This review provides an overview of the clinical issue of poorly controlled postoperative pain
and therapeutic approaches that may help to address this common unresolved health-care …

G protein-coupled receptors (GPCRs) are the largest class of drug targets, largely owing to
their druggability, diversity and physiological efficacy. Many drugs selectively target specific …

Biased agonism at G protein–coupled receptors describes the phenomenon whereby some
drugs can activate some downstream signaling activities to the relative exclusion of others …

Opioids are the most effective drugs for the treatment of severe pain, but they also cause
addiction and overdose deaths, which have led to a worldwide opioid crisis. Therefore, the …

Objectives The clinical utility of conventional IV opioids is limited by the occurrence of opioid‐
related adverse events. Oliceridine is a novel G protein–biased μ‐opioid receptor agonist …

G protein coupled receptors (GPCRs) convey signals across membranes via interaction with
G proteins. Originally, an individual GPCR was thought to signal through one G protein …

Analgesic design and evaluation have been driven by the desire to create high-affinity high-
selectivity mu (μ)-opioid peptide (MOP) receptor agonists. Such ligands are the mainstay of …

Purpose Oliceridine is a novel G protein-biased µ-opioid receptor agonist designed to
provide intravenous (IV) analgesia with a lower risk of opioid-related adverse events …

Opioids evoke analgesia through activation of opioid receptors (predominantly the μ opioid
receptor) in the central nervous system. Opioid receptors are abundant in multiple regions of …

Between 2000 and 2005 several studies revealed that morphine is more potent and exhibits
fewer side effects in beta-arrestin 2 knockout mice. These findings spurred efforts to develop …