Abstract
We evaluated the potencies of radioiodinated (−)-o-iodovesamicol [(−)-oIV] as a selective vesicular acetylcholine transporter (VAChT) mapping agent. (−)-[125I]oIV exhibited significant accumulation (about 2.8% of the injected dose) in rat brain. The regional brain distribution of radioactivity was similar for both (−)-[125I]oIV and (−)-[3H]vesamicol. The accumulation of (−)-[125I]oIV in the brain was significant reduced by post-administration of unlabeled vesamicol (0.5 μmol/kg−1) and (−)-oIV (0.5 μmol/kg−1). On the other hand, the post-administration of sigma ligands hardly affected the accumulation of (−)-[125I]oIV in the brain. These studies showed that (−)-[125I]oIV, as well as [3H]vesamicol, bound to VAChT with high affinity in the rat brain. Furthermore, (−)-[125I]oIV binding in the ipsilateral cortex to the lesion was significantly reduced by 17.0%, compared with that in the contralateral cortex in a unilateral NBM-lesioned rat. These results suggested that radioiodinated (−)-oIV may potentially be useful for the diagnosis of cholinergic neurodegenerative disorders.
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Shiba, K., Mori, H. & Tonami, N. Evaluation of radioiodinated (−)-o-iodovesamicol as a radiotracer for mapping the vesicular acetylcholine transporter. Ann Nucl Med 17, 451–456 (2003). https://doi.org/10.1007/BF03006433
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DOI: https://doi.org/10.1007/BF03006433