Discovery and development of brain-penetrant 18F-labeled radioligands for neuroimaging of the sigma-2 receptors

Discovery and development of brain-penetrant 18F-labeled radioligands for neuroimaging of the sigma-2 receptors

We have discovered and synthesized a series of indole-based derivatives as novel sigma-2 (σ2) receptor ligands. Two ligands with high σ2 receptor affinity and subtype selectivity were then radiolabeled with F-18 in good radiochemical yields and purities, and evaluated in rodents. In biodistribution...

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Bibliographic Details
Main Authors: Ying Zhang, Tao Wang, Xiaojun Zhang, Winnie Deuther-Conrad, Hualong Fu, Mengchao Cui, Jinming Zhang, Peter Brust, Yiyun Huang, Hongmei Jia
Format: Article
Language:English
Published: Elsevier 2022-03-01
Series:Acta Pharmaceutica Sinica B
Subjects:
Indole-based derivatives
σ2 receptor
Fluorine-18
Positron emission tomography
Neuroimaging
Online Access:http://www.sciencedirect.com/science/article/pii/S2211383521003397

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