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µ Opioid Receptors

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https://www.readbyqxmd.com/read/29899455/structure-of-the-%C3%A2%C2%B5-opioid-receptor-g-i-protein-complex
#1
Antoine Koehl, Hongli Hu, Shoji Maeda, Yan Zhang, Qianhui Qu, Joseph M Paggi, Naomi R Latorraca, Daniel Hilger, Roger Dawson, Hugues Matile, Gebhard F X Schertler, Sebastien Granier, William I Weis, Ron O Dror, Aashish Manglik, Georgios Skiniotis, Brian K Kobilka
The μ-opioid receptor (μOR) is a G-protein-coupled receptor (GPCR) and the target of most clinically and recreationally used opioids. The induced positive effects of analgesia and euphoria are mediated by μOR signalling through the adenylyl cyclase-inhibiting heterotrimeric G protein Gi . Here we present the 3.5 Å resolution cryo-electron microscopy structure of the μOR bound to the agonist peptide DAMGO and nucleotide-free Gi . DAMGO occupies the morphinan ligand pocket, with its N terminus interacting with conserved receptor residues and its C terminus engaging regions important for opioid-ligand selectivity...
June 13, 2018: Nature
https://www.readbyqxmd.com/read/29886241/analgesic-effects-of-systemic-fentanyl-on-cancer-pain-are-mediated-by-not-only-central-but-also-peripheral-opioid-receptors-in-mice
#2
Akira Shinohara, Tsugunobu Andoh, Ikuo Saiki, Yasushi Kuraishi
Fentanyl is an opioid commonly prescribed for cancer pain. Using melanoma-bearing mice, we investigated whether peripheral action would contribute to fentanyl analgesia in cancer pain. Intravenous injection of fentanyl inhibited mechanical nociception in healthy mice, which was markedly inhibited by the opioid antagonist naloxone, but not naloxone methiodide, a peripherally acting opioid antagonist. Melanoma-bearing mice showed mechanical allodynia and spontaneous licking, a pain-related behavior, which were suppressed by intravenous and local injections of fentanyl...
June 7, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29885086/aerobic-exercise-modulates-anticipatory-reward-processing-via-the-%C3%AE-opioid-receptor-system
#3
Tiina Saanijoki, Lauri Nummenmaa, Jetro J Tuulari, Lauri Tuominen, Eveliina Arponen, Kari K Kalliokoski, Jussi Hirvonen
Physical exercise modulates food reward and helps control body weight. The endogenous µ-opioid receptor (MOR) system is involved in rewarding aspects of both food and physical exercise, yet interaction between endogenous opioid release following exercise and anticipatory food reward remains unresolved. Here we tested whether exercise-induced opioid release correlates with increased anticipatory reward processing in humans. We scanned 24 healthy lean men after rest and after a 1 h session of aerobic exercise with positron emission tomography (PET) using MOR-selective radioligand [11 C]carfentanil...
June 8, 2018: Human Brain Mapping
https://www.readbyqxmd.com/read/29883706/induction-of-oxidative-stress-by-long-term-treatment-of-live-hek293-cells-with-therapeutic-concentration-of-lithium-is-associated-with-down-regulation-of-%C3%AE-opioid-receptor-amount-and-function
#4
Miroslava Vosahlikova, Hana Ujcikova, Stanislav Musil, Lenka Roubalova, Martin Alda, Petr Svoboda
The functional state of δ-opioid receptor signalling cascade in live cells exposed to a therapeutic concentration of lithium for a prolonged period of time (weeks) is not known because the previous studies of Li interference with OR were oriented to µ-OR only. The same applies to the analysis of the prolonged effect of Li on oxidative stress in context with δ-OR function. HEK293 cells stably expressing δ-OR were cultivated in the presence or absence of 1 mM LiCl for 7 or 21 days, homogenized and the post-nuclear (PNS) and plasma membrane (PM) fractions prepared from all four types of cells...
June 5, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29871387/cebranopadol-a-novel-first-in-class-strong-analgesic-results-from-a-randomized-phase-iia-clinical-trial-in-postoperative-acute-pain
#5
Andrea Scholz, John Bothmer, Maurits Kok, Kornelia Hoschen, Stephen Daniels
BACKGROUND: Cebranopadol is a potent, first-in-class analgesic with a novel mechanistic approach combining nociceptin/orphanin FQ peptide (NOP) and opioid peptide receptor agonism. OBJECTIVE: We aim to evaluate, for the first time, the analgesic efficacy, safety, and tolerability of cebranopadol in patients suffering from moderate to severe acute pain following bunionectomy. STUDY DESIGN: We conducted a phase IIa, randomized, multi-center, double-blind, double-dummy, placebo- and active-controlled, parallel group clinical trial...
