In vitro and in vivo pharmacological activities of 14-o-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice [PDF]
, 2018 Pain, particularly chronic pain, is still an unsolved medical condition. Central goals in pain control are to provide analgesia of adequate efficacy and to reduce complications associated with the currently available drugs.
Lattanzi, Roberta +4 more
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Butorphanol: Effects of a Prototypical Agonist-Antagonist Analgesic on κ-Opioid Receptors
Journal of Pharmacological Sciences, 2005 The opioid analgesic, butorphanol (17-cyclobutylmethyl-3,14-dihydroxymorphinan) tartrate is a prototypical agonist-antagonist opioid analgesic agent whose potential for abuse has been the cause of litigation in the United States.
Stephen Commiskey +3 more
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Molecules, 2020 Achieving effective pain management is one of the major challenges associated with modern day medicine. Opioids, such as morphine, have been the reference treatment for moderate to severe acute pain not excluding chronic pain modalities.
Abdelfattah Faouzi +2 more
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Life, 2021 Cross-talk between opioid and adrenergic receptors is well-characterized and involves second messenger systems, the formation of receptor heterodimers, and the presence of extracellular allosteric binding regions for the complementary ligand; however ...
Robert Root-Bernstein, Beth Churchill
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Opioid-induced mitogen-activated protein kinase signaling in rat enteric neurons following chronic morphine treatment. [PDF]
PLoS ONE, 2014 Opioids, acting at μ opioid receptors, are commonly used for pain management. Chronic opioid treatment induces cellular adaptations, which trigger long-term side effects, including constipation mediated by enteric neurons.
Celine Duraffourd +4 more
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Molecular Perspectives for mu/delta Opioid Receptor Heteromers as Distinct, Functional Receptors
Cells, 2014 Opioid receptors are the sites of action for morphine and the other opioid drugs. Abundant evidence now demonstrates that different opioid receptor types can physically associate to form heteromers.
Edmund W. Ong, Catherine M. Cahill
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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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High-affinity naloxone binding to filamin a prevents mu opioid receptor-Gs coupling underlying opioid tolerance and dependence. [PDF]
PLoS ONE, 2008 Ultra-low-dose opioid antagonists enhance opioid analgesia and reduce analgesic tolerance and dependence by preventing a G protein coupling switch (Gi/o to Gs) by the mu opioid receptor (MOR), although the binding site of such ultra-low-dose opioid ...
Hoau-Yan Wang +2 more
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Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates [PDF]
, 2016 Fentanyl is a powerful opiate analgesic typically used for the treatment of severe and chronic pain, but its prescription is strongly limited by the well-documented side-effects.
Benyhe, Sa ́ndor +18 more
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The Efficacy of Peripheral Opioid Antagonists in Opioid-Induced Constipation and Postoperative Ileus: A Systematic Review of the Literature. [PDF]
, 2017 Opioid-induced constipation has a negative impact on quality of life for patients with chronic pain and can affect more than a third of patients. A related but separate entity is postoperative ileus, which is an abnormal pattern of gastrointestinal ...
Baratta, Jaime L. +5 more
core +1 more source