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https://www.readbyqxmd.com/read/29785888/the-impact-of-oprm1-s-genetic-polymorphisms-on-methadone-maintenance-treatment-in-opioid-addicts-a-systematic-review
#1
Bilel Oueslati, Olfa Moula, Rim Ghachem
AIM: Methadone is a long-acting opioid receptor agonist. It is prescribed to patients with opioid-related use disorders. The OPRM1 gene encodes for methadone's main receptor. It appears that polymorphisms in OPRM1 may affect the efficacy of methadone maintenance treatment (MMT). OBJECTIVE: Our purpose was to identify all relevant published papers dealing with the impact ofOPRM1's SNPs  on MMT's efficacy and to summarize results in order to evaluate the relevance of conducting pretherapeutic genotyping in opioid addicts prior to the onset of MMT...
May 22, 2018: Pharmacogenomics
https://www.readbyqxmd.com/read/29785554/interactions-between-kappa-and-mu-opioid-receptor-agonists-effects-of-the-ratio-of-drugs-in-mixtures
#2
Vanessa Minervini, Hannah Y Lu, Jahnavi Padarti, Daniela C Osteicoechea, Charles P France
RATIONALE: Pain is the leading reason for seeking health care, and mu opioid receptor agonists continue to be prescribed despite well-documented adverse effects. Kappa opioid receptor agonists have antinociceptive effects with little to no abuse liability and might be useful for treating pain in mixtures. Kappa:mu opioid mixtures might be useful if therapeutic effects of each drug can be selectively increased while reducing or avoiding the adverse effects that occur with larger doses of each drug alone...
May 22, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29779230/role-of-mu-but-not-delta-or-kappa-opioid-receptors-in-context-induced-reinstatement-of-oxycodone-seeking
#3
Jennifer M Bossert, Jennifer K Hoots, Ida Fredriksson, Sweta Adhikary, Michelle Zhang, Marco Venniro, Yavin Shaham
Relapse to nonmedical use of prescription opioids often occurs after exposure to places previously associated with drug use. Here, we describe a rat model of context-induced reinstatement of oxycodone seeking after repeated cycles of drug self-administration and extinction-induced abstinence. We also determined the role of mu, delta, and kappa opioid receptors (MOR, DOR, KOR) in this reinstatement. We trained rats to self-administer oxycodone for 6 h/d in Context A; lever pressing was paired with a discrete cue...
May 19, 2018: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29740093/differential-contributions-of-peripheral-and-central-mechanisms-to-pain-in-a-rodent-model-of-osteoarthritis
#4
Adrian R Haywood, Gareth J Hathway, Victoria Chapman
The mechanisms underlying the transition from acute nociceptive pain to centrally maintained chronic pain are not clear. We have studied the contributions of the peripheral and central nervous systems during the development of osteoarthritis (OA) pain. Male Sprague-Dawley rats received unilateral intra-articular injections of monosodium iodoacetate (MIA 1 mg) or saline, and weight-bearing (WB) asymmetry and distal allodynia measured. Subgroups of rats received intra-articular injections of, QX-314 (membrane impermeable local anaesthetic) + capsaicin, QX-314, capsaicin or vehicle on days 7, 14 or 28 post-MIA and WB and PWT remeasured...
May 8, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29734749/synthesis-and-structure-activity-relationships-of-cis-n-normetazocine-based-lp1-derivatives
#5
Lorella Pasquinucci, Carmela Parenti, Emanuele Amata, Zafiroula Georgoussi, Paschalina Pallaki, Valeria Camarda, Girolamo Calò, Emanuela Arena, Lucia Montenegro, Rita Turnaturi
(−)- cis - N -Normetazocine represents a rigid scaffold able to mimic the tyramine moiety of endogenous opioid peptides, and the introduction of different N -substituents influences affinity and efficacy of respective ligands at MOR (mu opioid receptor), DOR (delta opioid receptor), and KOR (kappa opioid receptor). We have previously identified LP1, a MOR/DOR multitarget opioid ligand, with an N -phenylpropanamido substituent linked to (−)- cis - N -Normetazocine scaffold. Herein, we report the synthesis, competition binding and calcium mobilization assays of new compounds 10 ⁻ 16 that differ from LP1 by the nature of the N -substituent...
