Correlation between lipophilicity of the ligands and the hepatobiliary properties of the radiopharmaceuticals: Approach to the development of new IDA derivatives
Само за регистроване кориснике
2000
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
The partition coefficient (log P) for n-octanol/water system was calculated applying PACO program for various theoretically possible mono and dihalogenated IDA derivatives. Some of the synthesized ligands (SOLCOIODIDA, IODIDA and DIIODIDA) were labeled with the technetium-99m. The biodistribution and influence of bilirubin on their biokinetics were investigated in rats. The correlation between partition coefficients of ligands increase (log P) and better hepatobiliary properties of Tc-99m-IDA derivatives was determined. The values of log P increase from 1.16 for SOLCOIODIDA, 3.11 for IODIDA to 3.47 for DIIODIDA. In correlation with these results, biliary excretion decreased for 59% for Tc-99m-SOLCOIODIDA and 11% for Tc-99m-IODIDA and Tc-99m-DIIODIDA under hyperbilirubinemia (3.5 min after injection) and 45%, 11% and 0.38% respectively (15 min after injection). The highest biliary excretion had Tc-99m-DIIODIDA (55.4% for 3.5 min). Considering the correlation between hepatobiliary proper...ties and log P, the evaluation of biological properties for various trifluoromethyl mono and dihalogenated IDA derivatives was performed on the basis of the calculated log P in order to synthetize a new radiopharmaceutical for hepatobiliary scintigraphy.
Извор:
Journal of Radioanalytical and Nuclear Chemistry, 2000, 245, 3, 555-560Издавач:
- Kluwer Academic Publ, Dordrecht
DOI: 10.1023/A:1006709310527
ISSN: 0236-5731
WoS: 000089673500015
Scopus: 2-s2.0-0033802493
Институција/група
PharmacyTY - JOUR AU - Jovanović, MS AU - Brborić, Jasmina AU - Vladimirov, S AU - Suturkova, L PY - 2000 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/236 AB - The partition coefficient (log P) for n-octanol/water system was calculated applying PACO program for various theoretically possible mono and dihalogenated IDA derivatives. Some of the synthesized ligands (SOLCOIODIDA, IODIDA and DIIODIDA) were labeled with the technetium-99m. The biodistribution and influence of bilirubin on their biokinetics were investigated in rats. The correlation between partition coefficients of ligands increase (log P) and better hepatobiliary properties of Tc-99m-IDA derivatives was determined. The values of log P increase from 1.16 for SOLCOIODIDA, 3.11 for IODIDA to 3.47 for DIIODIDA. In correlation with these results, biliary excretion decreased for 59% for Tc-99m-SOLCOIODIDA and 11% for Tc-99m-IODIDA and Tc-99m-DIIODIDA under hyperbilirubinemia (3.5 min after injection) and 45%, 11% and 0.38% respectively (15 min after injection). The highest biliary excretion had Tc-99m-DIIODIDA (55.4% for 3.5 min). Considering the correlation between hepatobiliary properties and log P, the evaluation of biological properties for various trifluoromethyl mono and dihalogenated IDA derivatives was performed on the basis of the calculated log P in order to synthetize a new radiopharmaceutical for hepatobiliary scintigraphy. PB - Kluwer Academic Publ, Dordrecht T2 - Journal of Radioanalytical and Nuclear Chemistry T1 - Correlation between lipophilicity of the ligands and the hepatobiliary properties of the radiopharmaceuticals: Approach to the development of new IDA derivatives VL - 245 IS - 3 SP - 555 EP - 560 DO - 10.1023/A:1006709310527 ER -
@article{ author = "Jovanović, MS and Brborić, Jasmina and Vladimirov, S and Suturkova, L", year = "2000", abstract = "The partition coefficient (log P) for n-octanol/water system was calculated applying PACO program for various theoretically possible mono and dihalogenated IDA derivatives. Some of the synthesized ligands (SOLCOIODIDA, IODIDA and DIIODIDA) were labeled with the technetium-99m. The biodistribution and influence of bilirubin on their biokinetics were investigated in rats. The correlation between partition coefficients of ligands increase (log P) and better hepatobiliary properties of Tc-99m-IDA derivatives was determined. The values of log P increase from 1.16 for SOLCOIODIDA, 3.11 for IODIDA to 3.47 for DIIODIDA. In correlation with these results, biliary excretion decreased for 59% for Tc-99m-SOLCOIODIDA and 11% for Tc-99m-IODIDA and Tc-99m-DIIODIDA under hyperbilirubinemia (3.5 min after injection) and 45%, 11% and 0.38% respectively (15 min after injection). The highest biliary excretion had Tc-99m-DIIODIDA (55.4% for 3.5 min). Considering the correlation between hepatobiliary properties and log P, the evaluation of biological properties for various trifluoromethyl mono and dihalogenated IDA derivatives was performed on the basis of the calculated log P in order to synthetize a new radiopharmaceutical for hepatobiliary scintigraphy.", publisher = "Kluwer Academic Publ, Dordrecht", journal = "Journal of Radioanalytical and Nuclear Chemistry", title = "Correlation between lipophilicity of the ligands and the hepatobiliary properties of the radiopharmaceuticals: Approach to the development of new IDA derivatives", volume = "245", number = "3", pages = "555-560", doi = "10.1023/A:1006709310527" }
Jovanović, M., Brborić, J., Vladimirov, S.,& Suturkova, L.. (2000). Correlation between lipophilicity of the ligands and the hepatobiliary properties of the radiopharmaceuticals: Approach to the development of new IDA derivatives. in Journal of Radioanalytical and Nuclear Chemistry Kluwer Academic Publ, Dordrecht., 245(3), 555-560. https://doi.org/10.1023/A:1006709310527
Jovanović M, Brborić J, Vladimirov S, Suturkova L. Correlation between lipophilicity of the ligands and the hepatobiliary properties of the radiopharmaceuticals: Approach to the development of new IDA derivatives. in Journal of Radioanalytical and Nuclear Chemistry. 2000;245(3):555-560. doi:10.1023/A:1006709310527 .
Jovanović, MS, Brborić, Jasmina, Vladimirov, S, Suturkova, L, "Correlation between lipophilicity of the ligands and the hepatobiliary properties of the radiopharmaceuticals: Approach to the development of new IDA derivatives" in Journal of Radioanalytical and Nuclear Chemistry, 245, no. 3 (2000):555-560, https://doi.org/10.1023/A:1006709310527 . .