The effect of lipophilicity on the hepatobiliary properties of iminodiacetic acid derivatives in the conditions of hyperbilirubinemia
Samo za registrovane korisnike
2013
Autori
Brborić, JasminaJovanović, M.S.
Vranješ-Đurić, Sanja D.
Čudina, Olivera
Marković, Bojan
Vladimirov, Sote
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
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.
Ključne reči:
DIETHYLIODIDA / DIISOPROPYLIODIDA / BROMIDA / Lipophilicity / Hepatobiliary scintigraphyIzvor:
Applied Radiation and Isotopes, 2013, 74, 31-35Izdavač:
- Pergamon-Elsevier Science Ltd, Oxford
Finansiranje / projekti:
- Razvoj molekula sa antiinflamatornim i kardioproaktivnim dejstvom: strukturne modifikacije, modelovanje, fizičkohemijska karakterizacija i formulaciona ispitivanja (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
Institucija/grupa
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 . .