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https://www.readbyqxmd.com/read/28097916/exploring-the-first-rimonabant-analog-opioid-peptide-hybrid-compound-as-bivalent-ligand-for-cb1-and-opioid-receptors
#1
Adriano Mollica, Sveva Pelliccia, Valeria Famiglini, Azzurra Stefanucci, Giorgia Macedonio, Annalisa Chiavaroli, Giustino Orlando, Luigi Brunetti, Claudio Ferrante, Stefano Pieretti, Ettore Novellino, Sandor Benyhe, Ferenc Zador, Anna Erdei, Edina Szucs, Reza Samavati, Szalbolch Dvrorasko, Csaba Tomboly, Rino Ragno, Alexandros Patsilinakos, Romano Silvestri
Cannabinoid (CB) and opioid systems are both involved in analgesia, food intake, mood and behavior. Due to the co-localization of µ-opioid (MOR) and CB1 receptors in various regions of the central nervous system (CNS) and their ability to form heterodimers, bivalent ligands targeting to both these systems may be good candidates to investigate the existence of possible cross-talking or synergistic effects, also at sub-effective doses. In this work, we selected from a small series of new Rimonabant analogs one CB1R reverse agonist to be conjugated to the opioid fragment Tyr-D-Ala-Gly-Phe-NH2...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28093716/syphilitic-chancre-and-condylomata-lata-possibly-coexisting-with-neurosyphilis
#2
Yoav C Metzger, Mor Miodovnik, Shmuel Epshteyn
No abstract text is available yet for this article.
January 17, 2017: International Journal of Dermatology
https://www.readbyqxmd.com/read/28093054/impact-of-psychological-stress-on-pain-perception-in-an-animal-model-of-endometriosis
#3
Siomara Hernandez, Myrella L Cruz, Inevy I Seguinot, Annelyn Torres-Reveron, Caroline B Appleyard
PURPOSE: Pain in patients with endometriosis is considered a significant source of stress but does not always correlate with severity of the condition. We have demonstrated that stress can worsen endometriosis in an animal model. Here, we tested the impact of a psychological stress protocol on pain thresholds and pain receptors. METHODS: Endometriosis was induced in female rats by suturing uterine horn tissue next to the intestinal mesentery. Sham rats had sutures only...
January 1, 2017: Reproductive Sciences
https://www.readbyqxmd.com/read/28092666/loss-of-%C3%AE-opioid-receptor-signaling-in-nociceptors-but-not-microglia-abrogates-morphine-tolerance-without-disrupting-analgesia
#4
Gregory Corder, Vivianne L Tawfik, Dong Wang, Elizabeth I Sypek, Sarah A Low, Jasmine R Dickinson, Chaudy Sotoudeh, J David Clark, Ben A Barres, Christopher J Bohlen, Grégory Scherrer
Opioid pain medications have detrimental side effects including analgesic tolerance and opioid-induced hyperalgesia (OIH). Tolerance and OIH counteract opioid analgesia and drive dose escalation. The cell types and receptors on which opioids act to initiate these maladaptive processes remain disputed, which has prevented the development of therapies to maximize and sustain opioid analgesic efficacy. We found that μ opioid receptors (MORs) expressed by primary afferent nociceptors initiate tolerance and OIH development...
January 16, 2017: Nature Medicine
https://www.readbyqxmd.com/read/28081042/detection-of-hydrocodone-and-morphine-as-metabolites-in-oral-fluid-by-lc-ms-ms-in-patients-prescribed-codeine
#5
Robert E West, Maria G Guevara, Charles Mikel, Ruben Gamez
A retrospective analysis of oral fluid drug testing results using LC-MS/MS was performed to determine the prevalence rates in oral fluid for codeine (COD) and 3 COD metabolites-morphine (MOR), norhydrocodone (NHC), and hydrocodone (HCOD). Oral fluid samples were collected using Quantisal oral fluid collection device (Immunalysis Inc.) and submitted to Millennium Health, LLC for the routine drug analysis by LC-MS/MS. Consistent with previously published literature, COD was the primary analyte detected in oral fluid after the use of COD...
February 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/28080056/metadynamics-simulations-distinguish-short-and-long-residence-time-inhibitors-of-cyclin-dependent-kinase-8
#6
Donatella Callegari, Alessio Lodola, Daniele Pala, Silvia Rivara, Marco Mor, Andrea Rizzi, Anna Maria Capelli
The duration of drug efficacy in vivo is a key aspect primarily addressed during the lead optimization phase of drug discovery. Hence, the availability of robust computational approaches that can predict the residence time of a compound at its target would accelerate candidate selection. Nowadays the theoretical prediction of this parameter is still very challenging. Starting from methods reported in the literature, we set up and validated a new metadynamics (META-D)-based protocol that was used to rank the experimental residence times of 10 arylpyrazole cyclin-dependent kinase 8 (CDK8) inhibitors for which target-bound X-ray structures are available...
January 12, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28078797/in-situ-incubation-of-iron-sulfur-mineral-reveals-a-diverse-chemolithoautotrophic-community-and-a-new-biogeochemical-role-for-thiomicrospira
#7
Roman A Barco, Colleen L Hoffman, Gustavo A Ramírez, Brandy M Toner, Katrina J Edwards, Jason B Sylvan
Sulfide mineral precipitation occurs at mid-ocean ridge (MOR) spreading centers, both in the form of plume particles and seafloor massive sulfide structures. A common constituent of MOR is the iron-bearing sulfide mineral pyrrhotite, which was chosen as a substrate for in-situ incubation studies in shallow waters of Catalina Island, CA to investigate the colonization of iron-oxidizing bacteria. Microbial community datasets were obtained from in-situ incubated pyrrhotite, allowing for direct comparison to microbial communities of iron-sulfides from active and inactive chimneys in deep-sea environments...
