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Review
, 716 (1-3), 78-93

Sigma 1 Receptor: A New Therapeutic Target for Pain

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Review

Sigma 1 Receptor: A New Therapeutic Target for Pain

Daniel Zamanillo et al. Eur J Pharmacol.

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.

Keywords: Analgesia; Neuropathic; Opioid; Pain; Sensitization; Sigma 1 receptor.

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