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https://www.readbyqxmd.com/read/28926935/identification-of-circulating-mirnas-differentially-regulated-by-opioid-treatment
#1
Kaoru Toyama, Naoki Kiyosawa, Kenji Watanabe, Hitoshi Ishizuka
Emerging evidence demonstrates functional contributions of microRNAs (miRNAs) to μ-opioid receptor (MOR) signaling, but the information so far has been mostly limited to their intracellular regulatory mechanisms. The present study aimed to investigate changes in plasma miRNA profiles elicited by opioid treatment in blood samples collected from clinical studies. Healthy male subjects were orally administered with hydromorphone or oxycodone and blood samples were collected at a specified time after the drug treatment...
September 16, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28924009/site-specific-regulation-of-p2x7-receptor-function-in-microglia-gates-morphine-analgesic-tolerance
#2
Heather Leduc-Pessah, Nicholas L Weilinger, Churmy Y Fan, Nicole E Burma, Roger J Thompson, Tuan Trang
Tolerance to the analgesic effects of opioids is a major problem in chronic pain management. Microglia are implicated in opioid tolerance, but the core mechanisms regulating their response to opioids remain obscure. By selectively ablating microglia in the spinal cord using a saporin-conjugated antibody to Mac1, we demonstrate a causal role for microglia in the development, but not maintenance, of morphine tolerance in male rats. Increased P2X7 receptor (P2X7R) activity is a cardinal feature of microglial activation, and in this study we found that morphine potentiates P2X7R-mediated Ca(2+) responses in resident spinal microglia acutely isolated from morphine tolerant rats...
September 18, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28923480/impact-of-morphine-on-the-expression-of-insulin-receptor-and-protein-levels-of-insulin-igfs-in-rat-neural-stem-cells
#3
Sadegh Salarinasab, AliReza Nourazarian, Masoud Nikanfar, Nima Abdyazdani, Masoumeh Kazemi, Navid Feizy, Reza Rahbarghazi
Alzheimer's disease is correlated with neuronal degeneration and loss of neuronal precursors in different parts of the brain. It has been found disturbance in the homeostasis neural stem cells (NSCs) can cause neurodegeneration. Morphine, an analgesic agent, can disrupt the dynamic and normal state of NSCs. However, more investigations are required to clearly address underlying mechanisms. The current experiment aimed to investigate the effects of morphine on the cell distribution of insulin factor and receptor and insulin-like growth factors (IGF1, IGF2) in NSCs...
September 15, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28923348/stimulation-of-accumbal-gabaa-receptors-inhibits-delta2-but-not-delta1-opioid-receptor-mediated-dopamine-efflux-in-the-nucleus-accumbens-of-freely-moving-rats
#4
Yuri Aono, Yuri Kiguchi, Yuriko Watanabe, John L Waddington, Tadashi Saigusa
The nucleus accumbens contains delta-opioid receptors that may reduce inhibitory neurotransmission. Reduction in GABAA receptor-mediated inhibition of accumbal dopamine release due to delta-opioid receptor activation should be suppressed by stimulating accumbal GABAA receptors. As delta-opioid receptors are divided into delta2- and delta1-opioid receptors, we analysed the effects of the GABAA receptor agonist muscimol on delta2- and delta1-opioid receptor-mediated accumbal dopamine efflux in freely moving rats using in vivo microdialysis...
September 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28922338/does-the-%C3%AE-receptor-antagonist-esmolol-have-analgesic-effects-a-randomised-placebo-controlled-cross-over-study-on-healthy-volunteers-undergoing-the-cold-pressor-test
#5
Fredrik Ander, Anders Magnuson, Alex de Leon, Rebecca Ahlstrand
BACKGROUND: Esmolol may attenuate the sympathetic response to pain and reduce postoperative opioid consumption. It is not clear whether esmolol has an analgesic effect per se. OBJECTIVES: The aim of this study was to evaluate the analgesic effect of esmolol in the absence of anaesthetics and opioids. We tested the hypothesis that esmolol would reduce the maximum pain intensity perceived during the cold pressor test (CPT) by 2 points on a 0 to 10 numeric pain rating scale (NRS) compared to placebo...
