Synthesis, labelling and biological characteristics of derivatives of Mercaptoacetyltriglycine with two amide functions

Eight novel derivatives of MAG3, containing in their structure two instead of three amide functions, have been synthesized and evaluated. The synthesized ligands were labelled with 99mTc by exchange labelling at 100°C and/or by a direct labelling method at room temperature. After labelling with 99mT...

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Veröffentlicht in:	Journal of labelled compounds & radiopharmaceuticals 2002-02, Vol.45 (2), p.115-137
Hauptverfasser:	Okarvi, S. M., Verbeke, K., Adriaens, P., Verbruggen, A. M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Contrast media. Radiopharmaceuticals diamides MAG3 Medical sciences Pharmacology. Drug treatments radiolabelling renal agents technetium-99m
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container_title	Journal of labelled compounds & radiopharmaceuticals
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creator	Okarvi, S. M. Verbeke, K. Adriaens, P. Verbruggen, A. M.
description	Eight novel derivatives of MAG3, containing in their structure two instead of three amide functions, have been synthesized and evaluated. The synthesized ligands were labelled with 99mTc by exchange labelling at 100°C and/or by a direct labelling method at room temperature. After labelling with 99mTc, the reaction mixtures were analyzed by radio‐HPLC. Biological evaluation of different 99mTc‐diamide complexes in mice and a baboon indicated that substitution in one amide function of MAG3 structure greatly influences the renal handling of these compounds. It was found that the diamide derivatives containing at least one inverted amide exhibit biological behavior comparable to that of 99mTc‐MAG3. Copyright © 2002 John Wiley & Sons, Ltd.
doi_str_mv	10.1002/jlcr.538
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It was found that the diamide derivatives containing at least one inverted amide exhibit biological behavior comparable to that of 99mTc‐MAG3. Copyright © 2002 John Wiley & Sons, Ltd.</description><subject>Biological and medical sciences</subject><subject>Contrast media. Radiopharmaceuticals</subject><subject>diamides</subject><subject>MAG3</subject><subject>Medical sciences</subject><subject>Pharmacology. 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subjects	Biological and medical sciences Contrast media. Radiopharmaceuticals diamides MAG3 Medical sciences Pharmacology. Drug treatments radiolabelling renal agents technetium-99m
title	Synthesis, labelling and biological characteristics of derivatives of Mercaptoacetyltriglycine with two amide functions
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