title: Sigma 1 receptor: a new therapeutic target for pain.
abstract: Sigma 1 receptor (σ₁ receptor) is a unique ligand-regulated molecular chaperone located mainly in the endoplasmic reticulum and the plasma membrane. σ₁ receptor is activated under stress or pathological conditions and interacts with several neurotransmitter receptors and ion channels to modulate their function. The effects reported preclinically with σ₁ receptor ligands are consistent with a role for σ₁ receptor in central sensitization and pain hypersensitivity and suggest a potential therapeutic use of σ₁ receptor antagonists for the management of neuropathic pain as monotherapy. Moreover, data support their use in opioid adjuvant therapy: combination of σ₁ receptor antagonists and opioids results in potentiation of opioid analgesia, without significant increases in opioid-related unwanted effects. Results from clinical trials using selective σ₁ receptor antagonists in several pain conditions are eagerly awaited to ascertain the potential of σ₁ receptor modulation in pain therapy.
authors.affiliation: Esteve, Drug Discovery and Preclinical Development. Parc Científic de Barcelona. Carrer Baldiri Reixac, 4-8. 08028 Barcelona, Spain.
authors.forename: Daniel
authors.initials: D
authors.lastname: Zamanillo
authors.forename: Luz
authors.initials: L
authors.lastname: Romero
authors.forename: Manuel
authors.initials: M
authors.lastname: Merlos
authors.forename: José Miguel
authors.initials: JM
authors.lastname: Vela
mesh_terms: D000700:Analgesics / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D006801:Humans; D058990:Molecular Targeted Therapy / Q000379:methods*; D059225:Nociception / Q000187:drug effects; D010146:Pain / Q000188:drug therapy* / Q000378:metabolism / Q000523:psychology; D017480:Receptors, sigma / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000097605:Sigma-1 Receptor
chemical_list: D000700:Analgesics; D017480:Receptors, sigma; D000097605:Sigma-1 Receptor
keywords: Analgesia; Neuropathic; Opioid; Pain; Sensitization; Sigma 1 receptor