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µ Opioid Receptors

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https://www.readbyqxmd.com/read/29211767/investigating-endogenous-%C3%A2%C2%B5-opioid-receptors-in-human-keratinocytes-as-pharmacological-targets-using-novel-fluorescent-ligand
#1
Cheryl Leong, Christine Neumann, Srinivas Ramasamy, Bhimsen Rout, Lim Yi Wee, Mei Bigliardi-Qi, Paul L Bigliardi
Opioids in skin function during stress response, regeneration, ageing and, particularly in regulating sensation. In chronic pruritus, topical treatment with Naltrexone changes μ-opioid receptor (μ-OR) localization to relieve itch. The molecular mechanisms behind the effects of Naltrexone on μ-OR function in reduction of itching behavior has not been studied. There is an immediate need to understand the endogenous complexity of μ-OR dynamics in normal and pathological skin conditions. Here we evaluate real-time behavior of μ-OR-Endomorphine complexes in the presence of agonist and antagonists...
2017: PloS One
https://www.readbyqxmd.com/read/29165386/alterations-in-rat-accumbens-endocannabinoid-and-gaba-content-during-fentanyl-treatment-the-role-of-ghrelin
#2
Magdalena Sustkova-Fiserova, Chrysostomos Charalambous, Tereza Havlickova, Marek Lapka, Pavel Jerabek, Nina Puskina, Kamila Syslova
The opioid-induced rise of extracellular dopamine, endocannabinoid anandamide and γ-aminobutyric acid (GABA) concentrations triggered by opioids in the nucleus accumbens shell (NACSh) most likely participate in opioid reward. We have previously demonstrated that systemic administration of ghrelin antagonist (JMV2959) significantly decreased morphine-induced dopamine and anandamide (N-arachidonoylethanolamine, AEA) increase in the NACSh. Fentanyl is considered as a µ-receptor-selective agonist. The aim of this study was to test whether JMV2959, a growth hormone secretagogue receptor (GHS-R1A) antagonist, can influence the fentanyl-induced effects on anandamide, 2-arachidonoylglycerol (2-AG) and GABA in the NACSh and specify the involvement of GHS-R1A located in the ventral tegmental area (VTA) and nucleus accumbens (NAC)...
November 22, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29141251/opioid-receptors-contribute-to-antinociceptive-effect-of-tianeptine-on-colorectal-distension-induced-visceral-pain-in-rats
#3
S Sırrı Bilge, Fatih İlkaya, Özge Darakcı, Engin Çiftcioğlu, Ayhan Bozkurt
Tianeptine is a clinically effective atypical antidepressant with distinct neurochemical properties. In this study, we aimed to investigate the contribution of opioid receptors in the antinociceptive effect of tianeptine on visceral pain in awake rats and to differentiate the subtype and the localization (central and/or peripheral) of these opioid receptors involved in this antinociception. Visceromotor response to noxious colorectal distension (CRD) was quantified with electromyographic recordings, obtained from previously implanted electrodes into the external oblique musculature of rats under anesthesia, before and after tianeptine administration...
November 15, 2017: Pharmacology
https://www.readbyqxmd.com/read/29132133/endomorphins-promising-endogenous-opioid-peptides-for-the-development-of-novel-analgesics
#4
Zheng-Hui Gu, Bo Wang, Zhen-Zhen Kou, Yang Bai, Tao Chen, Yu-Lin Dong, Hui Li, Yun-Qing Li
Endomorphin-1 (EM1) and endomorphin-2 (EM2) are two endogenous ligands that belong to the opioid peptide family and have the highest affinity and selectivity for the µ-opioid receptor (MOR). The neuroanatomical distribution, ultrastructural features and neural circuitry of EM-containing neuronal structures have been morphologically demonstrated. In addition, the modulation effects of the EMs in different areas reflect their potential endogenous roles in many major physiological processes, including their remarkable roles in the transmission and modulation of noxious information...
November 13, 2017: Neuro-Signals
https://www.readbyqxmd.com/read/29127441/verification-of-a-genetic-locus-for-methamphetamine-intake-and-the-impact-of-morphine
#5
Emily C Eastwood, Amy J Eshleman, Aaron Janowsky, Tamara J Phillips
A quantitative trait locus (QTL) on proximal chromosome (Chr) 10 accounts for > 50% of the genetic variance in methamphetamine (MA) intake in mice selectively bred for high (MAHDR) and low (MALDR) voluntary MA drinking. The µ-opioid receptor (MOP-r) gene, Oprm1, resides at the proximal end of Chr 10, and buprenorphine reduces MA intake in MAHDR mice. However, this drug has only partial agonist effects at MOP-r. We investigated the impact of a full MOP-r agonist, morphine, on MA intake and saccharin intake, measured MOP-r density and affinity in several brain regions of the MA drinking lines and their C57BL/6J (B6) and DBA/2J (D2) progenitor strains, and measured MA intake in two congenic strains of mice to verify the QTL and reduce the QTL interval...
November 10, 2017: Mammalian Genome: Official Journal of the International Mammalian Genome Society
https://www.readbyqxmd.com/read/29092627/evidence-based-review-of-pharmacotherapy-for-opioid-induced-constipation-in-noncancer-pain
#6
Julie A Murphy, Erica A Sheridan
OBJECTIVE: To summarize and evaluate the existing literature regarding medications to treat opioid-induced constipation (OIC) in patients with chronic noncancer pain (CNCP). DATA SOURCES: PubMed, EMBASE, and Web of Science were searched using the following terms: constipation, opioid, chronic, pain, noncancer, nonmalignant, methylnaltrexone, alvimopan, lubiprostone, naloxegol, and naldemedine. STUDY SELECTION AND DATA EXTRACTION: The search was limited to randomized controlled trials reporting human outcomes...
