1. A dual nociceptin and mu opioid receptor agonist exhibited robust antinociceptive effect with decreased side effects.
- Author
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Hsu, Ying-Ting, Chen, Shen-Ren, Chang, Yung-Chiao, Chang, Hsiao-Fu, Yeh, Teng-Kuang, Chuang, Jian-Ying, Loh, Horace H., Hsieh, Hsing-Pang, Ueng, Shau-Hua, and Yeh, Shiu-Hwa
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OPIOID receptors , *PEPTIDE receptors , *NOCICEPTIN , *PEPTIDES , *DRUGS , *LABORATORY mice - 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. [Display omitted] • Compound 14 is a bifunctional agonist of mu opioid receptor and nociceptin-orphanin FQ opioid peptide receptor. • Compound 14 exhibits robust anticonception from the thermal nociceptive mouse model. • Compound 14 validated reduced side effects such as constipation, reward, tolerance and withdrawal effects. [ABSTRACT FROM AUTHOR]
- Published
- 2023
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