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

The antidepressant desipramine (DMI) and its principal metabolite 2-hy droxydesipramine (HDMI) have been radiolabeled with C-11 for PET studi es. The normethyl precursors of DMI and HDMI were synthesized from imi nodibenzyl in 35% and 11% overall yield, respectively, Direct methylat ion of the normethyl precursor with [C-11]CH3I, followed by HPLC purif ication, provided [C-11]DMI and [C-11]HDMI in 18-30% and 15-23% decay- corrected radiochemical yields, respectively, in a 45 min synthesis ti me from end of bombardment. The specific activities of the two radiotr acers were > 1459 Ci/mmol at the end of synthesis. [C-11]DMI and [C-11 ]HDMI have potential utility as PET radiotracers for the norepinephrin e transporter. (C) 1997 Elsevier Science Inc.