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Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
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Biased Opioid Ligands.

Abdelfattah Faouzi1, Balazs R Varga1, Susruta Majumdar1

  • 1Center for Clinical Pharmacology, St. Louis College of Pharmacy and Washington University School of Medicine, St. Louis, MO 63131, USA.

Molecules (Basel, Switzerland)
|September 19, 2020
PubMed
Summary
This summary is machine-generated.

Developing safer pain relievers is crucial. Biased opioid receptor ligands offer a promising strategy to achieve effective pain relief without the dangerous side effects and addiction potential of traditional opioids.

Keywords:
G-protein biasanalgesiaarrestin recruitmentmitragynineopioid receptorsrespiration

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Drug Discovery

Background:

  • Opioids are vital for pain management but have significant side effects like addiction and respiratory depression.
  • Existing opioid receptor agonists (MOR, KOR, DOR) have limitations, including adverse effects and limited clinical utility.
  • The nociceptin opioid peptide receptor (NOP receptor) and mixed MOR/NOP agonists show potential for analgesia and treating substance abuse.

Purpose of the Study:

  • To review the design and pharmacological outcomes of biased ligands targeting opioid receptors.
  • To explore biased agonism as a strategy for developing safer analgesics with reduced side effect profiles.
  • To achieve functional selectivity at opioid receptors for improved pain management.

Main Methods:

  • Review of preclinical and clinical literature on biased opioid receptor ligands.
  • Analysis of signaling pathways (G-protein vs. β-arrestin) activated by different ligands.
  • Pharmacological characterization of biased ligands for opioid receptor subtypes.

Main Results:

  • Biased ligands aim to activate specific downstream pathways, avoiding detrimental effects like tolerance and addiction.
  • Ligands that do not recruit β-arrestin 2 or favor G-protein signaling show potential for safer analgesia.
  • Functional selectivity offers a pathway to dissociate therapeutic effects from adverse events across opioid receptor subtypes.

Conclusions:

  • Biased agonism represents a key strategy in developing novel analgesics with improved safety profiles.
  • Targeting opioid receptors with biased ligands could overcome the limitations of current pain management therapies.
  • Further research into biased ligands holds promise for effective and safer pain relief.