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µ Opioid Receptors

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https://www.readbyqxmd.com/read/28216062/nalmefene-reduces-reward-anticipation-in-alcohol-dependence-an-experimental-functional-magnetic-resonance-imaging-study
#1
Darren R Quelch, Inge Mick, John McGonigle, Anna C Ramos, Remy S A Flechais, Mark Bolstridge, Eugenii Rabiner, Matthew B Wall, Rexford D Newbould, Björn Steiniger-Brach, Franz van den Berg, Malcolm Boyce, Dorrit Østergaard Nilausen, Lasse Breuning Sluth, Didier Meulien, Christoph von der Goltz, David Nutt, Anne Lingford-Hughes
BACKGROUND: Nalmefene is a µ- and δ-opioid receptor antagonist, κ-opioid receptor partial agonist that has recently been approved in Europe for treating alcohol dependence. It offers a treatment approach for alcohol-dependent individuals with "high-risk drinking levels" to reduce their alcohol consumption. However, the neurobiological mechanism underpinning its effects on alcohol consumption remains to be determined. Using a randomized, double-blind, placebo-controlled, within-subject crossover design we aimed to determine the effect of a single dose of nalmefene on striatal blood oxygen level-dependent (BOLD) signal change during anticipation of monetary reward using the monetary incentive delay task following alcohol challenge...
January 10, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28125215/molecular-docking-molecular-dynamics-and-structure-activity-relationship-explorations-of-14-oxygenated-n-methylmorphinan-6-ones-as-potent-%C3%AE-opioid-receptor-agonists
#2
Stefan M Noha, Helmut Schmidhammer, Mariana Spetea
Among opioids, morphinans are of major importance as the most effective analgesic drugs acting primarily via μ-opioid receptor (μ-OR) activation. Our long-standing efforts in the field of opioid analgesics from the class of morphinans led to N-methylmorphinan-6-ones differently substituted at positions 5 and 14 as μ-OR agonists inducing potent analgesia and fewer undesirable effects. Herein we present the first thorough molecular modeling study and structure-activity relationship (SAR) explorations aided by docking and molecular dynamics (MD) simulations of 14-oxygenated N-methylmorphinan-6-ones to gain insights into their mode of binding to the μ-OR and interaction mechanisms...
February 9, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28097916/exploring-the-first-rimonabant-analog-opioid-peptide-hybrid-compound-as-bivalent-ligand-for-cb1-and-opioid-receptors
#3
Adriano Mollica, Sveva Pelliccia, Valeria Famiglini, Azzurra Stefanucci, Giorgia Macedonio, Annalisa Chiavaroli, Giustino Orlando, Luigi Brunetti, Claudio Ferrante, Stefano Pieretti, Ettore Novellino, Sandor Benyhe, Ferenc Zador, Anna Erdei, Edina Szucs, Reza Samavati, Szalbolch Dvrorasko, Csaba Tomboly, Rino Ragno, Alexandros Patsilinakos, Romano Silvestri
Cannabinoid (CB) and opioid systems are both involved in analgesia, food intake, mood and behavior. Due to the co-localization of µ-opioid (MOR) and CB1 receptors in various regions of the central nervous system (CNS) and their ability to form heterodimers, bivalent ligands targeting to both these systems may be good candidates to investigate the existence of possible cross-talking or synergistic effects, also at sub-effective doses. In this work, we selected from a small series of new Rimonabant analogs one CB1R reverse agonist to be conjugated to the opioid fragment Tyr-D-Ala-Gly-Phe-NH2...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28093646/mechanisms-of-inhibitory-action-of-trk-130-naltalimide-a-%C3%AE-opioid-receptor-partial-agonist-on-the-micturition-reflex
#4
Morihiro Fujimura, Naoki Izumimoto, Sayoko Kanie, Ryosuke Kobayashi, Satoru Yoshikawa, Shinobu Momen, Mikito Hirakata, Toshikazu Komagata, Satoshi Okanishi, Masashi Iwata, Tadatoshi Hashimoto, Takayuki Doi, Naoki Yoshimura, Koji Kawai
PURPOSE: To clarify the mechanism of inhibitory action of TRK-130 (Naltalimide), a unique µ-opioid receptor partial agonist, on the micturition reflex. METHODS: The effect of TRK-130 on isovolumetric rhythmic bladder contractions (RBCs) was examined in guinea pigs, the effect of which was clarified by co-treatment with naloxone or in spinal cord transection. The effect of TRK-130 on urodynamic parameters was also observed in guinea pigs. In addition, the effect of TRK-130 on bladder contraction induced by peripheral stimulation of the pelvic nerve was investigated in rats...
