Jalilian A R, Rowshanfarzad P, Sabet M, Shafiee A
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.
Appl Radiat Isot. 2006 Mar;64(3):337-41. doi: 10.1016/j.apradiso.2005.08.002. Epub 2005 Nov 15.
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.
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。