September 15, 2017: European Journal of Anaesthesiology
https://www.readbyqxmd.com/read/28920461/discovery-and-development-of-tramadol-for-the-treatment-of-pain
#6
Lidia Bravo, Juan Antonio Mico, Esther Berrocoso
Tramadol is an opioid drug that, unlike classic opioids, also modulates the monoaminergic system by inhibiting noradrenergic and serotoninergic reuptake. For this reason, tramadol is considered an atypical opioid. These special pharmacological characteristics have made tramadol one of the most commonly prescribed analgesic drugs to treat moderate to severe pain. Areas covered: The aim of this review is to provide a historical description of the biochemistry, pharmacokinetics and particularly, the mechanisms of action of tramadol...
September 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28919062/progress-and-challenges-in-anti-obesity-pharmacotherapy
#7
REVIEW
Daniel H Bessesen, Luc F Van Gaal
Obesity is a serious and growing worldwide health challenge. Healthy lifestyle choices are the foundation of obesity treatment. However, weight loss can lead to physiological adaptations that promote weight regain. As a result, lifestyle treatment alone typically produces only modest weight loss that is difficult to sustain. In other metabolic diseases, pharmacotherapy is an accepted adjunct to lifestyle. Several anti-obesity drugs have been approved in the USA, European Union, Australia, and Japan including sympathomimetics, pancreatic lipase inhibitors, GABAA receptor activators, a serotonin 2C receptor agonist, opioid antagonist, dopamine-norepinephrine reuptake inhibitor, and glucagon-like peptide-1 (GLP-1) receptor agonists...
September 14, 2017: Lancet Diabetes & Endocrinology
https://www.readbyqxmd.com/read/28916574/systematic-review-of-the-gastrointestinal-effects-of-a1-compared-with-a2-%C3%AE-casein
#8
REVIEW
Simon Brooke-Taylor, Karen Dwyer, Keith Woodford, Natalya Kost
This is the first systematic review, to our knowledge, of published studies investigating the gastrointestinal effects of A1-type bovine β-casein (A1) compared with A2-type bovine β-casein (A2). The review is relevant to nutrition practice given the increasing availability and promotion in a range of countries of dairy products free of A1 for both infant and adult nutrition. In vitro and in vivo studies (all species) were included. In vivo studies were limited to oral consumption. Inclusion criteria encompassed all English-language primary research studies, but not reviews, involving milk, fresh-milk products, β-casein, and β-casomorphins published through 12 April 2017...
September 2017: Advances in Nutrition
https://www.readbyqxmd.com/read/28916251/mk-801-but-not-naloxone-attenuates-high-dose-dextromethorphan-induced-convulsive-behavior-possible-involvement-of-the-glun2b-receptor
#9
Hai-Quyen Tran, Yoon Hee Chung, Eun-Joo Shin, The-Vinh Tran, Ji Hoon Jeong, Choon-Gon Jang, Seung-Yeol Nah, Kiyofumi Yamada, Toshitaka Nabeshima, Hyoung-Chun Kim
Dextromethorphan (DM) is a dextrorotatory isomer of levorphanol, a typical morphine-like opioid. When administered at supra-antitussive doses, DM produces psychotoxic and neurotoxic effects in humans. Although DM abuse has been well-documented, few studies have examined the effects of high-dose DM. The present study aimed to explore the effects of a single high dose of DM on mortality and seizure occurrence. After intraperitoneal administration with a high dose of DM (80mg/kg), Sprague-Dawley rats showed increased seizure occurrence and intensity...
September 13, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28913486/the-switch-from-buprenorphine-to-tapentadol-is-it-worth
#10
REVIEW
Adriana Miclescu
Opioid analgesia continues to be the primary pharmacologic intervention for managing acute pain and malignant pain in both hospitalized and ambulatory patients. The increasing use of opioids in chronic nonmalignant pain is more problematic. Opioid treatment is complicated with the risks raised by adverse effects, especially cognitive disturbance, respiratory depression but also the risk of tolerance, opioid abuse and drug-disease interactions. Despite the growing number of available opioids within the last years, adequate trials of opioid rotation are lacking and most of the information is anecdotal...
