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抗人膀胱癌单克隆抗体BDI-1通过2-巯基乙醇直接还原法标记得-99m制备了99mTc-BDI-1。质量控制实验结果表明,标记率为69.9%,分离纯化后标记抗体的放化纯度高于90%。标记抗体的免疫活性分数为81%,亲和常数为1.22x109M-1。本文在上述结果基础上,研究了标记抗体在荷人膀胱癌裸鼠体内的分布及放射免疫显像。99mTc-BDI-1经尾静脉注射后,分别在4,16及22小时γ照相后断颈处死小鼠,取脏器称湿重并计数。99mTc-BDI-1注射后22小时肿瘤清晰显示,肿瘤对标记抗体的吸收率为20.7%ID/g:平均T/NT为10.52,最小T/NT为2.90(肿瘤/肾脏);最大T/NT为20.7(肿瘤/小肠或肌)。上述研究结果为进一步临床应用奠定基础。
99mTc-BDI-1 was prepared by anti-human bladder cancer monoclonal antibody BDI-1 labeled with -99m by 2-mercaptoethanol direct reduction method. The results of quality control experiments showed that the labeling efficiency was 69.9%, and the radiochemical purity of the labeled antibody was higher than 90% after isolation and purification. The labeled antibody had an immunocompetent fraction of 81% and an affinity constant of 1.22 × 109 M-1. Based on the above results, we studied the distribution and radioimmunoimaging of labeled antibody in human bladder cancer nude mice. After injection of 99mTc-BDI-1 via the caudal vein, mice were sacrificed at 4, 16 and 22 hours after gamma photography, respectively. The organs were weighed and wet-weighted. At 22 hours after injection of 99mTc-BDI-1, tumors clearly showed a 20.7% ID / g absorbance of the labeled antibody for the tumor: an average T / NT of 10.52 and a minimum T / NT of 2.90 (tumor / kidney ); Maximum T / NT was 20.7 (tumor / small intestine or muscle). The above findings lay the foundation for further clinical application.