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首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >Preparation of [Cu-61]-2-acetylpyridine thiosemicarbazone complex as a possible PET tracer for malignancies
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Preparation of [Cu-61]-2-acetylpyridine thiosemicarbazone complex as a possible PET tracer for malignancies

机译：制备[Cu-61] -2-乙酰基吡啶硫半脲复合物作为可能的恶性PET示踪剂

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摘要

Due to the interesting anti-proliferative properties of copper-thiosemicarbazone complexes, the production of a Cu-61-labeled thiosemicarbazone, i.e. 2-acetylpyridine thiosemicarbazone (APTS) was investigated. Copper-61 (T-1/2 = 3.33 h) was produced via the Zn-64(p,alpha)Cu-61 nuclear reaction using a natural zinc target irradiated with 22 MeV protons for 500 mu Ah. The Cu-61 was separated from the irradiated target material by a two-step method and converted to acetate; this yielded a final activity of 222 GBq (6.0 Ci), with a radiochemical yield of > 95%. The Cu-61-acetate was mixed with 2-acetylpyridine thiosemicarbazone for 30 min at room temperature to yield [Cu-61]APTS with a radiochemical yield of more than 80%. Colorimetric methods showed that residual chemical impurities in the product were below the accepted limits. Radio thin layer chromatography (RTLC) showed a radiochemical purity of more than 99% after C-18 column chromatography. A specific activity of about 370-740 MBq/mmol (10-20 Ci/mmol) was obtained. The stability of the final product was checked in the absence and presence of human serum at 37 degrees C for up to 3 h. The partition coefficient of the final complex was also determined. (c) 2005 Elsevier Ltd. All rights reserved.
机译：由于铜-硫代氨基脲复合物具有令人感兴趣的抗增殖性能，因此研究了Cu-61标记的硫代氨基脲，即2-乙酰基吡啶硫代氨基脲（APTS）的生产。通过使用22 MeV质子辐照500μAh Ah的天然锌靶，通过Zn-64（p，α）Cu-61核反应生成铜61（T-1 / 2 = 3.33小时）。通过两步法将Cu-61与被辐照的目标材料分离，并转化为乙酸盐;最终活性为222 GBq（6.0 Ci），放射化学产率> 95％。在室温下，将Cu-61-乙酸盐与2-乙酰基吡啶硫代半碳酸盐混合30分钟，以产生[Cu-61] APTS，放射化学产率超过80％。比色法显示产品中残留的化学杂质低于可接受的限度。放射性薄层色谱（RTLC）在C-18柱色谱分析后显示出超过99％的放射化学纯度。获得约370-740 MBq / mmol（10-20 Ci / mmol）的比活。在37℃下在不存在和存在人血清的情况下检查最终产品的稳定性达3小时。还确定了最终络合物的分配系数。 （c）2005 Elsevier Ltd.保留所有权利。

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