Science Signaling, 2018 High-efficacy opioids enhance receptor desensitization due to rapid and sustained GRK2/β-arrestin interactions. Controlling opioid receptor desensitization Chronic opioid use leads to tolerance and the need for increasing doses to achieve pain relief ...
E. Miess +13 more
semanticscholar +1 more source
Opioid regulation of Mu receptor internalisation: relevance to the development of tolerance and dependence [PDF]
, 2010 Internalisation of the mu opioid receptor from the surface of cells is generally achieved by receptor occupancy with agonist ligands of high efficacy. However, in many situations the potent analgesic morphine fails to promote internalisation effectively ...
Lopez-Gimenez, J.F., Milligan, G.
core +2 more sources
Structural insights into μ-opioid receptor activation
Nature, 2015 Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X-ray crystal structure of the murine μOR bound to the morphinan ...
Weijiao Huang +17 more
semanticscholar +1 more source
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
doaj +1 more source
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
core +3 more sources
Rubsicolins are naturally occurring G-protein-biased delta opioid receptor peptides
bioRxiv, 2018 The impact that β-arrestin proteins have on G-protein-coupled receptor trafficking, signaling and physiological behavior has gained much appreciation over the past decade.
Robert J. Cassell +6 more
semanticscholar +1 more source
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
doaj +1 more source
Stress-Dependent Impairment Of Passive-Avoidance Memory By Propranolol Or Naloxone [PDF]
, 2011 Previous work has shown that the effect of opioid-receptor blockade on memory modulation is critically dependent upon the intensity of stress. The current study determined the effect of adrenergic-receptor blockade on memory modulation under varied ...
Atapattu, Ranga Keshani, , \u2708 +3 more
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Dopamine-D1 and δ-opioid receptors co-exist in rat striatal neurons [PDF]
, 2006 Cocaine’s enhancement of dopaminergic neurotransmission in the mesolimbic pathway plays a critical role in the initial reinforcing properties of this drug. However, other neurotransmitter systems are also integral to the addiction process.
Ambrose-Lanci, L. M. +3 more
core +2 more sources
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
doaj +1 more source