N,N?,N?,N?-tetraalkylcyclam derivatives: synthesis,99mTc-labelling and biological properties
作者:Jae Min Jeong、Sung Hyun Hong、Young Joo Kim、Dong Soo Lee、June-Key Chung、Jung-Hyuck Cho、Myung Chul Lee
DOI:10.1002/jlcr.448
日期:2001.3.30
We synthesized N,N′,N″,N‴-tetraalkylcyclam derivatives in which alkyl groups were ethyl, propyl, butyl, methoxyethyl, and ethoxyethyl. We attempted to label the compounds with 99mTc. The cyclams with methyl, ethyl, and propyl could be labelled. The labelled N,N′,N″,N‴-tetraalkylcyclam derivatives showed +1 charge. They excreted rapidly through the kidney in mice. The liver-uptake increased slightly as the lipophilicity increased. However, the myocardial uptake was low unlikely with the +1 charged myocardial imaging agents. Copyright © 2001 John Wiley & Sons, Ltd.
我们合成了 N,N′,N″,N‴-四烷基环丙胺衍生物,其中的烷基包括乙基、丙基、丁基、甲氧基乙基和乙氧基乙基。我们尝试用 99mTc 标记这些化合物。含有甲基、乙基和丙基的环戊烷可以被标记。被标记的 N,N′,N″,N‴-四烷基环丙烷衍生物显示+1电荷。它们在小鼠体内通过肾脏迅速排泄。随着亲脂性的增加,肝脏摄取量也略有增加。不过,心肌摄取量较低,这与+1电荷心肌成像剂的摄取量不同。Copyright © 2001 John Wiley & Sons, Ltd. All Rights Reserved.