摘要
无载体放射性碘标记间碘苄胍(no-carrier-added,n.c.a.123/131I-MIBG)在肿瘤、心肌显像和神经内分泌肿瘤的治疗方面有理论上优势。首先合成了以多氟化合物为支持体的标记前体,对该前体进行了放射性碘标记、纯化和初步生物分布实验。结果显示,无载体放射性碘125I标记MIBG在正常小鼠的心、脾、肺和肾上腺中的摄取显著高于目前商用的放射性碘标记MIBG。利用该方法标记后产物不需要使用HPLC进行纯化,适用于大规模临床应用。
No-carrier-added meta-[*I]iodobenzylguanidine((n. c. a. )[^123/131I]MIBG) has been considered to be promising diagnostic agents for oncology and cardiology, or as targeted radiotherapeutics for neuroendocrine tumors. The synthesis of a fluorous supported precursor for the purification without HPLC of n. c. a. [*I]MIBG was presented and its structure was determined. The precursor was labeled with radioactive iodine and the preliminary biodistribution of n. e. a. [*I]MIBG was studied. The uptake of n. c. a.[^125I] MIBG were significantly higher than that of c. a.[^125I]MIBG in heart, spleen, lung and adrenals. This facile preparation method of n. c. a.[*I] MIBG would allow its wider application in clinic.
出处
《同位素》
CAS
2015年第3期148-154,共7页
Journal of Isotopes
关键词
间碘苄胍
无载体
多氟化合物支持体
MIBG
no-carrier-added
fluorous supported
radioactive iodine labeling