The two β-arrestins, β-arrestin-1 and-2 (systematic names: arrestin-2 and-3, respectively),
are multifunctional intracellular proteins that regulate the activity of a very large number of …

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 …

Opioids are effective analgesics, but their use is beset by serious side effects, including
addiction and respiratory depression, which contribute to the ongoing opioid crisis. The …

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 …

Etonitazene and related 2-benzylbenzimidazoles are potent analgetics invented in the
research laboratories of the Swiss pharmaceutical giant CIBA in the late 1950s. Though the …

Synthetic opioids are increasingly challenging to combat the opioid epidemic and act
primarily at opioid receptors, chiefly the G protein-coupled receptor (GPCR) μ-opioid …

Fentanyl derivatives (FENS) belongs to the class of Novel Synthetic Opioids that emerged in
the illegal drug market of New Psychoactive Substances (NPS). These substances have …

The κ-opioid receptor (KOR) has recently emerged as an alternative therapeutic target for
the development of pain medications, without deleterious side effects associated with the μ …

Abstract Background and Purpose Opioid‐induced respiratory depression limits the use of μ‐
opioid receptor agonists in clinical settings and is the main cause of opioid overdose …

The type-1 cannabinoid receptor (CB 1) is a promising drug target for a wide range of
diseases. However, many existing and novel candidate ligands for CB 1 have shown only …