May 2018: Pain Physician
https://www.readbyqxmd.com/read/29858157/cyclic-biphalin-analogues-with-a-novel-linker-lead-to-potent-agonist-activities-at-mu-delta-and-kappa-opioid-receptors
#6
Michael Remesic, Giorgia Macedonio, Adriano Mollica, Frank Porreca, Victor Hruby, Yeon Sun Lee
In an effort to improve biphalin's potency and efficacy at the µ-(MOR) and δ-opioid receptors (DOR), a series of cyclic biphalin analogues 1-5 with a cystamine or piperazine linker at the C-terminus were designed and synthesized by solution phase synthesis using Boc-chemistry. Interestingly, all of the analogues showed balanced opioid agonist activities at all opioid receptor subtypes due to enhanced κ-opioid receptor (KOR) activity. Our results indicate that C-terminal flexible linkers play an important role in KOR activity compared to that of the other cyclic biphalin analogues with a hydrazine linker...
May 26, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29782380/negative-modulation-of-spinal-%C3%AE%C2%BA-opioid-receptor-mediated-antinociception-by-the-%C3%A2%C2%B5-opioid-receptor-at-selective-doses-of-pentazocine
#7
Douglas L Robinson, Subodh Nag, Sukhbir S Mokha
The mixed-action κ-opioid receptor (KOR) agonist, pentazocine, binds to both KOR and the µ-opioid receptor (MOR). Racemic (±)-pentazocine and (-)-pentazocine, each administered systemically, have been shown to produce antinociception in various animal models. In contrast, racemic (±)-pentazocine failed to produce antinociception when administered intrathecally (i.t.). However, whether spinal activation of KOR and MOR by (-)-pentazocine produces antinociception and the relative contribution of KOR and MOR in mediating antinociception remain unknown...
May 18, 2018: Neuroreport
https://www.readbyqxmd.com/read/29769636/molecular-details-of-dimerization-kinetics-reveal-negligible-populations-of-transient-%C3%A2%C2%B5-opioid-receptor-homodimers-at-physiological-concentrations
#8
Derya Meral, Davide Provasi, Diego Prada-Gracia, Jan Möller, Kristen Marino, Martin J Lohse, Marta Filizola
Various experimental and computational techniques have been employed over the past decade to provide structural and thermodynamic insights into G Protein-Coupled Receptor (GPCR) dimerization. Here, we use multiple microsecond-long, coarse-grained, biased and unbiased molecular dynamics simulations (a total of ~4 milliseconds) combined with multi-ensemble Markov state models to elucidate the kinetics of homodimerization of a prototypic GPCR, the µ-opioid receptor (MOR), embedded in a 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC)/cholesterol lipid bilayer...
May 16, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29753041/nociceptin-orphanin-fq-opioid-peptide-nop-receptor-and-%C3%A2%C2%B5-opioid-peptide-mop-receptors-both-contribute-to-the-anti-hypersensitive-effect-of-cebranopadol-in-a-rat-model-of-arthritic-pain
#9
Klaus Schiene, Wolfgang Schröder, Klaus Linz, Stefanie Frosch, Thomas M Tzschentke, Ulla Jansen, Thomas Christoph
Cebranopadol is a novel, first-in-class analgesic with agonist activity at the nociceptin/orphanin FQ opioid peptide (NOP) receptor as well as the classical opioid peptide receptors. This study investigated the anti-hypersensitive effect of cebranopadol in a rat model of arthritic pain. Selective antagonists were used to probe the involvement of the NOP receptor and the µ-opioid peptide (MOP) receptors. Experimental mono-arthritis was induced by intra-articular injection of complete Freund's adjuvant into the left hind knee joint...
May 9, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29745328/non-fatal-overdose-with-u-47700-identification-in-biological-matrices
#10
Susanna Vogliardi, Giulia Stocchero, Sergio Maietti, Marianna Tucci, Alessandro Nalesso, Rossella Snenghi, Donata Favretto
BACKGROUND/OBJECTIVE: We report on a case of severe intoxication after insufflation of U- 47700, a synthetic opioid that acts as a selective agonist of the μ-opioid receptor, and is several times more potent than morphine. A man in his 30s was found irresponsive in his apartment and was brought to the emergency department of a local hospital. A comatose state and severe respiratory depression were present. Hetero anamnesis revealed that the patient could have taken the substance named “U- 47700”, bought on the Internet...
