Synthesis and biodistribution of ^<11>C-imipramine and ^<11>C-methamphetamine

(1)以^<11>CH_3l与clesipramine反应制备^<11> c -丙咪嗪。所有作业均在11bb0 CH_3l捕集结束后30分钟内完成。在供应结束时，每次运行的放射化学产率从26到53 Ci/mmol不等。(2)静脉注射后1 min内，小鼠体内c -丙咪嗪的生物分布以肺部积聚最多，血液中含量较低。纹状体和下丘脑的放射性高于大脑其他部位。用八段匀浆进行^ 3h -丙咪嗪的结合测定。提示该药物的受体位于下丘脑和纹状体。大剂量冷丙咪嗪预处理后的8个脑切片中^<11> c -丙咪嗪的分布大于未处理的对照组。(3)用与^<11> c -丙咪嗪类似的方法合成^<11> c -甲基苯丙胺^<11> c -甲基苯丙胺。所有作业均在^< 11bb0 CH_3l捕集结束后30 min内完成。(4) ^<11> c -甲基苯丙胺在小鼠体内的生物分布在肾脏中较高，而在大脑中不高。静脉注射后1分钟内血液放射性降至低水平。随着甲基苯丙胺剂量的增加，直至接近LD_<50>。大脑、血液和肾脏中c -甲基苯丙胺放射性浓度呈线性增加。小鼠脑内8个部位的放射性保持15分钟后逐渐降低。下丘脑、皮层、纹状体、海马的放射性高于中脑、小脑和延髓。在高剂量冰毒处理前后，^<11> c -甲基苯丙胺在8个脑区的分布大于未处理对照组和^<11> c -丙咪嗪。

(1) Synthesis of ^<11>C-imipramine^<11>C-lmipramine was prepared by the reaction of ^<11>CH_3l with clesipramine. All operations were completed within 30 min after the end of ^<11>CH_3l trapping. The radiochemical yield of each run ranged from 26 to 53 Ci/mmol at the end of the supply.(2) The biodistribution of ^<11>C-imipramine in mice^<11>C-lmipramine accumulation was the highest in the lung and low level in blood within 1 min after the iv injection. The radioactivity in striatum and hypothalamus was higher than in other sections of brain. The binding assay of ^3H-imipramine was examined using the eight sectional homogenates. This result suggests that receptor of this drug locates in gypothalamus and striatum. The distribution of ^<11>C-imipramine in eight sections of brain was greater after pretreatment of higy-dose of cold imipramine rather than that of the non-treated control.(3) Synthesis of ^<11>C-methamphetamine^<11>C-Methamphetamine was obtained by a similar method for ^<11>C-imipramine. All operations were completed with 30 min after the end of ^<11>CH_3l trapping.(4) Hte biodistribution of ^<11>C-methamphetamine in mice^<11>C-Methamphetamine distribution was high in the kidney but not high in the brain. The radioactivity in blood decreased to a low level within 1 min after the iv injection. As the dose of methamphetamine increased upto near the LD_<50>. the concentration of ^<11>C-methamphetamine radioactivity in the brain as well as in the blood and kidney increased linearly. The radioactivities in eight sections of mice brain were retained for 15 min and thereafter decreased. The radioactivities in hypothalamus, cortex, striatum, hippocampus was higher than that in midbrain, cerebellum and medulla oblongata. The distribution of ^<11>C-methamphetamine in eight sections of brain was greater after pre- or post-treatment of high doses of cold methamphetamine rather than those of the non-treated control as well as ^<11>C-imipramine.