新型99mTc氧代和氮代配合物的合成、表征及生物分布，这些配合物与由2-氨基环戊烯-1-二硫代羧酸衍生的双齿和四齿不饱和NS及N2S2席夫碱形成，作为潜在的心脏成像剂。

Synthesis, characterization and biodistribution of new 99mTc oxo and nitrido complexes with bi- and tetradendate unsaturated NS and N2S2 Schiff bases derived from 2-aminocyclopentene-1-dithiocarboxylic acid as potential heart imaging agents.

作者信息

Coulais Y, Cros G, Darbieu M H, Tafani J A, Belhadj-Tahar H, Bellande E, Pasqualini R, Guiraud R

机构信息

Laboratoire de Biophysique et de Médecine Nucléaire, Faculté de Médecine Toulouse-Purpan, France.

出版信息

Nucl Med Biol. 1994 Feb;21(2):263-8. doi: 10.1016/0969-8051(94)90018-3.

DOI:10.1016/0969-8051(94)90018-3

PMID:9234292

Abstract

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.

摘要

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。