Synthesis and evaluation of the (99m)tc-complexes of L-cysteine acetyldiglycine (a hybrid of MAG3 and L,L-EC) and of L-beta-homocysteine acetyldiglycine.
L-Cysteine acetyldiglycine (L-CAG2), a hybrid compound of L,L-EC and MAG3, and its L-beta-homocysteine analogue L-HAG2 were synthesized. After labeling with (99m)Tc, (99m)Tc-L-CAG2 and (99m)Tc-L-HAG2 gave two peaks on high performance liquid chromatography. Urinary excretion of both isomers of (99m)Tc-L-CAG2 and (99m)Tc-L-HAG2 was slower than for the "parent" complexes (99m)Tc-MAG3 or (99m)Tc-L,L-EC. Isomer B of (99m)Tc-L-CAG2 showed pronounced kidney retention in mice (57% of ID in kidneys at 30 min postinjection), but further evaluation in baboon did not reproduce this phenomenon.
Mang'era
K
K
Laboratory of Radiopharmaceutical Chemistry F.F.W., Leuven, Belgium.
Vanbilloen
H
H
Cleynhens
B
B
de Groot T
Bormans
G
G
Verbruggen
A
A
Verbeke
K
K
D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D007553:Isotope Labeling; D007668:Kidney / Q000000981:diagnostic imaging / Q000378:metabolism*; D008297:Male; D051379:Mice; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D010215:Papio; D011485:Protein Binding; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D014018:Tissue Distribution
D001798:Blood Proteins; D009842:Oligopeptides; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C422190:technetium Tc 99m cysteine acetyldiglycine; C422191:technetium Tc 99m homocysteine acetyldiglycine