Synthesis of [11C]tetrabenazine, a vesicular monoamine uptake inhibitor, for PET imaging studies.
Tetrabenazine (TBZ), a high affinity and specific inhibitor of the vesicular monoamine transporter, has been labeled with carbon-11 as a potential probe for in vivo positron emission tomographic imaging of monoaminergic neuronal losses in neurodegenerative diseases. [11C]TBZ was synthesized by O-[11C]methylation of the 9-O-desmethylTBZ using [11C]methyl iodide in the presence of tetrabutylammonium hydroxide. The radiochemical yields were 35-55% (decay corrected) and the synthesis time 32-37 min from EOB. [11C]TBZ was obtained with specific activities of 2000-2500 Ci/mmol (EOS) and radiochemical and chemical purities were > 95%. [11C]Tetrabenazine is a promising new radioligand for the in vivo study of monoaminergic neurons using PET.
DaSilva
J N
JN
Department of Internal Medicine, University of Michigan Medical Center, Ann Arbor 48109.
Kilbourn
M R
MR
Mangner
T J
TJ
D002250:Carbon Radioisotopes; D007553:Isotope Labeling / Q000379:methods; D014179:Neurotransmitter Uptake Inhibitors; D013747:Tetrabenazine; D014055:Tomography, Emission-Computed
D002250:Carbon Radioisotopes; D014179:Neurotransmitter Uptake Inhibitors; D013747:Tetrabenazine