keyword
MENU ▼
Read by QxMD icon Read
search

Mu receptor

keyword
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
#1
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/29221201/functional-fgfr4-gly388arg-polymorphism-contributes-to-oral-squamous-cell-carcinoma-susceptibility
#2
Chia-Hsuan Chou, Ming-Ju Hsieh, Chun-Yi Chuang, Jen-Tsun Lin, Chia-Ming Yeh, Pao-Yu Tseng, Shun-Fa Yang, Mu-Kuan Chen, Chiao-Wen Lin
Aberrations of the fibroblast growth factor receptor 4 (FGFR4) genomic region include amplification of FGFR4, activation of FGFR4 kinase domain mutations, and overexpression of FGFR4, which lead to sustained cell proliferation and contribute to tumor development. However, the association between FGFR4 single-nucleotide polymorphisms (SNPs) and risk of oral squamous cell carcinoma (OSCC) remains to be determined. We investigated the relationships between FGFR4 genetic polymorphisms, OSCC development and clinicopathological variables...
November 10, 2017: Oncotarget
https://www.readbyqxmd.com/read/29220536/cd36-deficiency-attenuates-immune-mediated-hepatitis-in-mice-by-modulating-the-proapoptotic-effects-of-cxcl10
#3
Che Xu, Chen Zhang, Jie Ji, Chao Wang, Jing Yang, Biao Geng, Ting Zhao, Hong Zhou, Xianmin Mu, Jinshun Pan, Shi Hu, Yuanfang Lv, Xingguo Chen, Hao Wen, Qiang You
The scavenger receptor, CD36, recognizes a diverse set of ligands, and has been implicated in a wide variety of normal and pathological processes, including lipid metabolism, angiogenesis, atherosclerosis, and phagocytosis. In particular, recent findings have demonstrated its crucial functions in sterile inflammation and tumor metastasis. However, the role of CD36 in immune-mediated hepatitis remains unclear. Concanavalin A (Con A)-induced liver injury is a well-established experimental T cell-mediated hepatitis...
December 8, 2017: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
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
#4
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/29210823/peripherally-acting-mu-opioid-receptor-antagonists
#5
(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
#6
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/29209331/sialic-acids-in-the-immune-response-during-sepsis
#7
REVIEW
Yan-Cun Liu, Mu-Ming Yu, Yan-Fen Chai, Song-Tao Shou
Sialic acid-binding immunoglobulin-type lectins (Siglecs) are a group of cell surface transmembrane receptors expressed on immune cells, and regulate immune balance in inflammatory diseases. Sepsis is a life-threatened inflammatory syndrome induced by infection, and the pathogenesis of sepsis includes immune dysregulation, inflammation, and coagulation disorder. Here, we reviewed the various roles acted by Siglecs family in the pathogenesis of sepsis. Siglec-1, Siglec-5, and Siglec-14 play bidirectional roles through modulation of inflammation and immunity...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/29207922/effect-of-steady-state-methadone-on-high-fructose-corn-syrup-consumption-in-rats
#8
Stephen Daniels, Mick Pratt, Yan Zhou, Francesco Leri
Patients undergoing methadone maintenance treatment self-report enhanced preferences for, and excessive consumption of, foods rich in sugar. However, it is unclear whether these are direct pharmacological effects of methadone or the consequences of metabolic dysfunctions induced by addiction to illicit opiates. Hence, the current study in drug-naïve male Sprague-Dawley rats explored the effects of steady-state methadone delivered by osmotic mini-pumps (13 days; 0, 10, 30 mg/kg/day) on consumption of rat chow and a palatable, sweet, liquid high fructose corn syrup solution...
December 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/29207108/integrated-analysis-of-gene-expression-and-copy-number-variations-in-met-proto%C3%A2-oncogene%C3%A2-transformed-human-primary-osteoblasts
#9
Ru-Jiang Jia, Chun-Gen Lan, Xiu-Chao Wang, Chun-Tao Gao
The aim of the present study was to screen the potential osteosarcoma (OS)‑associated genes and to obtain additional insight into the pathogenesis of OS. Transcriptional profile (ID: GSE28256) and copy number variations (CNV) profile were downloaded from Gene Expression Omnibus database. Differentially expressed genes (DEGs) between MET proto‑oncogene‑transformed human primary osteoblast (MET‑HOB) samples and the control samples were identified using the Linear Models for Microarray Data package. Subsequently, CNV areas and CNVs were identified using cut‑off criterion of >30%‑overlap within the cases using detect_cnv...
