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Current Pain and Headache Reports
Published in: Current Pain and Headache Reports 5/2019

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.
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Metadata
Title
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
Publication date
01-05-2019
Publisher
Springer US
Published in
Current Pain and Headache Reports / Issue 5/2019
Print ISSN: 1531-3433
Electronic ISSN: 1534-3081
DOI
https://doi.org/10.1007/s11916-019-0773-1

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