SYNTHESIS OF C-11-LABELED DESIPRAMINE AND ITS METABOLITE 2-HYDROXYDESIPRAMINE - POTENTIAL RADIOTRACERS FOR PET STUDIES OF THE NOREPINEPHRINE TRANSPORTER

摘要

The antidepressant desipramine (DMI) and its principal metabolite 2-hydroxydesipramine (HDMI) have been radiolabeled with C-11 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 [C-11]CH3I, followed by HPLC purification, provided [C-11]DMI and [C-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. [C-11]DMI and [C-11]HDMI have potential utility as PET radiotracers for the norepinephrine transporter. (C) 1997 Elsevier Science Inc. [References: 14]