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

Author: Glennon, R. A.

Source: Mini Reviews in Medicinal Chemistry, Volume 5, Number 10, October 2005 , pp. 927-940(14)

Publisher: Bentham Science Publishers

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Abstract:

At least two different types of sigma sgr

(

1 and

2) receptors have been identified. A structural feature common to high-affinity (Ki <10 nM) sgr

1 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

Document Type: Review article

DOI: http://dx.doi.org/10.2174/138955705774329519

Affiliations: 1: Department of Medicinal Chemistry, School of Pharmacy, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, Virginia 23298-0540, USA.

Publication date: 2005-10-01

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