文章摘要
王 俊,邵国强,崔 璨,姚晓晨,邵婉怡,朱建成,王 峰,王自正.99Tcm-MPO用于早期心肌灌注显像的动物实验研究[J].南京医科大学学报,2015,(1):119~124
99Tcm-MPO用于早期心肌灌注显像的动物实验研究
An experimental study of 99Tcm-MPO for early myocardial perfusion imaging
投稿时间:2014-05-30  
DOI:10.7655/NYDXBNS20150131
中文关键词: 99Tcm-MPO  早期  心肌灌注显像  99Tcm-MIBI  99Tcm-替曲膦
英文关键词: 99Tcm-MPO  early  myocardial perfusion imaging  99Tcm-MIBI  99Tcm-tetrofosmin
基金项目:江苏省自然科学基金(SBK20134281);南京市医学科技发展基金(QRX11253)
作者单位
王 俊 南京医科大学附属南京医院核医学科,江苏 南京 210006 
邵国强 南京医科大学附属南京医院核医学科,江苏 南京 210006 
崔 璨 南京医科大学附属南京医院核医学科,江苏 南京 210006 
姚晓晨 南京医科大学附属南京医院核医学科,江苏 南京 210006 
邵婉怡 南京医科大学附属南京医院核医学科,江苏 南京 210006 
朱建成 南京医科大学附属南京医院心内科,江苏 南京 210006 
王 峰 南京医科大学附属南京医院核医学科,江苏 南京 210006 
王自正 南京医科大学附属南京医院核医学科,江苏 南京 210006 
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中文摘要:
      目的:制备99mTc-2-巯基吡啶N-氧化物-N-乙氧基乙基-N,N-二[2-(二(3-甲氧基丙基)膦)乙基]胺([99mTc N(MPO)(PNP5)]+,简称99Tcm-MPO),考察其体内生物分布及其作为新型心肌灌注示踪剂的应用价值。方法:二步法合成99Tcm-MPO,采用高效液相色谱仪(HPLC)分析其标记率及体外稳定性,鼠尾静脉注射99Tcm-MPO(3.7 MBq)后不同时间进行生物学分布研究,新西兰兔耳缘静脉注射99Tcm-MPO后行单光子发射断层扫描(SPECT)平面序列显像,以99Tcm-替曲膦(37 MBq)和99Tcm-甲氧基异丁基异腈(99Tcm-MIBI,37 MBq)为对照组;实验小型猪冠状动脉左回旋支(LCX)球囊血流阻断后,静脉注射99Tcm-MPO后15?60 min分别行心脏灌注显像(MPI)显像。结果:99Tcm-MPO标记率为(98.8 ± 1.0)%,体外放置12 h放化纯为(96.5 ± 0.8)%。体内生物分布显示:5 min时,99Tcm-MPO肾脏摄取与99Tcm-替曲膦类似,均低于99Tcm-MIBI,99Tcm-MPO肝脏摄取为(30.38 ± 0.43)%ID/g,略高于99Tcm-MIBI和99Tcm-替曲膦,但99Tcm-MPO肝脏排泄快,15 min时99Tcm-MPO心脏摄取(9.38 ± 0.70)%ID/g略低于99Tcm-MIBI,但差异无统计学意义,而99Tcm-MPO心/肝比值(2.21 ± 0.44)明显高于99Tcm-MIBI(0.62 ± 0.02)和99Tcm-替曲膦(0.89 ± 0.06,F=22.29,P=0.016);静脉注射99Tcm-MPO后5 min兔平面显像可见心?肝清晰显影,15 min肝脏放射性摄取显著降低,心/肝比值为(0.85 ± 0.32),高于99Tcm-MIBI(0.71 ± 0.15)和99Tcm-替曲膦(0.59 ± 0.64),差异无统计学意义。猪心肌缺血模型SPECT/CT显像示注射后15 min外侧壁心肌可见99Tcm-MPO明显放射性缺损区,心/肝比值与60 min差异无统计学意义。结论:99Tcm-MPO 作为新型心肌显像剂,心脏摄取多,肝脏清除快,15 min心/肝放射性摄取高于99Tcm-MIBI和99Tcm-替曲膦,预期可用于早期心肌灌注显像,具有良好的临床应用前景。
英文摘要:
      Objective:To study 99Tcm-MPO ([99mTc N (MPO) (PNP5)+: 2-mercapto pyridine N-oxide and N-ethoxy ethyl-N, N-two [2 (two (3-methoxy propyl) phosphine) ethyl] amine) biodistribution in normal mice,and to study the biodistribution in vivo and its application as a new myocardial perfusion imaging tracer on the clinical application value. Methods:99Tcm-MPO was synthesized in two steps, and HPLC method was performed to analyze the radiolabeling rate and in vitro stability of 99Tcm-MPO. The normal Kunming rats as experimental group received injection of 99Tcm-MPO 3.7 MBq via the tail vein, while the control group was