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https://www.readbyqxmd.com/read/28642332/morphine-worsens-the-severity-and-prevents-pancreatic-regeneration-in-mouse-models-of-acute-pancreatitis
#1
Usman Barlass, Raini Dutta, Hassam Cheema, John George, Archana Sareen, Ajay Dixit, Zuobiao Yuan, Bhuwan Giri, Jingjing Meng, Santanu Banerjee, Sulagna Banerjee, Vikas Dudeja, Rajinder K Dawra, Sabita Roy, Ashok K Saluja
BACKGROUND: Opioids such as morphine are widely used for the management of pain associated with acute pancreatitis. Interestingly, opioids are also known to affect the immune system and modulate inflammatory pathways in non-pancreatic diseases. However, the impact of morphine on the progression of acute pancreatitis has never been evaluated. In the current study, we evaluated the impact of morphine on the progression and severity of acute pancreatitis. METHODS: Effect of morphine treatment on acute pancreatitis in caerulein, L-arginine and ethanol-palmitoleic acid models was evaluated after induction of the disease...
June 22, 2017: Gut
https://www.readbyqxmd.com/read/28626834/effects-of-local-and-spinal-administrations-of-mu-opioids-on-postoperative-pain-in-aged-versus-adult-mice
#2
Jennifer Mecklenburg, Mayur J Patil, Wouter Koek, Armen N Akopian
No abstract text is available yet for this article.
January 2017: Pain Reports (Baltimore, Md.)
https://www.readbyqxmd.com/read/28621702/short-duration-physical-activity-prevents-the-development-of-activity-induced-hyperalgesia-through-opioid-and-serotoninergic-mechanisms
#3
Lucas V Lima, Josimari M DeSantana, Lynn A Rasmussen, Kathleen A Sluka, Lucas Vasconcelos Lima
Regular physical activity prevents development of chronic muscle pain through modulation of central mechanisms that involve rostral ventromedial medulla (RVM). We tested if pharmacological blockade or genetic deletion of mu-opioid receptors in physically active mice modulates excitatory and inhibitory systems in the RVM in an activity-induced hyperalgesia model. We examined response frequency to mechanical stimulation of the paw, muscle withdrawal thresholds, and expression of phosphorylation of the NR1 subunit of the NMDA receptor (p-NR1) and serotonin transporter (SERT) in the RVM...
June 8, 2017: Pain
https://www.readbyqxmd.com/read/28594147/casein-kinase-1-epsilon-deletion-increases-mu-opioid-receptor-dependent-behaviors-and-binge-eating
#4
Lisa R Goldberg, Stacey L Kirkpatrick, Neema Yazdani, Kimberly P Luttik, Olga A Lacki, R Keith Babbs, David F Jenkins, W Evan Johnson, Camron D Bryant
Genetic and pharmacological studies indicate that casein kinase-1 epsilon (Csnk1e) contributes to psychostimulant, opioid, and ethanol motivated behaviors. We previously used pharmacological inhibition to demonstrate that Csnk1e negatively regulates the locomotor stimulant properties of opioids and psychostimulants. Here, we tested the hypothesis that Csnk1e negatively regulates opioid and psychostimulant reward using genetic inhibition and the conditioned place preference assay in Csnk1e knockout mice. Similar to pharmacological inhibition, Csnk1e knockout mice showed enhanced opioid-induced locomotor activity with the mu opioid receptor agonist fentanyl (0...
June 8, 2017: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/28590714/reaching-out-for-sensitive-evaluation-of-the-mu-opioid-receptor-in-vivo-positron-emission-tomography-imaging-of-the-agonist-11c-ah7921
#5
Waqas Rafique, Shivashankar Khanapur, Mona Milde Spilhaug, Patrick J Riss
Imaging of the mu-opioid receptor availability with PET is a pertinent challenge in Neuroscience. Both, regulation of receptor expression and occupancy by endogeneous opioids play into cognitive and behavioural phenotypes of healthy function and disease. Receptor expression in the active and inactive states can be measured using high affinity radioagonist and radioanatonist PET tracers, respectively. Occupancy assessment requires radioligands showing competitive and reversible binding with moderate affinity to the MOR, which may lead to physical extinction of the receptor specific signal in vivo...
