CAJ | 학술논문

进行了二乙三胺五乙酸酸酐(cDTPAA)平阳霉素偶联后的153Sm标记。研究了平阳霉素与cDTPAA的偶联条件、偶联物化学计量组成，探讨了153Sm与偶联物的络合条件及络合物的稳定性。在弱碱性介质中，当cDTPAA与平阳霉素的摩尔比大于10时，平阳霉素的偶联率可达80%；当摩尔比大于15时，偶联物的平均化学计量组成为平阳霉素与DTPA的摩尔比为1∶2；在pH7～9体系中，偶联物与153Sm摩尔比大于8，室温反应30min，标记率可达98%；标记物较稳定，生理pH下6d内放化纯度大于96%。
진행료이을삼알오을산산항(cDTPAA)평양매소우련후적153Sm표기。연구료평양매소여cDTPAA적우련조건、우련물화학계량조성，탐토료153Sm여우련물적락합조건급락합물적은정성。재약감성개질중，당cDTPAA여평양매소적마이비대우10시，평양매소적우련솔가체80%；당마이비대우15시，우련물적평균화학계량조성위평양매소여DTPA적마이비위1∶2；재pH7～9체계중，우련물여153Sm마이비대우8，실온반응30min，표기솔가체98%；표기물교은정，생리pH하6d내방화순도대우96%。
Bleomycin A5(BLMA5) is conjugated with cyclic DTPA anhydride andlabeled with 153Sm. The conditions of conjugation and labeling are investigated. The possible composition of BLMA5-DTPA is analyzed by measurement and computation. The results show that bleomycin A5 can conjugate with DTPA anhydride easily when the mole ratio of cDTPAA to BLMA5 is more than 10 in weak basic media, and the conjugating yield is more than 80%;A molecule of BLMA5 conjugate with 2 molecule of cDTPAA when the mole ratio of cDTPAA to BLMA5 is not less than 15, and the conjugative positions is on 2 different N atoms. The results of labeling experiments indicate that the labeling yield of 153Sm-DTPAA-BLMA5 is 98% at pH7～9 and room temperature for 30 min when the mole ratio of DTPA-BLMA5 to 153Sm is more than 8. 153Sm-BLMA5-DTPA is stable and the radiochemical purity is more than 96% at room temperature for 6 days.