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碘化d-[11C]氧苯鎓的合成,一种通过正电子发射断层扫描在体内可视化人胆碱能毒蕈碱受体位点的潜在放射性配体。

Synthesis of d-[11C]oxyphenonium iodide, a potential radioligand for in vivo visualization of human cholinergic muscarinic receptor-sites by positron emission tomography.

作者信息

Vlek J W, Feitsma K G, van der Mark T W, Drenth B F, Paans A M, Vaalburg W

机构信息

Department of Nuclear Medicine, University Hospital, The Netherlands.

出版信息

Int J Rad Appl Instrum A. 1990;41(5):453-6. doi: 10.1016/0883-2889(90)90004-z.

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%.

摘要

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%。

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