Synthesis and evaluation of novel 18F-labeled spirocyclic piperidine derivatives as σ1 receptor ligands for positron emission tomography imaging

Y Li, X Wang, J Zhang, W Deuther-Conrad…

Index: Maisonial, Aurelie; Grosse Maestrup, Eva; Wiese, Christian; Hiller, Achim; Schepmann, Dirk; Fischer, Steffen; Deuther-Conrad, Winnie; Steinbach, Joerg; Brust, Peter; Wuensch, Bernhard Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 1 p. 257 - 269

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Citation Number: 11

Abstract

A series of spirocyclic piperidine derivatives were designed and synthesized as σ1 receptor ligands. In vitro competition binding assays showed that 1′-(4-(2-fluoroethoxy) benzyl)-3 H- spiro [2-benzofuran-1, 4′-piperidine](19) possessed high σ1 receptor affinity (K i= 0.79 nM)