【摘要】 本文探讨99Tcm标记2-(2-乙基-咪唑-1-基)-1-羟基乙烷-1,1-双膦酸(EIDP)用于骨显像的可能性。以2-乙基咪唑为原料,经3步反应制得EIDP。以SnCI2为还原剂,制得99Tcm-EIDP。正常小鼠尾静脉注射1.0MBq(0.2mL)99Tcm-EIDP,取不同时间处死小鼠的心、肝、脾、肺、肾、肌肉、骨和血,测量放射性,计算每克组织百分注射剂量率(%ID/g)及骨中放射性与各组织中放射性的比值,并计算血药清除动力学方程和各参数。新西兰兔静脉注射99Tcm-EIDP后于不同时间显像。EIDP的制备总收率为35.5%。99Tcm-EIDP的标记率和放化纯均>95%。在注射99Tcm-EIDP1h后小鼠骨摄取99Tcm-EIDP的量达到最大值Am骨为23.76%ID/g,Am骨/Am血为33.94,Am骨/Am肌肉为95.04。血药动力学方程为C=1090.736e-6.982t+84.956e-0.379t。兔显像结果表明,2h时即可获得清晰的兔骨显像图。99Tcm-EIDP制备方便,骨显像清晰,是一种较有潜力的新型骨显像剂。更多还原

【Abstract】 To evaluate the feasibility of 99Tcm-2-(2-ethylicimidazol-1-yl)-1-hydroxyethane-1,1-diphosphonic acid (EIDP) as a bone imaging agent, EIDP was synthesized by three-step reactions from 2-ethylicimidazol and 99Tcm-EIDP was prepared with SnCI2 in 10 min at room temperature. Normal mice were injected intravenously with 1.0 MBq 99Tcm-EIDP of 0.2 ml and sacrificed at different phase after injection. Samples of heart, liver, spleen, lung, kidney, muscle, bone and blood were taken for uptake (in %ID/g) measurement, and the bone-to-organ uptake ratios were calculated. The blood clearance kinetics was calculated, too. Bone imaging was performed in normal rabbit after intravenous injection. The total yield for the preparation of EIDP was 35.5%. Both the labeling yield and radiochemi- cal purity of 99Tcm-EIDP were over 95%. The bone uptake is up to 23.76 %ID/g at 1h after the injection. The bone-to-blood and bone-to-muscle uptake ratios were 33.94 and 95.04, respectively. The kinetics equation was: C = 1090.736e-6.982t + 84.956e-0.379t, and the initial half life and late half life were 4.76 and 105.5 min respectively. A clear bone imaging of rabbit was obtained 2h after injection. The 99Tcm-EIDP, which can be prepared conveniently, exhibited high uptake in bone and would be a potential bone imaging agent.更多还原