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Drugs Fut 2009, 34(2): 137
ISSN 0377-8282
Copyright 2009 Clarivate Analytics
CCC: 0377-8282
DOI: 10.1358/dof.2009.034.02.1336115
The sigma-1 (delta-1) receptor and its role in the treament of mood disorders
Hayashi, T., Stahl, S.M.
Sigma (s) receptors have long been implicated in a variety of neuronal and brain functions, although their precise biochemical and physiological role, and potential involvement in neurological and psychiatric disorders, remains elusive. However, nearly 30 years after their characterization, evidence arising from various research fields has begun to unveil the biological function and clinical implications of s receptors. These receptors are intracellular molecules consisting of at least two subtypes - s1 and s2. The s1 receptor, an integral membrane protein with two transmembrane domains, mainly localizes at the endoplasmic reticulum (ER). A recent study identified the s1 receptor as possessing innate biological activity as a molecular chaperone, activity that can be activated/inactivated by synthetic compounds that bind to s1 receptors. The s1 receptor regulates Ca2+ signaling, ion channel activity, trophic factor signaling, cell survival, myelination and synaptogenesis. Certain clinically used antidepressants and steroids bind to the s1 receptor, and selective s1 agonists have demonstrated relatively rapid antidepressant-like actions in preclinical studies; such agents have been introduced into clinical trials. The recent discoveries regarding the hitherto enigmatic s receptor have fueled expectation that this receptor class may provide novel opportunities for pharmacological interventions. In this review, we present current data supporting the notion that this novel ligand-operated molecular chaperone may provide a new intracellular target for future therapeutic agents.

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