A number of MAG 3 -derivatives, containing the three-amide functions modified by inverting the sequence -CO-NH-to -NH-CO-in the firstand/or second-amide functions, have been labelled with 99m Tc in order to study the renal characteristics of the resulting MAG 3 -derivatives versus the reference 99m
Synthesis, labelling and biological characteristics of derivatives of Mercaptoacetyltriglycine with two amide functions
β Scribed by S. M. Okarvi; K. Verbeke; P. Adriaens; A. M. Verbruggen
- Publisher
- John Wiley and Sons
- Year
- 2002
- Tongue
- French
- Weight
- 188 KB
- Volume
- 45
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.538
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β¦ Synopsis
Abstract
Eight novel derivatives of MAG~3~, containing in their structure two instead of three amide functions, have been synthesized and evaluated. The synthesized ligands were labelled with ^99m^Tc by exchange labelling at 100Β°C and/or by a direct labelling method at room temperature. After labelling with ^99m^Tc, the reaction mixtures were analyzed by radioβHPLC. Biological evaluation of different ^99m^Tcβdiamide complexes in mice and a baboon indicated that substitution in one amide function of MAG~3~ 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 ^99m^TcβMAG~3~. Copyright Β© 2002 John Wiley & Sons, Ltd.
π SIMILAR VOLUMES
99m Tc-MAG 3 is widely used in clinical nuclear medicine as a potential replacement of 131 I-OIH for renal function studies. The terminal carbonylglycine in the MAG 3 backbone is assumed to be essential for maintaining its efficient renal handling characteristics. A number of MAG 3 -derivatives have
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