October 2016: Rom J Anaesth Intensive Care
https://www.readbyqxmd.com/read/28911965/physiological-roles-of-cns-muscarinic-receptors-gained-from-knockout-mice
#11
REVIEW
Morgane Thomsen, Gunnar Sørensen, Ditte Dencker
Because the five muscarinic acetylcholine receptor subtypes have overlapping distributions in many CNS tissues, and because ligands with a high degree of selectivity for a given subtype long remained elusive, it has been difficult to determine the physiological functions of each receptor. Genetically engineered knockout mice, in which one or more muscarinic acetylcholine receptor subtype has been inactivated, have been instrumental in identifying muscarinic receptor functions in the CNS, at the neuronal, circuit, and behavioral level...
September 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28910112/modular-approach-to-pseudo-neoclerodanes-as-designer-%C3%AE%C2%BA-opioid-ligands
#12
Alexander M Sherwood, Samuel E Williamson, Rachel S Crowley, Logan M Abbott, Victor W Day, Thomas E Prisinzano
Informed by previous semisynthetic work on salvinorin A, a modular total synthesis has been developed capable of producing novel compounds targeting the κ-opioid receptor. The strategy has permitted the deliberate simplification and introduction of functionality about the target molecule to provide access to molecular features on salvinorin A otherwise unattainable by semisynthesis. Using this approach, a potent pseudo-neoclerodane κ-opioid receptor ligand (2) has been realized.
September 14, 2017: Organic Letters
https://www.readbyqxmd.com/read/28902684/estrogens-synthesized-and-acting-within-a-spinal-oligomer-suppress-spinal-endomorphin-2-antinociception-ebb-and-flow-over-the-rat-reproductive-cycle
#13
Nai-Jiang Liu, Vijaya Murugaiyan, Emiliya M Storman, Stephen A Schnell, Martin W Wessendorf, Alan R Gintzler
The magnitude of antinociception elicited by intrathecal endomorphin 2 (EM2), an endogenous mu-opioid receptor (MOR) ligand, varies across the rat estrous cycle. We now report that phasic changes in analgesic responsiveness to spinal EM2 result from plastic interactions within a novel membrane-bound oligomer containing estrogen receptors (mERs), aromatase (aka estrogen synthase), metabotropic glutamate receptor 1 (mGluR1), and MOR. During diestrus, spinal mERs, activated by locally synthesized estrogens, act with mGluR1 to suppress spinal EM2/MOR antinociception...
June 21, 2017: Pain
https://www.readbyqxmd.com/read/28902183/patient-characteristics-affect-the-response-to-ketamine-and-opioids-during-the-treatment-of-vaso-occlusive-episode-related-pain-in-sickle-cell-disease
#14
Raissa Nobrega, Kathy A Sheehy, Caroline Lippold, Amy L Rice, Julia C Finkel, Zenaide M N Quezado
BackgroundN-methyl-D-aspartate receptor activation has been implicated in the pathobiology of inflammatory, nociceptive and neuropathic pain, opioid tolerance, opioid-induced hyperalgesia, and central sensitization. Some of those mechanisms underlie sickle cell disease(SCD)-associated pain.MethodsWe conducted an exploratory cohort study of SCD patients who during vaso-occlusive episodes (VOEs) received subanesthetic doses of the N-methyl-D-aspartate receptor antagonist, ketamine, as an adjunct to opioids. We sought to identify predictors of changes in pain scores and of the percentage of ketamine infusions associated with meaningful changes (≥20% reduction) in pain and opioid consumption...
