دورية أكاديمية
[Radiosynthesis of peripheral benzodiazepine receptor radioligand [N-methyl-(11)C]PK 11195 as an imaging agent for positron emission tomography].
| العنوان: | [Radiosynthesis of peripheral benzodiazepine receptor radioligand [N-methyl-(11)C]PK 11195 as an imaging agent for positron emission tomography]. |
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| المؤلفون: | Wang MF; China Institute of Atomic Energy, Beijing 102413, China. mfwang@china.com, Tang GH, Li BY, Liang MQ, Luo ZF |
| المصدر: | Nan fang yi ke da xue xue bao = Journal of Southern Medical University [Nan Fang Yi Ke Da Xue Xue Bao] 2009 Dec; Vol. 29 (12), pp. 2425-8. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | Chinese |
| بيانات الدورية: | Publisher: Nanfang yi ke da xue xue bao bian ji bu Country of Publication: China NLM ID: 101266132 Publication Model: Print Cited Medium: Print ISSN: 1673-4254 (Print) Linking ISSN: 16734254 NLM ISO Abbreviation: Nan Fang Yi Ke Da Xue Xue Bao Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Guangzhou : Nanfang yi ke da xue xue bao bian ji bu, 2005- |
| مواضيع طبية MeSH: | Positron-Emission Tomography*, Contrast Media/*chemical synthesis , Isoquinolines/*chemical synthesis , Receptors, GABA-A/*metabolism, Animals ; Carbon Radioisotopes ; Isoquinolines/adverse effects ; Mice ; Radioligand Assay ; Radiopharmaceuticals/adverse effects ; Radiopharmaceuticals/chemical synthesis |
| مستخلص: | Objective: To establish a protocol of automated synthesis of 1-(2-chlorophenyl)-N-[(11)C]methyl-N-(1-methylpropyl)-3-isoquinoline carboxamide ((11)C-PK11195) as the positron-emitter-labeled ligand for peripheral benzodiazepine receptor (PBR) using a commercial synthesizer and explore the quality control methods for the resulting product. Methods: (11)C-methyl iodide ((11)C-CH(3)I) was synthesized via liquid-phase distillation approach using a (11)C-iodomethane synthesizer. (11)C-PK11195 was prepared by (11)C-methylation of 1-(2-chlorophenyl)-N-(1-methylpropyl)-3-isoquinoline carboxamide (N-demethyl-PK 11195) as the precursor with (11)C-CH(3)I and purified by semi-preparative reversed phase high performance liquid chromatography (HPLC). The radiochemical purity, chemical purity and stability of the product were evaluated by HPLC, and the toxicity was assessed in normal mice. The factors that affected (11)C-PK11195 synthesis were also studied. Results: (11)C-PK11195 was successfully synthesized using the TracerLab FX(F-N) synthesizer. The synthesis time was about 35 min from the end of (11)C-carbon dioxide production by cyclotron to the end of (11)C-PK11195 synthesis (EOS), with a (11)C-methylation reaction time of 3-4 min. The uncorrected radiochemical yield for (11)C-methylation was (33-/+5)%. Analysis with radio-analytical HPLC showed a radiochemical purity and chemical purity of the product both exceeding 99%, with a specific radioactivity of 30-65 GBq/micromol at EOS (from the end of radionuclide production). The (11)C-PK11195 synthesized was radiochemically stable at room temperature and showed low toxicity in normal mice. Conclusion: The (11)C-PK11195 injection can be conveniently prepared using an automated synthesizer for clinical use in positron emission tomography. |
| المشرفين على المادة: | 0 (Carbon Radioisotopes) 0 (Contrast Media) 0 (Isoquinolines) 0 (Radiopharmaceuticals) 0 (Receptors, GABA-A) YNF83VN1RL (PK 11195) |
| تواريخ الأحداث: | Date Created: 20091226 Date Completed: 20110331 Latest Revision: 20161125 |
| رمز التحديث: | 20231215 |
| PMID: | 20034893 |
| قاعدة البيانات: | MEDLINE |
| تدمد: | 1673-4254 |
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