The preparation of123/125I-clioquinol for the study of Aβ protein in Alzheimer's disease
| العنوان: | The preparation of123/125I-clioquinol for the study of Aβ protein in Alzheimer's disease |
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| المؤلفون: | Victor L. Villemagne, Andrew Katsifis, Terri Jackson, Vahan Papazian, T. Pham, Christopher C. Rowe, Christian Loc'h, C.L. Masters, Ivan Greguric, Xiang Liu |
| المصدر: | Journal of Labelled Compounds and Radiopharmaceuticals. 48:473-484 |
| بيانات النشر: | Wiley, 2005. |
| سنة النشر: | 2005 |
| مصطلحات موضوعية: | Chemistry, Clioquinol, Organic Chemistry, Radiochemistry, chemistry.chemical_element, Halogenation, Zinc, Biochemistry, High-performance liquid chromatography, Analytical Chemistry, Spect imaging, Drug Discovery, Iodine-123, medicine, Radiology, Nuclear Medicine and imaging, Chelation, Specific activity, Spectroscopy, medicine.drug |
| الوصف: | Clioquinol or 5-chloro-7-iodo-8-hydroxyquinoline (CQ) is a lipophilic hydroxyquinoline currently under investigation for the treatment of Alzheimer's disease by targeted copper and zinc chelation. CQ was radiolabelled with no-carrier-added iodine-123/125 to give high specific activity analogs for SPECT imaging and biochemical studies. 123I-clioquinol (123I-CQ) was prepared by direct iodination of the activated hydroxyquinoline using a variety of oxidants. Highest yields (>85%) and purity were obtained when chloramine-T or iodogen at pH 4–5 was used. Large-scale radiolabelled 123I-CQ was purified by reverse-phase HPLC using a C-18 small ‘Rocket®’ column. The radiochemical purity of 123I-CQ as assessed by analytical HPLC was 99.1±0.6% (n = 9) with specific activity higher than 3 GBq/nmol for 123I-CQ and 80 MBq/nmol for 125I-CQ. The total preparation time was 40 min and starting from 3.7 GBq of iodine-123, more than 2.5 GBq of formulated 123I-CQ as radiopharmaceutical was available for clinical investigations. Using the same method of preparation, 125I-CQ was produced in radiochemical and chemical purity higher than 97% with a specific activity of 80 MBq/nmol. Copyright © 2005 John Wiley & Sons, Ltd. |
| تدمد: | 1099-1344 0362-4803 |
| DOI: | 10.1002/jlcr.942 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_________::e50611c7989902aaf930f343b026a9ca https://doi.org/10.1002/jlcr.942 |
| Rights: | CLOSED |
| رقم الانضمام: | edsair.doi...........e50611c7989902aaf930f343b026a9ca |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 10991344 03624803 |
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| DOI: | 10.1002/jlcr.942 |