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https://www.readbyqxmd.com/read/29241414/molecular-mechanisms-of-allosteric-probe-dependence-in-%C3%AE-opioid-receptor
#1
Damian Bartuzi, Agnieszka A Kaczor, Dariusz Matosiuk
Allostery is one of the most important features of proteins. It greatly contributes to the complexity of life, since it enables possibility of precise tuning of protein function, as well as performing more than one function per protein. Probe dependence is one of unique features of allostery. It allows a protein to respond differently to the same allosteric modulator when different drugs or transmitters are bound. Unfortunately, allosteric mechanisms are difficult to investigate experimentally. Instead, they can be reproduced artificially in simulations...
December 14, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29240768/the-association-between-the-nicotinic-acetylcholine-receptor-%C3%AE-4-subunit-gene-chrna4-rs1044396-and-internet-gaming-disorder-in-korean-male-adults
#2
Jo-Eun Jeong, Je-Keun Rhee, Tae-Min Kim, Su-Min Kwak, Sol-Hee Bang, Hyun Cho, Young-Hoon Cheon, Jung Ah Min, Gil Sang Yoo, Kyudong Kim, Jung-Seok Choi, Sam-Wook Choi, Dai-Jin Kim
The primary aim of this study was to investigate the genetic predisposition of Internet gaming disorder (IGD), and the secondary aim was to compare the results to those of alcohol dependence (AD). Two independent case-control studies were conducted. A total of 30 male participants with IGD, diagnosed according to the 5th edition of the Diagnostic and Statistical Manual of Mental Disorders (DSM-5) criteria, and 30 sex-matched controls participated in study 1. We designed targeted exome sequencing (TES) to test for 72 candidate genes that have been implicated in the pathogenesis of addiction...
2017: PloS One
https://www.readbyqxmd.com/read/29239974/additive-and-subadditive-antiallodynic-interactions-between-%C3%AE-opioid-agonists-and-n-methyl-d-aspartate-antagonists-in-male-rhesus-monkeys
#3
Jeremy C Cornelissen, Floyd F Steele, Kenner C Rice, Katherine L Nicholson, Matthew L Banks
μ-Opioid agonists are clinically effective analgesics, but also produce undesirable effects such as sedation and abuse potential that limit their clinical utility. Glutamatergic systems also modulate nociception and N-methyl D-aspartate (NMDA) receptor antagonists have been proposed as one useful adjunct to enhance the therapeutic effects and/or attenuate the undesirable effects of μ-opioid agonists. Whether NMDA antagonists enhance the antiallodynic effects of μ-agonists in preclinical models of thermal hypersensitivity (i...
December 12, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/29237725/abin-1-negatively-regulates-%C3%AE-opioid-receptor-function
#4
Peilan Zhou, Jiebing Jiang, Hui Yan, Yulei Li, Junru Zhao, Xiao Wang, Ruibin Su, Zehui Gong
The μ-opioid receptor (MOR) is a Gi/o protein-coupled receptor that mediates analgesic, euphoric, and reward effects. Using a bacterial two-hybrid screen, we reported that the carboxyl tail of the rat MOR associates with A20-binding inhibitor of nuclear factor (NF)-κB (ABIN-1) (Zhou et al., 2015). This interaction was confirmed by direct protein - protein binding and co-immunoprecipitation of MOR and ABIN-1 proteins in cell lysates. Saturation binding studies showed that ABIN-1 had no effect on MOR binding...
December 13, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29236034/gastric-emptying-and-gastrointestinal-transit-compared-among-native-and-hydrolyzed-whey-and-casein-milk-proteins-in-an-aged-rat-model
#5
Julie E Dalziel, Wayne Young, Catherine M McKenzie, Neill W Haggarty, Nicole C Roy
Little is known about how milk proteins affect gastrointestinal (GI) transit, particularly for the elderly, in whom digestion has been observed to be slowed. We tested the hypothesis that GI transit is faster for whey than for casein and that this effect is accentuated with hydrolysates, similar to soy. Adult male rats (18 months old) were fed native whey or casein, hydrolyzed whey (WPH) or casein (CPH), hydrolyzed blend (HB; 60% whey:40% casein), or hydrolyzed soy for 14 days then treated with loperamide, prucalopride, or vehicle-control for 7 days...
