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Development of Recombinant Proteins to Treat Chronic Pain
Published on: April 11, 2018
Sigma 1 receptor: a new therapeutic target for pain
Daniel Zamanillo1, Luz Romero, Manuel Merlos
1Esteve, Drug Discovery and Preclinical Development. Parc Científic de Barcelona. Carrer Baldiri Reixac, 4-8. 08028 Barcelona, Spain.
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.
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