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The effect of lipophilicity on the hepatobiliary properties of iminodiacetic acid derivatives in the conditions of hyperbilirubinemia.

Abstract
The partition coefficients (log P) of theoretically possible alkyliodinated iminodiacetic acid (IDA) derivatives and commercial IDA derivatives were calculated using two computer programs: ChemSketch Log P and ChemOffice Ultra. Newly synthesized ligands (DIETHYLIODIDA and DIISOPROPYLIODIDA) with the highest calculated log P were labeled with technetium-99m. The biodistribution and the influence of bilirubin on their biokinetics were investigated in rats and compared to corresponding results for commercial (99m)Tc-BROMIDA. Log P of (99m)Tc-complexes of synthesized ligands were determined experimentally as well as the protein binding. In comparison to (99m)Tc-BROMIDA, (99m)Tc-DIETHYLIODIDA has: (a) better biliary excretion (2.76±0.15%ID/g versus 1.83±0.10%ID/g); (b) faster hepatic clearance (2.90±0.21%ID/g versus 7.47±0.70%ID/g) and decreased biliary excretion (for 14% versus 22%) in conditions of hyperbilirubinemia after 15min. It is proved that (99m)Tc-DIISOPROPYLIODIDA has a prolonged hepatic transit time and decreased biliary excretion.
AuthorsJ Brborić, M S Jovanović, S Vranješ-Đurić, O Cudina, B Marković, S Vladimirov
JournalApplied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine (Appl Radiat Isot) Vol. 74 Pg. 31-5 (Apr 2013) ISSN: 1872-9800 [Electronic] England
PMID23353095 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2012 Elsevier Ltd. All rights reserved.
Chemical References
  • Aniline Compounds
  • Imino Acids
  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • Technetium Tc 99m Diethyl-iminodiacetic Acid
  • technetium Tc 99m mebrofenin
  • Technetium Tc 99m Disofenin
  • Glycine
  • iminodiacetic acid
Topics
  • Aniline Compounds
  • Animals
  • Biliary Tract (diagnostic imaging)
  • Glycine
  • Hyperbilirubinemia (diagnostic imaging)
  • Imino Acids (chemistry)
  • Liver (diagnostic imaging)
  • Molecular Structure
  • Organotechnetium Compounds (chemistry)
  • Radionuclide Imaging
  • Radiopharmaceuticals (chemistry)
  • Rats
  • Rats, Wistar
  • Software
  • Technetium Tc 99m Diethyl-iminodiacetic Acid (chemistry)
  • Technetium Tc 99m Disofenin (chemistry)

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