December 13, 2017: Nutrients
https://www.readbyqxmd.com/read/29233847/pharmacological-evidence-for-a-putative-conserved-allosteric-site-on-opioid-receptors
#6
Kathryn E Livingston, M Alexander Stanczyk, Neil Burford, Andrew Alt, Merixtell Canals, John R Traynor
Allosteric modulators of G protein-coupled receptors (GPCRs), including opioid receptors, have been proposed as possible therapeutic agents with enhanced selectivity. BMS-986122 is a positive allosteric modulator (PAM) of the mu-opioid receptor (μ-OR). BMS-986187 is a structurally distinct PAM for the delta-opioid receptor (δ-OR) that has been reported to show 100-fold selectivity in promoting δ-OR over μ-OR agonism. Here we use ligand binding and second messenger assays to show that BMS-986187 is actually an effective PAM at μ-OR and at the kappa opioid receptor (κ-OR), but is ineffective at the nociceptin receptor (NOPR)...
December 12, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29232769/antiparkinsonian-and-antidyskinetic-profiles-of-two-novel-potent-and-selective-nociceptin-orphanin-fq-receptor-agonists
#7
Ludovico Arcuri, Salvatore Novello, Martina Frassineti, Daniela Mercatelli, Clarissa Anna Pisanò, Ilaria Morella, Stefania Fasano, Blair V Journigan, Michael E Meyer, Willma E Polgar, Riccardo Brambilla, Nurulain T Zaveri, Michele Morari
BACKGROUND AND PURPOSE: We previously showed that Nociceptin/orphanin FQ opioid peptide (NOP) receptor agonists attenuate the expression of levodopa-induced dyskinesia in animal models of Parkinson's disease. We now investigate the efficacy of two novel, potent and chemically distinct NOP receptor agonists, AT-390 and AT-403, to improve parkinsonian disabilities and attenuate dyskinesia development and expression. EXPERIMENTAL APPROACH: Binding affinity and functional efficacy of AT-390 and AT-403 at the opioid receptors were determined in radioligand displacement assays and in GTPγS binding assay respectively, conducted in Chinese hamster ovary cells...
December 12, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29232630/opioid-drugs-and-stercoral-perforation-of-the-colon-case-report-and-review-of-literature
#8
Renée Poitras, Daun'Lee Warren, Sylvanus Oyogoa
INTRODUCTION: Stercoral perforation of the colon is a rare pathology, which is believed to be caused by an increased intraluminal pressure created by a fecaloma. Opioid induced constipation is a rare and often unsuspected cause of colonic perforation. PRESENTATION OF CASE: We report the case of a 58-year-old woman, who presented to the emergency department (ED) with severe hypotension, abdominal pain and gastrointestinal bleeding. She was found to have a diffusely tender and distended abdomen...
December 7, 2017: International Journal of Surgery Case Reports
https://www.readbyqxmd.com/read/29231613/-effects-of-electroacupuncture-on-expression-of-%C3%AE-opioid-receptor-in-nucleus-ceruleus-in-rats-with-bone-cancer-pain-morphine-tolerance
#9
Taofang Fu, Lingling Wang, Junying Du, Feng Chen, Junfan Fang, Yi Liang, Jianqiao Fang
OBJECTIVE: To observe the effects of electroacupuncture (EA) on pain behavior in rats with bone cancer pain and morphine tolerance, and to explore partial action mechanism. METHODS: Forty-two SD healthy female rats were randomly divided into a sham operation group (7 rats), a bone cancer pain group (8 rats), a morphine tolerance group (9 rats), an EA group (9 rats) and a sham EA group (9 rats). The rats in the sham operation group were treated with injection of phosphate buffer saline at medullary cavity of left-side tibia, and the rats in the remaining groups were injected with MRMT-1 breast cancer cells...
