PMID: 3746816Sep 1, 1986Paper

Potential tumor- or organ-imaging agents. 26. Polyiodinated 2-substituted triacylglycerols as hepatographic agents

Journal of Medicinal Chemistry
J P WeichertR E Counsell

Abstract

A series of omega-(3-amino-2,4,6-triiodophenyl)alkanoic acids and the corresponding 1,3-dipalmitoylglycerol 2-[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. Acid analogues 1d and 1e afforded relatively high levels of radioactivity in the liver (45 and 49% injected dose) 5 min after intravenous administration to rats. These acids displayed a marked propensity to become bound to plasma albumin. In contrast, triacylglycerol analogues 10a and 10c did not become immediately associated with plasma albumin but instead rapidly became associated with plasma lipoproteins and showed a different tissue distribution profile than free acids 1a and 1c. Although long-chain triacylglycerol analogues 10d and 10e exhibited some capacity to accumulate in the liver at 5 and 30 min, respectively, analysis of the plasma revealed significant in vivo ester hydrolysis. It would thus appear that liver radioactivity following administration of 10d and 10e was due to uptake of the free acid and not the intact triacylglycerol. Triacylglycerol analogues 10a and 10c, on the other hand, were ...Continue Reading

Citations

Nov 1, 1993·Magnetic Resonance in Medicine : Official Journal of the Society of Magnetic Resonance in Medicine·B GallezP Dumont
Jul 31, 2013·Pharmaceutical Research·Nicolas Anton, Thierry F Vandamme
Oct 18, 2000·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·D M Lambert
May 22, 2002·Academic Radiology·Julie K Doerr-StevensJamey P Weichert
Aug 3, 2014·Advanced Drug Delivery Reviews·Xiang LiThierry Vandamme
Mar 1, 1994·Journal of Pharmaceutical Sciences·D J YangS Wallace

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