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Sigma‐1 receptor modulation of opioid receptor signaling
Author(s) -
Kim Felix J,
Kovalyshyn Ivanka,
Pasternak Gavril W
Publication year - 2006
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.20.4.a111-a
Subject(s) - sigma 1 receptor , receptor , opioid receptor , sigma receptor , context (archaeology) , opioid , molecular pharmacology , pharmacology , chemistry , biology , biochemistry , agonist , paleontology
Sigma‐1 receptors (S1R) have been linked to numerous, diverse biological phenomena. However, current knowledge of S1R biology remains largely descriptive, and no clear molecular mechanisms of S1R action have been established. Previous work from our laboratory showed that S1R peptide ligands could modulate opiate analgesia in vivo. Opioid receptors have been shown to form functional heterodimers, and are likely to form complex receptor assemblies with other cellular factors in a context dependent manner. Understanding how such receptor complexes are formed and regulated is essential to deciphering mechanisms of analgesia, drug tolerance, and addiction. Using opioid receptor expressing cell lines, we tested the ability of S1R ligands to modulate the pharmacology of these receptor systems at the cellular level. In our experiments, S1R‐selective ligands differentially modulated the functional potency of opiates, and demonstrated a novel mechanism of regulation wherein S1R molecules act as a modulatory component of opioid receptor function.