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

• Main Authors: Ying Zhang (Author), Tao Wang (Author), Xiaojun Zhang (Author), Winnie Deuther-Conrad (Author), Hualong Fu (Author), Mengchao Cui (Author), Jinming Zhang (Author), Peter Brust (Author), Yiyun Huang (Author), Hongmei Jia (Author)
• Format: Book
• Published: Elsevier, 2022-03-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...