May 12, 2017: Zhongguo Zhen Jiu, Chinese Acupuncture & Moxibustion
https://www.readbyqxmd.com/read/29228935/dosimetrically-administered-nebulized-morphine-for-breathlessness-in-very-severe-chronic-obstructive-pulmonary-disease-a-randomized-controlled-trial
#10
Piotr Janowiak, Małgorzata Krajnik, Zygmunt Podolec, Tomasz Bandurski, Iwona Damps-Konstańska, Piotr Sobański, David C Currow, Ewa Jassem
BACKGROUND: Systemic morphine has evidence to support its use for reducing breathlessness in patients with severe chronic obstructive pulmonary disease (COPD). The effectiveness of the nebulized route, however, has not yet been confirmed. Recent studies have shown that opioid receptors are localized within epithelium of human trachea and large bronchi, a target site for a dosimetric nebulizer. The aim of this study was to compare any clinical or statistical differences in breathlessness intensity between nebulized 2...
December 11, 2017: BMC Pulmonary Medicine
https://www.readbyqxmd.com/read/29224002/the-protective-effects-of-%C3%AE-opioid-receptor-stimulation-in-hypoxic-pulmonary-hypertension-involve-inhibition-of-autophagy-through-the-ampk-mtor-pathway
#11
Yaguang Zhou, Yuanbo Wang, Xu Wang, Xin Tian, Shumiao Zhang, Fan Yang, Haitao Guo, Rong Fan, Na Feng, Min Jia, Xiaoming Gu, Yuemin Wang, Juan Li, Jianming Pei
BACKGROUND/AIMS: In a previous study, we showed that κ-opioid receptor stimulation with the selective agonist U50,488H ameliorated hypoxic pulmonary hypertension (HPH). However, the roles that pulmonary arterial smooth muscle cell (PASMC) proliferation, apoptosis, and autophagy play in κ-opioid receptor-mediated protection against HPH are still unknown. The goal of the present study was to investigate the role of autophagy in U50,488H-induced HPH protection and the underlying mechanisms...
December 8, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29222847/synthesis-of-novel-norsufentanil-analogues-via-a-four-component-ugi-reaction-and-in-vivo-docking-and-qsar-studies-of-their-analgesic-activity
#12
Majid Nami, Peyman Salehi, Minoo Dabiri, Morteza Bararjanian, Sajjad Gharaghani, Mona Khoramjouy, Ahmed Al-Harrasi, Mehrdad Faizi
Novel substituted amino acid tethered norsufentanil derivatives were synthesized by the four-component Ugi reaction. Norsufentanil was reacted with succinic anhydride to produce the corresponding carboxylic acid. The resulting carboxylic acid has undergone a multicomponent reaction with different aldehydes, amines, and isocyanides to produce a library of the desired compounds. In all cases, amide bond rotation was observed in the NMR spectra. In vivo analgesic activity of the synthesized compounds was evaluated by a tail flick test...
December 8, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29222646/evidence-for-the-involvement-of-opioid-system-in-the-antidepressant-like-effect-of-ascorbic-acid
#13
Morgana Moretti, Camille M Ribeiro, Vivian B Neis, Luis Eduardo B Bettio, Priscila B Rosa, Ana Lúcia S Rodrigues
Considering the involvement of the opioid system in major depressive disorder (MDD), mainly concerning refractory MDD, and the evidence that ascorbic acid may exert a beneficial effect for the treatment of this disorder, this study investigated the involvement of the opioid system in the antidepressant-like effect of ascorbic acid in the tail suspension test (TST). Treatment of Swiss mice with the non-selective opioid receptor antagonist naloxone (1 mg/kg, i.p.) prevented the reduced immobility time caused by ascorbic acid (1 mg/kg, p...
