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https://www.readbyqxmd.com/read/27909965/correction-of-negative-effect-of-antenatal-hypoxia-on-liver-tissue-homeostasis-in-newborn-albino-rats-with-opioid-peptides
#1
O G Pinaeva, E N Sazonova, O A Lebed'ko, S S Timoshin
We studied the possibility of correction of the negative effects of antenatal hypoxia on the liver tissue homeostasis in 7-day-old albino rats by administration of opioid peptides in a dose of 100 μg/kg on postnatal days 2-6. Administration of mixed μ/δ-opioid receptor agonist Dalargin neutralized deviations of gravimetric indicators, parameters of proliferative activity, and activity of the nucleolar apparatus of hepatocytes. Administration of the non-opiate Leu-enkephalin analogue did not normalize gravimetric parameters and nucleolar apparatus parameters, however, it significantly increased the pool of proliferating hepatocytes...
December 2, 2016: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/27799813/local-analgesic-effect-of-tramadol-is-mediated-by-opioid-receptors-in-late-postoperative-pain-after-plantar-incision-in-rats
#2
José Oswaldo de Oliveira Junior, Milena Fernandes de Freitas, Carolina Bullara de Andrade, Marucia Chacur, Hazem Adel Ashmawi
Tramadol is a drug used to treat moderate to severe pain. It is known to present a peripheral effect, but the local mechanisms underlying its actions remain unclear. The role of peripheral opioid receptors in postoperative pain is not well understood. In the present study, we examined the peripheral opioid receptors to determine the local effect of tramadol in a plantar incision pain model. Rats were subjected to plantar incision and divided into four groups on postoperative day (POD) 1: SF_SF, 0.9% NaCl injected into the right hindpaw; SF_TraI, 0...
2016: Journal of Pain Research
https://www.readbyqxmd.com/read/27778232/a-computational-systems-biology-approach-for-identifying-candidate-drugs-for-repositioning-for-cardiovascular-disease
#3
Alvin Z Yu, Stephen A Ramsey
We report an in silico method to screen for receptors or pathways that could be targeted to elicit beneficial transcriptional changes in a cellular model of a disease of interest. In our method, we integrate: (1) a dataset of transcriptome responses of a cell line to a panel of drugs; (2) two sets of genes for the disease; and (3) mappings between drugs and the receptors or pathways that they target. We carried out a gene set enrichment analysis (GSEA) test for each of the two gene sets against a list of genes ordered by fold-change in response to a drug in a relevant cell line (HL60), with the overall score for a drug being the difference of the two enrichment scores...
October 24, 2016: Interdisciplinary Sciences, Computational Life Sciences
https://www.readbyqxmd.com/read/27775047/repetitive-electroacupuncture-attenuates-cold-induced-hypertension-through-enkephalin-in-the-rostral-ventral-lateral-medulla
#4
Min Li, Stephanie C Tjen-A-Looi, Zhi-Ling Guo, John C Longhurst
Acupuncture lowers blood pressure (BP) in hypertension, but mechanisms underlying its action are unclear. To simulate clinical studies, we performed electroacupuncture (EA) in unanesthetized rats with cold-induced hypertension (CIH) induced by six weeks of cold exposure (6 °C). EA (0.1 - 0.4 mA, 2 Hz) was applied at ST36-37 acupoints overlying the deep peroneal nerve for 30 min twice weekly for five weeks while sham-EA was conducted with the same procedures as EA except for no electrical stimulation...
October 24, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27734456/-opioidergic-postconditioning-of-heart-muscle-during-ischemia-reperfusion-injury
#5
Marcin Kunecki, Wojciech Płazak, Tomasz Roleder, Jolanta Biernat, Tomasz Oleksy, Piotr Podolec, Krzysztof Stanisław Gołba
BACKGROUND: Ischemic preconditioning (IPC) and postconditioning (POC) are the novel strategies of attaining cardioprotection against ischemia/reperfusion (I/R) injury. Previous studies suggested the role of opioid pathway, however the class of opioid receptors responsible for this effect in humans remains unknown. The aim of the study was to assess the influence of opioids on simulated I/R injury outcomes in the human myocardium. METHODS: Trabeculae of the human right atrium were electrically driven in organ bath and subjected to simulated I/R injury...