January 16, 2017: International Urology and Nephrology
https://www.readbyqxmd.com/read/28054242/anti-nociceptive-and-anti-inflammatory-actions-of-sulforaphane-in-chronic-constriction-injury-induced-neuropathic-pain-mice
#5
Cheng Wang, Congpin Wang
Neuropathic pain is still considered as incurable disease as current therapies are not ideal in terms of efficacy and tolerability. It is imperative to search for novel drugs to obtain better treatments. Sulforaphane (SFN), a derivative of glucoraphanin present in cruciferous vegetables, exhibits therapeutic effects on inflammation-related diseases. Since inflammation plays an important role in regulating chronic pain, in the present study, we investigated anti-nociceptive effects of SFN and its underlying mechanisms in a neuropathic pain mouse model, sciatic nerve chronic constriction injury (CCI)...
February 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28035588/clinical-pharmacokinetics-and-pharmacodynamics-of-naloxegol-a-peripherally-acting-%C3%A2%C2%B5-opioid-receptor-antagonist
#6
REVIEW
Khanh Bui, Diansong Zhou, Hongmei Xu, Eike Floettmann, Nidal Al-Huniti
Naloxegol is a peripherally acting µ-opioid receptor antagonist approved for use as an orally administered tablet (therapeutic doses of 12.5 and 25 mg) for the treatment of opioid-induced constipation. Over a wide dose range (i.e. single supratherapeutic doses up to 1000 mg in healthy volunteers), the pharmacokinetic properties of naloxegol appear to be time- and dose-independent. Naloxegol is rapidly absorbed, with mean time to maximum plasma concentration of <2 h. Following once-daily administration, steady state is achieved within 2-3 days and minimal accumulation is observed...
December 29, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28035035/analysis-of-u-47700-a-novel-synthetic-opioid-in-human-urine-by-lc-ms-ms-and-lc-qtof
#7
Steven W Fleming, Justin C Cooley, Leonard Johnson, C Clinton Frazee, Kristina Domanski, Kurt Kleinschmidt, Uttam Garg
The illicit drug market has rapidly evolved from synthetic cannabinoids to cathinone derivatives and now a new emerging threat of synthetic opioids. These compounds were mostly developed by pharmaceutical companies during drug discovery. The new psychoactive substances are not routinely covered in drug screening and may go undetected. Recently fentanyl analogous, AH-7921, MT-45 and now U-47700 have been encountered in clinical and forensic casework. U-47700 is gaining popularity on drug user forms as a legal alternative to heroin...
December 29, 2016: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28031268/distinct-roles-of-opioid-and-dopamine-systems-in-lateral-hypothalamic-intracranial-self-stimulation
#8
Soichiro Ide, Takehiro Takahashi, Yukio Takamatsu, George R Uhl, Hiroaki Niki, Ichiro Sora, Kazutaka Ikeda
BACKGROUND: Opioid and dopamine systems play crucial roles in reward. Similarities and differences in the neural mechanisms of reward that are mediated by these two systems have remained largely unknown. Thus, in the present study, we investigated the differences in reward function in both µ-opioid receptor knockout (MOP KO) mice and dopamine transporter knockout (DAT KO) mice, important molecules in the opioid and dopamine systems. METHODS: Mice were implanted with electrodes into the right lateral hypothalamus (lh)...
December 28, 2016: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28001096/targeting-delta-opioid-receptors-for-pain-treatment-drugs-in-phase-i-and-ii-clinical-development
#9
Viola Spahn, Christoph Stein
Opioids are widely used to treat severe pain. Most clinically used opioids activate µ-opioid receptors (MOR). Their ligands induce potent analgesia but also adverse effects. The δ-opioid receptor (DOR) is another member of the opioid receptor family that has been under intense investigation with the aim to avoid MOR-induced side effects. Areas covered: This article reviews DOR ligands which appeared to be promising after preclinical evaluation. A literature search using Pubmed, Cochrane library, ClinicalTrials...
