Opioids are a mainstay of acute pain management but can have many adverse effects,
contributing to problematic long-term use. Opioid tolerance (increased dose needed for …

The visual/β-arrestins, a small family of proteins originally described for their role in the
desensitization and intracellular trafficking of G protein–coupled receptors (GPCRs), have …

G protein-biased agonists of the μ-opioid receptor (MOPr) have been proposed as an
improved class of opioid analgesics. Recent studies have been unable to reproduce the …

Opioid analgesics are powerful pain relievers; however, over time, pain control diminishes
as analgesic tolerance develops. The molecular mechanisms initiating tolerance have …

Morphine and related µ-opioid receptor (MOR) agonists remain among the most effective
drugs known for acute relief of severe pain. A major problem in treating painful conditions is …

Opioid receptors have been targeted for the treatment of pain and related disorders for
thousands of years and remain the most widely used analgesics in the clinic. Mu (μ), kappa …

Opiates are among the oldest medications available to manage a number of medical
problems. Although pain is the current focus, early use initially focused upon the treatment of …

Opioid overdoses, many of which are attributed to use of illicit fentanyl, are currently one of
the leading causes of death in the US Although fentanyl has been used safely for decades in …

A great deal of experimental evidence suggests that ligands can stabilize different receptor
active states that go on to interact with cellular signaling proteins to form a range of different …

The concept of ligand bias at G protein-coupled receptors broadens the possibilities for
agonist activities and provides the opportunity to develop safer, more selective therapeutics …