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Image Search Results
Journal: The Journal of Pharmacology and Experimental Therapeutics
Article Title: Preclinical Testing of Nalfurafine as an Opioid-sparing Adjuvant that Potentiates Analgesia by the Mu Opioid Receptor-targeting Agonist Morphine
doi: 10.1124/jpet.118.255661
Figure Lengend Snippet: Nalfurafine is a potent G protein-biased KOR agonist. Comparison of G protein and β-arrestin signaling outcomes with a variety of KOR ligands (at indicated concentrations) compared with the reference standard U50,488. (A) G protein signaling was assessed with a GloSensor assay of cyclic AMP inhibition. (B) β-arrestin recruitment to the activated KOR was assessed via the Tango assay. (C and D) Results from GloSensor and Tango assays used to calculate bias factors for each compound from observed maximal efficacy (Emax or “Max”) and potency (EC50) values. ∆∆log(Max/EC50) values, with their 95% confidence intervals (CIs), are plotted in (D) for each compound to indicate relative (to U50,488) bias toward G protein signaling. All compounds were tested in triplicate alongside the reference standard U50,488. N ≥ 3 for all compounds.
Article Snippet: Quantification of G protein signaling-dependent changes in intracellular cyclic AMP (cAMP) levels was conducted using a
Techniques: Comparison, Inhibition