May 5, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29729777/methadone-maximizing-safety-and-efficacy-for-pain-control-in-patients-with-cancer
#6
REVIEW
Mary Lynn McPherson, Ryan C Costantino, Alexandra L McPherson
Methadone is a valuable opioid in the management of patients who have cancer with pain. Methadone is a mu-, kappa-, and delta-opioid agonist, and an N-methyl-D-aspartate receptor antagonist. These mechanisms of action make methadone an attractive option for complex pain syndromes. It is critically important that providers consider a patient's risk status before beginning methadone. Careful consideration must be given to dosing methadone in both opioid-naïve and opioid-tolerant patients, with vigilant monitoring for therapeutic effectiveness and potential toxicity until the patient achieves steady state...
June 2018: Hematology/oncology Clinics of North America
https://www.readbyqxmd.com/read/29708942/a-bifunctional-biased-mu-opioid-agonist-neuropeptide-ff-receptor-antagonist-as-analgesic-with-improved-acute-and-chronic-side-effects
#7
Armand Drieu la Rochelle, Karel Guillemyn, Maria Dumitrascuta, Charlotte Martin, Valérie Utard, Raphaëlle Quillet, Séverine Schneider, François Daubeuf, Tom Willemse, Pieter Mampuys, Bert U W Maes, Nelly Frossard, Frédéric Bihel, Mariana Spetea, Frédéric Simonin, Steven Ballet
Opioid analgesics, such as morphine, oxycodone and fentanyl, are the cornerstones for treating moderate to severe pain. However, upon chronic administration, their efficiency is limited by prominent side effects such as analgesic tolerance and dependence liability. Neuropeptide FF (NPFF) and its receptors (NPFF1R and NPFF2R) are recognized as an important pronociceptive system involved in opioid-induced hyperalgesia and analgesic tolerance. Herein, we report the design of multitarget peptidomimetic compounds that show high affinity binding to the mu opioid receptor (MOPr) and NPFFRs...
April 26, 2018: Pain
https://www.readbyqxmd.com/read/29706406/parental-overcontrol-x-oprm1-genotype-interaction-predicts-school-aged-children-s-sympathetic-nervous-system-activation-in-response-to-performance-challenge
#8
Lindsey C Partington, Jessica L Borelli, Patricia Smiley, Ella Jarvik, Hannah F Rasmussen, Lauren C Seaman, Erika L Nurmi
Parental overcontrol (OC), the excessive regulation of a child's behavior, cognition, and emotion, is associated with the development of child anxiety. While studies have shown that genetic factors may increase sensitivity to stress, genetic vulnerability to parental OC has not been examined in anxiety etiology. A functional polymorphism in the mu opioid receptor OPRM1 (A118G, rs1799971) has been shown to impact stress reactivity. Using a community sample of children (N = 85, 9-12 years old), we examined the main and interactive effects of maternal OC and child OPRM1 genotype in predicting children's sympathetic nervous system reactivity during a performance stressor...
April 26, 2018: Research in Developmental Disabilities
https://www.readbyqxmd.com/read/29684591/in-vitro-and-in-vivo-activity-of-opioid-cyclopeptide-with-mu-delta-agonist-profile-biased-toward-%C3%AE-arrestin
#9
Katarzyna Gach-Janczak, Justyna Piekielna-Ciesielska, Anna Adamska-Bartłomiejczyk, Karol Wtorek, Federica Ferrari, Girolamo Calo, Agata Szymaszkiewicz, Joanna Piasecka-Zelga, Anna Janecka
Replacement of the tyrosine residue in the mu-selective opioid ligand Tyr-c[D-Lys-Phe-Asp]NH2 with 2',6'-dimethyltyrosine (Dmt) produced a cyclopeptide Dmt-c[D-Lys-Phe-Asp]NH2 with mu/delta opioid receptor agonist profile. This new analog showed improved antinociception in the hot-plate test as compared to the parent but also significantly inhibited the gastrointestinal transit. Using the bioluminescence resonance energy transfer (BRET) assay it was shown that this analog was biased toward β-arrestin.
