μ-Opioid receptors are among the most studied G protein-coupled receptors because of the
therapeutic value of agonists, such as morphine, that are used to treat chronic pain …

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 …

Morphine and other agonists of the μ‐opioid receptor are used clinically for acute and
chronic pain relief and are considered to be the gold standard for pain medication. However …

While mu opioid receptor (MOR) agonists are especially effective as broad-spectrum pain
relievers, it has been exceptionally difficult to achieve a clear separation of analgesia from …

Opioid receptors are 7‐transmembrane domain receptors that couple to heterotrimeric G
proteins. The endogenous ligands for opioid receptors are peptides which bind to the …

Allosteric modulators of G protein-coupled receptors (GPCRs) have a number of potential
advantages compared to agonists or antagonists that bind to the orthosteric site of the …

The classic model of GPCR activation proposed that all agonists induce the same active
receptor conformation. However, research over the last decade has shown that GPCRs exist …

Opioids such as morphine—acting at the mu opioid receptor—are the mainstay for treatment
of moderate to severe pain and have good efficacy in these indications. However, these …

Conventional opioids mediate analgesia as well as severe adverse effects via G-protein
coupled opioid receptors (OR) in both inflamed (peripheral injured tissue) and healthy …

Despite the critical need, no previous research has substantiated safe opioid analgesics
without abuse liability in primates. Recent advances in medicinal chemistry have led to the …