99Tcm-TP1093的制备及其在健康动物体内的生物分布及动力学特点.docVIP

99Tcm-TP1093的制备及其在健康动物体内的生物分布及动力学特点 任 浩，查 林，冯世斌，唐 波，李前伟 （400038 重庆，第三军医大学西南医院核医学科） 99Tcm-TP1093，探讨其在健康动物体内的生物分布及动力学特点。化学合成-Aba-ATAQSAYG-NH2（TP1093）还原法99Tcm标记TP1093，纸层析测定标记率；体外稳定性实验、血清蛋白结合实验及／水分配实验鉴定99Tcm-TP1093的理化性质；标记在兔体内小鼠体内生物分布；兔99Tcm-TP1093显像观察放射性动态分布变化，利用region of interest，ROI）技术分析重要组织器官的-放射曲线。　99Tcm-TP1093的标记率为97.2±0.9）%，±0.6）TBq/mmol。标记室温放置4 h放化纯±0.9）%。标记多肽与血清蛋白无明显结合，脂/水分配系数lg P＝－（1.68±0.1）。标在权重为1/c的二室模型t1/2α为（2.689±0.541）min，t1/2β为（69.156±20.342）min，CL 为（5.029±4.381）mL/kg。小鼠体内家兔血液清除，未见放射性浓聚，主要经泌尿系统排。99Tcm-TP1093标记方法简便，标记率与比活度高，可制备成一步法冻干药盒，具有良好的稳定性、体内生物分布及动力学性质。 [关键词肿瘤坏死因子；TP1093，多肽；99Tcm，标记动物实验Preparation of 99Tcm-TP1093 and its experimental studys in health animals Ren Hao，Zha Lin，Feng Shibin，Tang Bo，Li Qianwei（Department of Nuclear MedicineSouthwest Hospital,Third Military Medical University,Chongqing,400038,China） [Abstract] Objective To prepare 99Tcm-TP1093 that is suitable for imaging with a high labeling rate, and to investigate its bio-distribution and dynamic characteristic in healthy animals. Methods G(D)AGG-Aba-ATAQSAYG-NH2 (TP1093) was synthesized and radiolabeled by 99Tcm using stannous chloride as the reductive agent. The labeling rate and specific activity were determined using paper chromatography. The physicochemical properties of the radiolabeled peptide were determined by stability test in vitro, serum albumin binding test and oil-water distribution test. The tracer kinetics in healthy rabbits and biodistribution of 99Tcm-TP1093 in normal mice were observed through caudal vein injection of the labeled peptide. The dynamic distribution of 99Tcm-TP1093 in organs of the rabbits was observed by SPECT imaging, and the time-activity curve of the main organs was drawn using ROI technology. Results The labeling rate and specific activity of 99Tcm-TP1093 was (97.2±0.9)% and (15.9±0.6)TBq/mmol, respectively. The radiochemical purity of 99Tcm-TP1093 was (93.3±0.9)% after placed at room temperature for 4 h. There was no significant combinati