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 Tc-99m-BROMIDA. Log P of Tc-99m-complexes of synthesized ligands were determined experimentally as well as the protein binding. In comparison to Tc-99m-BROMIDA, Tc-99m-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 15 min. It is proved that Tc-99m-DIISOPROPYLIODIDA has... a prolonged hepatic transit time and decreased biliary excretion.
TY - JOUR
AU - Brborić, Jasmina
AU - Jovanović, M.S.
AU - Vranješ-Đurić, Sanja D.
AU - Čudina, Olivera
AU - Marković, Bojan
AU - Vladimirov, Sote
PY - 2013
UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1932
AB - 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 Tc-99m-BROMIDA. Log P of Tc-99m-complexes of synthesized ligands were determined experimentally as well as the protein binding. In comparison to Tc-99m-BROMIDA, Tc-99m-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 15 min. It is proved that Tc-99m-DIISOPROPYLIODIDA has a prolonged hepatic transit time and decreased biliary excretion.
PB - Pergamon-Elsevier Science Ltd, Oxford
T2 - Applied Radiation and Isotopes
T1 - The effect of lipophilicity on the hepatobiliary properties of iminodiacetic acid derivatives in the conditions of hyperbilirubinemia
VL - 74
SP - 31
EP - 35
DO - 10.1016/j.apradiso.2012.12.014
ER -
@article{
author = "Brborić, Jasmina and Jovanović, M.S. and Vranješ-Đurić, Sanja D. and Čudina, Olivera and Marković, Bojan and Vladimirov, Sote",
year = "2013",
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 Tc-99m-BROMIDA. Log P of Tc-99m-complexes of synthesized ligands were determined experimentally as well as the protein binding. In comparison to Tc-99m-BROMIDA, Tc-99m-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 15 min. It is proved that Tc-99m-DIISOPROPYLIODIDA has a prolonged hepatic transit time and decreased biliary excretion.",
publisher = "Pergamon-Elsevier Science Ltd, Oxford",
journal = "Applied Radiation and Isotopes",
title = "The effect of lipophilicity on the hepatobiliary properties of iminodiacetic acid derivatives in the conditions of hyperbilirubinemia",
volume = "74",
pages = "31-35",
doi = "10.1016/j.apradiso.2012.12.014"
}
Brborić, J., Jovanović, M.S., Vranješ-Đurić, S. D., Čudina, O., Marković, B.,& Vladimirov, S.. (2013). The effect of lipophilicity on the hepatobiliary properties of iminodiacetic acid derivatives in the conditions of hyperbilirubinemia. in Applied Radiation and Isotopes
Pergamon-Elsevier Science Ltd, Oxford., 74, 31-35.
https://doi.org/10.1016/j.apradiso.2012.12.014
Brborić J, Jovanović M, Vranješ-Đurić SD, Čudina O, Marković B, Vladimirov S. The effect of lipophilicity on the hepatobiliary properties of iminodiacetic acid derivatives in the conditions of hyperbilirubinemia. in Applied Radiation and Isotopes. 2013;74:31-35.
doi:10.1016/j.apradiso.2012.12.014 .
Brborić, Jasmina, Jovanović, M.S., Vranješ-Đurić, Sanja D., Čudina, Olivera, Marković, Bojan, Vladimirov, Sote, "The effect of lipophilicity on the hepatobiliary properties of iminodiacetic acid derivatives in the conditions of hyperbilirubinemia" in Applied Radiation and Isotopes, 74 (2013):31-35,
https://doi.org/10.1016/j.apradiso.2012.12.014 . .
