Synthesis of 11C-Labeled Desipramine and Its Metabolite 2-Hydroxydesipramine: Potential Radiotracers for PET Studies of the Norepinephrine Transporter
- 作者：Van Dort ; Marcian E. ; Kim ; Jae-Hoon ; Tluczek ; Louis ; Wieland ; Donald M.
- 关键词：Desipramine ; 2-Hydroxydesipramine ; Carbon-11 ; Radiotracer ; Antidepressant ; Norepinephrine transporter ; Positron emission tomography
- 刊名：Nuclear Medicine and Biology
- 出版年：1997
- 期刊代码：43_09698051
- 类别：ph
- 出版时间：November, 1997
- 卷：24
- 期：8
- 页码：707-711
- 文件大小：477 K
摘要
The antidepressant desipramine (DMI) and its principal metabolite 2-hydroxydesipramine (HDMI) have been radiolabeled with 11C for PET studies. The normethyl precursors of DMI and HDMI were synthesized from iminodibenzyl in 35%and 11%overall yield, respectively. Direct methylation of the normethyl precursor with [11C]CH3I, followed by HPLC purification, provided [11C]DMI and [11]HDMI in 18-30%and 15-23%decay-corrected radiochemical yields, respectively, in a 45 min synthesis time from end of bombardment. The specific activities of the two radiotracers were >1459 Ci/mmol at the end of synthesis. [11C]DMI and [11C]HDMI have potential utility as PET radiotracers for the norepinephrine transporter.