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: Daniel Zamanillo, Luz Romero, Manuel Merlos, José Miguel Vela
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 716 Issue 1-3 Pg. 78-93 (Sep 15 2013) ISSN: 1879-0712 [Electronic] Netherlands
• PMID: 23500210 (Publication Type: Journal Article, Review)
• Copyright: © 2013 Elsevier B.V. All rights reserved.

Chemical References

• Analgesics
• Receptors, sigma

Topics

• Analgesics (pharmacology, therapeutic use)
• Animals
• Humans
• Molecular Targeted Therapy (methods)
• Nociception (drug effects)
• Pain (drug therapy, metabolism, psychology)
• Receptors, sigma (antagonists & inhibitors, metabolism)
• Sigma-1 Receptor