Potential tumor- or organ-imaging agents. 27. Polyiodinated 1,3-disubstituted and 1,2,3-trisubstituted triacylglycerols.
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.
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006801:Humans; D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D007553:Isotope Labeling / Q000379:methods; D008099:Liver / Q000000981:diagnostic imaging*; D009682:Magnetic Resonance Spectroscopy; D009369:Neoplasms / Q000000981:diagnostic imaging*; D011877:Radionuclide Imaging; D051381:Rats; D011919:Rats, Inbred Strains; D013053:Spectrophotometry; D013329:Structure-Activity Relationship; D014018:Tissue Distribution; D014280:Triglycerides / Q000138:chemical synthesis / Q000378:metabolism
D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D014280:Triglycerides