Binding characteristics of sigma2 receptor ligands

Sigma (sigma) receptors, once considered a type of opioid receptor, are now recognized as representing a unique receptive entity and at least two different types of sigma receptors have been identified: sigma1 and sigma2 receptors. Evidence suggests that these receptors might be targeted and exploited for the development of agents potentially useful for the treatment of several central disorders. This review primarily describes some of our efforts to understand those structural features that contribute to sigma2 receptor binding, and some recent work by other investigators is also included. Despite an inability to formulate a unified pharmacophore model for sigma2 binding due to the diversity of structure-types that bind at the receptor, and to the conformational flexibility of these ligands, significant progress has been made toward the development of some very high-affinity agents.

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Bibliographic Details
Main Author: Glennon,Richard A.
Format: Digital revista
Language:English
Published: Divisão de Biblioteca e Documentação do Conjunto das Químicas da Universidade de São Paulo 2005
Online Access:http://old.scielo.br/scielo.php?script=sci_arttext&pid=S1516-93322005000100002
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