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https://www.readbyqxmd.com/read/29044528/endomorphins-potentiate-asic-currents-and-enhance-the-lactic-acid-mediated-increase-in-arterial-blood-pressure-effects-amplified-in-hindlimb-ischemia
#1
Mohamed Farrag, Julie K Drobish, Henry L Puhl, Joyce S Kim, Paul B Herold, Marc P Kaufman, Victor Ruiz-Velasco
Chronic muscle ischemia leads to accumulation of lactic acid and other inflammatory mediators with a subsequent drop in interstitial pH. Acid-sensing ion channels (ASICs), expressed in thin muscle afferents, sense the decrease in pH and evoke a pressor reflex known to increase mean arterial pressure. The naturally occurring endomorphins are also released by primary afferents under ischemic conditions. We examined whether high affinity mu opioid receptor (MOR) agonists, endomorphin-1 (E-1) and -2 (E-2), modulate ASIC currents and the lactic acid-mediated pressor reflex...
October 16, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/29040826/maintenance-on-naltrexone-amphetamine-decreases-cocaine-vs-food-choice-in-male-rhesus-monkeys
#2
Megan J Moerke, Matthew L Banks, Kejun Cheng, Kenner C Rice, S Stevens Negus
BACKGROUND: Cocaine use disorder remains a significant public health issue for which there are no FDA-approved pharmacotherapies. Amphetamine maintenance reduces cocaine use in preclinical and clinical studies, but the mechanism of this effect is unknown. Previous studies indicate a role for endogenous opioid release and subsequent opioid receptor activation in some amphetamine effects; therefore, the current study examined the role of mu-opioid receptor activation in d-amphetamine treatment effects in an assay of cocaine-vs-food choice...
October 13, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29038479/probing-ligand-recognition-of-the-opioid-pan-antagonist-at-076-at-nociceptin-kappa-mu-and-delta-opioid-receptors-through-structure-activity-relationships
#3
V Blair Journigan, Willma E Polgar, Edward W Tuan, James Lu, Pankaj R Daga, Nurulain T Zaveri
Few opioid ligands binding to the three classic opioid receptor subtypes, mu, kappa and delta, have high affinity at the fourth opioid receptor, the nociceptin/orphanin FQ receptor (NOP). We recently reported the discovery of AT-076 (1), (R)-7-hydroxy-N-((S)-1-(4-(3-hydroxyphenyl)piperidin-1-yl)-3-methylbutan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide, a pan antagonist with nanomolar affinity for all four subtypes. Since AT-076 binds with high affinity at all four subtypes, we conducted a structure-activity relationship (SAR) study to probe ligand recognition features important for pan opioid receptor activity, using chemical modifications of key pharmacophoric groups...
October 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29033825/acute-stress-affects-the-expression-of-hippocampal-mu-oscillations-in-an-age-dependent-manner
#4
Samir Takillah, Jérémie Naudé, Steve Didienne, Claude Sebban, Brigitte Decros, Esther Schenker, Michael Spedding, Alexandre Mourot, Jean Mariani, Philippe Faure
Anxiolytic drugs are widely used in the elderly, a population particularly sensitive to stress. Stress, aging and anxiolytics all affect low-frequency oscillations in the hippocampus and prefrontal cortex (PFC) independently, but the interactions between these factors remain unclear. Here, we compared the effects of stress (elevated platform, EP) and anxiolytics (diazepam, DZP) on extracellular field potentials (EFP) in the PFC, parietal cortex and hippocampus (dorsal and ventral parts) of adult (8 months) and aged (18 months) Wistar rats...
2017: Frontiers in Aging Neuroscience
https://www.readbyqxmd.com/read/29029015/an-experimental-study-comparing-the-respiratory-effects-of-tapentadol-and-oxycodone-in-healthy-volunteers
#5
R van der Schrier, K Jonkman, M van Velzen, E Olofsen, A M Drewes, A Dahan, M Niesters
Background: There is a clinical need for potent opioids that produce little or no respiratory depression. In the current study we compared the respiratory effects of tapentadol, a mu-opioid receptor agonist and noradrenaline reuptake inhibitor, and oxycodone, a selective mu-opioid receptor agonist. We hypothesize that tapentadol 100 mg has a lesser effect on the control of breathing than oxycodone 20 mg. Methods: Fifteen healthy volunteers were randomized to receive oral tapentadol (100 and 150 mg), oxycodone 20 mg or placebo immediate release tablets in a crossover double-blind randomized design...
