Longino M A, Glazer G M, Weichert J P, Groziak M P, Schwendner S W, Counsell R E
J Comput Assist Tomogr. 1984 Dec;8(6):1099-104. doi: 10.1097/00004728-198412000-00010.
The synthesis and preliminary biodistribution data for a series of sterol-like esters of iopanoic acid having potential value as liver-specific CT contrast agents are described. Structural modification of the sterol portion of the iopanoate ester afforded a group of compounds that displayed tissue specificity similar to cholesteryl iopanoate, the prototype ester of this series, but were rapidly cleared from the target tissues after hydrolysis. From the biodistribution data, the most promising of these agents, pregnenolone iopanoate (PI), was evaluated by CT in rabbits receiving a radiologic dose equivalent to 30 mg I/kg. The hepatic parenchyma was enhanced within 2 h of infusion to a maximal level of 31 HU above precontrast values. Hepatic CT attenuation returned to normal within 24 h. However, CT performed after PI infusion into Vx2 tumor-bearing rabbits failed to provide superior images compared with those acquired following bolus administration of urographic contrast.
描述了一系列具有作为肝脏特异性CT造影剂潜在价值的碘番酸类甾醇酯的合成及初步生物分布数据。对碘番酸盐酯甾醇部分进行结构修饰，得到了一组化合物，它们表现出与该系列原型酯胆甾醇碘番酸盐相似的组织特异性，但在水解后能迅速从靶组织中清除。根据生物分布数据，在接受相当于30mg I/kg放射剂量的兔中，通过CT对这些试剂中最有前景的孕烯醇酮碘番酸盐（PI）进行了评估。输注后2小时内肝实质增强，比造影前值最高增加31HU。肝CT衰减在24小时内恢复正常。然而，与静脉注射尿路造影剂后获得的图像相比，将PI注入VX2荷瘤兔后进行的CT未能提供更好的图像。
