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

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(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.