
Bibliographic record
Nucl. Med. Rev 2004;7(1):1-5.
Keywords
Technetium-99m
[99mTc(CO)3(H2O)3]+
labelling
EHIDA
DPD
Authors
Divna Dj. Djokić
Drina Lj. Janković
Ljiljana Lj. Stamenković
Ioannis Pirmettis