The Utilization of Mu-Opioid Receptor Biased Agonists: Oliceridine, an Opioid Analgesic with Reduced Adverse Effects

  • Ivan UritsEmail author
  • Omar Viswanath
  • Vwaire Orhurhu
  • Kyle Gress
  • Karina Charipova
  • Alan D. Kaye
  • Anh Ngo
Hot Topics in Pain and Headache (N. Rosen, Section Editor)
Part of the following topical collections:
  1. Topical Collection on Hot Topics in Pain and Headache


Purpose of Review

The purpose of this review is to summarize the current understanding of opioid pathways in mediating and/or modulating analgesia and adverse effects. Oliceridine is highlighted as a novel mu-opioid receptor agonist with selective activation of G protein and β-arrestin signaling pathways.

Recent Findings

Oliceridine (TRV130; [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro[4.5]decan-9-yl]ethyl})amine) is a novel MOR agonist that selectively activates G protein and β-arrestin signaling pathways. A growing body of evidence suggests that compared to existing MOR agonists, Oliceridine and other G protein-selective modulators may produce therapeutic analgesic effects with reduced adverse effects.


Oliceridine provides analgesic benefits of a pure opioid agonist while limiting related adverse effects mediated through the β-arrestin pathway. Recent insights into the function and structure of G protein-coupled receptors has led to the development of novel analgesic therapies.


Oliceridine TRV130 G protein-coupled receptors (GPCR) Partial opioid agonists 


Compliance with Ethical Standards

Conflict of Interest

Ivan Urits, Omar Viswanath, Vwaire Orhurhu, Kyle Gress, Karina Charipova, and Anh Ngo declare no conflict of interest. Alan D. Kaye serves on the Speakers Bureau of Depomed and Merck.

Human and Animal Rights and Informed Consent

This article does not contain any studies with human or animal subjects performed by any of the authors.


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Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  • Ivan Urits
    • 1
    Email author
  • Omar Viswanath
    • 2
    • 3
    • 4
  • Vwaire Orhurhu
    • 1
  • Kyle Gress
    • 5
  • Karina Charipova
    • 5
  • Alan D. Kaye
    • 6
  • Anh Ngo
    • 1
  1. 1.Beth Israel Deaconess Medical Center, Department of Anesthesia, Critical Care, and Pain MedicineHarvard Medical SchoolBostonUSA
  2. 2.Valley Anesthesiology and Pain ConsultantsPhoenixUSA
  3. 3.University of Arizona College of Medicine-PhoenixPhoenixUSA
  4. 4.Creighton University School of MedicineOmahaUSA
  5. 5.Georgetown University School of MedicineWashington, DCUSA
  6. 6.Department of AnesthesiologyLouisiana State University Health Sciences CenterNew OrleansUSA

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