A dual nociceptin and mu opioid receptor agonist exhibited robust antinociceptive effect with decreased side effects

Copyright © 2023 Elsevier Masson SAS. All rights reserved..

The compelling demand of a consummate analgesic medication without addiction is rising due to the clinical mistreatment. Additionally, the series of severe untoward effects usually deterred the utilization while coping with serious pain. As a possible turning point, we revealed that compound 14 is a dual agonist of mu opioid receptor (MOR) and nociceptin-orphanin FQ opioid peptide (NOP) receptor in this study. More importantly, compound 14 achieves pain relieving at very small doses, meanwhile, reduces several unwanted side effects such as constipation, reward, tolerance and withdrawal effects. Here, we evaluated the antinociception and side effects of this novel compound from wild type and humanized mice to further develop a safer prescription analgesic drug.

Medienart:

E-Artikel

Erscheinungsjahr:

2023

Erschienen:

2023

Enthalten in:

Zur Gesamtaufnahme - volume:258

Enthalten in:

European journal of medicinal chemistry - 258(2023) vom: 05. Okt., Seite 115608

Sprache:

Englisch

Beteiligte Personen:

Hsu, Ying-Ting [VerfasserIn]
Chen, Shen-Ren [VerfasserIn]
Chang, Yung-Chiao [VerfasserIn]
Chang, Hsiao-Fu [VerfasserIn]
Yeh, Teng-Kuang [VerfasserIn]
Chuang, Jian-Ying [VerfasserIn]
Loh, Horace H [VerfasserIn]
Hsieh, Hsing-Pang [VerfasserIn]
Ueng, Shau-Hua [VerfasserIn]
Yeh, Shiu-Hwa [VerfasserIn]

Links:

Volltext

Themen:

Addiction
Analgesics
Analgesics, Opioid
Antinociception
Antinociceptive tolerance
Constipation
Journal Article
Mu-opioid receptor
Nociceptin Receptor
Opioid Peptides
Receptors, Opioid
Receptors, Opioid, mu
Reward effect

Anmerkungen:

Date Completed 19.07.2023

Date Revised 13.12.2023

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1016/j.ejmech.2023.115608

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM359381650