Referenced in: none

Automatically associated channels: Kv10.1

Title: Sigma 1 receptor: A new therapeutic target for pain.

Authors: Daniel Zamanillo, Luz Romero, Manuel Merlos, Jose Miguel Vela

Journal, date & volume: Eur. J. Pharmacol., 2013 Mar 13 , ,

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23500210

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.