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Pharmacophore Identification for Sigma-1 (σ1) Receptor Binding: Application of the "Deconstruction - Reconstruction - Elaboration" Approach

[ Vol. 5 , Issue. 10 ]


R. A. Glennon   Pages 927 - 940 ( 14 )


At least two different types of sigma σ (σ1 and σ2) receptors have been identified. A structural feature common to high-affinity (Ki < 10 nM) σ1 ligands is: C-N(R)-X-Ph; both C and Ph are associated with regions of bulk tolerance. Numerous other ligands bind, but typically do so with lower affinity.


sigma receptors, arylalkylamines, arylpentylamines piperazines, piperidines, pharmacophore


Department of Medicinal Chemistry, School of Pharmacy, Medical College of Virginia Campus,Virginia Commonwealth University, Richmond, Virginia 23298-0540, USA.

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