制备[61Cu]-2-乙酰基吡啶硫代半卡巴腙配合物作为一种可能用于恶性肿瘤的正电子发射断层显像（PET）示踪剂。

Preparation of [61Cu]-2-acetylpyridine thiosemicarbazone complex as a possible PET tracer for malignancies.

作者信息

Jalilian A R, Rowshanfarzad P, Sabet M, Shafiee A

机构信息

Cyclotron and Nuclear Medicine Department, Nuclear Research Center for Agriculture and Medicine, Atomic Energy Organization of Iran, Rajaeeshahr, P.O. Box 31485-498 Karaj, Iran.

出版信息

Appl Radiat Isot. 2006 Mar;64(3):337-41. doi: 10.1016/j.apradiso.2005.08.002. Epub 2005 Nov 15.

DOI:10.1016/j.apradiso.2005.08.002

PMID:16293418

Abstract

Due to the interesting anti-proliferative properties of copper-thiosemicarbazone complexes, the production of a (61)Cu-labeled thiosemicarbazone, i.e. 2-acetylpyridine thiosemicarbazone (APTS) was investigated. Copper-61 (T(1/2)=3.33 h) was produced via the (64)Zn(p,alpha)(61)Cu nuclear reaction using a natural zinc target irradiated with 22 MeV protons for 500 microAh. The (61)Cu 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 (61)Cu-acetate was mixed with 2-acetylpyridine thiosemicarbazone for 30 min at room temperature to yield [(61)Cu]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.

摘要

由于铜硫代卡巴腙配合物具有有趣的抗增殖特性，因此对一种（61）Cu标记的硫代卡巴腙即2-乙酰基吡啶硫代卡巴腙（APTS）的制备进行了研究。通过（64）Zn（p，α）（61）Cu核反应，使用天然锌靶在22 MeV质子照射下500微安时来制备铜-61（T（1/2）=3.33小时）。通过两步法将（61）Cu与辐照后的靶材料分离并转化为醋酸盐；最终活度为222 GBq（6.0 Ci），放射化学产率>95%。将（61）Cu-醋酸盐与2-乙酰基吡啶硫代卡巴腙在室温下混合30分钟，得到放射化学产率超过80%的[（61）Cu]APTS。比色法表明产品中的残留化学杂质低于可接受限度。放射性薄层色谱法（RTLC）显示在C（18）柱色谱后放射化学纯度超过99%。获得了约370-740 MBq/mmol（10-20 Ci/mmol）的比活度。在37℃下，在有无人血清存在的情况下对最终产品的稳定性进行了长达3小时的检查。还测定了最终配合物的分配系数。