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https://www.readbyqxmd.com/read/28506204/antibiotic-effects-of-loperamide-homology-of-human-targets-of-loperamide-with-targets-in-acanthamoeba-spp
#1
Abdul Mannan Baig, Zohaib Rana, M Mohsin Mannan, S Sumayya Tariq, H R Ahmad
BACKGROUND: Loperamide is an anti-diarrheal drug prescribed for non-infectious diarrhea. The drug is an opioid receptor agonist, a blocker of voltage-dependent calcium channel (Cav) and a calmodulin (CaM) inhibitor on human cells. Loperamide has been reported to exert anti-amoebic effects against pathogenic strains of Acanthamoeba castellanii. OBJECTIVES: The precise mode of antibiotic action, cellular target homology with human counterparts and the pattern of cell death induced by loperamide in Acanthamoeba castellanii remain to be established...
April 25, 2017: Recent Patents on Anti-infective Drug Discovery
https://www.readbyqxmd.com/read/28501425/the-effects-of-kratom-on-restraint-stress-induced-analgesia-and-its-mechanisms-of-action
#2
José Luis Vázquez López, Lorenz Schild, Thomas Günther, Stefan Schulz, Hartmud Neurath, Axel Becker
ETHNOPHARMACOLOGICAL RELEVANCE: Mitragyna speciosa and its extracts are called kratom (dried leaves, extract). They contain several alkaloids with an affinity for different opioid receptors. They are used in traditional medicine for the treatment of different diseases, as a substitute by opiate addicts, and to mitigate opioid withdrawal symptoms. Apart from their medical properties, they are used to enhance physical endurance and as a means of overcoming stress. PURPOSE: The aim of this study was to determine the mechanisms underlying the effects of kratom on restraint-stress-induced analgesia which occurs during or following exposure to a stressful or fearful stimulus...
May 10, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28488261/use-of-tramadol-in-psychiatric-care-a-comprehensive-review-and-report-of-two-cases
#3
Ansgar Rougemont-Bücking, Franziska Gamma, Jaak Panksepp
Tramadol is widely prescribed for treating acute and chronic forms of pain. It is a weak mu-receptor opioid agonist and also increases concentrations of serotonin and noradrenaline within the limbic system of the brain. The therapeutic range of tramadol is relatively wide. Compared with other opioid agonists, there is little risk for developing tolerance and for abuse. Recent models of depression emphasise the subjective experience of a depressive mood as being, in part, a psychologically painful state. It is well established that psychological stress due to social separation/loss, disruption or be-trayal of pre-existent significant interpersonal bonds is mediated by the activation of the mammalian PANIC (separation-distress) system...
May 10, 2017: Swiss Medical Weekly
https://www.readbyqxmd.com/read/28484480/single-event-resolution-of-plant-plasma-membrane-protein-endocytosis-by-tirf-microscopy
#4
Alexander Johnson, Grégory Vert
Endocytosis is a key process in the internalization of extracellular materials and plasma membrane proteins, such as receptors and transporters, thereby controlling many aspects of cell signaling and cellular homeostasis. Endocytosis in plants has an essential role not only for basic cellular functions but also for growth and development, nutrient delivery, toxin avoidance, and pathogen defense. The precise mechanisms of endocytosis in plants remain quite elusive. The lack of direct visualization and examination of single events of endocytosis has greatly hampered our ability to precisely monitor the cell surface lifetime and the recruitment profile of proteins driving endocytosis or endocytosed cargos in plants...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28483563/losartan-a-selective-antagonist-of-at1-receptor-attenuates-seawater-inhalation-induced-lung-injury-via-modulating-jak2-stats-and-apoptosis-in-rat
#5
Congcong Li, Liyan Bo, Pengcheng Li, Xi Lu, Wangping Li, Lei Pan, Yani Sun, Deguang Mu, Wei Liu, Faguang Jin
Losartan is a selective antagonist of AngⅠ type (AT1) receptor of Angiotensin Ⅱ (Ang Ⅱ), which is widely used as a clinical medicine for the hypertension. Recent studies have shown that losartan was shown to protect from acute lung injury (ALI). However, the underlying mechanism remains unclear. The aim of this research was to clarify whether Ang Ⅱ participated in the inflammatory response of ALI induced by seawater inhalation, and whether losartan had the protective effects on ALI by blocking the combination of Ang Ⅱ and AT1 receptor...