May 9, 2018: Current Pharmaceutical Biotechnology
https://www.readbyqxmd.com/read/29733100/does-nalbuphine-have-a-niche-in-managing-pain
#11
Mellar P Davis, Carlos Fernandez, Sally Regel, Mary Lynn McPherson
Nalbuphine has been commercially available for 40 years for the treatment of acute pain; few studies have centered on management of chronic pain. Nalbuphine unique pharmacology is an advantage in pain management. It is µ antagonist, partial κ agonist for G-proteins and beta-arrestin-2. Benefits are related to G-protein interactions resulting in less nausea, pruritus, and respiratory depression than morphine. At low doses, nalbuphine reduces side effects particularly respiratory depression without loss of analgesia when combined with potent opioids...
March 2018: Journal of Opioid Management
https://www.readbyqxmd.com/read/29731678/expression-of-%C3%A2%C2%B5-opioid-receptor-in-ca1-hippocampal-astrocytes
#12
Min-Ho Nam, Kyung-Seok Han, Jaekwang Lee, Jin Young Bae, Heeyoung An, Seahyung Park, Soo-Jin Oh, Eunju Kim, Eunmi Hwang, Yong Chul Bae, C Justin Lee
µ-opioid receptor (MOR) is a class of opioid receptors with a high affinity for enkephalins and beta-endorphin. In hippocampus, activation of MOR is known to enhance the neuronal excitability of pyramidal neurons, which has been mainly attributed to a disinhibition of pyramidal neurons via activating Gαi subunit to suppress the presynaptic release of GABA in hippocampal interneurons. In contrast, the potential role of MOR in hippocampal astrocytes, the most abundant cell type in the brain, has remained unexplored...
April 2018: Experimental Neurobiology
https://www.readbyqxmd.com/read/29686804/can-oliceridine-trv130-an-ideal-novel-%C3%A2%C2%B5-receptor-g-protein-pathway-selective-%C3%A2%C2%B5-gps-modulator-provide-analgesia-without-opioid-related-adverse-reactions
#13
REVIEW
Hwoe Gyeong Ok, Su Young Kim, Su Jung Lee, Tae Kyun Kim, Billy K Huh, Kyung Hoon Kim
All drugs have both favorable therapeutic and untoward adverse effects. Conventional opioid analgesics possess both analgesia and adverse reactions, such as nausea, vomiting, and respiratory depression. The opioid ligand binds to µ opioid receptor and non-selectively activates two intracellular signaling pathways: the G protein pathway induce analgesia, while the β-arrestin pathway is responsible for the opioid-related adverse reactions. An ideal opioid should activate the G protein pathway while deactivating the β-arrestin pathway...
April 2018: Korean Journal of Pain
https://www.readbyqxmd.com/read/29677019/mu-opioid-receptors-in-nociceptive-afferents-produce-a-sustained-suppression-of-hyperalgesia-in-chronic-pain
#14
Amie Severino, Wenling Chen, Joshua K Hakimian, Brigitte L Kieffer, Claire Gaveriaux-Ruff, Wendy Walwyn, Juan Carlos Marvizon
The latent sensitization model of chronic pain reveals that recovery from some types of long-term hyperalgesia is an altered state in which nociceptive sensitization persists but is suppressed by the ongoing activity of analgesic receptors such as µ-opioid receptors (MORs). To determine whether these MORs are the ones present in nociceptive afferents, we bred mice expressing Cre-recombinase under the Nav1.8 channel promoter (Nav1.8cre) with MOR-floxed mice (flMOR). These Nav1.8cre/flMOR mice had reduced MOR expression in primary afferents, as revealed by quantitative PCR, in situ hybridization and immunofluorescence colocalization with the neuropeptide CGRP...
April 17, 2018: Pain
https://www.readbyqxmd.com/read/29649035/pharmacological-characterization-of-levorphanol-a-g-protein-biased-opioid-analgesic
#15
Valerie Le Rouzic, Ankita Narayan, Amanda Hunkle, Gina F Marrone, Zhigang Lu, Susruta Majumdar, Jin Xu, Ying-Xian Pan, Gavril W Pasternak
BACKGROUND: Levorphanol is a potent analgesic that has been used for decades. Most commonly used for acute and cancer pain, it also is effective against neuropathic pain. The recent appreciation of the importance of functional bias and the uncovering of multiple µ opioid receptor splice variants may help explain the variability of patient responses to different opioid drugs. METHODS: Here, we evaluate levorphanol in a variety of traditional in vitro receptor binding and functional assays...
