Abstract

The immunomodulatory effects of κ-opioid agonists at the intestinal epithelial level are not well characterized. In the present study, we determined that Caco-2 cells express the κ-opioid receptor and its activation by trans-(±)-3,4-dichloro- N-methyl- N[2-(1-pyrolidinyl)cyclohexyl]benzeneacetamide methanesulfonate (U-50488) leads to decreased interleukin-8 secretion in the presence of interleukin-1β. These effects were detected over a wide range (10 nM–50 μM) of U-50488 concentrations and were reversible using the κ-opioid receptor antagonist nor-binaltorphimine. Our data suggest that activation of κ-opioid receptors on Caco-2 cells decreases interleukin-8 secretion and thus may alter the chemotactic stimulus at the epithelial level.

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