injected with 99Tcm-MIBI 3.7 MBq, and the biodistribution (%ID/g) in dissected organs were measured respectively at 5, 15, 30, 60 and 120 min post-injection (p.i.). Two normal New Zealand rabbits were intravenously injected with 99Tcm-MPO and 99Tcm-MIBI 37MBq at the ear margin, and static images were performed by SPECT at 5, 15, 30, 60 min p.i., respectively. We respectively proceed SPECT/CT imaging at 15 and 60 min p.i. after blocking blood flow with a balloon in the experimental miniature pigs' coronary artery left circumflex branch. Results:99Tcm-MPO had high radiolabeling yield of (98.8 ± 1.0)% and radiochemical purity after 12 h of (96.5 ± 0.8)% in vivo. In vivo biodistribution study demonstrated that uptake of 99Tcm-MPO in the kidneys was similar to 99Tcm-tetrofosmin at 5 min p.i.. The uptake of 99Tcm-MPO in liver was(30.38 ± 0.43)% ID/g at 5 min, slightly more than 99Tcm-MIBI and 99Tcm-tetrofosmin, but 99Tcm-MPO has a faster liver clearance. The uptake of 99Tcm-MPO in the heart was (9.38 ± 0.70)%ID/g at 15min p.i., slightly lower than 99Tcm-MIBI, but there was no significant difference. The factor that 99Tcm-MPO has a significantly higher heart/liver ratios than 99Tcm-MIBI and 99Tcm-tetrofosmin at 15min p.i. (heart/liver ratios: 2.21 ±0.44 vs. 0.62 ± 0.02 for 99Tcm-MIBI and 0.89 ± 0.06 for 99Tcm-tetrofosmin, F=22.29, P=0.016). The rabbits planar imaging after intravenous injection 99Tcm-MPO showed visible images of the heart and liver at 5 min p.i., and the radioactivity uptake in liver significantly reduced at 15 min p.i.. 99Tcm-MPO has higher heart-liver ratios than 99Tcm-MIBI and 99Tcm-tetrofosmin at 15min p.i. (heart-liver ratios: 0.85 ±0.32 vs. 0.71 ± 0.15 for 99Tcm-MIBI and 0.59 ± 0.64 for 99Tcm-tetrofosmin), but there was no significant difference. SPECT/CT showed decreased uptake of 99Tcm-MPO by lesions with ischemia and reperfusion injury in porcine models, and there was no significant difference. Conclusion:99Tcm-MPO is a new myocardial perfusion imaging tracer. Compared with 99Tcm-MIBI,99Tcm-MPO showed higher uptake in heart, longer myocardial radioactivity retention time, and quicker liver clearance. The heart-liver radioactivity uptake was higher than 99Tcm-MIBI and 99Tcm-tetrofosmin at 15min p.i.. 99Tcm-MPO may be used for early myocardial perfusion imaging, and has a good prospect of clinical application.
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