Published in:
01-05-2019 | Opioids | Hot Topics in Pain and Headache (N. Rosen, Section Editor)
The Utilization of Mu-Opioid Receptor Biased Agonists: Oliceridine, an Opioid Analgesic with Reduced Adverse Effects
Authors:
Ivan Urits, Omar Viswanath, Vwaire Orhurhu, Kyle Gress, Karina Charipova, Alan D. Kaye, Anh Ngo
Published in:
Current Pain and Headache Reports
|
Issue 5/2019
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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.
Summary
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.