1‑(4‑[18F]Fluorobenzyl)-4-[(tetrahydrofuran-2-yl)methyl]piperazine: A Novel Suitable Radioligand with Low Lipophilicity for Imaging σ1 Receptors in the Brain

• Published in: Journal of medicinal chemistry Vol. 60; no. 10; pp. 4161 - 4172
• Main Authors: He, Yingfang, Xie, Fang, Ye, Jiajun, Deuther-Conrad, Winnie, Cui, Bixiao, Wang, Liang, Lu, Jie, Steinbach, Jörg, Brust, Peter, Huang, Yiyun, Jia, Hongmei
• Format: Journal Article
• Language: English
• Published: American Chemical Society 25.05.2017

We have designed and synthesized novel piperazine compounds with low lipophilicity as σ1 receptor ligands. 1-(4-Fluorobenzyl)-4-[(tetrahydrofuran-2-yl)­methyl]­piperazine (10) possessed a low nanomolar σ1 receptor affinity and a high selectivity toward the vesicular acetylcholine transporter (>20...