Historical Background
Sigma receptors [σRs] are a relatively novel group of receptors originally discovered in the central nervous system [CNS] of mammals in 1976. They represent a ubiquitously expressed unique binding site in the CNS and other peripheral tissues. σRs are a member of the orphan receptor class for which no endogenous ligand was known until recently – dimethyltryptamine [DMT] (Fontanilla et al. 2009). They also bind with high affinity to several classes of chemically unrelated ligands such as neurosteroids, neuroleptics, dextrobenzomorphans, and several psychostimulants such as cocaine, methamphetamine, methylenedioxymethamphetamine, and methacathinone. Consequently, it is thought that the σR may mediate the immunosuppressant, antipsychotic, and neuroprotective effects of many drugs (Niitsu et al. 2012).
Historically, the σR was identified as one of the subtypes of opiate receptors, differentiated using a chronic spinal...
This is a preview of subscription content, log in via an institution to check access.
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
References
Fontanilla D, Johannessen M, Hajipour AR, Cozzi NV, Jackson MB, Ruoho AE. The hallucinogen N,N-dimethyltryptamine (DMT) is an endogenous sigma-1 receptor regulator. Science. 2009;323(5916):934–7.
Hayashi T, Su TP. Sigma-1 receptor ligands: potential in the treatment of neuropsychiatric disorders. CNS Drug. 2004;18(5):269–84.
Hayashi T, Su TP. The potential role of sigma-1 receptors in lipid transport and lipid raft reconstitution in the brain: implication for drug abuse. Life Sci. 2005;77(14):1612–24.
Kourrich S, Su TP, Fujimoto M, Bonci A. The sigma-1 receptor: roles in neuronal plasticity and disease. Trends Neurosci. 2012;35(12):762–71.
Marriott KS, Prasad M, Thapliyal V, Bose HS. sigma-1 receptor at the mitochondrial-associated endoplasmic reticulum membrane is responsible for mitochondrial metabolic regulation. J Pharmacol Exp Ther. 2012;343(3):578–86.
Megalizzi V, Le Mercier M, Decaestecker C. Sigma receptors and their ligands in cancer biology: overview and new perspectives for cancer therapy. Med Res Rev. 2012;32(2):410–27.
Niitsu T, Iyo M, Hashimoto K. Sigma-1 receptor agonists as therapeutic drugs for cognitive impairment in neuropsychiatric diseases. Curr Pharm Des. 2012;18(7):875–83.
Pal A, Fontanilla D, Gopalakrishnan A, Chae YK, Markley JL, Ruoho AE. The sigma-1 receptor protects against cellular oxidative stress and activates antioxidant response elements. Eur J Pharmacol. 2012;682(1–3):12–20.
Rousseaux CG, Greene SF. Sigma receptors [σRs]: biology in normal and diseased states. J Recept Signal Transduct Res. 2015;9:1–62.
Su TP, Hayashi T. Understanding the molecular mechanism of sigma-1 receptors: towards a hypothesis that sigma-1 receptors are intracellular amplifiers for signal transduction. Curr Med Chem. 2003;10(20):2073–80.
Su TP, Hayashi T, Maurice T, Buch S, Ruoho AE. The sigma-1 receptor chaperone as an inter-organelle signaling modulator. Trends Pharmacol Sci. 2010;31(12):557–66.
Author information
Authors and Affiliations
Corresponding author
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2018 Springer International Publishing AG
About this entry
Cite this entry
Rousseaux, C.G. (2018). Sigma Receptor (σR). In: Choi, S. (eds) Encyclopedia of Signaling Molecules. Springer, Cham. https://doi.org/10.1007/978-3-319-67199-4_101870
Download citation
DOI: https://doi.org/10.1007/978-3-319-67199-4_101870
Published:
Publisher Name: Springer, Cham
Print ISBN: 978-3-319-67198-7
Online ISBN: 978-3-319-67199-4
eBook Packages: Biomedical and Life SciencesReference Module Biomedical and Life Sciences