(+)-p-([F-18]fluorobenzyl)spirotrozamicol{(+)-[F-18]spiro-FBT}: Synthesis and biological evaluation of a high-affinity ligand for the vesicular acetylcholine transporter (VAChT)

(+)-1'-[4-Hydroxy-1-(4-fluorobenzyl)piperidin-3-yl]spiro[1H-indene-1,4'-pip eridine] {(+)- Spiro-FBT}, a high-affinity vesicular acetylcholine transpor ter ligand, was labeled with fluorine-18, and evaluated in the rat and monk ey. In the rat brain, (+)-[F-18]Spiro-FBT accumulated preferentially in the striatum, hippocampus, and cortex, brains regions containing high-to-moder ate densities of cholinergic terminals. However, due to rapid metabolism, n o preferential accumulation of the radiotracer was observed in correspondin g regions of the monkey brain. Consequently, rapid metabolism renders (+)-[ F-18]Spiro-FBT unsuitable for studying cholinergic function with positron e mission tomography. NUCL MED BIOL 26;2: 189-192, 1999. (C) 1999 Elsevier Sc ience Inc. All rights reserved.