February 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/27997452/effect-of-tapentadol-on-splenic-cytokine-production-in-mice
#10
Silvia Franchi, Giada Amodeo, Marta Gandolla, Giorgia Moschetti, Alberto Emilio Panerai, Paola Sacerdote
BACKGROUND: Opioid drugs affect immunity, but not all opioid drugs share the same immunomodulatory properties. Tapentadol is an analgesic drug with a dual synergistic mechanism of action: µ-opioid receptor agonism and noradrenaline reuptake inhibition. Weaker µ-opioid receptor agonism combined with noradrenaline reuptake inhibition results in potent analgesia with reduced opioid side effects. We evaluated the impact of tapentadol on splenic cytokine in normal and in hyperalgesia/allodynia mice, comparing it with morphine and reboxetine, a noradrenaline reuptake inhibitor...
March 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/27926949/efficacy-and-tolerability-of-co-administering-full-%C3%A2%C2%B5-opioid-receptor-agonists-with-buprenorphine-and-mixed-opioid-agonists
#11
X Ruan, J Luo, A Kaye
No abstract text is available yet for this article.
December 7, 2016: Drug Research
https://www.readbyqxmd.com/read/27801588/conformational-heterogeneity-of-intracellular-loop-3-of-the-%C3%AE-opioid-g-protein-coupled-receptor
#12
Jing Huang, Sirish Kaushik Lakkaraju, Andrew Coop, Alexander D MacKerell
G-protein coupled receptors (GPCRs), including the μ-opioid receptor, interact with G-proteins and other proteins via their intracellular face as required for signal transduction. However, characterization of the structure of the intracellular face of GPCRs is complicated by the experimental methods used for structural characterization. In the present study we undertook a series of long-time molecular dynamics (MD) simulations, ranging from 1 to 5 μs, on the μ-opioid receptor in both the dimeric and monomeric states...
November 23, 2016: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/27778501/how-oliceridine-trv-130-binds-and-stabilizes-a-%C3%AE-opioid-receptor-conformational-state-that-selectively-triggers-g-protein-signaling-pathways
#13
Sebastian Schneider, Davide Provasi, Marta Filizola
Substantial attention has recently been devoted to G protein-biased agonism of the μ-opioid receptor (MOR) as an ideal new mechanism for the design of analgesics devoid of serious side effects. However, designing opioids with appropriate efficacy and bias is challenging because it requires an understanding of the ligand binding process and of the allosteric modulation of the receptor. Here, we investigated these phenomena for TRV-130, a G protein-biased MOR small-molecule agonist that has been shown to exert analgesia with less respiratory depression and constipation than morphine and that is currently being evaluated in human clinical trials for acute pain management...
November 22, 2016: Biochemistry
https://www.readbyqxmd.com/read/27744679/identification-of-the-first-marine-derived-opioid-receptor-balanced-agonist-with-a-signaling-profile-that-resembles-the-endorphins
#14
Tyler A Johnson, Laura Milan-Lobo, Tao Che, Madeline Ferwerda, Eptisam Lambo, Nicole L McIntosh, Fei Li, Li He, Nicholas Lorig-Roach, Phillip Crews, Jennifer Lynne Whistler
Opioid therapeutics are excellent analgesics, whose utility is compromised by dependence. Morphine (1) and its clinically relevant derivatives such as OxyContin® (4), Vicodin® (5) and Dilaudid® (6) are "biased" agonists at the µ opioid receptor (OR), wherein they engage G-protein signaling but poorly engage β-arrestin and the endocytic machinery. In contrast, the endorphins, met-enkephalin (14) and β-endorphin (15), endogenous peptide agonists for ORs, are more potent analgesics then 1, show reduced liability for tolerance and dependence, and engage both G-protein and β-arrestin pathways as "balanced" agonists...
October 17, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27663572/cost-effectiveness-of-naloxegol-for-opioid-induced-constipation-in-the-uk
#15
Richard Lawson, James Ryan, Frederic King, Jo Wern Goh, Eszter Tichy, Kevin Marsh
BACKGROUND AND OBJECTIVES: Opioid-induced constipation (OIC) is the most common adverse effect reported in patients receiving opioids to manage pain. Initial treatment with laxatives provides inadequate response in some patients. Naloxegol is a peripherally acting µ-opioid receptor antagonist used to treat patients with inadequate response to laxative(s) (laxative inadequate responder [LIR]). A cost-effectiveness model was constructed from the UK payer perspective to compare oral naloxegol 25 mg with placebo in non-cancer LIR patients receiving opioids for chronic pain, and a scenario analysis of naloxegol 25 mg with rescue laxatives compared with placebo with rescue laxatives in the same patient population...
