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Synthesis and biological characteristics of the Technetium‐99m triamide derivatives of mercaptoacetyltriglycine (MAG 3 )
Author(s) -
Okarvi S. M.,
Adriaens P.,
Verbruggen A. M.
Publication year - 2003
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.645
Subject(s) - chemistry , technetium 99m , amide , baboon , sequence (biology) , stereochemistry , technetium , radiochemistry , medicinal chemistry , organic chemistry , nuclear chemistry , scintigraphy , biochemistry , nuclear medicine , medicine
A number of MAG 3 ‐derivatives, containing the three‐amide functions modified by inverting the sequence –CO–NH– to –NH–CO– in the first‐ and/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. Copyright © 2002 John Wiley & Sons, Ltd.