Synthesis and evaluation of a new vesamicol analog o-[C-11]methyl-trans-decalinvesamicol as a PET ligand for the vesicular acetylcholine transporter

摘要

We focused on the vesicle acetyl choline transporter (VAChT) as target for early diagnosis of Alzheimer's diseases because the dysfunction of the cholinergic nervous system is closely associated with the symptoms of AD, such as problem in recognition, memory, and learning. Due to its low binding affinity for the sigma receptors (sigma-1 and sigma-2), o-methyl-trans-decalinvesamicol (OMDV) demonstrated a high binding affinity and selectivity for vesicular acetyl choline transporter (VAChT). [C-11]OMDV was prepared and investigated the potential as a new PET ligand for VAChT imaging through in vivo evaluation.