A dual nociceptin and mu opioid receptor agonist exhibited robust antinociceptive effect with decreased side effects
Copyright © 2023 Elsevier Masson SAS. All rights reserved..
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.
Medienart: |
E-Artikel |
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Erscheinungsjahr: |
2023 |
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Erschienen: |
2023 |
Enthalten in: |
Zur Gesamtaufnahme - volume:258 |
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Enthalten in: |
European journal of medicinal chemistry - 258(2023) vom: 05. Okt., Seite 115608 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Hsu, Ying-Ting [VerfasserIn] |
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Links: |
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Anmerkungen: |
Date Completed 19.07.2023 Date Revised 13.12.2023 published: Print-Electronic Citation Status MEDLINE |
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doi: |
10.1016/j.ejmech.2023.115608 |
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funding: |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
NLM359381650 |
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500 | |a Citation Status MEDLINE | ||
520 | |a Copyright © 2023 Elsevier Masson SAS. All rights reserved. | ||
520 | |a 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 | ||
650 | 4 | |a Journal Article | |
650 | 4 | |a Addiction | |
650 | 4 | |a Antinociception | |
650 | 4 | |a Antinociceptive tolerance | |
650 | 4 | |a Constipation | |
650 | 4 | |a Mu-opioid receptor | |
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650 | 7 | |a Nociceptin Receptor |2 NLM | |
650 | 7 | |a Opioid Peptides |2 NLM | |
650 | 7 | |a Analgesics, Opioid |2 NLM | |
650 | 7 | |a Analgesics |2 NLM | |
700 | 1 | |a Chen, Shen-Ren |e verfasserin |4 aut | |
700 | 1 | |a Chang, Yung-Chiao |e verfasserin |4 aut | |
700 | 1 | |a Chang, Hsiao-Fu |e verfasserin |4 aut | |
700 | 1 | |a Yeh, Teng-Kuang |e verfasserin |4 aut | |
700 | 1 | |a Chuang, Jian-Ying |e verfasserin |4 aut | |
700 | 1 | |a Loh, Horace H |e verfasserin |4 aut | |
700 | 1 | |a Hsieh, Hsing-Pang |e verfasserin |4 aut | |
700 | 1 | |a Ueng, Shau-Hua |e verfasserin |4 aut | |
700 | 1 | |a Yeh, Shiu-Hwa |e verfasserin |4 aut | |
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