Technetium-99m Radiolabeled Ouabagenin-Cysteine Conjugate: Biological Evaluation in Animal Models
- 作者：Chatterjee ; Mita ; Ganguly ; Shantanu ; Sarkar ; Bharat R. ; Banerjee ; Somenath
- 关键词：Ouabagenin-cystein conjugates ; Heart to blood ratio ; Sugar
- 刊名：Nuclear Medicine and Biology
- 出版年：1996
- 期刊代码：43_09698051
- 类别：ph
- 出版时间：February, 1996
- 卷：23
- 期：2
- 页码：115-120
- 文件大小：602 K
摘要
Two ouabagenin-cysteine conjugates were synthesized by condensing 3-β monochloroacetyl and 3-β, 11-α dichloroacetyl ouabagenin with cysteine. The resulting ligands were radiolabeled with technetium-99m (99mTc) to furnish a single homogeneous 99mTc chelate in each case with good stability. The animal experiments with these 99mTc-labeled conjugates established the superiority of guinea pig over rat and rabbit as an animal model, as previously observed for other tritiated or radioiodinated cardiac glycosides or aglycones. In biodistribution experiments in guinea pig, these 99mTc chelates showed a favorable heart to liver (and other nontarget organ) uptake ratio, comparable to that of recently reported 125I-digoxigenin iodohistamine-3-oxime. The low heart to blood ratio in animal experiments with ouabagenin derivatives could be attributed to the absence of 3-β sugar residues in these molecules, which is in agreement with the previous observation reported in connection with radioiodinated digoxin and digoxigenin derivatives.