May 5, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28473894/role-of-%C3%AE-opioid-receptor-in-parafascicular-nucleus-of-thalamus-on-morphine-induced-antinociception-in-a-rat-model-of-acute-trigeminal-pain
#6
Esmaeal Tamaddonfard, Amir Erfanparast
The parafascicular nucleus (PFN) of thalamus, as a supraspinal structure, has an important role in processing of nociceptive information. In addition, μ-opioid receptor contributes to supraspinal modulation of nociception. In the present study, the effects of microinjection of naloxone (a non-specific opioid-receptor antagonist) and naloxonazine (a specific μ-opioid receptor antagonist) were investigated on morphine-induced antinociception in a rat model of acute trigeminal pain. Right and left sides of PFN of thalamus were implanted with two guide cannulas...
2017: Veterinary Research Forum
https://www.readbyqxmd.com/read/28467815/epigenetic-silencing-of-triple-negative-breast-cancer-hallmarks-by-withaferin-a
#7
Katarzyna Szarc Vel Szic, Ken Declerck, René A J Crans, Jolien Diddens, David B Scherf, Clarissa Gerhäuser, Wim Vanden Berghe
Triple negative breast cancer (TNBC) is characterized by poor prognosis and a DNA hypomethylation profile. Withaferin A (WA) is a plant derived steroidal lactone which holds promise as a therapeutic agent for treatment of breast cancer (BC). We determined genome-wide DNA methylation changes in weakly-metastatic and aggressive, metastatic BC cell lines, following 72h treatment to a sub-cytotoxic concentration of WA. In contrast to the DNA demethylating agent 5-aza-2'-deoxycytidine (DAC), WA treatment of MDA-MB-231 cells rather tackles an epigenetic cancer network through gene-specific DNA hypermethylation of tumor promoting genes including ADAM metallopeptidase domain 8 (ADAM8), urokinase-type plasminogen activator (PLAU), tumor necrosis factor (ligand) superfamily, member 12 (TNFSF12), and genes related to detoxification (glutathione S-transferase mu 1, GSTM1), or mitochondrial metabolism (malic enzyme 3, ME3)...
April 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28466423/chronic-pruritus-current-and-emerging-treatment-options
#8
REVIEW
Manuel P Pereira, Sonja Ständer
Chronic pruritus remains a central societal issue because of its high occurrence and the substantial decrease in quality of life it may cause to affected individuals. Not only dermatological conditions, but also systemic, neurological, or psychiatric diseases may lead to chronic pruritus. Additionally, various underlying conditions may coexist or the cause may be unknown. Due to its heterogeneity, the therapeutic approach is complex and remains a challenge for the clinician. Basic measures such as emollients to avoid xerosis and treatment of the underlying disease should be initiated regardless of the duration of the symptom...
June 2017: Drugs
https://www.readbyqxmd.com/read/28465483/crispr-cas9-mediated-apoe-and-ldlr-double-gene-knockout-in-pigs-elevates-serum-ldl-c-and-tc-levels
#9
Lei Huang, Zaidong Hua, Hongwei Xiao, Ying Cheng, Kui Xu, Qian Gao, Ying Xia, Yang Liu, Xue Zhang, Xinming Zheng, Yulian Mu, Kui Li
The traditional method to establish a cardiovascular disease model induced by high fat and high cholesterol diets is time consuming and laborious and may not be appropriate in all circumstances. A suitable pig model to study metabolic disorders and subsequent atherosclerosis is not currently available. For this purpose, we applied the CRISPR/Cas9 system to Bama minipigs, targeting apolipoprotein E (ApoE) and low density lipoprotein receptor (LDLR) gene simultaneously. Six biallelic knockout pigs of these two genes were obtained successfully in a single step...
April 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/28459460/magea1-interacts-with-fbxw7-and-regulates-ubiquitin-ligase-mediated-turnover-of-nicd1-in-breast-and-ovarian-cancer-cells
#10
J Zhao, Y Wang, C Mu, Y Xu, J Sang
Melanoma-associated antigen A1 (MAGEA1) is member of the MAGE gene family that is expressed in male germ line cells and placenta under normal physiological conditions. Although MAGEA1's expression levels have been evaluated as one of the cancer testis (CT) antigens for immunotherapy in melanoma and several other cancers, its functional role and signaling mechanisms are largely unknown. In this study, we examined the functional involvement and signaling mechanisms of MAGEA1 in breast and ovarian cancer cells...
