申请人:University Patents, Inc.
公开号:US04444690A1
公开(公告)日:1984-04-24
A new series of technetium chelating agents based on amide and mercaptide donor groups is described, exemplified by 2,3-bis(mercaptoacetamido)propanoic acid. Chelation of Tc-99 m with 2,3-bis(mercaptoacetamido)propanoic acid resulted in two components that were separable by high-performance liquid chromatography. The component that eluted first demonstrated high specificity for renal excretion with over 90% in the urine in rabbits at 35 minutes and 87% in the urine of mice at 2 hours and 1.6% or less in the intestines of mice. Excretion was rapid with the first component equal to or greater than I-131 Hippuran in the urine of rabbits at all times. The second or latter component demonstrated comparable specificity, but slower renal excretion kinetics. 2,3-Bis-(mercaptoacetamido)succinic acid forms similar chelates with technetium which are also useful as radiopharmaceuticals for the renal systems of mammals.
本文介绍了一系列基于酰胺和巯基供体基团的锝螯合剂,以2,3-双(巯乙酰胺基)丙酸为例。使用2,3-双(巯乙酰胺基)丙酸对Tc-99m进行螯合,结果得到两个组分,可通过高效液相色谱法分离。第一个洗脱组分表现出高度的肾排泄特异性,在35分钟内,兔子的尿液中有90%以上,小鼠的尿液中有87%在2小时内,小鼠肠道中的含量为1.6%或更少。第一个组分的排泄速度很快,在兔子的尿液中,第一个组分在任何时候都等于或高于I-131 Hippuran。第二个组分表现出类似的特异性,但肾排泄动力学较慢。2,3-双(巯乙酰胺基)琥珀酸与锝形成类似的螯合物,也可用作哺乳动物肾系统的放射性药物。