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目的研制新型心肌灌注显像剂99TcmN,N′亚乙基二(乙酰丙酮亚胺)二[三(3甲氧基1丙基)膦](简称Q3)。方法合成显像剂的配体N,N′亚乙基—二(乙酰丙酮亚胺)和三(3甲氧基1丙基)膦后,用SnCl2·2H2O在强碱性条件下,还原99TcmO-4标记N,N′亚乙基—二(乙酰丙酮亚胺),再加入三(3甲氧基1丙基)膦反应10min,制得99TcmQ3。进行99TcmQ3小鼠体内分布和家兔显像实验,以及体外稳定性和急性毒性实验。结果99TcmQ3的心肌摄取快,摄取率高,注射后5min时每克心肌组织的摄取约为注射剂量的2466%,滞留时间长,注射后4h心肌清除不明显;血液、肺、肝脏清除均快。该显像剂无毒副作用,稳定性达6h以上。结论99TcmQ3是提高心肌灌注显像质量的较理想的显像剂。
Objective To develop a new myocardial perfusion imaging agent 99Tcm N, N ethylene two (acetylacetoneimine) bis [tris (3 methoxy 1 propyl) phosphine] (referred to as Q3). Methods After synthesizing the ligands of N, N’-ethylene-bis (acetylacetoneimine) and tris (3-methoxy-1-propyl) phosphine, Under 99TcmO-4 labeled N, N’-ethylene-bis (acetylacetoneimine), and then added three (3 methoxy 1 propyl) phosphine reaction 10min, obtained 99Tcm Q3. 99Tcm Q3 mice in vivo distribution and imaging experiments in rabbits, as well as in vitro stability and acute toxicity experiments. Results The myocardial uptake of 99TcmQ3 was fast and the rate of uptake was high. The myocardial tissue intake per gram at 5 min after injection was about 2466% of the injected dose, with a long residence time and no significant myocardial clearance at 4h after injection. Blood, lung and liver Clear all soon. The imaging agent has no toxic side effects and the stability is up to 6 hours. Conclusion 99Tcm Q3 is to improve the quality of myocardial perfusion imaging ideal imaging agent.