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潜在的器官或肿瘤成像剂。18. 放射性碘化二胺和双季铵盐。

Potential organ- or tumor-imaging agents. 18. Radioiodinated diamines and bisquaternaries.

作者信息

Huang C C, Korn N, Counsell R E

出版信息

J Med Chem. 1979 Apr;22(4):449-52. doi: 10.1021/jm00190a018.

Abstract

The purpose of this research was to employ diamines and their quaternary derivatives as carrier molecules for gamma-emitting radiation. The diamine putrescine is widespread in nature and has been reported to selectively concentrate in the rat ventral prostate and pancreas. This study confirms the selective uptake of radioactivity in the rat ventral prostate, but not in the pancreas, following administration of [14C]putrescine. The radioiodinated analogues of putrescine showed no predilection for either of these organs. On the other hand, radioactivity associated with a radioidinated quaternary derivative (3) was found to accumulate incartilaginous tissues such as trachea, intervertebral disks, and chondrosarcoma tumor in a manner simular to hexamethonium.

摘要

本研究的目的是将二胺及其季铵衍生物用作发射γ射线的载体分子。二胺腐胺在自然界中广泛存在,据报道它能选择性地在大鼠腹侧前列腺和胰腺中富集。本研究证实,给予[14C]腐胺后,放射性在大鼠腹侧前列腺中选择性摄取,但在胰腺中则不然。腐胺的放射性碘代类似物对这两个器官均无偏好。另一方面,发现与放射性碘代季铵衍生物(3)相关的放射性以类似于六甲铵的方式在软骨组织如气管、椎间盘和软骨肉瘤肿瘤中蓄积。

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