CACPPA的~(99)Tc~m标记及其动物实验研究

  • 摘要: 在pH8.5~9.5的水溶液中,采用氯化亚锡还原法制备99Tcm-CACPPA,TLC和HPLC检测其标记率和放化纯均大于90%。小鼠体内分布表明,心肌最高摄取率为18.17±2.67%ID/g;小鼠血药动力学研究表明99Tcm-CACPPA的血液清除快,T1/2α为1.11min,T1/2β为20.08min,清除速率为0.407mL/min。99Tcm-CACPPA的体内外血浆蛋白结合率高,pH7.00和pH7.40时分配系数分别为10.98和11.45;代谢干预研究结果表明,葡萄糖胰岛素组心肌摄取升高,与对照组相比,差异具有显著性意义。

     

    Abstract: 99Tcm LABELING AND ANIMAL EXPERIME NTS OF CACPPA Wu Chunying\ Ji Shuren\ Fang Ping\ Zhou Xiang\ Chen Zhengping \ He Yongjun(State Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi, 214063)Abstract\ 99TcmCACPPA is prepared by the reduct ion of stannous chloride with Na99TcmO-4 in aqueous soluti on a t pH8.5~9.5,the labeling yield and radiochemical purity are over 90% determined by TLC and HPLC. Biodistribution of 99TcmCACPPA in mice demonstra tes that the highest myocardial uptake of 99TcmCACPPA is 18.17±2. 67% ID/g. When blood disappearance of 99TcmCACPPA is analyzed with a biexponential model, an initial half time of 1.11 min and a late half tim e of 20.08 min are obtained. 99TcmCACPPA exhibite high binding to HSA in vitro and in vivo, partition coefficients are 10.98 and 11.45 at pH7.00 a nd pH7.40 respectively. The study of metabolism intervention showes that myocard ial uptake of 99TcmCACPPA in the group of glucoseinsulin is high er than that of normal, which has significant difference after ttest.Keywords\ p(N,N′dicarboxymethyl)aminomethyl ca r boxyaminophenylpentadecanoic acid (CACPPA)\ 99TcmCACPPA\ anima l experiment

     

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