SYNTHESIS OF C-11 LABELED DESIPRAMINE AND ITS METABOLITE 2-HYDROXYDESIPRAMINE - POTENTIAL RADIOTRACERS FOR PET STUDIES OF THE NOREPINEPHRINE TRANSPORTER
Me. Vandort et al., SYNTHESIS OF C-11 LABELED DESIPRAMINE AND ITS METABOLITE 2-HYDROXYDESIPRAMINE - POTENTIAL RADIOTRACERS FOR PET STUDIES OF THE NOREPINEPHRINE TRANSPORTER, Nuclear medicine and biology, 24(8), 1997, pp. 707-711
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.