April 11, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29615610/alcohol-exposure-disrupts-mu-opioid-receptor-mediated-long-term-depression-at-insular-cortex-inputs-to-dorsolateral-striatum
#16
Braulio Muñoz, Brandon M Fritz, Fuqin Yin, Brady K Atwood
Drugs of abuse, including alcohol, ablate the expression of specific forms of long-term synaptic depression (LTD) at glutamatergic synapses in dorsal striatum (DS), a brain region involved in goal-directed and habitual behaviors. This loss of LTD is associated with altered DS-dependent behavior. Given the role of the µ-opioid receptor (MOR) in behavioral responding for alcohol, we explored the impact of alcohol on various forms of MOR-mediated synaptic depression that we find are differentially expressed at specific DS synapses...
April 3, 2018: Nature Communications
https://www.readbyqxmd.com/read/29589831/cellular-tolerance-at-the-%C3%A2%C2%B5-opioid-receptor-is-phosphorylation-dependent
#17
Seksiri Arttamangkul, Daniel A Heinz, James R Bunzow, Xianqiang Song, John T Williams
Phosphorylation of the μ-opioid receptor (MOR) is known as a key step in desensitization and internalization but the role in the development of long-term tolerance at the cellular level is not known. Viral expression of wild type (exWT) and mutant MORs, where all phosphorylation sites on the C-terminus (Total Phosphorylation Deficient (TPD)) were mutated to alanine, were examined in locus coeruleus neurons in a MOR knockout rat. Both receptors activated potassium conductance similar to endogenous receptors in wild type animals...
March 28, 2018: ELife
https://www.readbyqxmd.com/read/29554653/endomorphin-2-inhibits-the-activity-of-the-spinoparabrachial-projection-neuron-through-presynaptic-mechanisms-in-the-spinal-dorsal-horn-in-rats
#18
Jun-Bin Yin, Ya-Cheng Lu, Ban Feng, Zhen-Yu Wu, Ying-Biao Chen, Ting Zhang, Zhen-Zhen Kou, Ming-Ming Zhang, Han Zhang, Jin-Lian Li, Hui Li, Tao Chen, Yu-Lin Dong, Yun-Qing Li
BACKGROUND/AIMS: Spinal dorsal horn (SDH) is one of the most important regions for analgesia produced by endomorphin-2 (EM2), which has a higher affinity and specificity for the µ-opioid receptor (MOR) than morphine. Many studies have focused on substantia gelatinosa (SG, lamina II) neurons to elucidate the cellular basis for its antinociceptive effects. However, the complicated types and local circuits of interneurons in the SG make it difficult to understand the real effects of EM2...
March 15, 2018: Neuro-Signals
https://www.readbyqxmd.com/read/29542370/role-of-primary-care-physicians-in-intrathecal-pain-management-a-narrative-review-of-the-literature
#19
Gladstone C McDowell, Joseph Winchell
OBJECTIVES: The majority of patients seeking medical care for chronic pain consult a primary care physician (PCP). Because systemic opioids are commonly prescribed to patients with chronic pain, PCPs are attempting to balance the competing priorities of providing adequate pain relief while reducing risks for opioid misuse and overdose. It is important for PCPs to be aware of pain management strategies other than systemic opioid dose escalation when patients with chronic pain fail to respond to conservative therapies and to initiate a multimodal treatment plan...
March 28, 2018: Postgraduate Medicine
https://www.readbyqxmd.com/read/29516505/methadone-against-cancer-lost-in-translation
#20
REVIEW
Dirk Theile, Gerd Mikus
Recently, the opioid analgesic d,l-methadone has gained much attention as a potential antineoplastic compound, considerably triggered through lay press and media. In consequence, physicians and pharmacists are currently confronted with numerous patients willing to use d,l-methadone against their malignancies. Well-performed in vitro and in vivo models have in fact shown pro-apoptotic effects of d,l-methadone or other opioids, but also proliferation-stimulating properties. Moreover, the mechanisms of proposed opioid-stimulated apoptosis are incompletely described or contradicting...
March 8, 2018: International Journal of Cancer. Journal International du Cancer
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