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In Vivo and in Vitro Characteristics of Radiolabeled Vesamicol Analogs as the Vesicular Acetylcholine Transporter Imaging Agents
Authors
Ogawa Kazuma
Shiba Kazuhiro
小川 数馬
柴 和弘
Publication date
13 June 2018
Publisher
'Hindawi Limited'
Doi
Cite
Abstract
金沢大学疾患モデル総合研究センターThe vesicular acetylcholine transporter (VAChT), a presynaptic cholinergic neuron marker, is a potential internal molecular target for the development of an imaging agent for early diagnosis of neurodegenerative disorders with cognitive decline such as Alzheimer\u27s disease (AD). Since vesamicol has been reported to bind to VAChT with high affinity, many vesamicol analogs have been studied as VAChT imaging agents for the diagnosis of cholinergic neurodeficit disorder. However, because many vesamicol analogs, as well as vesamicol, bound to sigma receptors (σ1 and σ2) besides VAChT, almost all the vesamicol analogs have been shown to be unsuitable for clinical trials. In this report, the relationships between the chemical structure and the biological characteristics of these developed vesamicol analogs were investigated, especially the in vitro binding profile and the in vivo regional brain accumulation. © 2018 Kazuma Ogawa and Kazuhiro Shiba
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Last time updated on 28/06/2022