Coulais Y, Cros G, Darbieu M H, Tafani J A, Belhadj-Tahar H, Bellande E, Pasqualini R, Guiraud R
Laboratoire de Biophysique et de Médecine Nucléaire, Faculté de Médecine Toulouse-Purpan, France.
Nucl Med Biol. 1994 Feb;21(2):263-8. doi: 10.1016/0969-8051(94)90018-3.
The synthesis, characterization and 99mTc labelling of unsaturated diamino dithiol ligands with methyl dithiocarboxylate functions: 2-aminocyclopentene-1-dithiocarboxylic methyl ester (H2L1), N,N'-ethylene bis(methyl 2-aminocyclopentene-1-dithiocarboxylate) (H2L2) and N,N'-propylene bis (methyl 2-aminocyclopentene-1-dithiocarboxylate) (H2L3) are described. Cationic oxo (Tc = O) and neutral nitrido (Tc = N) complexes were obtained. Biodistribution studies in rat showed a good heart uptake of 99mTcN-L2 (2% ID at 5 min) with a high heart-to-blood ratio (5.8 at 5 min), but this complex also exhibited high lung and liver uptake.
具有甲基二硫代羧酸酯功能的不饱和二氨基二硫醇配体的合成、表征及99mTc标记：2-氨基环戊烯-1-二硫代羧酸甲酯（H2L1）、N,N'-亚乙基双（2-氨基环戊烯-1-二硫代羧酸甲酯）（H2L2）和N,N'-亚丙基双（2-氨基环戊烯-1-二硫代羧酸甲酯）（H2L3）。得到了阳离子氧代（Tc = O）和中性氮代（Tc = N）配合物。大鼠体内生物分布研究表明，99mTcN-L2在心脏摄取良好（5分钟时为2%注射剂量），心脏与血液的比例较高（5分钟时为5.8），但该配合物在肺和肝脏中的摄取也较高。