June 7, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28574864/methadone-management-of-withdrawal-associated-with-loperamide-related-opioid-use-disorder
#6
Raphael J Leo, Muhammad A Ghazi, Kelly S Jaziri
: Loperamide hydrochloride is an over-the-counter anti-diarrheal agent, acting via mu-opioid receptor agonist effects in the intestinal myenteric plexus. Although preclinical investigations suggested that abuse liability associated with loperamide use is low, there are increasing numbers of cases reported to the US Food and Drug Administration, of abuse, dependence, and withdrawal associated with loperamide use. A case of a patient with opioid use disorder, that is, in the form of protracted loperamide excess use, requiring management of withdrawal with methadone is presented...
June 1, 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28567699/effects-of-nalfurafine-on-the-reinforcing-thermal-antinociceptive-and-respiratory-depressant-effects-of-oxycodone-modeling-an-abuse-deterrent-opioid-analgesic-in-rats
#7
E Andrew Townsend, Jennifer E Naylor, S Stevens Negus, Shelley R Edwards, Hina N Qureshi, Hunter W McLendon, Christopher R McCurdy, Coco N Kapanda, Jussara M do Carmo, Fernanda S da Silva, John E Hall, Kenneth J Sufka, Kevin B Freeman
RATIONALE: Strategies to reduce the misuse of mu opioid agonists are critically needed. Previous work has shown that kappa opioid agonists can diminish the abuse-related effects and augment the antinociceptive effects of mu agonists. However, use of traditional kappa agonists is limited by their dysphoric side effects. OBJECTIVES: The current study examined the effects of nalfurafine, a clinically available atypical kappa agonist, on the reinforcing, thermal antinociceptive, and respiratory-depressant effects of oxycodone in male rats...
May 31, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28567065/the-psychoneuroendocrine-immunotherapy-of-cancer-historical-evolution-and-clinical-results
#8
REVIEW
Paolo Lissoni, Giusy Messina, Arianna Lissoni, Rovelli Franco
The prognosis of the neoplastic diseases depends not only on the biogenetic characteristics of cancer cells but also on the immunological response of patients, which may influence the biological features of cancer cells themselves as well as the angiogenic processes. Moreover, the immune system in vivo is under a physiological psychoneuroendocrine (PNE) regulation, mainly mediated by the brain opioid system and the pineal gland. In more detail, the anticancer immunity is stimulated by the pineal hormone melatonin (MLT) and inhibited by the opioid system, namely, through a mu-opioid receptor...
2017: Journal of Research in Medical Sciences: the Official Journal of Isfahan University of Medical Sciences
https://www.readbyqxmd.com/read/28559159/hdac-inhibitor-tsa-ameliorates-mechanical-hypersensitivity-and-potentiates-analgesic-effect-of-morphine-in-a-rat-model-of-bone-cancer-pain-by-restoring-%C3%AE-opioid-receptor-in-spinal-cord
#9
Xinran Hou, Yingqi Weng, Bihan Ouyang, Zhuofeng Ding, Zongbin Song, Wangyuan Zou, Changsheng Huang, Qulian Guo
Bone cancer pain (BCP) is a common complication with inadequate management in patients suffering from advanced cancer. Histone deacetylase inhibitors showed significant analgesic effect in multiple inflammatory and neuropathic pain models, but their effect in bone cancer pain has never been explored. In this study, we utilized a BCP rat model with intra-tibial inoculation of Walker 256 mammary gland carcinoma cells, which developed progressive mechanical hypersensitivity but not thermal hypersensitivity. Intrathecal application of trichostatin A (TSA), a classic pan-HDAC inhibitor, ameliorated tactile hypersensitivity and enhanced the analgesic effect of morphine in BCP rats...
May 27, 2017: Brain Research
https://www.readbyqxmd.com/read/28554003/opioids-and-opioid-receptors-orchestrate-wound-repair
#10
Ying Wang, Mihir Gupta, Tasneem Poonawala, Mariya Farooqui, Yunfang Li, Fei Peng, Sheldon Rao, Michael Ansonoff, John E Pintar, Kalpna Gupta
We have previously shown that topical opioids including morphine and its congeners promote healing of full thickness ischemic wounds in rats. We examined the contribution of mu opioid receptor (MOPr)-mediated healing of full thickness ischemic wounds using MOPr and delta or kappa opioid receptor knockout (KO) mice. Wound closure in the early (day 5) as well as later phases was delayed in topical morphine or PBS-treated MOPr-KO mice compared with reciprocal treatments of wounds in wild-type (WT) mice. MOPr expression was significantly upregulated at 30 min in the wound margins and colocalized with wound margins and vasculature in the epidermal and dermal layers of the skin...
