In vivo imaging of vesicular monoamine transporters in human brain using [11C]tetrabenazine and positron emission tomography.
The pharmacokinetics of [11C]tetrabenazine, a high-affinity radioligand for the monoamine vesicular transporter, were determined in living human brain using in vivo imaging by positron emission tomography (PET). The radiotracer showed high brain uptake and rapid washout from all brain regions with relatively slower clearance from regions of highest concentrations of monoamine vesicular transporters (striatum), resulting in clear differential visualization of these structures at short intervals after injection (10-20 min). As the first human PET imaging study of a vesicular neurotransmitter transporter, these experiments demonstrate that external imaging of vesicular transporters forms a new and valuable approach to the in vivo quantification of monoaminergic neurons, with potential application to the in vivo study of neurodegenerative disorders such as Parkinson's disease.
Department of Internal Medicine, University of Michigan School of Medicine, Ann Arbor.
M R
MR
Kilbourn
J N
JN
DaSilva
K A
KA
Frey
R A
RA
Koeppe
D E
DE
Kuhl
D000328:Adult; D001679:Biogenic Amines / Q000378:metabolism*; D001692:Biological Transport; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D002250:Carbon Radioisotopes; D003342:Corpus Striatum / Q000000981:diagnostic imaging / Q000378:metabolism; D006023:Glycoproteins / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009474:Neurons / Q000000981:diagnostic imaging / Q000378:metabolism*; D009479:Neuropeptides; D009928:Organ Specificity; D013747:Tetrabenazine / Q000378:metabolism* / Q000493:pharmacokinetics; D013997:Time Factors; D014055:Tomography, Emission-Computed / Q000379:methods; D050492:Vesicular Biogenic Amine Transport Proteins
D001679:Biogenic Amines; D002250:Carbon Radioisotopes; D006023:Glycoproteins; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009479:Neuropeptides; D050492:Vesicular Biogenic Amine Transport Proteins; D013747:Tetrabenazine