放射性碘化烷基磷胆碱衍生物在肿瘤中的选择性定位。

Selective localization of radioiodinated alkylphosphocholine derivatives in tumors.

作者信息

Plotzke K P, Haradahira T, Stancato L, Olken N M, Skinner S, Gross M D, Wahl R L, Counsell R E

机构信息

Department of Pharmacology, University of Michigan, Ann Arbor 48109.

出版信息

Int J Rad Appl Instrum B. 1992 Oct;19(7):765-73. doi: 10.1016/0883-2897(92)90138-o.

DOI:10.1016/0883-2897(92)90138-o

PMID:1399698

Abstract

We have designed and synthesized two radioiodinated analogs of hexadecylphosphocholine in order to evaluate their tumor imaging potential. 12-(m[125I]iodophenyl)dodecyl phosphocholine (NM-324) and hexadecyl-2-[N,N-dimethyl-N-(m[125I]iodobenzyl)-ammonium] ethyl phosphate (NM-326) demonstrated the ability of such compounds to localize in and thereby visualize the Walker 256 tumor in rats. However, the tumor avidity of NM-324 was far superior to NM-326. In addition, NM-324 showed excellent tumor localization in athymic mice bearing subcutaneous human tumors.

摘要

我们设计并合成了十六烷基磷胆碱的两种放射性碘化类似物，以评估它们的肿瘤成像潜力。12-(间[¹²⁵I]碘苯基)十二烷基磷胆碱(NM-324)和十六烷基-2-[N,N-二甲基-N-(间[¹²⁵I]碘苄基)铵]乙基磷酸酯(NM-326)证明了这类化合物在大鼠Walker 256肿瘤中定位并由此使其显影的能力。然而，NM-324对肿瘤的亲和力远优于NM-326。此外，NM-324在携带皮下人肿瘤的无胸腺小鼠中显示出优异的肿瘤定位效果。