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

Curr Pain Headache Rep. 2019 Mar 18;23(5):31. doi: 10.1007/s11916-019-0773-1.


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.

Keywords: G protein-coupled receptors (GPCR); Oliceridine; Partial opioid agonists; TRV130.

Publication types

  • Review

MeSH terms

  • Analgesics* / adverse effects
  • Analgesics* / therapeutic use
  • Analgesics, Opioid* / adverse effects
  • Analgesics, Opioid* / therapeutic use
  • Animals
  • Drug-Related Side Effects and Adverse Reactions*
  • Humans
  • Pain / drug therapy
  • Receptors, Opioid, mu / drug effects
  • Spiro Compounds / adverse effects
  • Spiro Compounds / therapeutic use*
  • Thiophenes / adverse effects
  • Thiophenes / therapeutic use*


  • ((3-methoxythiophen-2-yl)methyl)((2-(9-(pyridin-2-yl)-6-oxaspiro(4.5)decan-9-yl)ethyl))amine
  • Analgesics
  • Analgesics, Opioid
  • Receptors, Opioid, mu
  • Spiro Compounds
  • Thiophenes