In Vitro Effects of Ligand Bias on Primate Mu Opioid Receptor Downstream Signaling.

ABSTRACT: Interest has emerged in biased agonists at the mu opioid receptor (MOR) as a possible means for maintaining potent analgesis with reduced side effect profiles. While approaches measuring in vitro biased agonism are used in the development of these compounds, their therapeutic utility will ultimately be determined by in vivo functional effects. Nonhuman primates (NHPs) are the most translational model for evaluating the behavioral effects of candidate medications, but biased signaling of these drugs at NHP MOR receptors has been unstudied. The goal of the current work was to characterize MOR ligand bias in rhesus macaques, focusing on agonists that have previously been reported to show different patterns of biased agonism in rodents and humans. Downstream signaling pathways that responded t

SUBMITTER: Zhang X 

PROVIDER: S-EPMC7312292 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature