Design, synthesis, and SAR analysis of novel selective σ1 ligands

A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to σ1 and σ2 receptors. Many compounds exhibited nanomolar affinity for σ1 subtype receptor with good selectivity over σ2. A molecular modeling study was conducted in order to rationalize the experimental data, and the structure-receptor affinities are discussed.

The synthesis, SARs, and molecular modeling studies are reported.Figure optionsDownload as PowerPoint slide