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. 2009 Jul;36(5):489-93.
doi: 10.1016/j.nucmedbio.2009.02.007. Epub 2009 May 8.

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

Michael R Kilbourn  1 , Brian Hockley, Lihsueh Lee, Phillip Sherman, Carole Quesada, Kirk A Frey, Robert A Koeppe
Affiliations

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

Michael R Kilbourn et al. Nucl Med Biol. 2009 Jul.

Abstract

Introduction: 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.

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Figures

Fig. 1
Fig. 1
Representative tissue time-radioactivity concentration curves for microPET imaging of (-)-[18F]FEOBV in rat brain following bolus iv injection. STR = striatum, CTX = cortex, CBL = cerebellum.
Fig. 2
Fig. 2
Representative tissue time-radioactivity concentration curves for microPET imaging of (-)-[18F]FEOBV in rhesus monkey brain following bolus iv injection. STR = striatum, CTX = cortex, THAL = thalamus, CBL = cerebellum.
Fig 3
Fig 3
PET image of (-)-[18F]FEOBV uptake into rhesus monkey brain (transaxial image at 90-120 min).
See this image and copyright information in PMC

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