Regional brain imaging of vesicular acetylcholine transporter using o-[125I]iodo-trans-decalinvesamicol as a new potential imaging probe
Article first published online: 15 NOV 2013
Copyright © 2013 Wiley Periodicals, Inc.
Volume 68, Issue 3, pages 107–113, March 2014
How to Cite
Kozaka, T., Uno, I., Kitamura, Y., Miwa, D., Anwar-Ul Azim, M., Ogawa, K. and Shiba, K. (2014), Regional brain imaging of vesicular acetylcholine transporter using o-[125I]iodo-trans-decalinvesamicol as a new potential imaging probe. Synapse, 68: 107–113. doi: 10.1002/syn.21720
- Issue published online: 21 JAN 2014
- Article first published online: 15 NOV 2013
- Accepted manuscript online: 30 OCT 2013 11:16AM EST
- Manuscript Accepted: 11 SEP 2013
- Manuscript Received: 11 APR 2013
- vesamicol analogs;
- vesicular acetylcholine transporter;
- imaging probe;
- in vivo;
In this study, the regional rat brain distribution of radioiodinated o-iodo-trans-decalinvesamicol ([125I]OIDV) was determined in vivo to evaluate its potential as a single-photon emission computed tomography (SPECT) imaging probe for vesicular acetylcholine transporter (VAChT). Following intravenous injection, [125I]OIDV passed freely across the blood–brain barrier and accumulated in rat brain. The accumulation of [125I]OIDV in rat brain was significantly reduced by coadministration of (+/−)-vesamicol (0.125 µmol). In contrast, the coadministration of σ-receptor ligands, such as (+)-pentazocine (0.125 µmol) as a σ-1 receptor ligand and (+)−3-(3-hydroxyphenyl)-N-propylpiperidine (0.125 µmol) as a σ-1 and σ-2 receptor ligands, barely affected the accumulation of [125I]OIDV in rat brain. These findings in vivo were corroborated by autoradiographic analysis ex vivo. The authors found that the tracer binds with pharmacological selectivity to VAChT in rat brain and predicted that it may likewise serve in translational SPECT imaging studies of this marker in the integrity of cholinergic innervations. Synapse 68:107–113, 2014. © 2013 Wiley Periodicals, Inc.