NKTR-181
abuse liability
analgesia
mu opioid receptor
opioid use disorder
pre-clinical
Journal
Frontiers in pain research (Lausanne, Switzerland)
ISSN: 2673-561X
Titre abrégé: Front Pain Res (Lausanne)
Pays: Switzerland
ID NLM: 9918227269806676
Informations de publication
Date de publication:
2021
2021
Historique:
received:
15
04
2021
accepted:
15
07
2021
entrez:
17
3
2022
pubmed:
18
3
2022
medline:
18
3
2022
Statut:
epublish
Résumé
Mu opioid receptor (MOPr) agonists are well-known and frequently used clinical analgesics but are also rewarding due to their highly addictive and often abusive properties. This may lead to opioid use disorder (OUD) a disorder that effects millions of people worldwide. Therefore, novel compounds are urgently needed to treat OUD. As opioids are effective analgesics and OUD often occurs in conjunction with chronic pain, these novel compounds may be opioids, but they must have a low abuse liability. This could be mediated by diminishing or slowing blood-brain barrier transport, slowing target receptor binding kinetics, and showing a long half-life. NKTR-181 is a PEGylated oxycodol and a MOPr agonist that has slowed blood-brain barrier transport, a long half-life, and diminished likeability in clinical trials. In this study, we examined the signaling and behavioral profile of NKTR-181 in comparison with oxycodone to determine whether further therapeutic development of this compound may be warranted. For this preclinical study, we used a number of
Identifiants
pubmed: 35295409
doi: 10.3389/fpain.2021.695962
pmc: PMC8915576
doi:
Types de publication
Journal Article
Langues
eng
Pagination
695962Subventions
Organisme : NIGMS NIH HHS
ID : R25 GM055052
Pays : United States
Informations de copyright
Copyright © 2021 Lee, Tiwari, Bishop, Matossian, Romaneschi, Miyazaki, VanderVeen, Zalevsky, DeFea, Cahill and Walwyn.
Déclaration de conflit d'intérêts
KD was employed by company KiloDalton Consulting. The remaining authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.
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