Synthesis of d-[11C]oxyphenonium iodide,a potential radioligand for in vivo visualization of human cholinergic muscarinic receptor-sites by positron emission tomography |
| |
| Institution: | 1. Department of Nuclear Medicine, University Hospital, Oostersingel 59, 9713 EZ Groningen The Netherlands;2. Department of Pulmonary Diseases, University Hospital, Oostersingel 59, 9713 EZ Groningen The Netherlands;3. Department of Analytical Chemistry and Toxicology, State University Groningen, Antonius Deusinglaan 4, 9713 AW Groningen, The Netherlands;1. College of Food Science and Engineering, Northwest A&F University, 22 Xinong Road Yangling, 712100 Shaanxi, PR China;2. Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, 22 Xinong Road Yangling, 712100 Shaanxi, PR China;1. College of Life Science, Northwest Normal University, Lanzhou 730070, Gansu Province, China;2. Bioactive Products Engineering Research Center for Gansu Distinctive Plants, Lanzhou 730070, China;3. Institute of Rural Development and Research, Northwest Normal University, Lanzhou 730070, Gansu Province, China;4. Lanzhou Institute of Food and Drug Control, Lanzhou 740050, China;5. Nanjing Forestry University, Nanjing 210037, Jiangsu Province, China;1. Department of Science and Technology, Food and Nutrition Research Institute, Taguig City 1631, Philippines;2. Department of Chemistry, Ateneo de Manila University, Quezon City 1108, Philippines |
| |
| Abstract: | Carbon-11 labeled d-oxyphenonium iodide, a cholinergic antagonist is synthesized for in vivo visualization of muscarinic receptor-sites on airway tissue by positron emission tomography (PET). Methylation with 11C]CH3I of d-demethyloxyphenonium, followed by HPLC purification affords the desired radiopharmaceutical with a radiochemical yield of 66% (based on 11C]CH3I, and corrected for decay) and with a specific activity of 110–300 Ci/mmol. The biologically active labeled d-enantiomer is prepared within 40 min after EOB. Optical and chemical purity proved to be better than 99.9%. Radiochemical purity was determined to be higher than 99%. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
