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[⁹⁹Tc^mN（PNP5）（DTC）]⁺混配配合物的合成及其在小鼠体内的生物分布

Synthesis and Biodistribution in Mice of [⁹⁹Tc^mN（PNP5）（DTC）]⁺ Heterocomplexes

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【Author】 CHU Jin-feng1,WANG Xue-bin2(1.State Key Laboratory of Chemical Resource Engineering,Beijing University of Chemical Technology,Beijing 100029,China;2.Key Laboratory of Radiopharmaceuticals,Ministry of Education,College of Chemistry,Beijing Normal University,Beijing 100875,China)

【机构】北京化工大学化工资源有效利用国家重点实验室；北京师范大学化学学院放射性药物教育部重点实验室；

【摘要】通过配体交换反应制备了4种脂溶性阳离子配合物:[99TcmN(PNP5)(PODC)]+(PNP5:N,N-二[二(3-甲氧基丙基)膦基乙基]-2-乙氧基乙胺;PODC:N-甲氧基氨荒酸盐)、[99TcmN(PNP5)(BODC)]+(BODC:N-乙氧基氨荒酸盐)、[99TcmN(PNP5)(MOPDTC)]+(MOPDTC:N-甲氧基丙基氨荒酸盐)和[99TcmN(PNP5)(EOPDTC)]+(EOPDTC:N-乙氧基丙基氨荒酸盐),放化纯度均大于90%。小鼠生物分布结果显示:4种配合物在小鼠体内均有不同程度的心肌摄取和滞留,主要经肾排泄,在血、肝和肺等非靶组织中清除较快。其中,[99TcmN(PNP5)(EOPDTC)]+的靶与非靶组织放射性摄取比(T/NT)较高,30 min时,心脏与血、心脏与肺及心脏与肝的T/NT分别为23.75、3.45和3.63,利于快速心肌显像。若能通过结构修饰提高其心肌摄取,有望发展为一种新型心肌灌注显像剂。更多还原

【Abstract】 [99TcmN(PNP5)(PODC)]+(PNP5: bis(dimethoxypropylphosphinoethyl) ethoxyethylamine,PODC:N-methoxyethyl dithiocarbamate),[99TcmN(PNP5)(BODC)]+(BODC:N-ethoxyethyl dithiocarbamate),[99TcmN(PNP5)(MOPDTC)]+(MOPDTC:N-methoxypropyl dithiocar-bamate) and [99TcmN(PNP5)(EOPDTC)]+(EOPDTC: N-ethoxypropyl dithiocarbamate) four 99Tcm-nitride heterocomplexes were synthesized by ligand exchange reaction.They were lipophilic cations with good stability,and their radiochemical purities were over 90%.The results of biodistribution in mice showed that the four heterocomplexes had different degrees of myocardial uptake and retention,and could be washed out rapidly from blood,liver,lungs and other non-target tissues,and were mainly eliminated through kidneys.Among the four complexes,the uptake ratios of heart to blood,heart to lung and heart to liver at 30 min of [99TcmN(PNP5)(EOPDTC)]+ were 23.75,3.45,3.63,and it was conductive to rapid cardiac imaging,respecinely.It could be developed a novel myocardial perfusion imaging agent by structural optimization to improve its myocardial uptake.更多还原