潜在的肿瘤或器官成像剂。30. 放射性碘化磷脂醚。

Potential tumor or organ-imaging agents. 30. Radioiodinated phospholipid ethers.

作者信息

Meyer K L, Schwendner S W, Counsell R E

机构信息

Department of Medicinal Chemistry, University of Michigan, Ann Arbor 48109.

出版信息

J Med Chem. 1989 Sep;32(9):2142-7. doi: 10.1021/jm00129a020.

DOI:10.1021/jm00129a020

PMID:2769685

Abstract

A radioiodinated analogue of a naturally occurring alkyl lysophospholipid (ALP) was synthesized for evaluation as a potential tumor-localizing imaging agent. rac-1-[12-(m-Iodophenyl)dodecyl]-2-methylglycero-3-phosphocholine (ET-12IP-OMe, 14) was radiolabeled with iodine-125 via an isotope-exchange procedure. Tissue distribution studies with [125I]ET-12IP-OMe in tumor-bearing rats revealed an immediate tumor uptake of radioactivity. Although radioactivity was also present in nontarget tissues at this time, clearance of tracer from the tumor was much slower and thus provided a suitable tumor to nontarget tissue ratio at 24 h. As a result of this selective accumulation, it was possible to clearly delineate the tumor with gamma-camera scintigraphy.

摘要

合成了一种天然存在的烷基溶血磷脂（ALP）的放射性碘化类似物，以评估其作为潜在的肿瘤定位显像剂的性能。rac-1-[12-(间碘苯基)十二烷基]-2-甲基甘油-3-磷酸胆碱（ET-12IP-OMe，14）通过同位素交换程序用碘-125进行放射性标记。用[125I]ET-12IP-OMe对荷瘤大鼠进行的组织分布研究显示，放射性立即被肿瘤摄取。虽然此时非靶组织中也存在放射性，但示踪剂从肿瘤中的清除要慢得多，因此在24小时时提供了合适的肿瘤与非靶组织比率。由于这种选择性聚集，可以用γ相机闪烁显像清楚地勾勒出肿瘤轮廓。