【摘要】 本文系统研究了⁹⁹Tc^m通过双功能联接剂金属硫蛋白（MT）标记抗肿瘤单克隆抗体的化学问题,并发展了新的实验方法和技术。用交联剂戊二醛制备MT与抗体（Ab）偶联物（MT-Ab）,偶联率为58％。用还原标记法制备⁹⁹Tc^m-MT-Ab,放射性利用率高达90％以上,而非特异标记低于10％。体外试验表明,在强络合剂竞争时,标记物有较高的稳定性。抗结肠癌单抗CL-3标记物的免疫反应活性保留87％。更多还原

【Abstract】 Metallothionein (MT), a small cysteine-rich protein, was used as a bifunctional chelating agent in the radiolabelling of monoclonal antibodies with Tc-99m. Chemical problems associated with the preparation of the conjugate complexe were intensively studied, and thus a number of experimental techniques were developed.The efficiency of the conjugation reaction of MT with antibodies (Ab) was found as 58%,The yield of radiolabelling of Tc-99m to MT-Ab by reduction method was higher than 90%, while the unspecific radiolabelling occurred less than 10%. The Tc-99m-MT-Ab has proven to be satisfactory stable in Vitro in the presence of a couple of strong chelating agents. Immunoreactivity as high as 87% was remained for a radiolabelled anti-colorectal carcinoma monoclonal antibody CL-3 examined by ELISA method.Biodistri-bution in normal mice revealed that Tc-99m-MT-IgG metabolized typically as common IgG did. The preliminary biological experimental results in tumor-bearing nude mice indicated that the Tc-99m-labelled anti-colorectal carcinoma monoclonal antibody 2C10 had strong affinity toward tumor and was stable in vivo.更多还原