The opioid receptor: emergence through millennia of pharmaceutical sciences
Frontiers in Pain Research, 2023 Throughout history humanity has searched for an optimal approach to the use of opioids that maximizes analgesia while minimizing side effects. This review reflects upon the conceptualization of the opioid receptor and the critical role that the ...
Carolyn A. Fairbanks +4 more
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Receptors for morphine and opioids
General Pharmacology: The Vascular System, 1976 Two points concerning enzymatic systems acting on disposal of morphine are discussed, namely the multiplicity of glucuronyltransferase and the effect of nalorphine on N-demethylation of morphine. Evidences of the presence of at least two different glucuronyltransferases in microsomes of rat liver, kidney and intestine are presented. These evidences are
Sánchez, Emílio +2 more
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BmK-YA, an enkephalin-like peptide in scorpion venom. [PDF]
PLoS ONE, 2012 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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Modulation of Neurally Mediated Vasodepression and Bradycardia by Electroacupuncture through Opioids in Nucleus Tractus Solitarius. [PDF]
, 2018 Stimulation of vagal afferent endings with intravenous phenylbiguanide (PBG) causes both bradycardia and vasodepression, simulating neurally mediated syncope.
Fu, Liang-Wu +3 more
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Pharmacological Profiles of Oligomerized μ-Opioid Receptors
Cells, 2013 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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BU10038 as a safe opioid analgesic with fewer side-effects after systemic and intrathecal administration in primates [PDF]
, 2019 © 2019 British Journal of Anaesthesia. Published by Elsevier Ltd. All rights reserved.Background: The marked increase in mis-use of prescription opioids has greatly affected our society. One potential solution is to develop improved analgesics which have
Cami-Kobeci, Gerta +9 more
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Peripheral sensitization increases opioid receptor expression and activation by crotalphine in rats.
PLoS ONE, 2014 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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Molecules, 2021 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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M3 muscarinic acetylcholine receptor facilitates the endocytosis of mu opioid receptor mediated by morphine independently of the formation of heteromeric complexes [PDF]
, 2017 Morphine inefficiency to induce the internalization of mu opioid (MOP) receptors observed in numerous experimental models constitutes a paradigm of G-protein coupled receptor (GPCR) functional selectivity.
Alvarez-Curto, Elisa +2 more
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Molecular and cellular mechanisms of the age-dependency of opioid analgesia and tolerance
Molecular Pain, 2012 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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