Sigma receptors C
Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Overview
Although termed 'receptors', the evidence for coupling through conventional signalling pathways is lacking. Initially described as a subtype of opioid receptors, there is only a modest pharmacological overlap and no structural convergence with the G protein-coupled receptors; the crystal structure of the sigma1 receptor [6] suggests a trimeric structure of a single short transmembrane domain traversing the endoplasmic reticulum membrane, with the bulk of the protein facing the cytosol. A wide range of compounds, ranging from psychoactive agents to antihistamines, have been observed to bind to these sites.
Targets
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sigma non-opioid intracellular receptor 1
C
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Further reading
How to cite this family page
Database page citation:
Sigma receptors. Accessed on 14/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=785.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Buneman OP, Faccenda E, Harding SD, Spedding M, Cidlowski JA, Fabbro D, Davenport AP, Striessnig J, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Introduction and Other Protein Targets. Br J Pharmacol. 180 Suppl 2:S1-22.
(-)-Pentazocine also shows activity at opioid receptors. The sigma2 receptor has recently been reported to be TMEM97 [1], a 4TM protein partner of NPC1, the Niemann-Pick C1 protein, a 13TM cholesterol-binding protein.