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The effect of lipophilicity on the hepatobiliary properties of iminodiacetic acid derivatives in the conditions of hyperbilirubinemia.
MedLine Citation:
PMID:  23353095     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
J Brborić; M S Jovanović; S Vranješ-Đurić; O Cudina; B Marković; S Vladimirov
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-3
Journal Detail:
Title:  Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine     Volume:  74C     ISSN:  1872-9800     ISO Abbreviation:  Appl Radiat Isot     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-28     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9306253     Medline TA:  Appl Radiat Isot     Country:  -    
Other Details:
Languages:  ENG     Pagination:  31-35     Citation Subset:  -    
Copyright Information:
Copyright © 2012 Elsevier Ltd. All rights reserved.
Affiliation:
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, PO Box 146, Vojvode Stepe 450, 11000 Belgrade, Serbia.
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