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 …

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 …

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 …

Background and Purpose GPCRs can signal through both G proteins and β‐arrestin2. For
the μ‐opioid receptor, early experimental evidence from a single study suggested that G …

Opioids are the oldest and most potent drugs for the treatment of severe pain. Their clinical
application is undisputed in acute (eg, postoperative) and cancer pain, but their long-term …

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 …

Biased agonism describes the ability of ligands to stabilize different conformations of a
GPCR linked to distinct functional outcomes and offers the prospect of designing pathway …

In ligand bias different agonist drugs are thought to produce distinct signaling outputs when
activating the same receptor. If these signaling outputs mediate therapeutic versus adverse …

G protein coupled receptors have historically been one of the most druggable classes of
cellular proteins. The members of this large receptor gene family couple to primary effectors …

Buprenorphine is a Schedule III opioid analgesic with unique pharmacodynamic and
pharmacokinetic properties that may be preferable to those of Schedule II full μ-opioid …