It has been demonstrated that opioid agonists that preferentially act at μ-opioid receptors to
activate G protein signaling over βarrestin2 recruitment produce antinociception with less …

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 …

The mu opioid receptor-selective agonist, SR-17018, preferentially activates GTPγS binding
over βarrestin2 recruitment in cellular assays, thereby demonstrating signaling bias. In mice …

Background µ-Opioid receptor internalization is considered to be critically linked to
antinociceptive tolerance. Although µ-opioid receptor agonists have been administered …

Morphine is one of the most potent analgesic drugs. However, the utility of morphine in the
management of chronic pain is limited by its rapid development of tolerance. Morphine …

Morphine is a potent analgesic, yet, like most opioid narcotics, it exerts unwanted side
effects such as constipation and respiratory suppression, thereby limiting its clinical utility …

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

The ability of a ligand to preferentially promote engagement of one signaling pathway over
another downstream of GPCR activation has been referred to as signaling bias, functional …

Opioid tendency to generate analgesic tolerance has been previously linked to biased
internalization. Here, we assessed an alternative possibility; whether tolerance of delta …

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 …