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Comparative analyses of the pharmacophoric elements required for σ1 and nicotinic ligands led to the identification of a potent and selective σ1 ligand ( 15 ). Compound 15 displayed high selectivity for the σ1 receptor ( K  i , σ1 = 4.1 nM, K  i , σ2 = 1312 nM) with moderate binding affinity for the DAT ( K  i = 373 nM) and NET ( K  i = 203 nM) in the PDSP broad screening panel of common CNS neurotransmitter transporters and receptors. The key finding in this present work is that a subtle structural modifica tion could be used as a tool to switch a ligand's selectivity between nAChRs and sigma receptors.

From α4β2 Nicotinic Ligands to the Discovery of σ1 Receptor Ligands: Pharmacophore Analysis and Rational Design