The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders

Despite the increasing impact of opioid use disorders on society, there is a disturbing lack of effective medications for their clinical management. An interesting innovative strategy to treat these disorders consists in the protection of endogenous opioid peptides to activate opioid receptors, avoi...

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Detalles Bibliográficos
Autores: Álvarez-Pérez, Beltrán, Poras, Hervé, Maldonado, Rafael, 1961-
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2022
País:España
Institución:Universitat Pompeu Fabra
Repositorio:Repositorio Digital de la UPF
OAI Identifier:oai:repositori.upf.edu:10230/52218
Acceso en línea:http://hdl.handle.net/10230/52218
http://dx.doi.org/10.1111/bph.15656
Access Level:acceso abierto
Palabra clave:Aminopeptidase N
Dual enkephalinase inhibitor
Neprilysin
Opioid
Opioid use disorders
δ-opioid receptor
μ-opioid receptor
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repository_id_str
spelling The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disordersÁlvarez-Pérez, BeltránPoras, HervéMaldonado, Rafael, 1961-Aminopeptidase NDual enkephalinase inhibitorNeprilysinOpioidOpioid use disordersδ-opioid receptorμ-opioid receptorDespite the increasing impact of opioid use disorders on society, there is a disturbing lack of effective medications for their clinical management. An interesting innovative strategy to treat these disorders consists in the protection of endogenous opioid peptides to activate opioid receptors, avoiding the classical opioid-like side effects. Dual enkephalinase inhibitors (DENKIs) physiologically activate the endogenous opioid system by inhibiting the enzymes responsible for the breakdown of enkephalins, protecting endogenous enkephalins and increasing their half-lives and physiological actions. The activation of opioid receptors by the increased enkephalin levels, and their well-demonstrated safety, suggests that DENKIs could represent a novel analgesic therapy and a possible effective treatment for acute opioid withdrawal, as well as a promising alternative to opioid substitution therapy minimizing side effects. This new pharmacological class of compounds could bring effective and safe medications avoiding the major limitations of exogenous opioids, representing a novel approach to overcome the problem of opioid use disorders.Wiley202220222023info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfapplication/pdfhttp://hdl.handle.net/10230/52218http://dx.doi.org/10.1111/bph.15656reponame:Repositorio Digital de la UPFinstname:Universitat Pompeu FabraInglésBr J Pharmacol. 2023;180(7):879-93© 2021 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society. This is an open access article under the terms of the Creative Commons Attribution-NonCommercial License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited and is not used for commercial purposes.http://creativecommons.org/licenses/by-nc/4.0/info:eu-repo/semantics/openAccessoai:repositori.upf.edu:10230/522182026-06-12T07:21:37Z
dc.title.none.fl_str_mv The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders
title The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders
spellingShingle The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders
Álvarez-Pérez, Beltrán
Aminopeptidase N
Dual enkephalinase inhibitor
Neprilysin
Opioid
Opioid use disorders
δ-opioid receptor
μ-opioid receptor
title_short The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders
title_full The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders
title_fullStr The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders
title_full_unstemmed The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders
title_sort The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders
dc.creator.none.fl_str_mv Álvarez-Pérez, Beltrán
Poras, Hervé
Maldonado, Rafael, 1961-
author Álvarez-Pérez, Beltrán
author_facet Álvarez-Pérez, Beltrán
Poras, Hervé
Maldonado, Rafael, 1961-
author_role author
author2 Poras, Hervé
Maldonado, Rafael, 1961-
author2_role author
author
dc.subject.none.fl_str_mv Aminopeptidase N
Dual enkephalinase inhibitor
Neprilysin
Opioid
Opioid use disorders
δ-opioid receptor
μ-opioid receptor
topic Aminopeptidase N
Dual enkephalinase inhibitor
Neprilysin
Opioid
Opioid use disorders
δ-opioid receptor
μ-opioid receptor
description Despite the increasing impact of opioid use disorders on society, there is a disturbing lack of effective medications for their clinical management. An interesting innovative strategy to treat these disorders consists in the protection of endogenous opioid peptides to activate opioid receptors, avoiding the classical opioid-like side effects. Dual enkephalinase inhibitors (DENKIs) physiologically activate the endogenous opioid system by inhibiting the enzymes responsible for the breakdown of enkephalins, protecting endogenous enkephalins and increasing their half-lives and physiological actions. The activation of opioid receptors by the increased enkephalin levels, and their well-demonstrated safety, suggests that DENKIs could represent a novel analgesic therapy and a possible effective treatment for acute opioid withdrawal, as well as a promising alternative to opioid substitution therapy minimizing side effects. This new pharmacological class of compounds could bring effective and safe medications avoiding the major limitations of exogenous opioids, representing a novel approach to overcome the problem of opioid use disorders.
publishDate 2022
dc.date.none.fl_str_mv 2022
2022
2023
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/10230/52218
http://dx.doi.org/10.1111/bph.15656
url http://hdl.handle.net/10230/52218
http://dx.doi.org/10.1111/bph.15656
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Br J Pharmacol. 2023;180(7):879-93
dc.rights.none.fl_str_mv http://creativecommons.org/licenses/by-nc/4.0/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv http://creativecommons.org/licenses/by-nc/4.0/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Wiley
publisher.none.fl_str_mv Wiley
dc.source.none.fl_str_mv reponame:Repositorio Digital de la UPF
instname:Universitat Pompeu Fabra
instname_str Universitat Pompeu Fabra
reponame_str Repositorio Digital de la UPF
collection Repositorio Digital de la UPF
repository.name.fl_str_mv
repository.mail.fl_str_mv
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