Wadas Thaddeus J, Anderson Carolyn J
Mallinckrodt Institute of Radiology, Washington University School of Medicine, 510 South Kingshighway Boulevard, Campus Box 8225, St. Louis, Missouri 63110, USA.
Nat Protoc. 2006;1(6):3062-8. doi: 10.1038/nprot.2006.431.
The number of radiopharmaceuticals containing copper radionuclides for diagnostic imaging and targeted radiotherapy has grown considerably over the past few decades. This expansion has created the need for protocols allowing for the efficient chelation of 64Cu to peptide-chelator conjugates. Step 1A of this protocol describes a (64)Cu-radiolabeling procedure for 1,4,8,11-tetraazacyclododecane-1,4,8,11-tetraacetic acid (TETA)-conjugated peptides. This reaction is facile and requires the incubation of 64CuCl2 in 0.1 M ammonium acetate buffer with the TETA-peptide for 30 min at room temperature (20-23 degrees C). Step 1B of this protocol describes the radiolabeling procedure for 4,11-bis(carboxymethyl)-1,4,8,11-tetraazabicyclo[6.6.2]hexadecane (CB-TE2A)-conjugated peptides. The CB-TE2A-peptide can be labeled with 64Cu in 0.1 M ammonium acetate buffer in 2 h at 95 degrees C. In both cases, the conjugates can be radiolabeled with 64Cu at greater than 95% purity and with specific activities of 37-111 MBq microg(-1) (1-3 mCi microg(-1)). Both protocols are straightforward and can be completed within 3 h.
在过去几十年中，用于诊断成像和靶向放疗的含铜放射性药物的数量大幅增长。这种增长使得需要有相应方案来实现64Cu与肽 - 螯合剂共轭物的高效螯合。本方案的步骤1A描述了一种用于1,4,8,11 - 四氮杂环十二烷 - 1,4,8,11 - 四乙酸（TETA）共轭肽的（64）Cu放射性标记程序。该反应简便，需要在室温（20 - 23摄氏度）下，将64CuCl2在0.1 M醋酸铵缓冲液中与TETA - 肽孵育30分钟。本方案的步骤1B描述了4,11 - 双（羧甲基）-1,4,8,11 - 四氮杂双环[6.6.2]十六烷（CB - TE2A）共轭肽的放射性标记程序。CB - TE2A - 肽可以在95摄氏度下于0.1 M醋酸铵缓冲液中用64Cu标记2小时。在这两种情况下，共轭物都可以用64Cu进行放射性标记，纯度大于95%，比活度为37 - 111 MBq μg（-1）（1 - 3 mCi μg（-1））。这两个方案都很简单，并且可以在3小时内完成。
