In vitro profiling of opioid ligands using the cAMP formation inhibition assay and the beta-arrestin2 recruitment assay: No two ligands have the same profile

摘要

Previously, we showed that no two of seven opioids administered by the intracerebroventricular route had the same potency rank order for evoking antinociception, constipation and respiratory depression in rats. To gain insight at the cellular level, this study was designed to systematically investigate the activity profiles of six commonly used opioid ligands using the forskolin-stimulated cAMP assay and a beta-arrestin2 recruitment assay in cultured HEK-293 cells transfected with MOP(mu), DOP(delta) or KOP(kappa) receptors(-r).