May 1, 2017: Oncogene
https://www.readbyqxmd.com/read/28457972/the-rewarding-effects-of-ethanol-are-modulated-by-binge-eating-of-a-high-fat-diet-during-adolescence
#11
M Carmen Blanco-Gandía, Juan Carlos Ledesma, Auxiliadora Aracil-Fernández, Francisco Navarrete, Sandra Montagud-Romero, Maria A Aguilar, Jorge Manzanares, José Miñarro, Marta Rodríguez-Arias
Binge-eating is considered a specific form of overeating characterized by intermittent and high caloric food intake in a short period of time. Epidemiologic studies support a positive relation between the ingestion of fat and ethanol (EtOH), specifically among adolescent subjects. The aim of this work was to clarify the role of the compulsive, limited and intermittent intake of a high-fat food during adolescence on the rewarding effects of EtOH. After binge-eating for 2 h, three days a week from postnatal day (PND) 29, the reinforcing effects of EtOH were tested with EtOH self-administration (SA), conditioned place preference (CPP) and ethanol locomotor sensitization procedures in young adult mice...
April 27, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28456841/changes-in-gene-expression-and-sensitivity-of-cocaine-reward-produced-by-a-continuous-fat-diet
#12
M Carmen Blanco-Gandía, Auxiliadora Aracil-Fernández, Sandra Montagud-Romero, Maria A Aguilar, Jorge Manzanares, José Miñarro, Marta Rodríguez-Arias
RATIONALE: Preclinical studies report that free access to a high-fat diet (HFD) alters the response to psychostimulants. OBJECTIVES: The aim of the present study was to examine how HFD exposure during adolescence modifies cocaine effects. Gene expression of CB1 and mu-opioid receptors (MOr) in the nucleus accumbens (N Acc) and prefrontal cortex (PFC) and ghrelin receptor (GHSR) in the ventral tegmental area (VTA) were assessed. METHODS: Mice were allowed continuous access to fat from PND 29, and the locomotor (10 mg/kg) and reinforcing effects of cocaine (1 and 6 mg/kg) on conditioned place preference (CPP) were evaluated on PND 69...
April 29, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28456745/oprm1-methylation-contributes-to-opioid-tolerance-in-cancer-patients
#13
Chi T Viet, Dongmin Dang, Bradley E Aouizerat, Christine Miaskowski, Yi Ye, Dan T Viet, Kentaro Ono, Brian L Schmidt
Cancer patients in pain require high doses of opioids and quickly become opioid-tolerant. Previous studies have shown that both chronic cancer pain and high dose opioid use lead to mu-opioid receptor down-regulation. In this study we explore down-regulation of OPRM1, the mu-opioid receptor gene, as a mechanism f,or opioid tolerance in the setting of opioid use for cancer pain. We demonstrate in a cohort of 84 cancer patients that high dose opioid use correlates with OPRM1 hypermethylation in peripheral leukocytes of these patients...
April 26, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28455226/the-effect-of-selective-opioid-receptor-agonists-and-antagonists-on-epileptiform-activity-in-morphine-dependent-infant-mice-hippocampal-slices
#14
Yousef Panahi, Ehsan Saboory, Ali Rassouli, Goudarz Sadeghi-Hashjin, Shiva Roshan-Milani, Leila Derafshpour, Yousef Rasmi
Hippocampal slices of mouse brain were used to estimate how selective agonist and antagonist of opioid receptors alter Low-Mg(+2) artificial cerebrospinal fluid (LM-ACSF)-induced epileptiform activities in normal and morphine-dependent mice. Brain slices were obtained from control and morphine-dependent mice. The morphine-dependent group received morphine once a day for 5 consecutive days, and the control group received saline. All injections were administered subcutaneously (s.c) in a volume of 0.1mL on postnatal days 14-18...
April 25, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28454303/expression-of-er%C3%AE-gene-in-breast-carcinoma-and-the-relevance-in-neoadjuvant-therapy
#15
Jing Chang, Jihong Liu, Huiying Li, Jing Li, Yanling Mu, Bin Feng
In the present study, we examined the expression of the estrogen receptor β (ERβ) gene in breast cancer and its relevance in neoadjuvant therapy. In total, 120 breast cancer patients who were hospitalized in the Departments of Breast Disease and Medical Oncology served as the subjects of this study. The subjects were diagnosed with breast cancer phase II to phase IIIA, as confirmed by aspiration biopsy and iconography. The patients were divided into two groups in a randomized control manner, with 60 patients in each group...
