Opioid drugs and their receptors are one of the most extensively studied areas of pharmacology, and in relation to biased agonism in particular. Previous research indicated that biased agonist at the Il-opioid receptor (MOPr) can be detected. Biased agonism theory, when applied to MOPr, offers the possibility to synthesize opioid ligands, lacking such lifethreatening side effects as addiction, tolerance, hyperalgesia and respiratory depression. In the current project the ability of MOPr ligands to activate Extracellular signal-Regulated Kinases 1/2 (ERKl/2), a key mediator of GPCR actions in cells, was studied. The MOPr ligands (DAMGO, morphine, buprenorphine, methadone, oxycodone, etorphine, pentazocine and endomorphin-2) were used that display different degrees of bias between G-protein and arrestin pathways as well as different efficacies for G protein activation. The model system used was HEK293 cells stably expressing MOPr.
| Identifer | oai:union.ndltd.org:bl.uk/oai:ethos.bl.uk:688107 |
| Date | January 2015 |
| Creators | Tsisanova, Elena |
| Publisher | University of Bristol |
| Source Sets | Ethos UK |
| Detected Language | English |
| Type | Electronic Thesis or Dissertation |
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