Investigation of the labelling characteristics of 99mTc-mercaptoacetyltriglycine.
S-Benzyl-, S-benzamidomethyl- and S-benzoylmercaptoacetyltriglycine were synthesized and compared in exchange labelling experiments for the preparation of 99mTc-MAG3. The rate of exchange from 99mTc-tartrate to 99mTc-MAG3 starting from the respective precursors was determined in different conditions. Labelling proceeded most rapidly starting from the S-benzoyl protected precursor but efficient labelling was also accomplished using the more stable S-benzamidomethyl- and S-benzylmercaptoacetyltriglycine. 99mTc-MAG3 was also prepared by direct labelling of unprotected mercaptoacetyltriglycine at alkaline pH. Radiochemical purity in these conditions is mainly dependent on the pH during labelling.
Bormans
G
G
Laboratory of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, K. U. Leuven, Belgium.
Cleynhens
B
B
Adriaens
P
P
Vanbilloen
H
H
De Roo
M
M
Verbruggen
A
A
D000818:Animals; D001593:Benzyl Compounds / Q000138:chemical synthesis; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D007553:Isotope Labeling; D008024:Ligands; D008297:Male; D051379:Mice; D011854:Radiochemistry; D017263:Technetium Tc 99m Mertiatide / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D014018:Tissue Distribution
D001593:Benzyl Compounds; D008024:Ligands; D017263:Technetium Tc 99m Mertiatide