October 13, 2016: Cardiology Journal
https://www.readbyqxmd.com/read/27670390/allostatic-mechanisms-of-opioid-tolerance-beyond-desensitization-and-downregulation
#6
Catherine M Cahill, Wendy Walwyn, Anna M W Taylor, Amynah A A Pradhan, Christopher J Evans
Mechanisms of opioid tolerance have focused on adaptive modifications within cells containing opioid receptors, defined here as cellular allostasis, emphasizing regulation of the opioid receptor signalosome. We review additional regulatory and opponent processes involved in behavioral tolerance, and include mechanistic differences both between agonists (agonist bias), and between μ- and δ-opioid receptors. In a process we will refer to as pass-forward allostasis, cells modified directly by opioid drugs impute allostatic changes to downstream circuitry...
September 23, 2016: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/27665747/upregulation-and-activation-of-%C3%AE-%C3%A2-opioid-receptors-promotes-the-progression-of-human-breast-cancer
#7
Yang-Chao Wei, Bin Zhang, Xuan Li, Xiao-Meng Liu, Jing Zhang, Biao Lei, Bo Li, Run Zhai, Qian Chen, Yang Li
δ‑opioid receptor (DOR) belongs to the family of G protein‑coupled receptors (GPCRs). Numerous studies have shown that DOR is widely distributed in human peripheral tissues and is closely related to the development and progression of certain malignant tumours. However, there is controversy in the literature regarding whether DOR has an impact on the development and progression of human breast cancer. The present study comprehensively elaborates on the biological functions of DOR by determining the distribution of DOR expression in breast cancer tissues and cells and by further verifying the effects of DOR on breast cancer progression...
September 19, 2016: Oncology Reports
https://www.readbyqxmd.com/read/27647873/abuse-potential-and-pharmacodynamic-characteristics-of-oral-and-intranasal-eluxadoline-a-mixed-%C3%AE-and-%C3%AE%C2%BA-opioid-receptor-agonist-and-%C3%AE-opioid-receptor-antagonist
#8
Naama Levy-Cooperman, Gail McIntyre, Laura Bonifacio, Michael McDonnell, J Michael Davenport, Paul S Covington, Leonard S Dove, Edward M Sellers
Drugs with μ-opioid receptor (OR) activity can be associated with abuse and misuse. The peripherally acting mixed μ-OR and κ-OR agonist and δ-OR antagonist, eluxadoline, is approved in the US for the treatment of irritable bowel syndrome with diarrhea. In two separate crossover studies, we evaluated the oral and intranasal abuse potential of eluxadoline versus placebo and the active control oxycodone. Healthy recreational opioid users received eluxadoline 100, 300, and 1000 mg, oxycodone 30 and 60 mg, and placebo (oral study), or eluxadoline 100 and 200 mg, oxycodone 15 and 30 mg, and placebos matched to eluxadoline and oxycodone (intranasal study)...
September 19, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27646288/histone-deacetylase-inhibitor-induced-emergence-of-synaptic-%C3%AE-opioid-receptors-and-behavioral-antinociception-in-persistent-neuropathic-pain
#9
Wenjuan Tao, Wenjie Zhou, Yuping Wang, Tingting Sun, Haitao Wang, Zhi Zhang, Yan Jin
The efficacy of opioids in patients with chronic neuropathic pain remains controversial. Although activation of δ-opioid receptors (DORs) in the brainstem reduces inflammation-induced persistent hyperalgesia, it is not effective under persistent neuropathic pain conditions and these clinical problems remain largely unknown. In this study, by using a chronic constriction injury (CCI) of the sciatic nerve in rats, we found that in the brainstem nucleus raphe magnus (NRM), DORs emerged on the surface membrane of central synaptic terminals on day 3 after CCI surgery and disappeared on day 14...
December 17, 2016: Neuroscience
https://www.readbyqxmd.com/read/27582887/the-role-of-naloxegol-in-the-management-of-opioid-induced-bowel-dysfunction
#10
REVIEW
Wojciech Leppert, Jaroslaw Woron
Opioid-induced constipation (OIC) and other gastrointestinal (GI) symptoms of opioid-induced bowel dysfunction (OIBD) significantly deteriorate patients' quality of life and may lead to noncompliance with opioid schedule and undertreatment of pain. Although traditional oral laxatives are the first-line treatment of OIC, they do not address OIBD pathophysiology, and display numerous adverse effects. OIC treatment includes prokinetics (lubiprostone), opioid switch, and changing route of opioid administration...
