Synthesis of ^<11>C-Labeled Imipramine and Its Biodistribution in Mice : A Potential Tracer for Positorn Emission Tomography

概要

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A tricyclic antidepressant, ^<11>C-labeled imipramine was synthesized by N-methylation of desipramine with ^<11>CH_3I to assist in the imaging of the human imipramine receptor by positron emission tomography. The radiochemical yield after purification of ^<11>C-imipramine by high performance liquid chromatography was 28-63% at a specific activity of 26-53 Ci/mmol. The time required for synthesis, including purification was 30 min from the end of ^<11>CH_3I trapping. The organ distribution of ^<11>C-imipramine was investigated in mice at various times after i.v. injection. The main accumulation of radioactivity was in the kidney, followed by the lung and the heart. In the brain, the radioactivity levels in the hypothalamus and striatum were the highest and remained constant, differentiating them from other portions of the brain. Furthermore, the result of a binding assay with ^3H-labeled imipramine suggested that the regional distribution fo ^<11>C-imipramine in the same mouse brain correlated to that of the high affinity imipramine binding site.
社団法人日本薬学会の論文
1989-12-25