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Sigma-1 receptor and inflammatory pain

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Abstract

Introduction

The sigma-1 receptor (Sig-1R) is a unique ligand-regulated molecular chaperone that interacts with several protein targets such as G protein-coupled receptors and ion channels to modulate their activity. Sig-1R is located in areas of the central and peripheral nervous system that are key to pain control. Previous preclinical studies have suggested a potential therapeutic use of Sig-1R antagonists for the management of neuropathic pain.

Discussion

Recent studies using pharmacological and genetic tools have explored the role of Sig-1R in inflammatory pain conditions. Mice lacking the Sig-1R have shown different patterns of phenotypic responses to inflammatory injury. Systemic or peripheral administration of several Sig-1R antagonists, including the selective Sig-1R antagonist S1RA, inhibited both mechanical and thermal hypersensitivity in several preclinical models of inflammatory pain. These recent studies are summarized in the present commentary.

Conclusion

Central and peripheral pharmacological blockade of Sig-1R could be an effective option to treat inflammatory pain.

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Acknowledgments

Enrique J Cobos was partially supported by Grant SAF2013-47481-P from the Spanish Government (Madrid, Spain), FEDER funds, Grant CTS109 from the Junta de Andalucía (Seville, Spain), and the Research Program of the University of Granada.

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Authors and Affiliations

  1. Drug Discovery and Preclinical Development, ESTEVE, Baldiri Reixach, 4-8, 08028, Barcelona, Spain

    Georgia Gris, Daniel Zamanillo & Enrique Portillo-Salido

  2. Department of Pharmacology and Institute of Neuroscience, Faculty of Medicine, University of Granada, Granada, Spain

    Enrique José Cobos

Authors
  1. Georgia Gris
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  2. Enrique José Cobos
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  3. Daniel Zamanillo
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  4. Enrique Portillo-Salido
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Corresponding author

Correspondence to Enrique Portillo-Salido.

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Responsible Editor: Ji Zhang.

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Gris, G., Cobos, E.J., Zamanillo, D. et al. Sigma-1 receptor and inflammatory pain. Inflamm. Res. 64, 377–381 (2015). https://doi.org/10.1007/s00011-015-0819-8

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  • DOI: https://doi.org/10.1007/s00011-015-0819-8

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