Weichert J P, Longino M A, Bakan D A, Spigarelli M G, Chou T S, Schwendner S W, Counsell R E
Department of Radiology, University of Michigan Medical Center, Ann Arbor 48109.
J Med Chem. 1995 Feb 17;38(4):636-46. doi: 10.1021/jm00004a010.
A series of glyceryl 2-oleoyl 1,3-bis[omega-(3-amino-2,4,6-triiodophenyl)] alkanoates was synthesized, radioiodinated with iodine-125, emulsified, and evaluated for their ability to selectively localize in the liver for potential use as hepatographic agents in computed tomography. All seven analogs displayed rapid liver uptake wherein between 65 and 78% of the injected dose accumulated in the liver by 30 min. Liver values ranged from 46 to 93% 3 h after injection which corresponded to liver to blood ratios ranging from 21 to 450. Moreover, subsequent elimination of radioactivity from the liver was nearly linear with respect to alkyl chain length. Analogs with longer alkyl chain length were eliminated from the liver more rapidly than their shorter chain counterparts. Because of their biochemical similarities to naturally occurring triglycerides, these novel analogs may prove useful not only for high-resolution anatomic imaging of focal liver lesions, but also for evaluating a variety of diffuse diseases known to affect hepatic function and biochemistry.
合成了一系列2-油酰基-1,3-双[ω-(3-氨基-2,4,6-三碘苯基)]甘油链烷酸酯,用碘-125进行放射性碘化,制成乳剂,并评估它们在肝脏中选择性定位的能力,以作为计算机断层扫描中的肝脏造影剂。所有七种类似物均显示出快速的肝脏摄取,在30分钟时,注射剂量的65%至78%积聚在肝脏中。注射后3小时肝脏摄取值在46%至93%之间,这对应于肝脏与血液的比率在21至450之间。此外,肝脏中放射性的后续消除与烷基链长度几乎呈线性关系。烷基链长度较长的类似物比链长度较短的类似物从肝脏中消除得更快。由于它们与天然存在的甘油三酯具有生化相似性,这些新型类似物不仅可能对肝脏局灶性病变的高分辨率解剖成像有用,而且对评估已知影响肝功能和生物化学的各种弥漫性疾病也可能有用。