Title: Evaluation of Tc-99m-complexes with novel monoamine diamide (MADA) thiolate tetraligands: L-cysteine acetyldiglycine diethyl ester and L-beta-methylhomocysteinate acetyldiglycine ethyl ester
Authors: Mang'era, KO ×
Verbeke, Kristin
de Groot, Tjibbe
Bormans, Guy
Verbruggen, Alfons #
Issue Date: Oct-2000
Publisher: John wiley & sons ltd
Series Title: Journal of labelled compounds & radiopharmaceuticals vol:43 issue:12 pages:1173-1182
Abstract: Compounds with a monoamine diamide (MADA) thiolate tetraligand structure (L-cysteine acetyldiglycine diethyl ester, L-CAG2D and L-beta -methylhomocysteinate acetyldiglycine ethyl ester, L-HAG2ME) were synthesized and labelled with Tc-99m to investigate the Tc-99m-complexation characteristics of these tetraligands. On reversed-phase HPLC, Tc-99m-L-CAG2D and Tc-99m-L-HAG2ME each give two peaks, probably isomers. During electrophoresis, all isomers migrate towards the anode indicating a net anionic charge, Octanol-buffer partition coefficients were respectively -0.47 and -0.05 For the isomers of Tc-99m-L-CAG2D and -0.51 and -0.32 for the isomers of Tc-99m-L-HAG2ME. In addition, brain uptake of all HPLC- isolated isomers was low and did not exceed 0.1% of injected dose at 2 min, 10 min or 30 min post injection. It may be concluded that the MADA-type ligands lose their amine proton upon complexation with Tc-99m resulting in hydrophilic, negatively charged Tc-99m-complexes which do not exhibit significant brain uptake in mice.
ISSN: 0362-4803
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Radiopharmaceutical Research
Nuclear Medicine & Molecular Imaging
Translational Research in GastroIntestinal Disorders
× corresponding author
# (joint) last author

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