放射性碘化烷基磷胆碱衍生物在肿瘤中的选择性定位

Kathleen P. Plotzke , Terushi Haradahira , Louis Stancato , Norman M. Olken , Scott Skinner , Milton D. Gross , Richard L. Wahl , Raymond E. Counsell
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引用次数: 8

摘要

我们设计并合成了两种放射性碘化的十六烷基磷胆碱类似物,以评估它们的肿瘤成像潜力。12-(m[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-(m[125I]碘苯铵]磷酸乙酯(NM-326)证明了这些化合物在大鼠Walker 256肿瘤中的定位能力,从而使其可视化。但NM-324的肿瘤亲和性远优于NM-326。此外,NM-324在患有人皮下肿瘤的胸腺小鼠中表现出良好的肿瘤定位。
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Selective localization of radioiodinated alkylphosphocholine derivatives in tumors

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.

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