October 4, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29025923/plasticity-of-signaling-by-spinal-estrogen-receptor-alpha-kappa-opioid-receptor-and-mglurs-over-the-rat-reproductive-cycle-regulates-spinal-endomorphin-2-antinociception-relevance-of-endogenous-biased-agonism
#6
Nai-Jiang Liu, Vijaya Murugaiyan, Emiliya M Storman, Stephen A Schnell, Arjun Kumar, Martin W Wessendorf, Alan R Gintzler
We previously showed that intrathecal application of endomorphin 2 [EM2; the highly specific endogenous mu-opioid receptor (MOR) ligand] induces antinociception that varies with stage of the rat estrous cycle -- minimal during diestrus and prominent during proestrus. Earlier studies, however, did not identify proestrus-activated signaling strategies that enable spinal EM2 antinociception. We now report that in female rats, increased spinal dynorphin release and kappa-opioid receptor (KOR) signaling, as well as the emergence of glutamate-activated mGluR1 signaling, are critical to the transition from an EM2 non-responsive (during diestrus) to an analgesically responsive state (during proestrus)...
October 12, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29017487/curcumin-is-a-promising-inhibitor-of-genotype-2-porcine-reproductive-and-respiratory-syndrome-virus-infection
#7
Taofeng Du, Yunpeng Shi, Shuqi Xiao, Na Li, Qin Zhao, Angke Zhang, Yuchen Nan, Yang Mu, Yani Sun, Chunyan Wu, Hongtao Zhang, En-Min Zhou
BACKGROUND: Porcine reproductive and respiratory syndrome virus (PRRSV) could lead to pandemic diseases and huge financial losses to the swine industry worldwide. Curcumin, a natural compound, has been reported to serve as an entry inhibitor of hepatitis C virus, chikungunya virus and vesicular stomatitis virus. In this study, we investigated the potential effect of curcumin on early stages of PRRSV infection. RESULTS: Curcumin inhibited infection of Marc-145 cells and porcine alveolar macrophages (PAMs) by four different genotype 2 PRRSV strains, but had no effect on the levels of major PRRSV receptor proteins on Marc-145 cells and PAMs or on PRRSV binding to Marc-145 cells...
October 10, 2017: BMC Veterinary Research
https://www.readbyqxmd.com/read/29016850/mice-lacking-cyclin-dependent-kinase-like-5-manifest-autistic-and-adhd-like-behaviors
#8
Cian-Ling Jhang, Tzyy-Nan Huang, Yi-Ping Hsueh, Wenlin Liao
Neurodevelopmental disorders frequently share common clinical features and appear high rate of comorbidity, such as those present in patients with attention-deficit hyperactivity disorder (ADHD) and autism spectrum disorders (ASD). While characterizing behavioral phenotypes in the mouse model of cyclin-dependent kinase-like 5 (CDKL5) disorder, a neurodevelopmental disorder caused by mutations in the X-linked gene encoding CDKL5, we found that these mice manifested behavioral phenotypes mimicking multiple key features of ASD, such as impaired social interaction and communication, as well as increased stereotypic digging behaviors...
October 15, 2017: Human Molecular Genetics
https://www.readbyqxmd.com/read/28992341/a-prospective-study-of-inflammatory-markers-and-risk-of-endometriosis
#9
Fan Mu, Holly R Harris, Janet W Rich-Edwards, Susan E Hankinson, Eric B Rimm, Donna Spiegelman, Stacey A Missmer
A body of evidence suggests a role for inflammation in the pathogenesis of endometriosis. Numerous case-control studies have found that inflammatory markers were elevated in endometriosis cases compared to controls. However, results are not consistent and no prior prospective study exists. We conducted a case-control study study nested within the Nurses' Health Study II examining the associations between plasma levels of interleukin-1 beta (IL-1ß), IL-6, soluble tumor necrosis factor α receptor-1 (sTNFR-1), sTNFR-2, and high-sensitivity C-reactive protein and laparoscopically-confirmed endometriosis risk...
July 13, 2017: American Journal of Epidemiology
https://www.readbyqxmd.com/read/28989282/spotlight-on-eluxadoline-for-the-treatment-of-patients-with-irritable-bowel-syndrome-with-diarrhea
#10
REVIEW
Konstantinos C Fragkos
BACKGROUND: Irritable bowel syndrome with diarrhea (IBS-D) has limited options for treatment currently, including mainly anti-motility medications, antispasmodics, and antidepressants. This review discusses the properties of a new drug, eluxadoline, a gut-targeting mu- and kappa-opioid receptor agonist and a delta-opioid receptor antagonist, and its efficacy and safety in patients with IBS-D. MATERIALS AND METHODS: A systematic review of the literature was undertaken to identify studies that had investigated eluxadoline as a treatment in IBS-D...
