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

doi:10.1016/j.ejmech.2023.115608

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

Center of Applied Nanomedicine

Research output: Contribution to journal › Article › peer-review

1 Citation (Scopus)

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 language	English
Article number	115608
Journal	European Journal of Medicinal Chemistry
Volume	258
DOIs	https://doi.org/10.1016/j.ejmech.2023.115608
Publication status	Published - 2023 Oct 5

All Science Journal Classification (ASJC) codes

Pharmacology
Drug Discovery
Organic Chemistry

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10.1016/j.ejmech.2023.115608

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

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.",

author = "Hsu, {Ying Ting} and Chen, {Shen Ren} and Chang, {Yung Chiao} and Chang, {Hsiao Fu} and Yeh, {Teng Kuang} and Chuang, {Jian Ying} and Loh, {Horace H.} and Hsieh, {Hsing Pang} and Ueng, {Shau Hua} and Yeh, {Shiu Hwa}",

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AU - Hsu, Ying Ting

AU - Chen, Shen Ren

AU - Chang, Yung Chiao

AU - Chang, Hsiao Fu

AU - Yeh, Teng Kuang

AU - Chuang, Jian Ying

AU - Loh, Horace H.

AU - Hsieh, Hsing Pang

AU - Ueng, Shau Hua

AU - Yeh, Shiu Hwa

PY - 2023/10/5

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AB - 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.

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

Abstract

All Science Journal Classification (ASJC) codes

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