生长抑素受体显像剂^(99)Tc^m-HTOC的制备

Preparation of SSTR-positive tumor targeting tracer ^(99)Tc^m-HTOC

目的 研制99Tcm 标记的生长抑素受体 (SSTR)阳性肿瘤显像剂99Tcm 6 肼基烟酰基 [Tyr3] octreotide (HTOC)。方法 通过四步化学反应合成 ,HPLC纯化 ,得到HTOC ;用乙二胺 N ,N′ 二乙酸 (EDDA)作为配体进行99Tcm 标记 ,测定标记率与标记物稳定性。结果 所合成HTOC质谱的分子离子峰与HTOC相对分子质量一致 ,99Tcm HTOC标记率 >95 % ,标记后 6h放化纯仍 >95 %。结论该法研制的99Tcm HTOC标记率高 ,体外稳定性好。

Objective To explore the 99 Tc m-HYNIC-[Tyr 3]-octreotide (HTOC) which is 99 Tc m labeled somatostatin receptors (SSTR) imaging agent. Methods HTOC was obtained by four steps of chemical reaction,purified by HPLC and labeled with 99 Tc m using ethylenediamine diacetic acid (EDDA) as coligand;the labeling yield,radiochemical purity and stability in vitro were determined by instant thin layer chromatography-sillica gel (ITLC-SG) and HPLC. Results The structure of HTOC was confirmed by matrix assistant laser desorption ionization-time of flight-mass spectroscopy (MALDI-TOF-MS). The labeling yield was more than 95% and remained high in vitro by 6 h after labeling. Conclusion The labeling yield of 99 Tc m-HTOC prepared with the methodology reported here is high and the stability of 99 Tc m-HTOC in vitro and in vivo is good.