## 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 la
Synthesis and biological characteristics of the Technetium-99m triamide derivatives of mercaptoacetyltriglycine (MAG3)
β Scribed by S. M. Okarvi; P. Adriaens; A. M. Verbruggen
- Publisher
- John Wiley and Sons
- Year
- 2003
- Tongue
- French
- Weight
- 154 KB
- Volume
- 46
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.645
No coin nor oath required. For personal study only.
β¦ Synopsis
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 Tc-MAG 3 . The 99m Tc-MAG 3 -derivatives displayed HPLC-profiles similar to that of 99m Tc-MAG 3 . Furthermore, in mice they exhibited biological behaviour comparable or even superior to 99m Tc-MAG 3 , which indicates that the sequence of the first-and/or second-amide bond in 99m Tc-MAG 3 affects the biological behaviour only to a limited degree. However, in baboon the plasma clearance of the 99m Tc-MAG 3 -derivatives was relatively slower than 99m Tc-MAG 3 , which underlines the inter-species variability.
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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
## Abstract To exploit the tissue affinity of compounds for radiopharmaceutical purposes, attachment of chelating groups is usually necessary to facilitate technetiumβ99m binding and transport. The chelating group, iminodiacetic acid, previously used to modify lidocaine for hepatobiliary radiophar
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