• Georgia Gris, Enrique José Cobos, Daniel Zamanillo, and Enrique Portillo-Salido.
• Drug Discovery and Preclinical Development, ESTEVE, Baldiri Reixach, 4-8, 08028, Barcelona, Spain.
• Inflamm. Res. 2015 Jun 1;64(6):377-81.

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

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