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

[ Vol. 5 , Issue. 10 ]

Author(s):

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

Abstract:


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.

Keywords:

sigma receptors, arylalkylamines, arylpentylamines piperazines, piperidines, pharmacophore

Affiliation:

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



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