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.
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Authors | J Brborić, M S Jovanović, S Vranješ-Đurić, O Cudina, B Marković, S Vladimirov |
Journal | Applied 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 |
PMID | 23353095
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | Copyright © 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
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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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