Positron emission tomography imaging of (2R,3R)-5-[(18)F]fluoroethoxybenzovesamicol in rat and monkey brain: a radioligand for the vesicular acetylcholine transporter.
BACKGROUND
The regional brain distribution of (2R,3R)-5-[(18)F]fluoroethoxy-benzovesamicol ((-)-[(18)F]FEOBV), a radioligand for the vesicular acetylcholine transporter (VAChT), was examined in vivo in mice, rats and rhesus monkeys.


METHODS
Regional brain distributions of (-)-[(18)F]FEOBV in mice were determined using ex vivo dissection. MicroPET imaging was used to determine the regional brain pharmacokinetics of the radioligand in rat and rhesus monkey brains.


RESULTS
In all three species, clear heterogeneous regional brain distributions were obtained, with the rank order of brain tissues (striatum>thalamus>cortex>cerebellum) consistent with the distribution of cholinergic nerve terminals containing the VAChT.


CONCLUSIONS
(-)-[(18)F]FEOBV remains a viable candidate for further development as an in vivo imaging agent for positron emission tomography (PET) studies of the VAChT in the human brain.
Kilbourn
Michael R
MR
Department of Radiology, University of Michigan School of Medicine, Ann Arbor, 48109, USA. mkilbour@umich.edu
Hockley
Brian
B
Lee
Lihsueh
L
Sherman
Phillip
P
Quesada
Carole
C
Frey
Kirk A
KA
Koeppe
Robert A
RA
D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D008253:Macaca mulatta; D008297:Male; D051379:Mice; D010880:Piperidines / Q000138:chemical synthesis / Q000378:metabolism* / Q000493:pharmacokinetics; D049268:Positron-Emission Tomography; D051381:Rats; D013997:Time Factors; D014018:Tissue Distribution; D050494:Vesicular Acetylcholine Transport Proteins / Q000378:metabolism*
D008024:Ligands; D010880:Piperidines; D050494:Vesicular Acetylcholine Transport Proteins; C116169:fluoroethoxy-benzovesamicol