November 22, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29203627/favorable-vascular-actions-of-angiotensin-1-7-in-human-obesity
#10
Francesca Schinzari, Manfredi Tesauro, Augusto Veneziani, Nadia Mores, Nicola Di Daniele, Carmine Cardillo
Obese patients have vascular dysfunction related to impaired insulin-stimulated vasodilation and increased endothelin-1-mediated vasoconstriction. In contrast to the harmful vascular actions of angiotensin (Ang) II, the angiotensin-converting enzyme 2 product Ang-(1-7) has shown to exert cardiovascular and metabolic benefits in experimental models through stimulation of the Mas receptor. We, therefore, examined the effects of exogenous Ang-(1-7) on vasodilator tone and endothelin-1-dependent vasoconstriction in obese patients...
December 4, 2017: Hypertension
https://www.readbyqxmd.com/read/29199341/-expression-of-receptor-activator-of-nuclear-factor-%C3%AE%C2%BAb-ligand-in-keratocystic-odontogenic-tumor-before-and-after-decompression
#11
Bo Zhang, Wen-Cheng Ye, Ying Li, Xin-Mu Zhou, Yi-Ling Zhu
PURPOSE: To investigate the expression of receptor activator of nuclear factor-κB ligand (RANKL) in keratocystic odontogenic tumor (KCOT) before and after decompression. METHODS: Twenty two pairs of paraffin-embeded tissue specimens of KCOT were collected and subjected to immunohistochemical analysis of RANKL.The data were analyzed with SPSS17.0 software package for paired t test. RESULTS: RANKL positive cells were observed in the preoperative KCOT epithelium...
August 2017: Shanghai Kou Qiang Yi Xue, Shanghai Journal of Stomatology
https://www.readbyqxmd.com/read/29197517/dpi-289-a-novel-mixed-delta-opioid-agonist-mu-opioid-antagonist-dama-has-l-dopa-sparing-potential-in-parkinson-s-disease
#12
Tom H Johnston, Eboo Versi, Patrick A Howson, Paula Ravenscroft, Susan H Fox, Michael P Hill, Bruce E Reidenberg, Ronald Corey, Jonathan M Brotchie
L-DOPA-induced dyskinesia (LID) remains a significant problem in the management of Parkinson's disease (PD). In rodent and macaque models of PD, delta opioid receptor agonists have anti-parkinsonian actions while mu opioid antagonists can reduce the expression of LID. DPI-289 is a novel molecule with a unique combination of opioid receptor DAMA actions: delta agonist (Ki: 0.73 nM); mu antagonist (Ki: 12 nM). We demonstrated that DPI-289 has oral bioavailability and established its pharmacokinetic profile in both rat and primate...
November 29, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29196181/cyclopeptide-dmt-d-lys-p-cf3-phe-phe-asp-nh2-a-novel-g-protein-biased-agonist-of-the-mu-opioid-receptor
#13
Justyna Piekielna-Ciesielska, Federica Ferrari, Girolamo Calo', Anna Janecka
Opioid peptides and alkaloid drugs such as morphine, mediate their analgesic effects, but also undesired side effects, mostly through activation of the mu opioid receptor which belongs to the G protein-coupled receptor (GPCR) family. A new important pharmacological concept in the field of GPCRs is biased agonism. Two mu receptor ligands, Dmt-c[D-Lys-Phe-Phe-Asp]NH2 (C-36) and Dmt-c[D-Lys-Phe-p-CF3-Phe-Asp]NH2 (F-81), were evaluated in terms of their ability to promote or block mu receptor/G protein and mu receptor/β-arrestin interactions...
November 28, 2017: Peptides
https://www.readbyqxmd.com/read/29194445/safety-and-efficacy-of-an-oxycodone-vaccine-addressing-some-of-the-unique-considerations-posed-by-opioid-abuse
#14
M D Raleigh, S J Peterson, M Laudenbach, F Baruffaldi, F I Carroll, S D Comer, H A Navarro, T L Langston, S P Runyon, S Winston, M Pravetoni, P R Pentel
Among vaccines aimed at treating substance use disorders, those targeting opioids present several unique medication development challenges. 1) Opioid overdose is a common complication of abuse, so it is desirable for an opioid vaccine to block the toxic as well as the addictive effects of opioids. 2) It is important that an opioid vaccine not interfere with the action of opioid antagonists used to reverse opioid overdose or treat addiction. 3) Some opioids are immunosuppressive and chronic ongoing opioid use could interfere with vaccine immunogenicity...
2017: PloS One
https://www.readbyqxmd.com/read/29191857/evaluation-of-11c-me-nb1-as-a-potential-pet-radioligand-for-measuring-glun2b-containing-nmda-receptors-drug-occupancy-and-receptor-crosstalk
#15
Stefanie D Krämer, Thomas Betzel, Linjing Mu, Ahmed Haider, Adrienne Herde Müller, Anna K Boninsegni, Claudia Keller, Marina Szermerski, Roger Schibli, Bernhard Wünsch, Simon M Ametamey
Clinical and preclinical research with modulators binding to the NMDA receptor GluN2B N-terminal domain (NTD) aim for the treatment of various neurological diseases. However, the interpretation of the results is hampered by the lack of a suitable NMDA PET tracer for assessing the receptor occupancy of candidate drugs. We have developed [11C]Me-NB1 as a PET tracer for imaging GluN1/GluN2B-containing NMDA receptors and used it to investigate in rats the dose-dependent receptor occupancy of eliprodil, a GluN2B NTD modulator...