March 2017: Oncology Letters
https://www.readbyqxmd.com/read/28454238/dopamine-receptor-d2-is-correlated-with-gastric-cancer-prognosis
#16
Jiasheng Mu, Weidan Huang, Zhujun Tan, Maolan Li, Lin Zhang, Qichen Ding, Xiangsong Wu, Jianhua Lu, Yingbin Liu, Qian Dong, Haineng Xu
It has been reported previously that a dopamine receptor D2 (DRD2) antagonist was able to induce cancer cell apoptosis and that DRD2 was expressed at high levels in pituitary adenomas. However, the expression of DRD2 in gastric cancer and its correlation with the prognosis of patients with gastric cancer remain to be elucidated. In the present study, the expression of DRD2 in 84 paired gastric cancer tissues and respective adjacent non-cancerous tissues were detected using an immunohistochemical assay. The correlation between the expression of DRD2 and the with survival durations of the patients with gastric cancer was analyzed using Kaplan-Meier analysis...
March 2017: Oncology Letters
https://www.readbyqxmd.com/read/28454099/homoharringtonine-targets-smad3-and-tgf-%C3%AE-pathway-to-inhibit-the-proliferation-of-acute-myeloid-leukemia-cells
#17
Jian Chen, Qitian Mu, Xia Li, Xiufeng Yin, Mengxia Yu, Jing Jin, Chenying Li, Yile Zhou, Jiani Zhou, Shanshan Suo, Demin Lu, Jie Jin
Homoharringtonine (HHT) has long and widely been used in China for the treatment of acute myeloid leukemia (AML), the clinical therapeutic effect is significant but the working mechanism is poorly understood. The purpose of this study is to screen the possible target for HHT with virtual screening and verify the findings by cell experiments. Software including Autodock, Python, and MGL tools were used, with HHT being the ligand and proteins from PI3K-Akt pathway, Jak-stat pathway, TGF-β pathway and NK-κB pathway as the receptors...
April 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28450396/heat-shock-protein-90-hsp90-promotes-opioid-induced-anti-nociception-by-an-erk-mitogen-activated-protein-kinase-mapk-mechanism-in-mouse-brain
#18
Wei Lei, Nathan Mullen, Sarah McCarthy, Courtney Brann, Philomena Richard, James Cormier, Katie Edwards, Edward J Bilsky, John M Streicher
Recent advances in developing opioid treatments for pain with reduced side effects have focused on the signaling cascades of the mu opioid receptor (MOR). However, few such signaling targets have been identified for exploitation. To address this need, we explored the role of Heat shock protein 90 (Hsp90) in opioid-induced MOR signaling and pain, which has only been studied in 4 previous papers. First, in 4 cell models of MOR signaling, we found that Hsp90 inhibition for 24 hours with the inhibitor 17-N-allylamino-17-demethoxygeldanamycin (17-AAG) had different effects on protein expression and opioid signaling in each line, suggesting that cell models may not be reliable for predicting pharmacology with this protein...
April 27, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28450111/molecular-characterization-of-an-atpyl1-like-protein-brpyl1-as-a-putative-aba-receptor-in-brassica-rapa
#19
Yanlin Li, Dandan Wang, Congcong Sun, Xiaochen Hu, Xiaoqian Mu, Jingjiang Hu, Yongqing Yang, Yanfeng Zhang, Chang Gen Xie, Xiaona Zhou
Abscisic acid (ABA)-induced physiological changes are conserved in many land plants and underlie their responses to environmental stress and pathogens. The PYRABACTIN RESISTANCE1/PYR1-LIKE/REGULATORY COMPONENTS OF ABA RECEPTORS (PYLs)-type receptors perceive the ABA signal and initiate signal transduction. Here, we show that the genome of Brassica rapa encodes 24 putative AtPYL-like proteins. The AtPYL-like proteins in Brassica rapa (BrPYLs) can also be classified into 3 subclasses. We found that nearly all BrPYLs displayed high expression in at least one tissue...
April 24, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28446883/in-vitro-and-in-vivo-profile-of-ppl-101-and-ppl-103-mixed-opioid-partial-agonist-analgesics-with-low-abuse-potential
#20
Taline V Khroyan, Andrea Cippitelli, Nicholas Toll, John A Lawson, William Crossman, Willma E Polgar, Lawrence Toll
Opiates are still the most effective and widely used treatments for acute and chronic pain. However, the problems associated with morphine and other standard opioid analgesics severely limit their effectiveness in the clinic. PPL-101 and PPL-103 derived from morphine and morphinan ring systems contain a chiral N-substituent, which confers it with a unique combination of high-binding affinities and partial agonist activities at mu, delta, and kappa opioid receptors, leading to unique in vivo pharmacology compared to other conventional opioids...
2017: Frontiers in Psychiatry
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