February 2017: PharmacoEconomics
https://www.readbyqxmd.com/read/27626479/metabolism-and-pharmacokinetics-of-morphine-in-neonates-a-review
#16
Gian Maria Pacifici
Morphine is an agonist of the µ and k receptors, whose activation results in analgesia. Morphine-like agonists act through the µ opioid receptors to cause pain relief, sedation, euphoria and respiratory depression. Morphine is glucuronidated and sulfated at positions 3 and 6; the plasma concentration ratios correlate positively with birth weight, which probably reflects increased liver weight with increasing birth weight. Moreover, morphine clearance correlates positively with gestational age and birth weight...
August 2016: Clinics
https://www.readbyqxmd.com/read/27553975/evaluation-of-in-vitro-and-in-vivo-anti-inflammatory-effects-of-pseudosemiglabrin-a-major-phytoconstituent-isolated-from-tephrosia-apollinea-delile-dc
#17
Loiy Elsir Ahmed Hassan, Saad S Dahham, Samah M Fadul, Muhammad Ihtisham Umar, Aman Shah Abdul Majid, Kooi Yeong Khaw, Amin Malik Shah Abdul Majid
ETHNOPHARMACOLOGICAL RELEVANCE: Tephrosia apollinea (Delile) DC (Leguminosae) has been used in folk medicine in Arabian countries to treat inflammatory disorders. The plant has been described to treat swelling, bone fracture, bronchitis, cough, earache and wounds. AIM OF THE STUDY: the current study aims to evaluate the anti-inflammatory properties of the major active phytoconstituent of T. apollinea and elucidate the mechanisms by which it inhibits inflammation in vitro and in vivo...
December 4, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27141613/-effect-of-electroacupuncture-intervention-on-expression-of-pain-sensory-and-affective-proce-ssing-related-%C3%A2%C2%B5-opioid-receptor-etc-in-the-amygdala-in-chronic-neuropathy-pain-rats
#18
Ya-xia Yan, Xiu-mei Feng, Jun-ying Wang, Cheng-lin Duanmu, Shu-ping Chen, Yong-hui Gao, Yan-jing Han, Shuang-kun Wang, Jian-liang Zhang, Jun-ling Liu
OBJECTIVE: To observe the effect of electroacupuncture (EA) on expression of pain sensory and affective processing-related µ-opioid receptor (MOR), glutamatergic AMPA receptor subunit GIuA 1, extracellular signal-regulated kinase (ERK 1/2), cAMP response element binding protein(CREB) in the amygdala in chronic constrictive injury (CC) + negative affection(NA) rats, so as to reveal its mechanism underlying pain relief. METHODS: A total of 32 male Wistar rats were randomized into normal control, model, EA, and anesthesia+ EA (AEA) groups (n = 8 in each group)...
February 2016: Zhen Ci Yan Jiu, Acupuncture Research
https://www.readbyqxmd.com/read/27127846/nociceptin-orphanin-fq-receptor-expression-in-clinical-pain-disorders-and-functional-effects-in-cultured-neurons
#19
Praveen Anand, Yiangos Yiangou, Uma Anand, Gaurav Mukerji, Marco Sinisi, Michael Fox, Anthony McQuillan, Tom Quick, Yuri E Korchev, Peter Hein
The nociceptin/orphanin FQ peptide receptor (NOP), activated by its endogenous peptide ligand nociceptin/orphanin FQ (N/OFQ), exerts several effects including modulation of pain signalling. We have examined, for the first time, the tissue distribution of the NOP receptor in clinical visceral and somatic pain disorders by immunohistochemistry and assessed functional effects of NOP and μ-opioid receptor activation in cultured human and rat dorsal root ganglion (DRG) neurons. Quantification of NOP-positive nerve fibres within the bladder suburothelium revealed a remarkable several-fold increase in detrusor overactivity (P < 0...
September 2016: Pain
https://www.readbyqxmd.com/read/27097966/sublingual-sufentanil-a-new-opportunity-for-the-improvement-of-postoperative-pain-management-in-italy
#20
P Sacerdote, F Coluzzi, A Fanelli
Despite the availability of national and international guidelines, adequate postoperative pain (POP) management is still a challenge in Italy. One of the potential reasons for the high incidence of surgical patients complaining moderate to severe pain is the difficult application of the currently recommended analgesic techniques in clinical practice. In particular, morphine, the most commonly used systemic opioid in the POP treatment, has some unfavorable pharmacodynamic and pharmacokinetic characteristics for POP management, suggesting a potential relevant improvement by using different opioids...
April 2016: European Review for Medical and Pharmacological Sciences
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