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为探索中性心肌显像剂99mTcN(NOEt)2(NOEt:N乙氧基,N乙基氨荒酸钠盐)的制备方法及生物学特性,合成了制备中间体〔99mTc≡N〕2+所需试剂及NOEt。在N的供体及还原剂存在的条件下,先加热制备中间体〔99mTc≡N〕2+,再在常温下制备99mTcN(NOEt)2。试剂及配体经IR、NMR、MS及元素分析等鉴定与结构相符。标记物经HPLC和TLC检测,放化纯及标记率均大于90%,在体外6小时内稳定。pH值74时的分配系数为427。大鼠体内分布结果表明,药物能很快被心肌摄取,5分钟心肌摄取量为279%ID,90分钟为188%ID。结果表明,99mTcN(NOEt)2的体外性质稳定,心肌摄取快且高,滞留时间长,具有临床研究价值。
In order to explore the preparation and biological characteristics of neutral myocardial imaging agent 99mTcN (NOEt) 2 (NOEt: N-ethoxy, N-ethylamide), the preparation of intermediate [99mTc≡N] 2+ Reagents required and NOEt. In the presence of N donor and reducing agent, the intermediate [99mTc≡N] 2+ is prepared by heating and then 99mTcN (NOEt) 2 is prepared at normal temperature. Reagents and ligands identified by IR, NMR, MS and elemental analysis consistent with the structure. Labeled by HPLC and TLC, radiochemical purity and labeling rates were greater than 90%, in vitro stability within 6 hours. The partition coefficient at pH 7.4 is 427. The results of in vivo distribution in rats showed that the drug was rapidly taken up by the myocardium. The myocardial uptake at 5 minutes was 279% ID and that at 90 minutes was 188% ID. The results showed that the 99mTcN (NOEt) 2 was stable in vitro, fast and high in myocardial uptake and long residence time, and had clinical value.