Preparation and physicochemical characterization of novel [131I]I-pramipexole labeled compound as potential agents for brain imaging.

Autor: Wibawa, Teguh Hafiz Ambar, Widyasari, Eva Maria, Sriyani, Maula Eka, Wongso, Hendris, Setiadi, Yanuar, Febrian, Muhamad Basit, Rattyananda, Badra Sanditya, Mahendra, Isa, Kurniawan, Ahmad, Halimah, Iim, Kusumaningrum, Christerra Ellen, Rizaludin, Asep, Nuraeni, Witri, Rosyidiah, Endah, Mulyati, Titin Sri
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Zdroj: AIP Conference Proceedings; 2024, Vol. 2967 Issue 1, p1-10, 10p
Abstrakt: Brain imaging is a technique that scientists and physicians use to view and monitor brain areas to diagnose abnormalities in the brain. This study aimed to develop a potential labeled compound for non-invasive brain imaging. Pramipexole (a drug thµat has the ability to penetrate the blood-brain barrier) has been successfully labeled iodine-131 (131I) through a diazonium salt reaction, followed by a sandmeyer reaction at room temperature, and physicochemical characterization has been carried out. The reaction parameters studied were computation simulation, pramipexole and sodium nitrite amounts, diazotization reaction time, pH of the mixture, the optimum amount of chloramine T and sodium metabisulfite, and optimum reaction time. As for the physicochemical characterization, the parameters tested were: radiochemical purity, lipophilicity, plasma protein binding, electric charges, and stability. The [131I]I-Pramipexole labeled compound showed no significant energy difference between pramipexole and pramipexole labeled 131I; the optimum condition of reaction was: pramipexole amount 100 µg, sodium nitrite 50 µg, diazotization reaction time 2-3 hours, pH of the mixture 6, chloramine T amount 50 µg, sodium metabisulfite amount 50 µg, and labeling reaction time 15 minutes at room temperature. The physicochemical characterization showed that radiochemical purity was 97.54 ± 1.4%, lipophilicity score (log P) 0.03 ± 0.01, protein plasma binding score 44.95 ± 0.80%, neutral electric charges, and [131I]I-pramipexole remained stable until 4 hours at four °C, so the [131I]I-Pramipexole labeled compound is feasible to proceed to biological studies. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index