September 2016: Therapeutic Advances in Gastroenterology
https://www.readbyqxmd.com/read/27576463/%C3%AE-opioid-receptor-activation-and-microrna-expression-in-the-rat-heart-under-prolonged-hypoxia
#11
Feng Zhi, Lian Xue, Naiyuan Shao, Danni Deng, Xuezhi Kang, Dongman Chao, Yuan Xu, Rong Wang, Yilin Yang, Ying Xia
BACKGROUND: Hypoxic/ischemic injury to the heart is a frequently encountered clinical problem with limited therapeutic options. Since microRNAs (miRNAs) are involved in hypoxic/ischemic events, and δ-opioid receptor (DOR) activation is known to protect against hypoxic/ischemic injury, we speculated on the involvement of DOR activation in altering miRNA expression in the heart under hypoxic conditions. The present study aimed to test our hypothesis. METHODS: Male Sprague Dawley rats were exposed to hypoxia (9...
2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27561742/functional-modulation-on-macrophage-by-low-dose-naltrexone-ldn
#12
Zhe Yi, Shengnan Guo, Xu Hu, Xiaonan Wang, Xiaoqing Zhang, Noreen Griffin, Fengping Shan
Previously it was confirmed that naltrexone, a non-peptide δ-opioid receptor selective antagonist is mainly used for alcoholic dependence and opioid addiction treatment. However, there is increasing data on immune regulation of low dose naltrexone (LDN). The aim of this work was to explore the effect of LDN on the phenotype and function of macrophage. The changes of macrophage after treatment with LDN were examined using flow cytometry (FCM); FITC-dextran phagocytosis and enzyme-linked immunosorbent assay (ELISA)...
October 2016: International Immunopharmacology
https://www.readbyqxmd.com/read/27540116/clathrin-light-chains-role-in-selective-endocytosis-influences-antibody-isotype-switching
#13
Shuang Wu, Sophia R Majeed, Timothy M Evans, Marine D Camus, Nicole M L Wong, Yvette Schollmeier, Minjong Park, Jagan R Muppidi, Andrea Reboldi, Peter Parham, Jason G Cyster, Frances M Brodsky
Clathrin, a cytosolic protein composed of heavy and light chain subunits, assembles into a vesicle coat, controlling receptor-mediated endocytosis. To establish clathrin light chain (CLC) function in vivo, we engineered mice lacking CLCa, the major CLC isoform in B lymphocytes, generating animals with CLC-deficient B cells. In CLCa-null mice, the germinal centers have fewer B cells, and they are enriched for IgA-producing cells. This enhanced switch to IgA production in the absence of CLCa was attributable to increased transforming growth factor β receptor 2 (TGFβR2) signaling resulting from defective endocytosis...
August 30, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27517901/cytoprotection-against-hypoxic-and-or-mpp%C3%A2-%C2%BA-injury-effect-of-%C3%AE-opioid-receptor-activation-on-caspase-3
#14
Yuan Xu, Feng Zhi, Naiyuan Shao, Rong Wang, Yilin Yang, Ying Xia
The pathological changes of Parkinson's disease (PD) are, at least partially, associated with the dysregulation of PTEN-induced putative kinase 1 (PINK1) and caspase 3. Since hypoxic and neurotoxic insults are underlying causes of PD, and since δ-opioid receptor (DOR) is neuroprotective against hypoxic/ischemic insults, we sought to determine whether DOR activation could protect the cells from damage induced by hypoxia and/or MPP⁺ by regulating PINK1 and caspase 3 expressions. We exposed PC12 cells to either severe hypoxia (0...
2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27498137/%C3%AE-opioid-receptors-pivotal-role-in-intermittent-hypoxia-augmentation-of-cardiac-parasympathetic-control-and-plasticity
#15
Juan A Estrada, Mathew A Barlow, Darice Yoshishige, Arthur G Williams, H Fred Downey, Robert T Mallet, James L Caffrey
BACKGROUND: Intermittent hypoxia training (IHT) produces robust myocardial protection against ischemia-reperfusion induced infarction and arrhythmias. Blockade of this cardioprotection by antagonism of either β1-adrenergic or δ-opioid receptors (δ-OR) suggests autonomic and/or opioidergic adaptations. PURPOSE: To test the hypothesis that IHT shifts cardiac autonomic balance toward greater cholinergic and opioidergic influence. METHODS: Mongrel dogs completed 20d IHT, non-hypoxic sham training, or IHT with the δ-OR antagonist naltrindole (200μg/kgsc)...
