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

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

Citation

Ying-Ting Hsu, Shen-Ren Chen, Yung-Chiao Chang, Hsiao-Fu Chang, Teng-Kuang Yeh, Jian-Ying Chuang, Horace H Loh, Hsing-Pang Hsieh, Shau-Hua Ueng, Shiu-Hwa Yeh. A dual nociceptin and mu opioid receptor agonist exhibited robust antinociceptive effect with decreased side effects. European journal of medicinal chemistry. 2023 Oct 05;258:115608

Mesh Tags

Substances

PMID: 37437352

search → result