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为了提高放免显像的准确性和图像的分辨率,采用改进的Schwartz法进行~(99m)Tc标记抗胃癌单克隆抗体3H11的研究。还原剂2-巯基乙醇相对抗体过量1000倍摩尔比,室温反应30分钟,每个抗体分子暴露的巯基数约为2.3个。标记抗体的标记率>95%,最大标记比活度为2.2GBq/mg 3H11,用ELISA法测得的免疫活性>80%。高压液相色谱及体外竞争结合分析证实~(99m)Tc结合在抗体分子的高亲和结合位上。荷瘤裸鼠实验表明:注射~(99m)Tc-3H11 24小时后,除肾外,肿瘤中放射性最高,瘤/血比值>1.5,瘤/肝比值>2.5;2小时后肿瘤γ显像清晰,本底干扰较小。初步临床应用显示,~(99m)Tc-3H11体内稳定性好,能较好地定位于肿瘤病灶。
In order to improve the accuracy of radiopharyngeal imaging and the resolution of images, a modified Schwartz method was used to study the anti-gastric cancer monoclonal antibody 3H11 with ~ (99m) Tc labeling. Reducing agent 2-mercaptoethanol relative antibody excess 1000 fold molar ratio, reaction at room temperature for 30 minutes, each antibody molecule is exposed to about 2.3 mercapto groups. The labeling rate of the labeled antibody was> 95%, the maximum specific activity was 2.2GBq / mg 3H11, and the immunological activity was> 80% as measured by ELISA. High-pressure liquid chromatography and in vitro competitive binding assay confirmed that ~ (99m) Tc binds to the high affinity binding site of the antibody molecule. Tumor-bearing nude mice experiments showed that: after 24 hours of 99m Tc-3H11 injection, the tumor had the highest radioactivity, the tumor / blood ratio was> 1.5 and the tumor / liver ratio was> 2.5 after 2 hours; , The background interference is smaller. The preliminary clinical application shows that ~ (99m) Tc-3H11 has good in vivo stability and can be well located in tumor lesions.