Tse J W, Wiebe L I, Noujaim A A
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Canada.
J Nucl Med. 1989 Feb;30(2):202-8.
Enriched samarium oxide (98.2% 152Sm2O3) was irradiated in low neutron flux and high neutron flux reactors to produce 153Sm with specific activities of 14.3 GBq and 22.1 TBq mmol-1 Sm, respectively, at the time of use. Formulation of 153Sm as [153Sm]EDTA, with a 1:10 molar ratio of SM:EDTA, provided a stable radiotracer in vitro and in vivo. High specific activity [153Sm]EDTA showed superior uptake in cell culture (20.8 +/- 0.9% vs. 5.5 +/- 0.1% for 6 and 600 pmol Sm per 10(6) cells, respectively) and better tumor index values (51 vs. 37 at 10.9 nmol and 1.09 mumol Sm kg-1, respectively) in the BDF1 mouse/Lewis lung tumor model. High specific activity [153Sm]EDTA scintigrams of Copenhagen x Fisher rats bearing transplanted Dunning R3327 tumors clearly delineated the tumors within 6 hr, with moderate liver and bone uptake and low soft-tissue background. The injected radiotracer underwent rapid central compartment clearance and whole-body elimination. The absence of observed adverse histopathological toxicity combines with high image quality within 6 hr, to support the clinical tumor-imaging potential of this agent. Comparative studies with [67Ga]citrate at molar-equivalent doses indicated that high specific activity [153Sm]EDTA was a superior radiotracer in these in vitro and in vivo models.
富集氧化钐（98.2% 152Sm2O3）在低中子通量和高中子通量反应堆中进行辐照，以便在使用时分别产生比活度为14.3 GBq和22.1 TBq mmol-1 Sm的153Sm。将153Sm配制成[153Sm]EDTA，钐与乙二胺四乙酸（EDTA）的摩尔比为1:10，可在体外和体内提供一种稳定的放射性示踪剂。高比活度的[153Sm]EDTA在细胞培养中表现出更高的摄取率（每10(6)个细胞分别为6和600 pmol钐时，摄取率分别为20.8 +/- 0.9%和5.5 +/- 0.1%），并且在BDF1小鼠/刘易斯肺癌肿瘤模型中具有更好的肿瘤指数值（分别为10.9 nmol和1.09 μmol Sm kg-1时，肿瘤指数分别为51和37）。对患有移植性邓宁R3327肿瘤的哥本哈根×费希尔大鼠进行的高比活度[153Sm]EDTA闪烁扫描在6小时内清晰地勾勒出肿瘤，肝脏和骨骼摄取适中，软组织本底较低。注入的放射性示踪剂在中央室快速清除并从全身消除。未观察到不良组织病理学毒性，且在6小时内具有高图像质量，这支持了该药剂在临床肿瘤成像方面的潜力。在摩尔等效剂量下与[67Ga]柠檬酸盐进行的对比研究表明，在这些体外和体内模型中，高比活度的[153Sm]EDTA是一种更优的放射性示踪剂。
