Mu opioid receptor agonists are among the most powerful analgesic medications but also
among the most addictive. The current opioid crisis has energized a quest to develop opioid …

G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …

Decades of research advances have established a central role for endogenous opioid
systems in regulating reward processing, mood, motivation, learning and memory …

Positive allosteric modulators (PAMs) of the mu-opioid receptor (MOR) have been
hypothesized as potentially safer analgesics than traditional opioid drugs. This is based on …

Highlights•μ-OR biased agonists represent promising analgesics with improved therapeutic
profiles.•Protein-ligand interactions might account for biased ligands functional …

Opioids such as morphine and oxycodone are analgesics frequently prescribed for the
treatment of moderate or severe pain. Unfortunately, these medications are associated with …

Opioid receptors are important drug targets for pain management, addiction, and mood
disorders. Although substantial research on these important subtypes of G protein-coupled …

Allosteric modulators of G-protein-coupled receptors (GPCRs) enhance signaling by binding
to GPCRs concurrently with their orthosteric ligands, offering a novel approach to overcome …

Opioid analgesics represent a critical treatment for chronic pain in the analgesic ladder of
the World Health Organization. However, their use can result in a number of unwanted side …

In 2005, the first evidence of an allosteric binding site at the CB1R was provided by the
identification of three indoles of the company Organon that were allosteric enhancers of …