The Sigma 2 receptor promotes and the Sigma 1 receptor inhibits mu-opioid receptor-mediated antinociception.


Journal

Molecular brain
ISSN: 1756-6606
Titre abrégé: Mol Brain
Pays: England
ID NLM: 101468876

Informations de publication

Date de publication:
11 11 2020
Historique:
received: 16 07 2020
accepted: 22 09 2020
entrez: 12 11 2020
pubmed: 13 11 2020
medline: 6 8 2021
Statut: epublish

Résumé

The Sigma-1 receptor (σ1R) has emerged as an interesting pharmacological target because it inhibits analgesia mediated by mu-opioid receptors (MOR), and also facilitates the development of neuropathic pain. Based on these findings, the recent cloning of the Sigma-2 receptor (σ2R) led us to investigate its potential role as a regulator of opioid analgesia and of pain hypersensitivity in σ2R knockout mice. In contrast to σ1R deficient mice, σ2R knockout mice developed mechanical allodynia following establishment of chronic constriction injury-induced neuropathic pain, which was alleviated by the σ1R antagonist S1RA. The analgesic effects of morphine, [D-Ala, N-MePhe, Gly-ol]-encephalin (DAMGO) and β-endorphin increased in σ1R

Identifiants

pubmed: 33176836
doi: 10.1186/s13041-020-00676-4
pii: 10.1186/s13041-020-00676-4
pmc: PMC7659117
doi:

Substances chimiques

Analgesics 0
RNA, Messenger 0
Receptors, Opioid, mu 0
Receptors, sigma 0
sigma-2 receptor 0
Morphine 76I7G6D29C

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

150

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Auteurs

Pilar Sánchez-Blázquez (P)

Neuropharmacology, Cajal Institute, Consejo Superior de Investigaciones Científicas (CSIC), Doctor Arce 37, 28002, Madrid, Spain. psb@cajal.csic.es.

Elsa Cortés-Montero (E)

Neuropharmacology, Cajal Institute, Consejo Superior de Investigaciones Científicas (CSIC), Doctor Arce 37, 28002, Madrid, Spain.

María Rodríguez-Muñoz (M)

Neuropharmacology, Cajal Institute, Consejo Superior de Investigaciones Científicas (CSIC), Doctor Arce 37, 28002, Madrid, Spain.

Manuel Merlos (M)

Drug Discovery & Preclinical Development, Esteve, Barcelona, Spain.

Javier Garzón-Niño (J)

Neuropharmacology, Cajal Institute, Consejo Superior de Investigaciones Científicas (CSIC), Doctor Arce 37, 28002, Madrid, Spain.

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Classifications MeSH