July 2016: Autonomic Neuroscience: Basic & Clinical
https://www.readbyqxmd.com/read/27492364/remifentanil-preconditioning-protects-rat-cardiomyocytes-against-hypoxia-reoxygenation-injury-via-%C3%AE-opioid-receptor-mediated-activation-of-pi3k-akt-and-erk-pathways
#16
Meng-Yun Dou, Hao Wu, Hai-Juan Zhu, Shi-Yun Jin, Ye Zhang, Shu-Fang He
Remifentanil preconditioning has been demonstrated to reduce myocardial ischemia reperfusion injury in rat hearts, while the mechanisms are not fully understood. This study investigated the protective effects of remifentanil against hypoxia-reoxygenation injury in adult rat cardiomyocytes and the mechanisms involving opioid receptors and downstream phosphatidylinositol-3-kinase/protein kinase B (PI3K/Akt) and extracellular signal-regulated kinase (ERK) signaling pathways. Adult rat cardiomyocytes were pretreated with remifentanil at different concentrations and then subjected to 90min hypoxia followed by 120min reoxygenation...
October 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27479354/serial-femtosecond-crystallography-datasets-from-g-protein-coupled-receptors
#17
COMMENT
Thomas A White, Anton Barty, Wei Liu, Andrii Ishchenko, Haitao Zhang, Cornelius Gati, Nadia A Zatsepin, Shibom Basu, Dominik Oberthür, Markus Metz, Kenneth R Beyerlein, Chun Hong Yoon, Oleksandr M Yefanov, Daniel James, Dingjie Wang, Marc Messerschmidt, Jason E Koglin, Sébastien Boutet, Uwe Weierstall, Vadim Cherezov
We describe the deposition of four datasets consisting of X-ray diffraction images acquired using serial femtosecond crystallography experiments on microcrystals of human G protein-coupled receptors, grown and delivered in lipidic cubic phase, at the Linac Coherent Light Source. The receptors are: the human serotonin receptor 2B in complex with an agonist ergotamine, the human δ-opioid receptor in complex with a bi-functional peptide ligand DIPP-NH2, the human smoothened receptor in complex with an antagonist cyclopamine, and finally the human angiotensin II type 1 receptor in complex with the selective antagonist ZD7155...
2016: Scientific Data
https://www.readbyqxmd.com/read/27474249/study-on-the-molecular-mechanism-of-antinociception-induced-by-ghrelin-in-acute-pain-in-mice
#18
Fu-Yan Liu, Min-Min Zhang, Ping Zeng, Wen-Wen Liu, Jing-Lei Wang, Bei Yang, Qun Dai, Jie Wei
Ghrelin has been identified as the endogenous ligand for the GHS-R1α (growth hormone secretagogue receptor 1 alpha). Our previous experiments have indicated that ghrelin (i.c.v.) induces antinociceptive effects in acute pain in mice, and the effects were mediated through the central opioid receptors and GHS-R1α. However, which opioid receptor (OR) mediates the antinociceptive effects and the molecular mechanisms are also needed to be further explored. In the present study, the antinociceptive effects of ghrelin (i...
September 2016: Peptides
https://www.readbyqxmd.com/read/27471903/central-oxytocin-receptor-stimulation-attenuates-the-orexigenic-effects-of-butorphanol-tartrate
#19
Pawel K Olszewski, Oscar A Klockars, Anica Klockars, Allen S Levine
Butorphanol tartrate (BT), a mixed µ/κ/δ opioid receptor agonist, is one of the most potent orexigens known to date. The central mechanisms through which BT causes hyperphagia are largely unknown. Interestingly, BT suppresses meal-end activation of neurons synthesizing anorexigenic neuropeptide, oxytocin (OT), which suggests that BT promotes hyperphagia by silencing OT-derived satiety signaling. As OT terminates consumption by acting by distinct hindbrain and forebrain circuits, we investigated whether stimulation of the OT receptor in the forebrain or the hindbrain [through lateral ventricular (LV) and fourth ventricular (4V) OT injections] leads to termination of food intake induced by BT...
September 28, 2016: Neuroreport
https://www.readbyqxmd.com/read/27464743/comparative-analysis-of-pharmacological-properties-of-xanomeline-and-n-desmethylclozapine-in-rat-brain-membranes
#20
Yuji Odagaki, Masakazu Kinoshita, Toshio Ota
BACKGROUND: 3(3-Hexyloxy-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-methylpyridine (xanomeline) and N-desmethylclozapine are of special interest as promising antipsychotics with better efficacy, especially for negative symptoms and/or cognitive/affective impairment. METHODS: The guanosine-5'-O-(3-[(35)S]thio)triphosphate ([(35)S]GTPγS) binding experiments were performed using (1) conventional filtration technique, (2) antibody-capture scintillation proximity assay, and (3) immunoprecipitation method, in brain membranes prepared from rat cerebral cortex, hippocampus, and striatum...
September 2016: Journal of Psychopharmacology
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