脑放射性药物碘代芳香胺构效关系的定量研究

    • 摘要: 根据Fick定律,假设放射性药物可以通过扩散机制穿透血脑屏障,经过对14种碘代芳香胺放射性药物的分析,首次得到了最初脑摄取量与药物的脂溶性、蛋白质结合率和分子量之间的定量关系,这对于脑放射性药物的设计和药物最初脑摄取量的预测具有一定的意义。

       

      Abstract: STUDY ON QSAR OF BRAIN RADIOPHARMACEUTICALS 0FIODOAMPHETAMINkSXU YEPING;LIU BOLI(Department of Chemistry,Beijing Normal University,Beijing, 100875)H.F. Kung(Department of Radiology,University of Pennsylvania P,A 19104,America)ABSTRACT According to the Fick's law,it is assumed that brain radiopharmaceuticals can pass throughBrain Blcod Barrier by simple diffusion process,After investigation of parameters of fourteeniodoamphetamines,a linear relationship among initial brain uptake,partition coefficient,proteinbinding and molecular weight has been established.This relationship may be useful in designingnew brain radiopharmaceuticals and predicting initial brain uptake. Key words Brain Radiopharmaceuticals Iodoamphetamine Structrue-activit Relationship

       

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