（166）钬-1,2-丙二胺四（亚甲基膦酸）作为一种可能的骨姑息治疗剂的研发。

Development of (166)Holmium-1,2 Propylene Di-amino Tetra (Methy1enephosphonicacid) as a Possible Bone Palliation Agent.

作者信息

Zolghadri Samaneh, Jalilian Amir Reza, Yousefnia Hassan, Bahrami-Samani Ali, Ghannadi-Maragheh Mohammad

机构信息

Radiopharmacy Research Group, Radiation Application Research School, Nuclear Science and Technology Research Institute, P.O.Box:14395-836, Tehran, Iran.

出版信息

World J Nucl Med. 2014 Jan;13(1):28-33. doi: 10.4103/1450-1147.138571.

DOI:10.4103/1450-1147.138571

PMID:25191109

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4149765/

Abstract

(166)Holmium-1,2-propylene di-amino tetra (methy1enephosphonicacid) ((166) Ho-PDTMP) complex was prepared successfully using an in-house synthesized PDTMP ligand and (166) HoCl 3 . Ho-166 chloride was obtained by thermal neutron irradiation (1 × 10 (13) n/cm (2) /s) of natural Ho (NO 3 ) 3 samples (specific activity = 3-5 GBq/mg), dissolved in acidic media. Radiochemical purity of (166) Ho-PDTMP was checked by instant thin layer chromatography (>99%). Stability studies of the complex in the final preparation and in the presence of human serum were performed up to 72 h. The biodistribution of (166) Ho-PDTMP and (166) HoCl 3 in wild-type rats was checked in animal tissues up to 48 h. The produced (166) Ho-PDTMP properties suggest a possible new bone palliative therapeutic to overcome the metastatic bone pains.

摘要

使用自行合成的二氨基四（亚甲基膦酸）丙酯（PDTMP）配体和氯化钬（166）HoCl₃成功制备了钬 - 1,2 - 丙二胺四（甲基膦酸）（（166）Ho - PDTMP）配合物。通过对天然硝酸钬（Ho(NO₃)₃）样品（比活度 = 3 - 5 GBq/mg）进行热中子辐照（1×10¹³ n/cm²/s）获得氯化钬（166）HoCl₃，将其溶解在酸性介质中。通过即时薄层色谱法检查（166）Ho - PDTMP的放射化学纯度（>99%）。对最终制剂中以及存在人血清时该配合物进行了长达72小时的稳定性研究。在野生型大鼠中检查了（166）Ho - PDTMP和（166）HoCl₃在动物组织中的生物分布，长达48小时。所制备的（166）Ho - PDTMP的性质表明它可能是一种新型的骨姑息治疗药物，用于克服转移性骨痛。