May 18, 2017: Translational Research: the Journal of Laboratory and Clinical Medicine
https://www.readbyqxmd.com/read/28548579/genetic-variation-of-the-mu-opioid-receptor-oprm1-and-dopamine-d2-receptor-drd2-is-related-to-smoking-differences-in-patients-with-schizophrenia-but-not-bipolar-disorder
#11
Mika Hirasawa-Fujita, Michael J Bly, Vicki L Ellingrod, Gregory W Dalack, Edward F Domino
It is not known why mentally ill persons smoke excessively. Inasmuch as endogenous opioid and dopaminergic systems are involved in smoking reinforcement, it is important to study mu opioid receptor (OPRM1) A118G (rs1799971), dopamine D2 receptor (DRD2) Taq1A (rs1800497) genotypes, and sex differences among patients with schizophrenia or bipolar disorder. Smokers and nonsmokers with schizophrenia (n=177) and bipolar disorder (n=113) were recruited and genotyped. They were classified into three groups: current smoker, former smoker, and never smoker by tobacco smoking status self-report...
2017: Clinical Schizophrenia & related Psychoses
https://www.readbyqxmd.com/read/28546566/a-diastereoselective-synthesis-of-cebranopadol-a-novel-analgesic-showing-nop-mu-mixed-agonism
#12
Anna Fantinati, Sara Bianco, Remo Guerrini, Severo Salvadori, Salvatore Pacifico, Maria Camilla Cerlesi, Girolamo Calo, Claudio Trapella
A diastereoselective synthesis of the title compound as a single E diastereomer has been efficiently accomplished by assembling the featured pyrano-indole scaffold of the spiro[cyclohexane-dihydropyrano[3,4-b]-indole]-amine framework through an oxa-Pictet-Spengler reaction, promoted by a cheap and green Zeolite catalyst. Basic pharmacological experiments demonstrate that Cebranopadol acts as a mixed nociception/orphanin FQ (NOP) and mu (MOP) opioid receptor agonist useful for treatment of chronic pain.
May 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28533693/dna-methylation-at-the-mu-1-opioid-receptor-gene-oprm1-promoter-predicts-preoperative-acute-and-chronic-postsurgical-pain-after-spine-fusion
#13
Vidya Chidambaran, Xue Zhang, Lisa J Martin, Lili Ding, Matthew T Weirauch, Kristie Geisler, Bobbie L Stubbeman, Senthilkumar Sadhasivam, Hong Ji
INTRODUCTION: The perioperative pain experience shows great interindividual variability and is difficult to predict. The mu-1 opioid receptor gene (OPRM1) is known to play an important role in opioid-pain pathways. Since deoxyribonucleic acid (DNA) methylation is a potent repressor of gene expression, DNA methylation was evaluated at the OPRM1 promoter, as a predictor of preoperative, acute, and chronic postsurgical pain (CPSP). METHODS: A prospective observational cohort study was conducted in 133 adolescents with idiopathic scoliosis undergoing spine fusion under standard protocols...
2017: Pharmacogenomics and Personalized Medicine
https://www.readbyqxmd.com/read/28532680/decreased-spinal-endomorphin-2-contributes-to-mechanical-allodynia-in-streptozotocin-induced-diabetic-rats
#14
Le Niu, Guang-Hai Dai, Gao-Le He, Ming Yang, Hui-Min Hu, Zhong-Kai Liu, Nian-Song Qian, Yong-Liang Chen
Diabetic neuropathic pain (DNP) plays a major role in decreased life quality of diabetes patients, however, the neural mechanisms underlying DNP remain unclear. Endomorphins are the endogenous ligands for mu-opioid receptor. There is increasing evidence implicating the involvement of spinal endomorphin-2 (EM2) in neuropathic pain. In this study, using a streptozotocin induced diabetic rat model that displayed obvious mechanical allodynia, it was found that the expression of spinal EM2 was significantly decreased in DNP rats...
May 19, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/28529734/differential-regulation-of-mouse-and-human-mu-opioid-receptor-gene-depends-on-the-single-stranded-dna-structure-of-its-promoter-and-%C3%AE-complex-protein-1
#15
Dong-Sun Lee, Ping-Yee Law, Wei Ln, Horace H Loh, Kyu Young Song, Hack Sun Choi
The Mu opioid receptor (MOR) mediates various functions of opioid-induced analgesia, euphoria and respiratory depression, and is a major target of opioid analgesics. Understanding of MOR gene expression among species is important for understanding its analgesic function in humans. In the current study, the polypyrimidine/polypurine (PPy/u) region, a key element of MOR gene expression, was compared in humans and mice. The mouse PPy/u element is highly homologous to its human element (84%), and the mouse MOR (mMOR) reporter drives luciferase activity 35-fold more effectively than the human MOR (hMOR) reporter...
