Weichert J P, Groziak M P, Longino M A, Schwendner S W, Counsell R E
J Med Chem. 1986 Dec;29(12):2457-65. doi: 10.1021/jm00162a007.
A series of glyceryl 1,3-bis- and 1,2,3-tris[omega-(3-amino-2,4,6-triiodophenyl)alkanoates] were synthesized, radioiodinated with iodine-125, and evaluated for their ability to selectively localize in the liver for potential use as hepatographic imaging agents. Of the nine target compounds synthesized and evaluated in rats, glyceryl 1,2,3-tris[3-(3-amino-2,4,6-triiodophenyl)propionate] (5b) displayed rapid and sustained liver specificity. This agent was found to accumulate in the liver in concentrations of 60, 75, and 86% of the administered dose at 5 min, 30 min, and 24 h, respectively. Moreover, the 24-h liver-to-blood ratio of 235 justifies further studies in higher animal species.
合成了一系列甘油1,3 - 双[ω-(3 - 氨基 - 2,4,6 - 三碘苯基)链烷酸酯]和甘油1,2,3 - 三[ω-(3 - 氨基 - 2,4,6 - 三碘苯基)链烷酸酯],用碘 - 125进行放射性碘化,并评估它们在肝脏中选择性定位的能力,以潜在用作肝脏造影成像剂。在合成并在大鼠中评估的九种目标化合物中,甘油1,2,3 - 三3 - (3 - 氨基 - 2,4,6 - 三碘苯基)丙酸酯表现出快速且持续的肝脏特异性。发现该药剂在5分钟、30分钟和24小时时在肝脏中的蓄积量分别为给药剂量的60%、75%和86%。此外,24小时肝脏与血液的比值为235,这证明有必要在更高等动物物种中进一步研究。