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µ Opioid Receptors

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https://www.readbyqxmd.com/read/29022702/development-of-bright-and-biocompatible-nanoruby-and-its-application-to-background-free-time-gated-imaging-of-g-protein-coupled-receptors
#1
Varun K A Sreenivasan, Wan Aizuddin W Razali, Kai Zhang, Rashmi R Pillai, Avishkar Saini, Denitza Denkova, Marina Santiago, Hannah Brown, Jeremy Thompson, Mark Connor, Ewa M Goldys, Andrei V Zvyagin
At the forefront of development of fluorescent probes for biological imaging applications are enhancements aimed at increasing their brightness, contrast, and photostability, especially towards demanding applications of single molecule detection. In comparison with existing probes, nanorubies exhibit unlimited photostability and a long emission lifetime (3.7 ms), which enable continuous imaging at single-particle sensitivity in highly scattering and fluorescent biological specimens. However, their wide application as fluorescence probes has so far been hindered by the absence of facile methods for scaled-up high volume production and molecularly-specific targeting...
October 12, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28991111/an-intraplantar-hypertonic-saline-assay-in-mice-for-rapid-screening-of-analgesics
#2
Yahya I Asiri, Timothy Fung, Stephan K W Schwarz, Khalid A Asseri, Ian D Welch, Catherine A Schuppli, Alasdair M Barr, Richard A Wall, Ernest Puil, Bernard A MacLeod
BACKGROUND: Development of new analgesics is limited by shortcomings of existing preclinical screening assays such as wide variations in response, suitability for a narrow range of analgesics, and propensity to induce tissue damage. Our aim was to determine the feasibility of a new in vivo animal assay as an analgesic screen based on nociceptive responses (licking and biting) after intraplantar (i.pl.) injection of hypertonic saline (HS) in mice. METHODS: With approval from the Institutional Animal Care Committee, we conducted a randomized, investigator-blinded in vivo study in adult CD-1 mice...
October 5, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28952976/effects-of-morphine-cp55940-mixtures-on-an-impulsive-choice-task-in-rhesus-monkeys
#3
Vanessa Minervini, Charles P France
µ-Opioid receptor agonists are commonly used to treat pain despite their adverse effects. In preclinical studies, cannabinoid receptor agonists increase the potency of opioids for producing antinociceptive but not reinforcing effects. It is unknown whether other adverse effects of these drugs, such as impairment of complex behavior, are enhanced by their co-administration. This study characterized the effects of morphine (µ-opioid receptor agonist; 0.32-5.6 mg/kg, subcutaneously) and CP55940 (CB1/CB2 cannabinoid receptor agonist; 0...
September 25, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28951361/-%C3%A2%C2%B5-opioid-receptors-in-the-central-nucleus-of-the-amygdala-mediate-sodium-intake-in-rats
#4
Jun-Bao Yan, Zhi-Hong Hu
OBJECTIVE: To investigate the opioidergic mechanism of the central nucleus of the amygdala (CeA) for regulating sodium appetite in rats. METHDOS: Using the elaborate invasive cerebral cannulation and brain microinjection method, we observed the effects of bilateral intra-CeA injections of DAMGO (a selective µ-opioid receptor agonist) and CTAP (a highly selective µ-opioid receptor antagonist), either alone or in combination, on NaCl solution (0.3 mol/L) and water intake by rats in different models of Na(+) ingestion...
September 20, 2017: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
https://www.readbyqxmd.com/read/28946783/peripherally-acting-%C3%A2%C2%B5-opioid-receptor-antagonists-for-the-treatment-of-opioid-related-side-effects-mechanism-of-action-and-clinical-implications
#5
John M Streicher, Edward J Bilsky
Opioid receptors are distributed throughout the central and peripheral nervous systems and on many nonneuronal cells. Therefore, opioid administration induces effects beyond analgesia. In the enteric nervous system (ENS), stimulation of µ-opioid receptors triggers several inhibitory responses that can culminate in opioid-induced bowel dysfunction (OBD) and its most common side effect, opioid-induced constipation (OIC). OIC negatively affects patients' quality of life (QOL), ability to work, and pain management...