November 30, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/29183835/antinociceptive-effects-of-mixtures-of-mu-opioid-receptor-agonists-and-cannabinoid-receptor-agonists-in-rats-impact-of-drug-and-fixed-dose-ratio
#16
David R Maguire, Charles P France
Pain is a significant clinical problem, and there is a need for effective pharmacotherapies with fewer adverse effects than currently available drugs (e.g., mu opioid receptor agonists). Cannabinoid receptor agonists enhance the antinociceptive effects of mu opioid receptor agonists, but it remains unclear which drugs and in what proportion will yield the most effective and safest treatments. The antinociceptive effects of the mu opioid receptor agonists etorphine and morphine alone and in combination with the cannabinoid receptor agonists Δ9-THC and CP55940 were studied in male Sprague-Dawley rats (n=16) using a warm water tail withdrawal procedure...
November 25, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29180970/cebranopadol-a-mixed-opioid-agonist-reduces-cocaine-self-administration-through-nociceptin-opioid-and-mu-opioid-receptors
#17
Qianwei Shen, Yulin Deng, Roberto Ciccocioppo, Nazzareno Cannella
Cocaine addiction is a widespread psychiatric condition still waiting for approved efficacious medications. Previous studies suggested that simultaneous activation of nociceptin opioid (NOP) and mu opioid (MOP) receptors could be a successful strategy to treat cocaine addiction, but the paucity of molecules co-activating both receptors with comparable potency has hampered this line of research. Cebranopadol is a non-selective opioid agonist that at nanomolar concentration activates both NOP and MOP receptors and that recently reached phase-III clinical trials for cancer pain treatment...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/29178253/kefir-peptides-prevent-hyperlipidemia-and-obesity-in-high-fat-diet-induced-obese-rats-via-lipid-metabolism-modulation
#18
Yu-Tang Tung, Hsiao-Ling Chen, Hsin-Shan Wu, Mei-Hsuan Ho, Kowit-Yu Chong, Chuan-Mu Chen
SCOPE: Obesity has reached epidemic proportions worldwide. Obesity is a complex metabolic disorder that is linked to numerous serious health complications with high morbidity. The present study evaluated the effects of kefir peptides on high fat diet-induced obesity in rats. METHODS AND RESULTS: Kefir peptides markedly improved obesity, including body weight gain, inflammatory reactions and the formation of adipose tissue fat deposits around the epididymis and kidney, and adipocyte size...
November 24, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/29177707/a-first-in-man-pet-study-of-18f-pss232-a-fluorinated-abp688-derivative-for-imaging-metabotropic-glutamate-receptor-subtype-5
#19
Geoffrey Warnock, Michael Sommerauer, Linjing Mu, Gloria Pla Gonzalez, Susanne Geistlich, Valerie Treyer, Roger Schibli, Alfred Buck, Stefanie D Krämer, Simon M Ametamey
PURPOSE: Non-invasive imaging of metabotropic glutamate receptor 5 (mGlu5) in the brain using PET is of interest in e.g., anxiety, depression, and Parkinson's disease. Widespread application of the most widely used mGlu5 tracer, [11C]ABP688, is limited by the short physical half-life of carbon-11. [18F]PSS232 is a fluorinated analog with promising preclinical properties and high selectivity and specificity for mGlu5. In this first-in-man study, we evaluated the brain uptake pattern and kinetics of [18F]PSS232 in healthy volunteers...
November 27, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/29170626/role-of-microrna-143-in-nerve-injury-induced-upregulation-of-dnmt3a-expression-in-primary-sensory-neurons
#20
Bo Xu, Jing Cao, Jun Zhang, Shushan Jia, Shaogen Wu, Kai Mo, Guihua Wei, Lingli Liang, Xuerong Miao, Alex Bekker, Yuan-Xiang Tao
Peripheral nerve injury increased the expression of the DNA methyltransferase 3A (Dnmt3a) mRNA and its encoding Dnmt3a protein in injured dorsal root ganglia (DRG). This increase is considered as an endogenous instigator in neuropathic pain genesis through epigenetic silencing of pain-associated genes (such as Oprm1) in injured DRG. However, how DRG DNMT3a is increased following peripheral nerve injury is still elusive. We reported here that peripheral nerve injury caused by the fifth spinal nerve ligation (SNL) downregulated microRNA (miR)-143 expression in injured DRG...
2017: Frontiers in Molecular Neuroscience
keyword
keyword
19461
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"