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Purpose  To develop a superior VAChT imaging probe for SPECT, radiolabeled (-)-OIDV and (+)-OIDV were isolated and investigated for differences in their binding affinity and selectivity to VAChT, as well as their  in vivo  activities.    Procedures  Radioiodinated  o -iodo- trans -decalinvesamicol ([ 125 I]OIDV) has a high binding affinity for vesicular acetylcholine transporter (VAChT) both  in vitro  and  in vivo . Racemic [ 125 I]OIDV was separated into its two optical isomers (-)-[ 125 I]OIDV and (+)-[ 125 I]OIDV by HPLC. To investigate VAChT binding affinity (Ki) of two OIDV isomers,  in vitro  binding assays were performed.  In vivo  biodistribution study of each [ 125 I]OIDV isomer in blood, brain regions and major organs of rats was performed at 2,30 and 60 min post-injection.  In vivo  blocking study were performed to reveal the binding selectivity of two [ 125 I]OIDV isomers to VAChT  in vivo .  Ex vivo  autoradiography were performed to reveal the regional brain distribution of two [ 125 I]OIDV isomers and (-)-[ 123 I]OIDV for SPECT at 60 min postinjection.    Results  VAChT binding affinity (Ki) of (-)-[ 125 I]OIDV and (+)-[ 125 I]OIDV was 22.1 nM and 79.0 nM, respectively. At 2 min post-injection, accumulation of (-)-[ 125 I]OIDV was the same as that of (+)-[ 125 I]OIDV. However, (+)-[ 125 I]OIDV clearance from the brain was faster than (-)-[ 125 I]OIDV. At 30 min post-injection, accumulation of (-)-[ 125 I]OIDV (0.62 ± 0.10%ID/g) was higher than (+)-[ 125 I]OIDV (0.46 ± 0.07%ID/g) in the cortex. Inhibition of OIDV binding showed that (-)-[ 125 I]OIDV was selectively accumulated in regions known to express VAChT in the rat brain, and  ex vivo  autoradiography further confirmed these results showing similar accumulation of (-)-[ 125 I]OIDV in these regions. Furthermore, (-)-[ 123 I]OIDV for SPECT showed the same regional brain distribution as (-)-[ 125 I]OIDV.    Conclusion  These results suggest that radioiodinated (-)-OIDV may be a potentially useful tool for studying presynaptic cholinergic neurons in the brain.

plos one

In Vivo Differences between Two Optical Isomers of Radioiodinated o-iodo-trans-decalinvesamicol for Use as a Radioligand for the Vesicular Acetylcholine Transporter