Mu-opioid receptor selective superagonists produce prolonged respiratory depression.

Cellular neuroscience Molecular neuroscience Neuroscience

Journal

iScience
ISSN: 2589-0042
Titre abrégé: iScience
Pays: United States
ID NLM: 101724038

Informations de publication

Date de publication:
21 Jul 2023
Historique:
received: 22 11 2022
revised: 17 03 2023
accepted: 09 06 2023
medline: 7 7 2023
pubmed: 7 7 2023
entrez: 7 7 2023
Statut: epublish

Résumé

Synthetic opioids are increasingly challenging to combat the opioid epidemic and act primarily at opioid receptors, chiefly the G protein-coupled receptor (GPCR) μ-opioid receptor (MOR), which signals through G protein-dependent and β-arrestin pathways. Using a bioluminescence resonance energy transfer (BRET) system, we investigate GPCR-signaling profiles by synthetic nitazenes, which are known to cause overdose and death due to respiratory depression. We show that isotonitazene and its metabolite,

Identifiants

pubmed: 37416459
doi: 10.1016/j.isci.2023.107121
pii: S2589-0042(23)01198-7
pmc: PMC10320493
doi:

Types de publication

Journal Article

Langues

eng

Pagination

107121

Subventions

Organisme : NIGMS NIH HHS
ID : T32 GM080202
Pays : United States

Informations de copyright

© 2023 The Author(s).

Déclaration de conflit d'intérêts

The authors declare no competing financial interests.

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Auteurs

Nicholas J Malcolm (NJ)

Department of Cell Biology, Neurobiology, and Anatomy, Medical College of Wisconsin, Milwaukee, WI 53226, USA.

Barbara Palkovic (B)

Department of Anesthesiology, Medical College of Wisconsin, Milwaukee, WI 53226, USA.

Daniel J Sprague (DJ)

Department of Cell Biology, Neurobiology, and Anatomy, Medical College of Wisconsin, Milwaukee, WI 53226, USA.

Maggie M Calkins (MM)

Department of Cell Biology, Neurobiology, and Anatomy, Medical College of Wisconsin, Milwaukee, WI 53226, USA.

Janelle K Lanham (JK)

Department of Cell Biology, Neurobiology, and Anatomy, Medical College of Wisconsin, Milwaukee, WI 53226, USA.

Adam L Halberstadt (AL)

Department of Psychiatry, University of California San Diego, La Jolla, CA 92093, USA.
Research Service, VA San Diego Healthcare System, San Diego, CA 92108, USA.

Astrid G Stucke (AG)

Department of Anesthesiology, Medical College of Wisconsin, Milwaukee, WI 53226, USA.

John D McCorvy (JD)

Department of Cell Biology, Neurobiology, and Anatomy, Medical College of Wisconsin, Milwaukee, WI 53226, USA.

Classifications MeSH