Bifunctional opioid receptor ligands as novel analgesics.
Analgesics
Bifunctional activity
Drug discovery
Nociceptin (NOP) receptor
Opioids
Tolerance
Journal
Neuropharmacology
ISSN: 1873-7064
Titre abrégé: Neuropharmacology
Pays: England
ID NLM: 0236217
Informations de publication
Date de publication:
06 2019
06 2019
Historique:
received:
02
11
2018
revised:
30
01
2019
accepted:
02
03
2019
pubmed:
13
3
2019
medline:
18
12
2019
entrez:
13
3
2019
Statut:
ppublish
Résumé
Prolonged treatment of chronic severe pain with opioid analgesics is frought with problematic adverse effects including tolerance, dependence, and life-threatening respiratory depression. Though these effects are mediated predominately through preferential activation of μ opioid peptide (μOP) receptors, there is an emerging appreciation that actions at κOP and δOP receptors contribute to the observed pharmacologic and behavioral profile of μOP receptor agonists and may be targeted simultaneously to afford improved analgesic effects. Recent developments have also identified the related nociceptin opioid peptide (NOP) receptor as a key modulator of the effects of μOP receptor signaling. We review here the available literature describing OP neurotransmitter systems and highlight recent drug and probe design strategies.
Identifiants
pubmed: 30858102
pii: S0028-3908(18)30833-5
doi: 10.1016/j.neuropharm.2019.03.006
pii:
doi:
Substances chimiques
Analgesics, Opioid
0
Receptors, Opioid
0
Nociceptin Receptor
0
OPRL1 protein, human
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
195-207Informations de copyright
Copyright © 2019 Elsevier Ltd. All rights reserved.