Complexes of technetium-99m with tetrapeptides containing one alanyl and three glycyl moieties

European Journal of Nuclear Medicine
H P VanbilloenA M Verbruggen

Abstract

Recently, we have shown that tetrapeptides can be efficiently labelled with technetium-99m by direct labelling at alkaline pH. Tetrapeptides can be considered derivatives of mercaptoacetyltriglycine (MAG3) in which the mercaptoacetyl moiety is replaced by an amino acid residue. In view of the interesting biological properties of some C-methyl substituted derivatives of 99mTc-MAG3, we have now synthesised and evaluated the complexes of 99mTc with tetrapeptides containing three glycyl (G) moieties and one D- or L-alanyl (A) moiety. In mice, 99mTc-L-GAGG, 99mTc-D-GGAG and 99mTc-L-GGAG showed a rapid and high renal excretion, comparable to that of 99mTc-MAG3. Renal handling was somewhat reduced for isomers d and l of 99mTc-AGGG and 99mTc-D-GAGG and markedly inferior for 99mTc-L-GGGA and 99mTc-D-GGGA. In the baboon, 99mTc-L-AGGG, 99mTc-D-AGGG and 99mTc-L-GAGG showed a comparable or even higher 1-h plasma clearance than 99mTc-MAG3. 99mTc-D-GAGG, 99mTc-L-GGAG and 99mTc-D-GGAG were characterised by a lower plasma clearance and the clearance of 99mTc-L-GGGA and 99mTc-D-GGGA was remarkably low. The three 99mTc-labelled tetrapeptides with the highest plasma clearance in a baboon were compared with 99mTc-MAG3 in a human volunteer. 99mTc-L-...Continue Reading

References

Apr 1, 1992·International Journal of Radiation Applications and Instrumentation. Part B, Nuclear Medicine and Biology·G BormansA VerBruggen
Jan 1, 1990·European Journal of Nuclear Medicine·A M Verbruggen
Jan 1, 1965·Journal of Theoretical Biology·A Despopoulos
Apr 1, 1995·Nuclear Medicine and Biology·H P VanbilloenA M Verbruggen
Mar 1, 1960·Proceedings of the Society for Experimental Biology and Medicine·M TUBISR A NORDYKE

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Citations

Feb 8, 2003·Trends in Biotechnology·Antonella LupettiErnest K J Pauwels
May 29, 2002·Nuclear Medicine and Biology·Mick M WellingPeter H Nibbering
Apr 8, 2003·The Lancet Infectious Diseases·Antonella LupettiPeter H Nibbering
Sep 2, 2014·Nuclear Medicine and Molecular Imaging·Malgorzata LipowskaAndrew T Taylor
Dec 26, 2001·Chemical Reviews·S Liu, D S Edwards
Aug 21, 2013·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Myriam LétourneauJocelyn Dupuis
Nov 5, 1997·Bioconjugate Chemistry·S LiuJ A Barrett

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