January 1, 2017: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/28930716/antinociceptive-effect-of-ghrelin-in-a-rat-model-of-irritable-bowel-syndrome-involves-trpv1-opioid-systems
#6
Yuqing Mao, Zhengyang Li, Kan Chen, Huafang Yu, Shaoren Zhang, Miao Jiang, Yuanhua Ma, Chunli Liang, Hongyan Liu, Huanqing Li, Qian Hua, Hao Zhou, Yonghong Sun, Xiaoming Fan
BACKGROUND/AIMS: Irritable bowel syndrome (IBS), defined as recurrent abdominal pain and changes in bowel habits, seriously affects quality of life and ability to work. Ghrelin is a brain-gut hormone, which has been reported to show antinociceptive effects in peripheral pain. We investigated the effect of ghrelin on visceral hypersensitivity and pain in a rat model of IBS. METHODS: Maternal deprivation (MD) was used to provide a stress-induced model of IBS in Wistar rats...
September 20, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28900175/dynamic-and-kinetic-elements-of-%C3%A2%C2%B5-opioid-receptor-functional-selectivity
#7
Abhijeet Kapoor, Gerard Martinez-Rosell, Davide Provasi, Gianni de Fabritiis, Marta Filizola
While the therapeutic effect of opioids analgesics is mainly attributed to µ-opioid receptor (MOR) activation leading to G protein signaling, their side effects have mostly been linked to β-arrestin signaling. To shed light on the dynamic and kinetic elements underlying MOR functional selectivity, we carried out close to half millisecond high-throughput molecular dynamics simulations of MOR bound to a classical opioid drug (morphine) or a potent G protein-biased agonist (TRV-130). Statistical analyses of Markov state models built using this large simulation dataset combined with information theory enabled, for the first time: a) Identification of four distinct metastable regions along the activation pathway, b) Kinetic evidence of a different dynamic behavior of the receptor bound to a classical or G protein-biased opioid agonist, c) Identification of kinetically distinct conformational states to be used for the rational design of functionally selective ligands that may eventually be developed into improved drugs; d) Characterization of multiple activation/deactivation pathways of MOR, and e) Suggestion from calculated transition timescales that MOR conformational changes are not the rate-limiting step in receptor activation...
September 12, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28871491/robust-age-but-limited-sex-differences-in-mu-opioid-receptors-in-the-rat-brain-relevance-for-reward-and-drug-seeking-behaviors-in-juveniles
#8
Caroline J W Smith, Aarane M Ratnaseelan, Alexa H Veenema
In the brain, the µ-opioid receptor (MOR) is involved in reward-seeking behaviors and plays a pivotal role in the mediation of opioid use disorders. Furthermore, reward-seeking behaviors and susceptibility to opioid addiction are particularly evident during the juvenile period, with a higher incidence of opioid use in males and higher sensitivity to opioids in females. Despite these age and sex differences in MOR-mediated behaviors, little is known regarding potential age and sex differences in the expression of MORs in the brain...
September 4, 2017: Brain Structure & Function
https://www.readbyqxmd.com/read/28857657/opioid-system-contribution-to-the-antidepressant-like-action-of-m-trifluoromethyl-diphenyl-diselenide-in-mice-a-compound-devoid-of-tolerance-and-withdrawal-syndrome
#9
Suzan G Rosa, Ana P Pesarico, Carolina F Tagliapietra, Sônia C A da Luz, Cristina W Nogueira
Animal and clinical researches indicate that the opioid system exerts a crucial role in the etiology of mood disorders and is a target for intervention in depression treatment. This study investigated the contribution of the opioid system to the antidepressant-like action of acute or repeated m-trifluoromethyl-diphenyl diselenide administration to Swiss mice. m-Trifluoromethyl-diphenyl diselenide (50 mg/kg, intragastric) produced an antidepressant-like action in the forced swimming test from 30 min to 24 h after treatment...
August 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28839004/ventilation-and-neurochemical-changes-during-%C3%A2%C2%B5-opioid-receptor-activation-or-blockade-of-excitatory-receptors-in-the-hypoglossal-motor-nucleus-of-goats
#10
Thomas M Langer, Suzanne E Neumueller, Emma Crumley, Nicholas J Burgraff, Sawan Talwar, Matthew Robert Hodges, Lawrence G Pan, Hubert V Forster
Neuromodulator interdependence posits that changes in one or more neuromodulators are compensated by changes in other modulators to maintain stability in the respiratory control network. Herein, we studied compensatory neuromodulation in the hypoglossal motor nucleus (HMN) after chronic implantation of microtubules unilaterally (n=5) or bilaterally (n=5) into the HMN. After recovery, receptor agonists or antagonists in mock cerebrospinal fluid (mCSF) were dialyzed during the awake and NREM sleep state. During day studies, dialysis of the µ-opioid inhibitory receptor agonist DAMGO (100 µM) decreased pulmonary ventilation (V̇I), breathing frequency (f), and genioglossus (GG) muscle activity, but did not alter neuromodulators measured in the effluent mCSF...
