G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …

Opioids are widely used as therapeutic agents against moderate to severe acute and
chronic pain. Still, these classes of analgesic drugs have many potential limitations as they …

Drugs targeting the μ-opioid receptor (μOR) are the most effective analgesics available but
are also associated with fatal respiratory depression through a pathway that remains …

Morphine is an alkaloid from the opium poppy used to treat pain. The potentially lethal side
effects of morphine and related opioids—which include fatal respiratory depression—are …

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 …

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 …

Mu-opioid receptor agonists represent mainstays of pain management. However, the
therapeutic use of these agents is associated with serious side effects, including potentially …

Agonists of seven-transmembrane receptors, also known as G protein-coupled receptors
(GPCRs), do not uniformly activate all cellular signalling pathways linked to a given seven …