Sigma receptors [σRs]: biology in normal and diseased states

Journal of Receptor and Signal Transduction Research
Colin G Rousseaux, Stephanie F Greene

Abstract

This review compares the biological and physiological function of Sigma receptors [σRs] and their potential therapeutic roles. Sigma receptors are widespread in the central nervous system and across multiple peripheral tissues. σRs consist of sigma receptor one (σ1R) and sigma receptor two (σ2R) and are expressed in numerous regions of the brain. The sigma receptor was originally proposed as a subtype of opioid receptors and was suggested to contribute to the delusions and psychoses induced by benzomorphans such as SKF-10047 and pentazocine. Later studies confirmed that σRs are non-opioid receptors (not an µ opioid receptor) and play a more diverse role in intracellular signaling, apoptosis and metabolic regulation. σ1Rs are intracellular receptors acting as chaperone proteins that modulate Ca2+ signaling through the IP3 receptor. They dynamically translocate inside cells, hence are transmembrane proteins. The σ1R receptor, at the mitochondrial-associated endoplasmic reticulum membrane, is responsible for mitochondrial metabolic regulation and promotes mitochondrial energy depletion and apoptosis. Studies have demonstrated that they play a role as a modulator of ion channels (K+ channels; N-methyl-d-aspartate receptors [NMDAR];...Continue Reading

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Citations

Feb 22, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mateusz KurcińskiJoanna Sadlej
Sep 12, 2019·Journal of Cellular and Molecular Medicine·Tao BaiYuling Sun
Apr 26, 2019·Journal of Psychoactive Drugs·Alexandra Vsl RodriguesMaria A Vieira-Coelho
Oct 23, 2020·Fundamental & Clinical Pharmacology·Deborah Guery, Sylvain Rheims
Oct 1, 2020·International Journal of Molecular Sciences·Mikhail V VoroninSergei B Seredenin
Feb 12, 2021·Briefings in Bioinformatics·Alisa PavelDario Greco
Feb 25, 2021·Journal of Neural Transmission·Wojciech DanyszPeter Riederer
Apr 17, 2019·Bioorganic & Medicinal Chemistry·Gladys AsongSeth Y Ablordeppey
Jul 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Giuseppe RomeoLoredana Salerno
May 22, 2020·ACS Medicinal Chemistry Letters·Daniele ZampieriMaria Grazia Mamolo
Feb 6, 2020·Molecular Pharmaceutics·Anna SchildtJanine Doorduin
Sep 26, 2017·Journal of Agricultural and Food Chemistry·Inés Reynoso-MorenoJuan Manuel Viveros-Paredes
Oct 12, 2021·Experimental and Therapeutic Medicine·Lixia LouWei Jing Liu

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Methods Mentioned

BETA
antisense oligonucleotides
GTPase
co-immunoprecipitation
transgenic
reverse transcription PCR
biopsies
confocal microscopy
light microscopy
xenograft

Software Mentioned

Prozac

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