December 8, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29220721/novel-effect-of-methionine-enkephalin-against-influenza-a-virus-infection-through-inhibiting-tlr7-myd88-traf6-nf-%C3%AE%C2%BAb-p65-signaling-pathway
#14
Jing Tian, Xue Jiao, Xiaonan Wang, Jin Geng, Reizhe Wang, Ning Liu, Xinhua Gao, Noreen Griffin, Fengping Shan
The morbidity and mortality associated with influenza A virus infections, have stimulated the search for novel prophylactic and therapeutic drugs. The purpose of this study was to investigate the prophylactic and therapeutic effect of synthetic methionine enkephalin (MENK) on mice infected by A/PR/8/34 influenza virus (H1N1) in vivo. The results showed that MENK could exert both prophylactic and therapeutic influences on infected mice, significantly improve the survival rate, relieve acute lung injury and decrease cytokine (IFN-α, IFN-β, TNF-α, IL-6, and IL-1β) levels...
December 5, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/29219169/pharmacokinetics-and-pharmacodynamics-of-sublingual-sufentanil-for-postoperative-pain-management
#15
REVIEW
T van de Donk, S Ward, R Langford, A Dahan
Achieving successful treatment of postoperative pain remains a challenge. Recently, a sufentanil sublingual tablet system has been developed for treatment of moderate-to-severe postoperative pain. The phenylpiperidine sufentanil is a potent analgesic that rapidly crosses the blood-brain barrier and selectively activates central μ-opioid receptors. The system makes use of a hand-held dispenser system, which contains forty 15-μg sufentanil sublingual micro-tablets. The patient can release one tablet at 20-min intervals using a unique radiofrequency adhesive tag, which is wrapped around the patient's thumb...
December 8, 2017: Anaesthesia
https://www.readbyqxmd.com/read/29215139/a-novel-and-selective-nociceptin-receptor-nop-agonist-1-1-cis-4-isopropylcyclohexyl-piperidin-4-yl-1h-indol-2-yl-methanol-at-312-decreases-acquisition-of-ethanol-induced-conditioned-place-preference-in-mice
#16
Nurulain T Zaveri, Paul V Marquez, Michael E Meyer, Willma E Polgar, Abdul Hamid, Kabirullah Lutfy
BACKGROUND: Nociceptin/Orphanin FQ (N/OFQ), the endogenous peptide agonist for the opioid receptor-like (ORL1) receptor (also known as NOP or the nociceptin receptor), has been shown to block the acquisition and expression of ethanol-induced conditioned place preference (CPP). Here, we report the characterization of a novel small-molecule NOP ligand AT-312 (1-(1-((cis)-4-isopropylcyclohexyl)piperidin-4-yl)-1H-indol-2-yl)methanol) in receptor binding and GTPγS functional assays in vitro...
December 7, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/29211767/investigating-endogenous-%C3%A2%C2%B5-opioid-receptors-in-human-keratinocytes-as-pharmacological-targets-using-novel-fluorescent-ligand
#17
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/29210823/peripherally-acting-mu-opioid-receptor-antagonists
#18
(no author information available yet)
No abstract text is available yet for this article.
November 2017: Gastroenterology Nursing: the Official Journal of the Society of Gastroenterology Nurses and Associates
https://www.readbyqxmd.com/read/29210822/peripherally-acting-mu-opioid-receptor-antagonists
#19
Stephanie Martinez-Cox, Karla Espinosa, Chad Friece, Anita Rahman
No abstract text is available yet for this article.
November 2017: Gastroenterology Nursing: the Official Journal of the Society of Gastroenterology Nurses and Associates
https://www.readbyqxmd.com/read/29210063/opioid-induced-inhibition-of-the-human-serotonin-and-norepinephrine-transporters-in-vitro-link-to-clinical-reports-of-serotonin-syndrome
#20
Anna Rickli, Evangelia Liakoni, Marius C Hoener, Matthias E Liechti
BACKGROUND AND PURPOSE: Opioids may inhibit the serotonin and norepinephrine transporters (SERT and NET, respectively). NET inhibition may contribute to analgesia, and SERT inhibition or interactions with serotonin receptors may cause serotonergic toxicity. However, the effects of different opioids on the human SERT, NET, and serotonin receptors have not been sufficiently studied. EXPERIMENTAL APPROACH: We determined the potencies of different opioids to inhibit the SERT and NET in vitro using human transporter-transfected cells...
December 6, 2017: British Journal of Pharmacology
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