May 2017: Biomedical Reports
https://www.readbyqxmd.com/read/28525512/parecoxib-supplementation-to-morphine-analgesia-decreases-incidence-of-delirium-in-elderly-patients-after-hip-or-knee-replacement-surgery-a-randomized-controlled-trial
#16
Dong-Liang Mu, Da-Zhi Zhang, Dong-Xin Wang, Geng Wang, Chun-Jing Li, Zhao-Ting Meng, Ya-Wei Li, Chao Liu, Xue-Ying Li
BACKGROUND: Severe pain and high-dose opioids are both associated with increased risk of postoperative delirium. The authors investigated whether parecoxib-supplemented IV morphine analgesia could decrease the incidence of delirium in elderly patients after total hip or knee replacement surgery. METHODS: In a randomized, double-blind, 2-center trial, patients of 60 years or older who underwent elective total hip or knee replacement surgery were assigned in a 1:1 ratio to receive either parecoxib (40 mg at the end of surgery and then every 12 hours for 3 days) or placebo (normal saline)...
June 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28506204/antibiotic-effects-of-loperamide-homology-of-human-targets-of-loperamide-with-targets-in-acanthamoeba-spp
#17
Abdul Mannan Baig, Zohaib Rana, M Mohsin Mannan, S Sumayya Tariq, H R Ahmad
BACKGROUND: Loperamide is an anti-diarrheal drug prescribed for non-infectious diarrhea. The drug is an opioid receptor agonist, a blocker of voltage-dependent calcium channel (Cav) and a calmodulin (CaM) inhibitor on human cells. Loperamide has been reported to exert anti-amoebic effects against pathogenic strains of Acanthamoeba castellanii. OBJECTIVES: The precise mode of antibiotic action, cellular target homology with human counterparts and the pattern of cell death induced by loperamide in Acanthamoeba castellanii remain to be established...
April 25, 2017: Recent Patents on Anti-infective Drug Discovery
https://www.readbyqxmd.com/read/28501425/the-effects-of-kratom-on-restraint-stress-induced-analgesia-and-its-mechanisms-of-action
#18
José Luis Vázquez López, Lorenz Schild, Thomas Günther, Stefan Schulz, Hartmud Neurath, Axel Becker
ETHNOPHARMACOLOGICAL RELEVANCE: Mitragyna speciosa and its extracts are called kratom (dried leaves, extract). They contain several alkaloids with an affinity for different opioid receptors. They are used in traditional medicine for the treatment of different diseases, as a substitute by opiate addicts, and to mitigate opioid withdrawal symptoms. Apart from their medical properties, they are used to enhance physical endurance and as a means of overcoming stress. PURPOSE: The aim of this study was to determine the mechanisms underlying the effects of kratom on restraint-stress-induced analgesia which occurs during or following exposure to a stressful or fearful stimulus...
May 10, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28496466/validated-spectrophtometric-method-for-simultaneous-determination-of-buprenorphine-and-naloxone-in-pharmaceutical-dosage-forms
#19
Effat Souri, Farzaneh Sadat Ahmadi, Maliheh Barazandeh Tehrani, Majid Mohammad Hosseini, Sedigheh Fadaye Vatan
Buprenorphine is a partial mu agonist and kappa antagonist which is used for the treatment of pain and opioid addiction. A mixture of buprenorphine hydrochloride and naloxone hydrochloride has been approved for the treatment of opioid dependence. In this study a third order derivative spectrophotometric method based on zero-crossing technique has been used for the simultaneous determination of buprenorphine hydrochloride and naloxone hydrochloride in tablets. The measurements were carried out at wavelengths of 257...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/28488261/use-of-tramadol-in-psychiatric-care-a-comprehensive-review-and-report-of-two-cases
#20
Ansgar Rougemont-Bücking, Franziska Gamma, Jaak Panksepp
Tramadol is widely prescribed for treating acute and chronic forms of pain. It is a weak mu-receptor opioid agonist and also increases concentrations of serotonin and noradrenaline within the limbic system of the brain. The therapeutic range of tramadol is relatively wide. Compared with other opioid agonists, there is little risk for developing tolerance and for abuse. Recent models of depression emphasise the subjective experience of a depressive mood as being, in part, a psychologically painful state. It is well established that psychological stress due to social separation/loss, disruption or be-trayal of pre-existent significant interpersonal bonds is mediated by the activation of the mammalian PANIC (separation-distress) system...
May 10, 2017: Swiss Medical Weekly
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