10th European Organic Chemistry Congress
The Scripps Research Institute-Florida, USA
Title: Addressing the opioid crisis with safer opioid pain relievers: Is it possible?
Biography: Thomas Bannister
Compounds that activate opioid receptors, especially the mu opioid receptor (MOR), have been used extensively since antiquity for pain relief and euphoria. Unfortunately poppy-derived compounds (e.g, morphine) as well as their modern synthetic functional mimics (e.g., fentanyl) also can elicit a host of unwanted side effects, include life-threatening respiratory suppression. In fact, the ongoing worldwide opioid crisis has made the dangers of opioid abuse quite clear. In our studies we have made probe molecules and potential drugs to untangle the mechanistic details of MOR signaling and its pharmacological effects. A wide respiratory safety window appears to require robust G-protein-mediated MOR signaling with almost no measurable beta arrestin involvement. We have identified functionally biased and drug-like MOR agonists with this specific profile. Further, we have found them to be robust pain relievers in mice, with greatly improved respiratory safety relative to currently available opioid drugs.