1. A dual nociceptin and mu opioid receptor agonist exhibited robust antinociceptive effect with decreased side effects.
- Author
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Hsu YT, Chen SR, Chang YC, Chang HF, Yeh TK, Chuang JY, Loh HH, Hsieh HP, Ueng SH, and Yeh SH
- Subjects
- Mice, Animals, Receptors, Opioid agonists, Nociceptin Receptor, Opioid Peptides pharmacology, Opioid Peptides therapeutic use, Analgesics, Opioid adverse effects, Pain chemically induced, Pain drug therapy, Analgesics adverse effects, Nociceptin, Receptors, Opioid, mu agonists, Drug-Related Side Effects and Adverse Reactions
- Abstract
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., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier Masson SAS. All rights reserved.)
- Published
- 2023
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