| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1228765 | Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy | 2016 | 6 Pages |
•Two ligands Met-ac-TE3A and Bis(thiosemicarbazone)- Biotin has been compared.•In vitro human serum stability of were found to be 96.5% and 97.0% respectively.•Blood kinetics of both ligands in normal rabbits showed biphasic clearance pattern.•Significant initial tumor uptake and high tumor/muscles ratio
2,2′,2″-(11-(2-((4-mercapto-1-methoxy-1-oxobutan-2-yl)amino)-2-oxoethyl)-1,4,8,11-tetraaza cyclotetradecane-1,4,8-triyl)triacetic acid, Met-ac-TE3A and (E)-N-methyl-2-((E)-3-(2-(2-(5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanoyl)hydrazinecarbono-thioyl)hydrazonobutan-2-ylidene)hydrazinecarbothioamide, Bis(thiosemicarbazone)- Biotin were synthesized and evaluated for imaging application. The pharmacokinetics of these ligands were determined by tracer methods. In vitro human serum stability of 99mTc Met-ac-TE3A/99mTc Bis(thiosemicarbazone)-Biotin after 24 h was found to be 96.5% and 97.0% respectively. Blood kinetics of both ligands in normal rabbits showed biphasic clearance pattern. Ex vivo biodistribution study revealed significant initial tumor uptake and high tumor/muscles ratio which is a pre-requisite condition for a ligand to work as SPECT-radiopharmaceutical for tumor imaging.
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