2017: Clinical and Experimental Gastroenterology
https://www.readbyqxmd.com/read/28984075/association-of-glucocorticoid-receptor-gene-polymorphisms-with-systemic-lupus-erythematosus-in-a-chinese-population
#11
Yang-Fan Chen, Jian-Hua Xu, Yan-Feng Zou, Li Lian, Fen Wang, Shan-Yu Chen, Jing Cai, Mu Li
OBJECTIVES: To identify the association of glucocorticoid receptor (GR) gene polymorphism with systemic lupus erythematosus (SLE). METHODS: A case-control study was carried out, in which 400 Chinese patients with SLE and 400 normal people were enrolled. DNA was extracted using a genomic DNA extraction kit, and tagged single nucleotide polymorphisms (SNPs) were identified by Haploview (4.0) Project from the Chinese HapMap Project. Eighteen tagged SNPs of the GR gene were genotyped by the Multiplex SNaPshot technique...
October 6, 2017: International Journal of Rheumatic Diseases
https://www.readbyqxmd.com/read/28970780/mulberry-branch-bark-powder-significantly-improves-hyperglycemia-and-regulates-insulin-secretion-in-type-ii-diabetic-mice
#12
Xiao-Lu Yin, Hua-Yu Liu, Yu-Qing Zhang
This experiment, based on the previous study on R. mori, introduces whole mulberry branch powder into the diet to treat diabetic mice. Mulberry branch bark powder (MBBP) was administered orally to streptozotocin (STZ)-induced type II diabetic (T2D) mice to investigate hypoglycemic effects. After a 4-week period of diet consumption containing 5%, 10% and 20% MBBP, the fasting blood glucose, body weight and the related western blotting were measured, pathologic and immunohistochemical were observed. The 20% MBBP group showed a significant reduction in hyperglycemia and hyperinsulinemia; fasting blood glucose and insulin decreased from 25...
2017: Food & Nutrition Research
https://www.readbyqxmd.com/read/28967123/antidepressant-like-effects-of-bu10119-a-novel-buprenorphine-analogue-with-mixed-kappa-mu-opioid-receptor-antagonist-properties-in-mice
#13
Abdulrahman Almatroudi, Mehrnoosh Ostovar, Christopher P Bailey, Stephen M Husbands, Sarah J Bailey
BACKGROUND AND PURPOSE: Κ-opioid receptor antagonists have potential for treating neuropsychiatric disorders. We have investigated the in vivo pharmacology of a novel buprenorphine analogue, BU10119, for the first time. EXPERIMENTAL APPROACH: To determine the opioid pharmacology of BU10119 (0.3-3 mg/kg, i.p.) in vivo, the warm-water tail withdrawal assay was used in adult male CD1 mice. A range of behavioural paradigms was used to investigate the locomotor effects, rewarding properties and antidepressant or anxiolytic potential of BU10119...
October 1, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28957799/epigallocatechin-3-gallate-inhibits-matrix-metalloproteinase-9-and-monocyte-chemotactic-protein-1-expression-through-the-67-%C3%AE%C2%BAda-laminin-receptor-and-the-tlr4-mapk-nf-%C3%AE%C2%BAb-signalling-pathway-in-lipopolysaccharide-induced-macrophages
#14
Ya-Fei Li, Hao Wang, Yi Fan, Hao-Jie Shi, Qi-Ming Wang, Bing-Rui Chen, Mohammad Reeaze Khurwolah, Qing-Qing Long, Si-Bo Wang, Ze-Mu Wang, Lian-Sheng Wang
BACKGROUND/AIMS: Epigallocatechin-3-gallate (EGCG), a major catechin found in green tea, has been shown to prevent cardiovascular diseases. Previously, Matrix metalloproteinase-9 (MMP-9), monocyte chemotactic protein-1 (MCP-1) and toll-like receptor 4 (TLR4) were confirmed to play an important role in atherosclerosis and plaque instability. Both TLR4 and its negative regulator, Toll-interacting protein (Tollip), could be mediated by EGCG. The present study aimed to examine the effect of physiological concentration of EGCG (1 µM) on the expression of MMP-9 and MCP-1 in lipopolysaccharide (LPS)-induced macrophages and the potential mechanisms underlying its actions...
September 29, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28947917/roux-en-y-gastric-bypass-surgery-suppresses-hypothalamic-ptp1b-protein-level-and-alleviates-leptin-resistance-in-obese-rats
#15
Jia-Yu Liu, Song Mu, Shu-Ping Zhang, Wei Guo, Qi-Fu Li, Xiao-Qiu Xiao, Jun Zhang, Zhi-Hong Wang
The present study aimed to explore the effect of Roux-en-Y gastric bypass (RYGB) surgery on protein tyrosine phosphatase 1B (PTP1B) expression levels and leptin activity in hypothalami of obese rats. Obese rats induced by a high-fat diet (HFD) that underwent RYGB (n=11) or sham operation (SO, n=9), as well as an obese control cohort (Obese, n=10) and an additional normal-diet group (ND, n=10) were used. Food efficiency was measured at 8 weeks post-operation. Plasma leptin levels were evaluated and hypothalamic protein tyrosine phosphatase 1B (PTP1B) levels and leptin signaling activity were examined at the genetic and protein levels...