April 20, 2018: Peptides
https://www.readbyqxmd.com/read/29680809/impact-of-dexmedetomidine-infusion-during-general-anaesthesia-on-incidence-of-postoperative-delirium-in-elderly-patients-after-major-non-cardiac-surgery-study-protocol-of-a-randomised-double-blinded-and-placebo-controlled-trial
#10
Bo-Jie Wang, Chun-Jing Li, Jian Hu, Huai-Jin Li, Chao Guo, Zhen-Han Wang, Qiao-Chu Zhang, Dong-Liang Mu, Dong-Xin Wang
INTRODUCTION: Delirium is a common complication in the elderly after surgery and is associated with worse outcomes. Multiple risk factors are related with postoperative delirium, such as exposure to general anaesthetics, pain and postoperative inflammatory response. Preclinical and clinical studies have shown that dexmedetomidine attenuated neurotoxicity induced by general anaesthetics, improved postoperative analgesia and inhibited inflammatory response after surgery. Several studies found that intraoperative use of dexmedetomidine can prevent postoperative delirium, but data were inconsistent...
April 21, 2018: BMJ Open
https://www.readbyqxmd.com/read/29680426/willis-ekbom-disease-restless-legs-syndrome-in-patients-with-opioid-withdrawal
#11
Ravi Gupta, Ramjan Ali, Rajat Ray
INTRODUCTION: Many patients with opioid use disorder report symptoms similar to restless legs syndrome (RLS) during withdrawal. However, whether these symptoms are true RLS, their predictors and effect of treatment with pregabalin are still unknown. METHOD: A total of 19 consecutive patients with opioid use disorder who were admitted for detoxification were included in this study after obtaining informed consent. Information regarding addiction was noted, and they were screened for RLS every morning and evening...
May 2018: Sleep Medicine
https://www.readbyqxmd.com/read/29677442/synthesis-and-pharmacological-evaluation-of-novel-c-8-substituted-tetrahydroquinolines-as-balanced-affinity-mu-delta-opioid-ligands-for-the-treatment-of-pain
#12
Anthony F Nastase, Nicholas W Griggs, Jessica P Anand, Thomas J Fernandez, Aubrie A Harland, Tyler J Trask, Emily M Jutkiewicz, John R Traynor, Henry I Mosberg
The use of opioids for the treatment of pain, while largely effective, is limited by detrimental side effects including analgesic tolerance, physical dependence, and euphoria, which may lead to opioid abuse. Studies have shown that compounds with a -opioid receptor (MOR) agonist/-opioid receptor (DOR) antagonist profile reduce or eliminate some of these side effects including development of tolerance and dependence. Herein we report the synthesis and pharmacological evaluation of a series of tetrahydroquinoline-based peptidomimetics with substitutions at the C-8 position...
April 20, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29677019/mu-opioid-receptors-in-nociceptive-afferents-produce-a-sustained-suppression-of-hyperalgesia-in-chronic-pain
#13
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/29673620/effects-of-opioid-and-non-opioid-analgesics-on-responses-to-psychosocial-stress-in-humans
#14
Anya K Bershad, Melissa A Miller, Greg J Norman, Harriet de Wit
Both preclinical and clinical evidence suggests that the endogenous opioid system is involved in responses to stress. For example, in animal models opioid agonists reduce isolation distress whereas opioid antagonists increase isolation distress. We recently reported that the mixed mu agonist and kappa antagonist buprenorphine dampened responses to acute psychosocial stress in humans. Now we extend this to study the effects of a pure mu-opioid agonist, hydromorphone, and a non-opioid analgesic, acetaminophen, on response to social stress...
April 16, 2018: Hormones and Behavior
https://www.readbyqxmd.com/read/29669731/involvement-of-activated-brain-stress-responsive-systems-in-excessive-and-relapse-alcohol-drinking-in-rodent-models-implications-for-therapeutics
#15
Yan Zhou, Mary Jeanne Kreek
Addictive diseases, including addiction to alcohol pose massive public health costs. Addiction is a chronic relapsing disease, caused by both the direct effects induced by drugs and persistent neuroadaptations at several (molecular, cellular and behavioral) levels. These drug-type specific neuro-adaptations are brought on largely by the reinforcing effects of drugs on the central nervous system and environment, including stress. Results from animal experiments have demonstrated important interactions between alcohol and the stress responsive systems...
