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

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Urits I, Viswanath O, Orhurhu V, Gress K, Charipova K, Kaye AD, Ngo A

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.

PubMed ID

30880365 [ View in PubMed

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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 beta-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 beta-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 beta-arrestin pathway. Recent insights into the function and structure of G protein-coupled receptors has led to the development of novel analgesic therapies.

DrugBank Data that Cites this Article

Drugs

Oliceridine

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Oliceridine	Mu-type opioid receptor	Protein	Humans	Yes	Agonist	Details