Vlek J W, Feitsma K G, van der Mark T W, Drenth B F, Paans A M, Vaalburg W
Department of Nuclear Medicine, University Hospital, The Netherlands.
Int J Rad Appl Instrum A. 1990;41(5):453-6. doi: 10.1016/0883-2889(90)90004-z.
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%.
碳-11标记的碘化d-氧苯鎓,一种胆碱能拮抗剂,通过正电子发射断层扫描(PET)合成用于气道组织上毒蕈碱受体位点的体内可视化。用[11C]CH3I对d-去甲基氧苯鎓进行甲基化,然后通过高效液相色谱(HPLC)纯化,得到所需的放射性药物,放射化学产率为66%(基于[11C]CH3I,并校正衰变),比活度为110 - 300 Ci/mmol。具有生物活性的标记d-对映体在EOB后40分钟内制备完成。光学和化学纯度证明优于99.9%。放射化学纯度测定高于99%。