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Quantifying Agonist Activity at G Protein-coupled Receptors
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Abuse Potential of Biased Mu Opioid Receptor Agonists

S Stevens Negus1, Kevin B Freeman2

  • 1Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, VA 23298, USA.

Trends in Pharmacological Sciences
|October 23, 2018
PubMed

Insights

G protein-biased mu opioid receptor (GPB-MOR) agonists, like oliceridine, show typical opioid-like abuse potential. Despite potential safety benefits, these emerging analgesics are expected to retain abuse risks.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Drug Development

Background:

  • G protein-biased mu opioid receptor (GPB-MOR) agonists represent a novel class of analgesics.
  • Conventional opioids carry significant risks of abuse and addiction.

Purpose of the Study:

  • To evaluate the abuse potential of GPB-MOR agonists.
  • To understand the safety profile of emerging opioid analgesics.

Main Methods:

  • Preclinical and clinical studies were conducted.
  • Abuse-related effects were assessed in rodents and humans.

Main Results:

  • The first-in-class GPB-MOR agonist, TRV130 (oliceridine), demonstrated typical opioid-like abuse-related effects.
  • Evidence suggests these effects occur in both animal models and human subjects.

Conclusions:

  • GPB-MOR agonists, while potentially safer on certain measures, are likely to retain abuse potential similar to conventional opioids.
  • Further research is needed to fully characterize the risks associated with this emerging drug class.
Keywords:
abuse potentialbiasmu opioid receptorreinforcementreward

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