Seevers R H, Groziak M P, Weichert J P, Schwendner S W, Szabo S M, Longino M A, Counsell R E
J Med Chem. 1982 Dec;25(12):1500-3. doi: 10.1021/jm00354a022.
A series of sterol esters of iopanoic acid was synthesized and evaluated for their potential to selectively localize in liver and steroid-secreting tissues for possible application in either computed tomography or nuclear medicine imaging. Unlike free iopanoic acid (1), which was rapidly cleared following intravenous administration to rats, cholesteryl iopanoate (2) was found to accumulate in liver, adrenal cortex, and ovary. At 24 h, the ovary was found to contain the highest concentration of 2. The ability of 2 to accumulate in the above tissues was attributed to its resistance to hydrolysis. Pregnenolone iopanoate (3) and dehydroepiandrosterone iopanoate (4), on the other hand, were shown to reach unusually high concentrations in the adrenal cortex within 0.5 h of administration but declined to much lower levels by 24 h. Lipid extraction of tissues showed 3 and 4 to be susceptible to in vivo hydrolysis, which undoubtedly was a major factor in their clearance from adrenal tissue.
合成了一系列碘番酸的甾醇酯，并评估了它们在肝脏和类固醇分泌组织中选择性定位的潜力，以用于计算机断层扫描或核医学成像。与静脉注射给大鼠后迅速清除的游离碘番酸（1）不同，碘番酸胆固醇酯（2）被发现积聚在肝脏、肾上腺皮质和卵巢中。在24小时时，发现卵巢中2的浓度最高。2在上述组织中积聚的能力归因于其抗水解性。另一方面，孕烯醇酮碘番酸酯（3）和脱氢表雄酮碘番酸酯（4）在给药后0.5小时内在肾上腺皮质中达到异常高的浓度，但到24小时时降至低得多的水平。组织的脂质提取显示3和4易受体内水解作用的影响，这无疑是它们从肾上腺组织中清除的主要因素。
