Computer-controlled large scale production of high specific activity [11C]RO 15-1788 for PET studies of benzodiazepine receptors

K. Suzuki, O. Inoue, K. Hashimoto, T. Yamasaki, M. Kuchiki, K. Tamate
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引用次数: 99

Abstract

Ethyl 8-fluoro-5,6-dihydro-5-[11C]methyl-6-oxo-4H-imidazo [1,5-a][1,4]benzodiazepine-3-carboxylate ([11C]RO 15-1788) has been prepared automatically with high specific activity for in vivo visualization or quantitative analysis of brain benzodiazepine receptors. The yield, radiochemical yield, radiochemical purity and specific activity of the product ready for an i.v. injection were 276 ± 76 mCi, 50.8 ± 7.8%,99.3 ± 0.3% and 2.9 ± 0.5 Ci/μmol, respectively, taking an average of the latest 3 runs. The time required was about 25 min. Each product was sufficient to carry out three successive clinical studies by positron emission tomography (PET). All the procedures other than evaporation and filtration at the final stage were carried out with specially designed equipment connected to a central control system for radioisotope production.

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计算机控制大规模生产高比活性[11C]RO 15-1788用于苯二氮卓类受体的PET研究
自动制备了具有高比活性的8-氟-5,6-二氢-5-[11C]甲基-6-氧- 4h -咪唑[1,5-a][1,4]苯二氮卓-3-羧酸乙酯([11C]RO 15-1788),用于脑苯二氮卓受体的体内可视化或定量分析。取最近3次运行的平均值,该产品的产率、放射化学产率、放射化学纯度和比活性分别为276±76 mCi、50.8±7.8%、99.3±0.3%和2.9±0.5 Ci/μmol。所需时间约为25分钟。每个产品足以通过正电子发射断层扫描(PET)连续进行三次临床研究。除最后阶段的蒸发和过滤外,所有程序都是用连接到放射性同位素生产中央控制系统的专门设计的设备进行的。
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