August 24, 2017: Journal of Applied Physiology
https://www.readbyqxmd.com/read/28826490/g-protein-%C3%AE-%C3%AE-subunits-inhibit-trpm3-ion-channels-in-sensory-neurons
#11
Talisia Quallo, Omar Alkhatib, Clive Gentry, David A Andersson, Stuart Bevan
Transient receptor potential (TRP) ion channels in peripheral sensory neurons are functionally regulated by hydrolysis of the phosphoinositide PI(4,5)P2 and changes in the level of protein kinase mediated phosphorylation following activation of various G protein coupled receptors. We now show that the activity of TRPM3 expressed in mouse dorsal root ganglion (DRG) neurons is inhibited by agonists of the Gi-coupled µ opioid, GABA-B and NPY receptors. These agonist effects are mediated by direct inhibition of TRPM3 by Gβγ subunits, rather than by a canonical cAMP mediated mechanism...
August 15, 2017: ELife
https://www.readbyqxmd.com/read/28826482/anti-nociceptive-action-of-peripheral-mu-opioid-receptors-by-g-beta-gamma-protein-mediated-inhibition-of-trpm3-channels
#12
Sandeep Dembla, Marc Behrendt, Florian Mohr, Christian Goecke, Julia Sondermann, Franziska M Schneider, Marlene Schmidt, Julia Stab, Raissa Enzeroth, Michael G Leitner, Paulina Nuñez-Badinez, Jochen Schwenk, Bernd Nürnberg, Alejandro Cohen, Stephan E Philipp, Wolfgang Greffrath, Moritz Bünemann, Dominik Oliver, Eleonora Zakharian, Manuela Schmidt, Johannes Oberwinkler
Opioids, agonists of µ-opioid receptors (µORs), are the strongest pain killers clinically available. Their action includes a strong central component, which also causes important adverse effects. However, µORs are also found on the peripheral endings of nociceptors and their activation there produces meaningful analgesia. The cellular mechanisms downstream of peripheral µORs are not well understood. Here, we show in neurons of murine dorsal root ganglia that pro-nociceptive TRPM3 channels, present in the peripheral parts of nociceptors, are strongly inhibited by µOR activation, much more than other TRP channels in the same compartment, like TRPV1 and TRPA1...
August 15, 2017: ELife
https://www.readbyqxmd.com/read/28820778/src-kinase-inhibition-attenuates-morphine-tolerance-without-affecting-reinforcement-or-psychomotor-stimulation
#13
Fiona A Bull, Daniel T Baptista-Hon, Claire Sneddon, Lisa Wright, Wendy Walwyn, Tim G Hales
BACKGROUND: Prolonged opioid administration leads to tolerance characterized by reduced analgesic potency. Pain management is additionally compromised by the hedonic effects of opioids, the cause of their misuse. The multifunctional protein β-arrestin2 regulates the hedonic effects of morphine and participates in tolerance. These actions might reflect µ opioid receptor up-regulation through reduced endocytosis. β-Arrestin2 also recruits kinases to µ receptors. We explored the role of Src kinase in morphine analgesic tolerance, locomotor stimulation, and reinforcement in C57BL/6 mice...
August 18, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28810695/long-term-safety-and-efficacy-of-subcutaneous-methylnaltrexone-in-patients-with-opioid-induced-constipation-and-chronic-noncancer-pain-a-phase-3-open-label-trial
#14
Lynn R Webster, Edward Michna, Arif Khan, Robert J Israel, Joseph R Harper
Objective: Methylnaltrexone, a peripherally acting µ-opioid receptor antagonist, alleviates opioid-induced constipation. Understanding its long-term safety and efficacy profile in patients with chronic noncancer pain is warranted given the persistence of opioid-induced constipation. Methods. : In this phase 3, multicenter, open-label trial, adults with chronic noncancer pain (N = 1034) received subcutaneous methylnaltrexone 12 mg once daily for 48 weeks...
