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Michael R. Kilbourn PET radioligands for the vesicular transporters for monoamines and acetylcholine Journal of Labelled Compounds and Radiopharmaceuticals 56

Article first published online: 24 APR 2013 | DOI: 10.1002/jlcr.2998

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The vesicular monoamine transporter 2 and vesicular acetylcholine transporter are proteins specifically located in presynaptic vesicles of monoaminergic and cholinergic neurons, respectively. Radiopharmaceutical chemistry efforts led to three radiotracers now used routinely for imaging these transporters in the human brain: (+)-[11C]dihydrotetrabenazine (DTBZ) and 9-(3-[18F]fluoropropyl)-dihydrotetrabenazine (AV-133) for the vesicular monoamine transporter 2, and 5-(2-[18F]fluoroethoxy)-benzovesamicol (FEOBV) for the vesicular acetylcholine transporter. These radiotracers represent the culmination of years of effort at the design, synthesis, and evaluation in animals of candidate radiolabeled ligands for vesicular transporters.

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