April 18, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29667742/genetic-association-and-expression-analyses-of-the-phosphatidylinositol-4-phosphate-5-kinase-pip5k1c-gene-in-alcohol-use-disorder-relevance-for-pain-signaling-and-alcohol-use
#16
Ji Soo Lee, Jill L Sorcher, Allison D Rosen, Ruslan Damadzic, Hui Sun, Melanie Schwandt, Markus Heilig, John Kelly, Kelsey L Mauro, Audrey Luo, Daniel Rosoff, Christine Muench, Jeesun Jung, Zachary A Kaminsky, Falk W Lohoff
BACKGROUND: The gene encoding Phosphatidylinositol-4-Phosphate 5-Kinase (PIP5K1C) has been recently implicated in pain regulation. Interestingly, a recent cross-tissue and cross-phenotypic epigenetic analysis identified the same gene in alcohol use disorder (AUD). Given the high comorbidity between AUD and chronic pain, we hypothesized that genetic variation in PIP5K1C might contribute to susceptibility to AUD. METHODS: We conducted a case-control association study of genetic variants in PIP5K1C...
April 18, 2018: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29663822/the-effect-of-intrathecal-sufentanil-preconditioning-against-myocardial-ischemia-reperfusion-injury
#17
Y Tire, G Sarkilar, H Esen, R Onoglu, S T Uzun
OBJECTIVES: We aimed to investigate the cardioprotective effect and hemodynamic response of intrathecally administered sufentanil on myocardial IR injury. BACKGROUND: Sufentanil, mu opioid receptor agonist, intravenously administered during clinical and experimental studies, has been shown to have a cardioprotective effect on myocardial ischemia-reperfusion injury. METHODS: Thirty-two New Zealand type rabbits, which were anesthetized, were divided into four equal groups: sham, ischemia-reperfusion, sufentanil and ischemia-reperfusion+sufentanil...
2018: Bratislavské Lekárske Listy
https://www.readbyqxmd.com/read/29655552/binge-eating-disorder-and-morbid-obesity-are-associated-with-lowered-mu-opioid-receptor-availability-in-the-brain
#18
Juho Joutsa, Henry K Karlsson, Joonas Majuri, Pirjo Nuutila, Semi Helin, Valtteri Kaasinen, Lauri Nummenmaa
Both morbid obesity and binge eating disorder (BED) have previously been linked with aberrant brain opioid function. Behaviorally these two conditions are however different suggesting also differences in neurotransmitter function. Here we directly compared mu-opioid receptor (MOR) availability between morbidly obese and BED subjects. Seven BED and nineteen morbidly obese (non-BED) patients, and thirty matched control subjects underwent positron emission tomography (PET) with MOR-specific ligand [11 C]carfentanil...
June 30, 2018: Psychiatry research. Neuroimaging
https://www.readbyqxmd.com/read/29649967/influence-of-maternal-and-own-genotype-at-tanning-dependence-related-snps-on-sun-exposure-in-childhood
#19
Jasmine Khouja, Sarah J Lewis, Carolina Bonilla
BACKGROUND: Research suggests there may be a genetic influence on the likelihood of becoming tanning dependent (TD). The way in which mothers regulate their children's sun exposure may be affected by being TD. We investigated the associations between single nucleotide polymorphisms (SNPs) related to being TD and early sun exposure. METHODS: Data from the Avon Longitudinal Study of Parents and Children (ALSPAC) were used. Associations between 17 TD related SNPs in children and their mothers and 10 sun exposure variables in children (assessed via questionnaire at age 8) were analyzed in logistic and ordinal logistic regressions...
April 12, 2018: BMC Medical Genetics
https://www.readbyqxmd.com/read/29649744/synthesis-of-7%C3%AE-hydroxy-8-ketone-opioid-derivatives-with-antagonist-activity-at-mu-and-delta-opioid-receptors
#20
Tiina J Ahonen, Maiju Rinne, Peter Grutschreiber, Kert Mätlik, Mikko Airavaara, Dieter Schaarschmidt, Heinrich Lang, David Reiss, Henri Xhaard, Claire Gaveriaux-Ruff, Jari Yli-Kauhaluoma, Vânia M Moreira
Despite extensive years of research, the direct oxidation of the 7,8-double bond of opioids has so far received little attention and knowledge about the effects of this modification on activity at the different opioid receptors is scarce. We herein report that potassium permanganate supported on iron(II) sulfate heptahydrate can be used as a convenient oxidant in the one-step, heterogeneous conversion of Δ7,8 -opioids to the corresponding 7β-hydroxy-8-ketones. Details of the reaction mechanism are given and the effects of the substituent at position 6 of several opioids on the reaction outcome is discussed...
March 26, 2018: European Journal of Medicinal Chemistry
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