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Synthesis, radiolabelling characteristics and biological evaluation of the derivatives of mercaptoacetyltriglycine

  • S. M. Okarvi , P. Adriaens and A. M. Verbruggen
Published/Copyright: September 25, 2009

Summary

Several derivatives of MAG3, in which one or both of the first two amide bonds are inverted and contain an additional methyl or carboxyl-substituent on the ligand backbone, have been synthesized and evaluated. This was realized by substituting a glycyl with a D- or L-alanyl moiety or by replacing cysteamine with an L-cysteine to investigate the renal characteristics of the resulting derivatives versus the reference 99mTc-MAG3. Labelling with 99mTc resulted in two main radioactive species, which probably are the isomeric oxo-technetium complexes. These complexes were separated by HPLC and evaluated in mice. The data suggest that the substitution in the amide functions and addition of a methyl or carboxyl moiety results in poor renal handling of these compounds. However, one of the derivatives 99mTc-C-LB, exhibits renal characteristics comparable to 99mTc-MAG3.

Received: 2002-1-3
Accepted: 2002-3-26
Published Online: 2009-9-25
Published in Print: 2002-7-1

© Oldenbourg Wissenschaftsverlag, München

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