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

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

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Article number115608
JournalEuropean Journal of Medicinal Chemistry
Volume258
DOIs
Publication statusPublished - 2023 Oct 5

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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