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Article

Naltrexone, Naloxone, Morphine, and Fentanyl Pharmacologically Chaperone a Mutant μ-Opioid Receptor via an Endoplasmic Reticulum Exit Site-Dependent Pathway.

Pharmacology research & perspectives - 1 Oct 2026

Grant Stephen N, Mulcahy Matthew J, Lester Henry A

Abstract excerpt

Opioid receptor antagonists increase the plasma membrane density of μ-opioid receptors (MOR) in vivo, thereby inducing "supersensitivity" to opioid agonists. This phenomenon increases the risk of overdose in patients that were being treated with naltrexone (Ntx), a popular MOR antagonist. Although there are many studies on the effects of ligands on the plasma membrane density of MORs, their effects on MOR...

Read the complete abstract on PubMed

Topics

Naltrexone
Receptors, Opioid, mu
Endoplasmic Reticulum
Morphine
Humans
Naloxone

Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

Narcotic Antagonists

Fentanyl

Protein Transport

Animals

Vesicular Transport Proteins

HEK293 Cells

Mutation

Fluorescence Resonance Energy Transfer

Source

Open in PubMed Open full text

Identifiers

PMID: 42752995
DOI: 10.1002/prp2.70315
PMCID: PMC13585096

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 23 Oct 2026.

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