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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Authors: Álvarez-Pérez, Beltrán; Poras, Hervé; Maldonado, Rafael, 1961-
Format: Article
Status:Published version
Publication date:2022
Country:España
Institution:Universitat Pompeu Fabra
Repository:Repositorio Digital de la UPF
OAI Identifier:oai:repositori.upf.edu:10230/52218
Online Access:http://hdl.handle.net/10230/52218
http://dx.doi.org/10.1111/bph.15656
Access Level:Open access
Keyword:Aminopeptidase N
Dual enkephalinase inhibitor
Neprilysin
Opioid
Opioid use disorders
δ-opioid receptor
μ-opioid receptor
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author Álvarez-Pérez, Beltrán
author2 Poras, Hervé
Maldonado, Rafael, 1961-
author2_role author
author
author_browse Maldonado, Rafael, 1961-
Poras, Hervé
Álvarez-Pérez, Beltrán
author_facet Álvarez-Pérez, Beltrán
Poras, Hervé
Maldonado, Rafael, 1961-
author_role author
collection Repositorio Digital de la UPF
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.
eu_rights_str_mv openAccess
format article
id ES_fa48df03ddcbefc7278cddfebbebcd90
institution Universitat Pompeu Fabra
instname_str Universitat Pompeu Fabra
network_acronym_str ES
network_name_str España
oai_identifier_str oai:repositori.upf.edu:10230/52218
publishDate 2022
publishDateSort 2022
publisher Wiley
publisherStr Wiley
reponame_str Repositorio Digital de la UPF
spelling The inhibition of enkephalin catabolism by dual enkephalinase inhibitor: A novel possible therapeutic approach for opioid use disorders Álvarez-Pérez, Beltrán Poras, Hervé Maldonado, Rafael, 1961- Aminopeptidase N Dual enkephalinase inhibitor Neprilysin Opioid Opioid use disorders δ-opioid receptor μ-opioid receptor 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. Wiley http://hdl.handle.net/10230/52218 http://dx.doi.org/10.1111/bph.15656
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
status_str publishedVersion
title 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_short 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
topic Aminopeptidase N
Dual enkephalinase inhibitor
Neprilysin
Opioid
Opioid use disorders
δ-opioid receptor
μ-opioid receptor
topic_facet Aminopeptidase N
Dual enkephalinase inhibitor
Neprilysin
Opioid
Opioid use disorders
δ-opioid receptor
μ-opioid receptor
url http://hdl.handle.net/10230/52218
http://dx.doi.org/10.1111/bph.15656