潜在的器官或肿瘤成像剂。22. 酰基标记的胆固醇酯。

Potential organ- or tumor-imaging agents. 22. Acyl-labeled cholesterol esters.

作者信息

Seevers R H, Schwendner S W, Swayze S L, Counsell R E

出版信息

J Med Chem. 1982 Jun;25(6):618-21. doi: 10.1021/jm00348a002.

Abstract

A series of cholesteryl phenylalkanoic esters was synthesized in which the acyl moiety served as the carrier for radioiodine. Tissue distribution studies in rats revealed that several of these radioiodinated esters selectively accumulated in steroid-secreting tissues, such as the adrenal cortex and ovary. Furthermore, this selective uptake was shown to correlate with the stability of these esters to in vivo hydrolysis. An unexpected finding was the unusually high propensity of some of these esters to localize in the ovary and thus afford a possible approach to ovarian imaging agents.

摘要

合成了一系列胆固醇基苯基链烷酸酯，其中酰基部分作为放射性碘的载体。对大鼠的组织分布研究表明，这些放射性碘化酯中的几种选择性地积聚在分泌类固醇的组织中，如肾上腺皮质和卵巢。此外，这种选择性摄取与这些酯在体内水解的稳定性相关。一个意外的发现是，其中一些酯具有异常高的倾向定位于卵巢，从而为卵巢成像剂提供了一种可能的方法。