September 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28946556/the-mechanism-of-selfheal-extract-in-treating-hyperprolactinemia
#16
Suxian Luan, Xiaomei Xu, Meiling Mu, Liangzhi Sun
OBJECTIVE: Selfheal has been used for many years in hyperprolactinemia induced galactorrhea, menstrual disorders, and dysgenesis with satisfactory curative effect. However, its mechanism is still unclear. This study intended to investigate the effect of selfheal extract on hyperprolactinemia in vivo and in vitro, in order to elucidate its mechanism of anti-hyperprolactinemia. PATIENTS AND METHODS: Hyperprolactinemia rat model was established. High dose (28.8 g/(kg⋅d)), middle dose (14...
September 15, 2017: Cancer Biomarkers: Section A of Disease Markers
https://www.readbyqxmd.com/read/28940943/associations-between-epidermal-growth-factor-receptor-mutations-and-histological-subtypes-of-lung-adenocarcinoma-according-to-the-iaslc-ats-ers-classification-in-chinese-patients
#17
Tengteng Wang, Yi Zhang, Baodong Liu, Mu Hu, Naikang Zhou, Xiuyi Zhi
BACKGROUND: This retrospective study was conducted to investigate the relationship between epidermal growth factor receptor (EGFR) mutation and histological subtypes of lung adenocarcinoma according to the International Association for the Study of Lung Cancer/American Thoracic Society/European Respiratory Society (IASLC/ATS/ERS) classification in Chinese patients. METHODS: Three hundred and seventy six surgically resected lung adenocarcinomas from Chinese PLA General Hospital were included in the study...
September 20, 2017: Thoracic Cancer
https://www.readbyqxmd.com/read/28939528/functional-activities-of-interferon-gamma-in-large-yellow-croaker-larimichthys-crocea
#18
Sisi Yang, Qiuhua Li, Yinnan Mu, Jingqun Ao, Xinhua Chen
Interferon gamma (IFN-γ) is a T helper cell type 1 (Th1) cytokine that plays important roles in almost all phases of immune and inflammatory responses. Although IFN-γ gene in large yellow croaker Larimichthys crocea has been reported, little is known about its bioactivity. In this study, large yellow croaker IFN-γ (LycIFN-γ) gene was found to be constitutively expressed in all tissues tested, with the highest levels in blood and heart. Based on stimulation with polyinosinic-polycytidylic acid [poly (I:C)] or inactivated trivalent bacterial vaccine, LycIFN-γ mRNA was significantly increased in spleen and head kidney tissues...
September 20, 2017: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/28939014/novel-endomorphin-analogs-are-more-potent-and-longer-lasting-analgesics-in-neuropathic-postoperative-inflammatory-and-visceral-pain-relative-to-morphine
#19
Amy K Feehan, Jenny Morgenweck, Xing Zhang, Ariel Amgott-Kwan, James E Zadina
Activation of the mu-opioid receptor provides the gold standard for pain relief, but a majority of opioids used clinically have adverse effects that have contributed to an epidemic of overdose deaths. We recently characterized mu-opioid receptor selective endomorphin (EM) analogs that provide potent antinociception with reduction or absence of a number of side effects of traditionally prescribed opioids including abuse liability, respiratory depression, motor impairment, tolerance, and inflammation [91]. The current study explores the effectiveness of these EM analogs relative to morphine in four major pain models by both intrathecal and intravenous administration in male, Sprague-Dawley rats and male CD-1 mice...
September 19, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28938465/serum-insulin-bioassay-reflects-insulin-sensitivity-and-requirements-in-type-1-diabetes
#20
Joseph A M J L Janssen, Gemma Llauradó, Aimee J Varewijck, Per-Henrik Groop, Carol Forsblom, Sonia Fernández-Veledo, Elisabeth S R van den Dungen, Joan Vendrell, Leo J Hofland, Hannele Yki-Järvinen
Background: Insulin resistance could increase insulin requirements in type 1 diabetes (TD1). Current insulin immunoassays do not detect insulin analogues. Kinase Insulin Receptor Activation (KIRA) bioassays specific for human insulin receptor isoforms A and B (IR-A and IR-B) permit assessment of all circulating insulin bioactivity. We studied whether IR-A and IR-B KIRA assays are related to direct measures of insulin sensitivity or insulin doses in TD1. Methods: We evaluated 31 adult patients with TD1 (age 45...
August 14, 2017: Journal of Clinical Endocrinology and Metabolism
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