The effect of lipophilicity on the hepatobiliary properties of iminodiacetic acid derivatives in the conditions of hyperbilirubinemia
Само за регистроване кориснике
2013
Аутори
Brborić, JasminaJovanović, M.S.
Vranješ-Đurić, Sanja D.
Čudina, Olivera
Marković, Bojan
Vladimirov, Sote
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
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.
Кључне речи:
DIETHYLIODIDA / DIISOPROPYLIODIDA / BROMIDA / Lipophilicity / Hepatobiliary scintigraphyИзвор:
Applied Radiation and Isotopes, 2013, 74, 31-35Издавач:
- Pergamon-Elsevier Science Ltd, Oxford
Финансирање / пројекти:
- Развој молекула са антиинфламаторним и кардиопроактивним дејством: структурне модификације, моделовање, физичкохемијска карактеризација и формулациона испитивања (RS-MESTD-Basic Research (BR or ON)-172041)
DOI: 10.1016/j.apradiso.2012.12.014
ISSN: 0969-8043
PubMed: 23353095
WoS: 000316978400007
Scopus: 2-s2.0-84872957304
Институција/група
PharmacyTY - 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 . .