Nuclear Medicine and Biology
Volume 36, Issue 5 , Pages 489-493, July 2009

Positron emission tomography imaging of (2R,3R)-5-[18F]fluoroethoxybenzovesamicol in rat and monkey brain: a radioligand for the vesicular acetylcholine transporter☆

Division of Nuclear Medicine, Department of Radiology, University of Michigan School of Medicine, Ann Arbor, MI 48109, USA

Received 23 January 2009; received in revised form 12 February 2009; accepted 17 February 2009. published online 12 May 2009.

Abstract 

Introduction

The regional brain distribution of (2R,3R)-5-[18F]fluoroethoxy-benzovesamicol ((−)-[18F]FEOBV), a radioligand for the vesicular acetylcholine transporter (VAChT), was examined in vivo in mice, rats and rhesus monkeys.

Methods

Regional brain distributions of (−)-[18F]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

(−)-[18F]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.

Keywords: Vesamicol, Vesicular transporter, PET

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☆ This work was supported by grants from the National Institutes of Health (MH66506) and the Office of Science, US Department of Energy (DE-FG02-87ER60561).

PII: S0969-8051(09)00052-3

doi:10.1016/j.nucmedbio.2009.02.007

Nuclear Medicine and Biology
Volume 36, Issue 5 , Pages 489-493, July 2009

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