IUPHAR Review - Bivalent and bifunctional opioid receptor ligands as novel analgesics
Though efficacious in managing chronic, severe pain, opioid analgesics are accompanied by significant adverse effects including constipation, tolerance, dependence, and respiratory depression.
Kyle J. Rehrauer+1 more
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Inhibition of activity of GABA transporter GAT1 by δ-opioid receptor [PDF]
Analgesia is a well-documented effect of acupuncture. A critical role in pain sensation plays the nervous system, including the GABAergic system and opioid receptor (OR) activation.
Fucke, Thomas+7 more
core +2 more sources
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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The effects of pioglitazone, a PPARγ receptor agonist, on the abuse liability of oxycodone among nondependent opioid users [PDF]
Aims: Activation of PPARγ by pioglitazone (PIO) has shown some efficacy in attenuating addictive-like responses in laboratory animals. The ability of PIO to alter the effects of opioids in humans has not been characterized in a controlled laboratory ...
Alonzo+74 more
core +1 more source
Delta-opioid receptor endocytosis in spinal cord after dermenkephalin activation
Background The delta(δ)-opioid receptors belong to the G protein-coupled receptors and in vitro studies have shown that δ-opioid receptors undergo an internalization process in response to agonist stimulation.
Gastard Myriam
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Delta opioid receptors regulate temporoammonic-activated feedforward inhibition to the mouse CA1 hippocampus. [PDF]
The opioid system influences learning and memory processes. However, neural mechanisms underlying the modulation of hippocampal activity by opioid receptors remain largely unknown. Here, we compared how mu and delta receptors operate within the mouse CA1
Xavier Rezai+3 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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Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates [PDF]
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
core +1 more source
Opioids are a mainstay in acute pain management and produce their effects and side effects (e.g., tolerance, opioid-use disorder and immune suppression) by interaction with opioid receptors.
David G. Lambert
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Butorphanol: Effects of a Prototypical Agonist-Antagonist Analgesic on κ-Opioid Receptors
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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