一种源自N-(2-吡啶甲基)-N'-(水杨醛亚胺基)-1,3-丙二胺的单阳离子铜(II)放射性药物的合成与评价

Synthesis and evaluation of a monocationic copper(II) radiopharmaceutical derived from N-(2-pyridylmethyl)-N'-(salicylaldimino)-1,3-propanediamine.

作者信息

Sri-Aran M, Mathias C J, Lim J K, Green M A

机构信息

Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana 47907-1333, USA.

出版信息

Nucl Med Biol. 1998 Feb;25(2):107-10. doi: 10.1016/s0969-8051(97)00164-9.

DOI:10.1016/s0969-8051(97)00164-9

PMID:9468024

Abstract

The monocationic 67Cu complex of N-(2-pyridylmethyl)-N'-(salicylaldimino)-1,3-propanediamine was obtained in high radiochemical purity by reaction of 67Cu2+ with the ligand in ethanol solution. Although this compound exhibited low heart uptake, the desired myocardial retention was observed over the 30 min time period studied in a rat model. Since the octanol/water partition coefficient of [67Cu]Cu(II)-N-(2-pyridylmethyl)-N'-(salicylaldiminato)-1,3- propanediamine] is lower than a value believed to be the optimal myocardial uptake, it is likely that derivatives of this compound with a higher lipophilicity merit further investigation for use in myocardial imaging with copper radioisotopes.

摘要

通过在乙醇溶液中使(^{67}Cu^{2 + })与配体反应，获得了放射性化学纯度高的(N - (2 - 吡啶甲基)-N' - (水杨醛亚氨基)-1,3 - 丙二胺的单阳离子(^{67}Cu)配合物。尽管该化合物在心脏中的摄取量较低，但在大鼠模型中研究的30分钟时间段内观察到了预期的心肌滞留。由于([^{67}Cu]Cu(II)-N - (2 - 吡啶甲基)-N' - (水杨醛亚胺基)-1,3 - 丙二胺])的正辛醇/水分配系数低于被认为是最佳心肌摄取的值，因此该化合物具有更高亲脂性的衍生物可能值得进一步研究，以用于铜放射性同位素心肌显像。