September 13, 2017: Pediatric Research
https://www.readbyqxmd.com/read/28901580/feeding-live-invertebrate-prey-in-zoos-and-aquaria-are-there-welfare-concerns
#15
REVIEW
Martha Keller
Invertebrates constitute more than 90% of all species on earth, however, as a rule, humans do not regard invertebrates as creatures that can suffer and they are generally seen as creatures that should be eliminated. As a result, the importance of their welfare may be grossly unappreciated. For instance, the feeding of live food is often viewed as a good method of enrichment and invertebrates are commonly used as live prey in many zoological facilities. As a result, zoos may send mixed messages to their patrons in that welfare is considered only for the invertebrates that are part of their zoological collection and not necessarily for the invertebrates used as feed...
September 13, 2017: Zoo Biology
https://www.readbyqxmd.com/read/28900175/dynamic-and-kinetic-elements-of-%C3%A2%C2%B5-opioid-receptor-functional-selectivity
#16
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/28894635/topical-naltrexone-is-a-safe-and-effective-alternative-to-standard-treatment-of-diabetic-wounds
#17
Patricia J McLaughlin, Jarrett D Cain, Michelle B Titunick, Joseph W Sassani, Ian S Zagon
Objective: Diabetes affects more than 29 million individuals in the United States, resulting in healthcare costs approaching $245 billion. Approximately 15% of these individuals will develop a chronic, non-healing foot ulcer (diabetic foot ulcer [DFU]) that, if untreated, may lead to amputation. The current treatments for DFU are expensive, have significant side-effects, and often result in non-compliance. A new topical treatment is described that accelerates cutaneous wound repair and is disease modifying by targeting underlying aberrant diabetic pathways...
September 1, 2017: Advances in Wound Care
https://www.readbyqxmd.com/read/28894357/advances-in-the-delivery-of-buprenorphine-for-opioid-dependence
#18
REVIEW
Richard N Rosenthal, Viral V Goradia
Opioid use disorders (OUDs) have long been a global problem, but the prevalence rates have increased over 20 years to epidemic proportions in the US, with concomitant increases in morbidity and all-cause mortality, but especially opioid overdose. These increases are in part attributable to a several-fold expansion in the prescription of opioid pain medications over the same time period. Opioid detoxification and psychosocial treatments alone have each not yielded sufficient efficacy for OUD, but μ-opioid receptor agonist, partial agonist, and antagonist medications have demonstrated the greatest overall benefit in OUD treatment...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28893975/agonist-dependent-and-independent-kappa-opioid-receptor-phosphorylation-showed-distinct-phosphorylation-patterns-and-resulted-in-different-cellular-outcomes
#19
Yi-Ting Chiu, Chongguang Chen, Daohai Yu, Stefan Schulz, Lee-Yuan Liu-Chen
We reported previously that the selective agonist U50,488H promoted phosphorylation of the mouse kappa opioid receptor (KOPR) at residues S356, T357, T363 and S369. Here, we found that agonist (U50,488H)-dependent KOPR phosphorylation at all the residues were mediated by Gi/oα proteins and multiple protein kinases [GRKs2, 3, 5 and 6 and protein kinase C (PKC)]. In addition, PKC activation by phorbol ester induced agonist-independent KOPR phosphorylation. Compared with U50,488H, PKC activation promoted much higher S356/T357 phosphorylation, much lower T363 phosphorylation and similar levels of S369 phosphorylation...
September 11, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28893017/a-comparative-study-of-analgesic-effect-of-intrathecal-nalbuphine-and-fentanyl-as-adjuvant-in-lower-limb-orthopaedic-surgery
#20
Shagufta Naaz, Usha Shukla, Swati Srivastava, Erum Ozair, Adil Asghar
INTRODUCTION: Intrathecal opioids when added to local anaesthetics decrease their dosage and provide haemodynamic stability. Nalbuphine is an agonist-antagonist and acts on kappa receptors providing analgesia. AIM: The study aims to compare the analgesic efficacy of fentanyl with that of two doses of nalbuphine when used with injection bupivacaine heavy in spinal anaesthesia. MATERIALS AND METHODS: A randomised, double blinded, prospective study on 90 patients of ASA I and II undergoing lower limb orthopaedic surgery under subarachnoid block was done...
July 2017: Journal of Clinical and Diagnostic Research: JCDR
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