摘要
采用间接标记方法，先合成对砹苯甲酸中间体，再与抗胃癌单抗３Ｈ１１偶联制得２１１Ａｔ－３Ｈ１１。２１１Ａｔ－３Ｈ１１的放化产率不低于２１１Ａｔ初始活度的３０％，其放射性比度可达１１１ＧＢｑ／ｇＭｃＡｂ。标记后２１１Ａｔ－３Ｈ１１的免疫活性与未标记的３Ｈ１１ＭｃＡｈ一致。核素前体参人法研究表明，２１１Ａｔ－３Ｈ１１对人胃癌细胞ＤＮＡ、ＲＮＡ合成的抑制效应强于Ｎａ２１１Ａｔ，尤其抑制ＲＮＡ合成，其作用呈量效关系。２１１Ａｔ－３Ｈ１１作用解除后，ＤＮＡ合成可逐渐恢复，提示２１１Ａｔ－３Ｈ１１为干扰代谢型药物。
At-3H11 McAb was prepared with an indirect labelling method which 211At was coupled to 3H11 McAb via paraastato-benzoic acid intermediate. At least 30% of the added 211At was found in the product, the specific activity of which was up to 111GBq/g McAb. Its radio￣unity was verified by ELISA method. Nuclide precursorincorporation techniques revealed that 211At-McAb inhibited the incorporation of 3H-TdR and 3H-UR into gastric cancer, especially the latter. The inhibition effect was dependent on the concentration of 211At-McAb and was stronger than that of Na211At.
出处
《核技术》
CAS
CSCD
北大核心
1994年第11期697-701,共5页
Nuclear Techniques
基金
高等学校博士点基金资助项目
关键词
单克隆抗体
胃癌
间接标记法
DNA
砹211
^(211)At
Monoclone antibody
Gastric cancer
Indirect labelling method
DNA, RNA
Incorporation