October 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/29090081/eluxadoline-in-irritable-bowel-syndrome-with-diarrhea-rationale-evidence-and-place-in-therapy
#7
REVIEW
Kenneth Barshop, Kyle Staller
Irritable bowel syndrome (IBS) is the most common gastrointestinal (GI) disorder worldwide, however treatment options for diarrhea-predominant IBS (IBS-D) remain limited. Eluxadoline, a µ- and κ-opioid receptor agonist and δ-opioid receptor antagonist, was recently approved for the treatment of IBS-D. A novel compound first described in 2008, eluxadoline was shown to normalize GI transit, with a subsequent phase I demonstrating its safety and tolerability in healthy adults. In 2016, two randomized, double-blind, placebo-controlled phase III trials studying eluxadoline use at 75 mg and 100 mg twice daily over 26 weeks demonstrated a significant improvement in stool consistency and many global symptoms of IBS...
November 2017: Therapeutic Advances in Chronic Disease
https://www.readbyqxmd.com/read/29062240/a-randomized-phase-iib-study-investigating-oliceridine-trv130-a-novel-%C3%A2%C2%B5-receptor-g-protein-pathway-selective-%C3%AE-gps-modulator-for-the-management-of-moderate-to-severe-acute-pain-following-abdominoplasty
#8
Neil Singla, Harold S Minkowitz, David G Soergel, David A Burt, Ruth Ann Subach, Monica Y Salamea, Michael J Fossler, Franck Skobieranda
BACKGROUND: Oliceridine (TRV130), a novel μ-receptor G-protein pathway selective (μ-GPS) modulator, was designed to improve the therapeutic window of conventional opioids by activating G-protein signaling while causing low β-arrestin recruitment to the μ receptor. This randomized, double-blind, patient-controlled analgesia Phase IIb study was conducted to investigate the efficacy, safety, and tolerability of oliceridine compared with morphine and placebo in patients with moderate to severe pain following abdominoplasty (NCT02335294; oliceridine is an investigational agent not yet approved by the US Food and Drug Administration)...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/29053268/synthesis-pharmacology-and-molecular-docking-studies-on-6-desoxo-n-methylmorphinans-as-potent-%C3%AE-opioid-receptor-agonists
#9
Maria Dumitrascuta, Tanila Ben Haddou, Elena Guerrieri, Stefan M Noha, Lea Schläfer, Helmut Schmidhammer, Mariana Spetea
Position 6 of the morphinan skeleton plays a key role in the μ-opioid receptor (MOR) activity in vitro and in vivo. We describe the consequence of the 6-carbonyl group deletion in N-methylmorphinan-6-ones 1-4 on ligand-MOR interaction, signaling, and antinociception. While 6-desoxo compounds 1a, 2a, and 4a show similar profiles to their 6-keto counterparts, the 6-desoxo-14-benzyloxy substituted 3a displays significantly increased MOR binding and agonist potency and a distinct binding mode compared with its analogue 3...
November 3, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29039297/the-impact-of-periconceptional-alcohol-exposure-on-fat-preference-and-gene-expression-in-the-mesolimbic-reward-pathway-in-adult-rat-offspring
#10
E S Dorey, C L Cullen, D Lucia, K M Mah, M-L Roy Manchadi, B S Muhlhausler, K M Moritz
Alcohol consumption around the time of conception is highly prevalent in Western countries. Exposure to ethanol levels during gestation has been associated with altered development of the mesolimbic reward pathway in rats and increased propensity to addiction, however the effect of exposure only around the time of conception is unknown. The current study investigated the effects of periconceptional alcohol exposure (PC:EtOH) on alcohol and palatable food preferences and gene expression in the ventral tegmental area (VTA) and the nucleus accumbens of the adult offspring...
October 17, 2017: Journal of Developmental Origins of Health and Disease
https://www.readbyqxmd.com/read/29035918/dopaminergic-mechanisms-in-periaqueductal-gray-mediated-antinociception
#11
Glaucia Tobaldini, Rafael A Reis, Natalia F Sardi, Mayla K Lazzarim, Dabna H Tomim, Marcelo M S Lima, Luana Fischer
As important as perceiving pain is the ability to modulate this perception in some contextual salient situations. The periaqueductal gray (PAG) is perhaps the most important site of endogenous pain modulation; however, little is known about dopaminergic mechanisms underlying PAG-mediated antinociception. In this study, we used a pharmacological approach to evaluate this subject. We found that µ-opioid receptor-induced antinociception (DAMGO, 0.3 μg) from PAG was blocked by the coadministration of either D1-like or D2-like dopaminergic antagonists (SCH23390, 2, 4, and 6 μg or raclopride, 2 and 4 μg, respectively) both in the tail-flick and in the mechanical paw-withdrawal test...
October 13, 2017: Behavioural Pharmacology
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
#12
Varun K A Sreenivasan, Wan Aizuddin Wan 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 developing fluorescent probes for biological imaging applications are enhancements aimed at increasing their brightness, contrast, and photostability, especially toward demanding applications of single-molecule detection. In comparison with existing probes, nanorubies exhibit unlimited photostability and a long emission lifetime (∼4 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...
November 2, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28991111/an-intraplantar-hypertonic-saline-assay-in-mice-for-rapid-screening-of-analgesics
#13
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
#14
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
#15
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
#16
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
#17
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...
2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28900175/dynamic-and-kinetic-elements-of-%C3%A2%C2%B5-opioid-receptor-functional-selectivity
#18
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
#19
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
#20
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
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