August 1, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28790193/assessing-the-value-of-the-zebrafish-conditioned-place-preference-model-for-predicting-human-abuse-potential
#15
A J Brock, S M G Goody, A N Mead, A Sudwarts, M O Parker, C H Brennan
Regulatory agencies recommend that centrally active drugs are tested for abuse potential before approval. Standard preclinical assessments are conducted in rats or non-human primates (NHPs). This study evaluated the ability of the zebrafish conditioned place preference (CPP) model to predict human abuse outcomes. Twenty-seven compounds from a variety of pharmacological classes were tested in zebrafish CPP, categorized as positive or negative, and analyzed using standard diagnostic tests of binary classification to determine the likelihood that zebrafish correctly predict robust positive signals in human subjective effects studies (+HSE) and/or Drug Enforcement Administration drug scheduling...
October 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28736107/cholinergic-opioid-interaction-in-anterior-cingulate-cortex-reduces-the-nociceptive-response-of-vocalization-in-guinea-pigs
#16
João Zugaib, Leda Menescal-de-Oliveira
The anterior cingulate cortex (ACC) is crucial in the modulation of the sensory, affective and cognitive aspects of nociceptive processing. Also, it participates in the planning and execution of behavioral responses evoked by nociceptive stimuli via descending projections to the brainstem. In laboratory animals nociceptive experimental tests evaluate behavioral responses that preferentially express the sensory-discriminative or affective-motivational component of pain. The objective of this study was to investigate the participation of opioid and cholinergic neurotransmission in the ACC on different nociceptive responses in guinea pigs...
July 20, 2017: Brain Research
https://www.readbyqxmd.com/read/28663556/desensitized-d2-autoreceptors-are-resistant-to-trafficking
#17
Brooks G Robinson, James R Bunzow, Jonathan B Grimm, Luke D Lavis, Joshua T Dudman, Jennifer Brown, Kim A Neve, John T Williams
Dendritic release of dopamine activates dopamine D2 autoreceptors, which are inhibitory G protein-coupled receptors (GPCRs), to decrease the excitability of dopamine neurons. This study used tagged D2 receptors to identify the localization and distribution of these receptors in living midbrain dopamine neurons. GFP-tagged D2 receptors were found to be unevenly clustered on the soma and dendrites of dopamine neurons within the substantia nigra pars compacta (SNc). Physiological signaling and desensitization of the tagged receptors were not different from wild type receptors...
June 29, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28654029/measuring-g-protein-coupled-receptor-signaling-via-radio-labeled-gtp-binding
#18
Chirag Vasavda, Nicholas W Zaccor, Paul C Scherer, Charlotte J Sumner, Solomon H Snyder
G-Protein-Coupled Receptors (GPCRs) are a large family of transmembrane receptors that play critical roles in normal cellular physiology and constitute a major pharmacological target for multiple indications, including analgesia, blood pressure regulation, and the treatment of psychiatric disease. Upon ligand binding, GPCRs catalyze the activation of intracellular G-proteins by stimulating the incorporation of guanosine triphosphate (GTP). Activated G-proteins then stimulate signaling pathways that elicit cellular responses...
June 9, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28642332/morphine-worsens-the-severity-and-prevents-pancreatic-regeneration-in-mouse-models-of-acute-pancreatitis
#19
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/28587388/roles-of-the-%C3%A2%C2%B5-opioid-receptor-and-its-related-signaling-pathways-in-the-pathogenesis-of-premenstrual-syndrome-liver-qi-stagnation
#20
Chunhong Song, Ling Xue
The present study aimed to investigate the roles of the µ-opioid receptor (MOR) and its related signaling pathways in the pathogenesis of premenstrual syndrome (PMS) liver-qi stagnation, along with the therapeutic effects of the Shu-Yu capsule in treating the condition. A PMS liver-qi stagnation rat model was established using a chronic restraint stress method. The protein expression level of MOR within rat hippocampal tissue was detected via western blot analysis and cyclic adenosine monophosphate (cAMP) levels within the supernatant of a rat hippocampal cell culture were determined by ELISA...
June 2017: Experimental and Therapeutic Medicine
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