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

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

Author information

1
Beth Israel Deaconess Medical Center, Department of Anesthesia, Critical Care, and Pain Medicine, Harvard Medical School, 330 Brookline Ave, Boston, MA, 02215, USA. iurits@bidmc.harvard.edu.
2
Valley Anesthesiology and Pain Consultants, Phoenix, AZ, USA.
3
University of Arizona College of Medicine-Phoenix, Phoenix, AZ, USA.
4
Creighton University School of Medicine, Omaha, NE, USA.
5
Beth Israel Deaconess Medical Center, Department of Anesthesia, Critical Care, and Pain Medicine, Harvard Medical School, 330 Brookline Ave, Boston, MA, 02215, USA.
6
Georgetown University School of Medicine, Washington, DC, USA.
7
Department of Anesthesiology, Louisiana State University Health Sciences Center, New Orleans, LA, USA.

Abstract

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

PMID:
30880365
DOI:
10.1007/s11916-019-0773-1

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