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The Use of Computational Approaches in the Discovery and Mechanism Study of Opioid Analgesics
Opioid receptors that belong to class A G protein-coupled receptors (GPCRs) are vital in pain control. In the past few years, published high-resolution crystal structures of opioid receptor laid a solid basis for both experimental and computational ...
Bangyi Zhao, Wei Li, Lijie Sun, Wei Fu
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Historical Review: Opiate Addiction and Opioid Receptors
Substance use disorders (SUDs), defined as a collection of symptoms including tolerance and withdrawal, are chronic illnesses characterized by relapse and remission. In the United States, billions of dollars have been lost due to SUDs.
Shaocheng Wang
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BmK-YA, an enkephalin-like peptide in scorpion venom. [PDF]
By screening extracts of venom from the Asian scorpion Buthus martensii Karsch (BmK) for their abilities to activate opioid receptors, we have identified BmK-YA, an amidated peptide containing an enkephalin-like sequence. BmK-YA is encoded by a precursor
Yan Zhang+5 more
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Pharmacological Profiles of Oligomerized μ-Opioid Receptors
Opioids are widely prescribed pain relievers with multiple side effects and potential complications. They produce analgesia via G-protein-protein coupled receptors: μ-, δ-, κ-opioid and opioid receptor-like 1 receptors.
Ing-Kang Ho, Cynthia Wei-Sheng Lee
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Activated opioid receptors transmit internal signals through two major pathways: the G-protein-mediated pathway, which exerts analgesia, and the β-arrestin-mediated pathway, which leads to unfavorable side effects. Hence, G-protein-biased opioid agonists
Yusuke Karasawa+12 more
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Peripheral sensitization increases opioid receptor expression and activation by crotalphine in rats.
Inflammation enhances the peripheral analgesic efficacy of opioid drugs, but the mechanisms involved in this phenomenon have not been fully elucidated. Crotalphine (CRP), a peptide that was first isolated from South American rattlesnake C.d.
Vanessa Olzon Zambelli+6 more
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Estradiol and Mu opioid-mediated reward: The role of estrogen receptors in opioid use
Opioid use and opioid use disorder are characterized by sex and gender differences, and some of these differences may be mediated by differences in the hormonal milieu within and across individuals.
Sarah B. Ethridge, Mark A. Smith
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Molecular and cellular mechanisms of the age-dependency of opioid analgesia and tolerance
The age-dependency of opioid analgesia and tolerance has been noticed in both clinical observation and laboratory studies. Evidence shows that many molecular and cellular events that play essential roles in opioid analgesia and tolerance are actually age-
Zhao Jing+4 more
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Targeting peripheral opioid receptors to promote analgesic and anti-inflammatory actions
Mechanisms of endogenous pain control are significant. Increasing studies have clearly produced evidence for the clinical usefulness of opioids in peripheral analgesia.
Katerina eIwaszkiewicz+2 more
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BackgroundOpioid receptors are expressed not only by neural cells in the central nervous system, but also by many solid tumor cancer cells. Whether perioperative opioids given for analgesia after tumor resection surgery might inadvertently activate tumor
Amparo Belltall+16 more
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