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Mini-Reviews in Medicinal Chemistry

Author(s): R. A. Glennon

DOI: 10.2174/138955705774329519

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

Page: [927 - 940] Pages: 14

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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