January 12, 2017: Environmental Microbiology
https://www.readbyqxmd.com/read/28077930/before-the-freeze-otoliths-from-the-eocene-of-seymour-island-antarctica-reveal-dominance-of-gadiform-fishes-teleostei
#8
Werner Schwarzhans, Thomas Mörs, Andrea Engelbrecht, Marcelo Reguero, Jürgen Kriwet
The first record of fossil teleostean otoliths from Antarctica is reported. The fossils were obtained from late Early Eocene shell beds of the La Meseta Formation, Seymour Island that represent the last temperate marine climate phase in Antarctica prior to the onset of cooling and subsequent glaciation during the late Eocene. A total of 17 otolith-based teleost taxa are recognized, with 10 being identifiable to species level containing nine new species and one new genus: Argentina antarctica sp. nov., Diaphus? marambionis sp...
2017: Journal of Systematic Palaeontology
https://www.readbyqxmd.com/read/28074831/rgs9-2-modulates-responses-to-oxycodone-in-pain-free-and-chronic-pain-states
#9
Sevasti Gaspari, Valeria Cogliani, Lefteris Manouras, Ethan M Anderson, Vasiliki Mitsi, Kleopatra Avrampou, Fiona B Carr, Venetia Zachariou
Regulator of G protein signalling 9-2 (RGS9-2) is a striatal enriched signal transduction modulator, known to play a critical role in the development of addiction-related behaviours following exposure to psychostimulants or opioids. RGS9-2 controls the function of several GPCRs, including dopamine and mu opioid (MOR) receptors. We previously showed that RGS9-2 complexes negatively control morphine analgesia, and promote the development of morphine tolerance. In contrast, RGS9-2 positively modulates the actions of other opioid analgesics, such as fentanyl and methadone...
January 11, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28073998/recent-health-care-use-and-medicaid-entry-of-medicare-beneficiaries
#10
Laura M Keohane, Amal N Trivedi, Vincent Mor
PURPOSE OF THE STUDY: To examine the relationship between Medicaid entry and recent health care use among Medicare beneficiaries. DESIGN AND METHODS: We identified Medicare beneficiaries without full Medicaid or use of hospital or nursing home services in 2008 (N = 2,163,387). A discrete survival analysis estimated beneficiaries' monthly likelihood of entry into the full Medicaid program between January 2009 and June 2010. RESULTS: During the 18-month study period, Medicaid entry occurred for 1...
January 9, 2017: Gerontologist
https://www.readbyqxmd.com/read/28071683/a-comparative-analysis-of-three-vector-borne-diseases-across-australia-using-seasonal-and-meteorological-models
#11
Margaret D Stratton, Hanna Y Ehrlich, Siobhan M Mor, Elena N Naumova
Ross River virus (RRV), Barmah Forest virus (BFV), and dengue are three common mosquito-borne diseases in Australia that display notable seasonal patterns. Although all three diseases have been modeled on localized scales, no previous study has used harmonic models to compare seasonality of mosquito-borne diseases on a continent-wide scale. We fit Poisson harmonic regression models to surveillance data on RRV, BFV, and dengue (from 1993, 1995 and 1991, respectively, through 2015) incorporating seasonal, trend, and climate (temperature and rainfall) parameters...
January 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28069848/aco-affiliated-hospitals-reduced-rehospitalizations-from-skilled-nursing-facilities-faster-than-other-hospitals
#12
Ulrika Winblad, Vincent Mor, John P McHugh, Momotazur Rahman
Medicare's more than 420 accountable care organizations (ACOs) provide care for a considerable percentage of the elderly in the United States. One goal of ACOs is to improve care coordination and thereby decrease rates of rehospitalization. We examined whether ACO-affiliated hospitals were more effective than other hospitals in reducing rehospitalizations from skilled nursing facilities. We found a general reduction in rehospitalizations from 2007 to 2013, which suggests that all hospitals made efforts to reduce rehospitalizations...
January 1, 2017: Health Affairs
https://www.readbyqxmd.com/read/28068789/pragmatic-trial-of-video-education-in-nursing-homes-the-design-and-rationale-for-a-pragmatic-cluster-randomized-trial-in-the-nursing-home-setting
#13
Vincent Mor, Angelo E Volandes, Roee Gutman, Constantine Gatsonis, Susan L Mitchell
Background/Aims Nursing homes are complex healthcare systems serving an increasingly sick population. Nursing homes must engage patients in advance care planning, but do so inconsistently. Video decision support tools improved advance care planning in small randomized controlled trials. Pragmatic trials are increasingly employed in health services research, although not commonly in the nursing home setting to which they are well-suited. This report presents the design and rationale for a pragmatic cluster randomized controlled trial that evaluated the "real world" application of an Advance Care Planning Video Program in two large US nursing home healthcare systems...
January 1, 2017: Clinical Trials: Journal of the Society for Clinical Trials
https://www.readbyqxmd.com/read/28067632/hcv-genotype-1-subtypes-and-resistance-associated-substitutions-in-drug-naive-and-in-direct-acting-antiviral-treatment-failure-patients
#14
Yael Gozlan, Ziv Ben-Ari, Roy Moscona, Rachel Shirazi, Avia Rakovsky, Arij Kabat, Ella Veizman, Tania Berdichevski, Peretz Weiss, Oranit Cohen-Ezra, Yoav Lurie, Inna Gafanovich, Marius Braun, Michal Cohen-Naftaly, Amir Shlomai, Oren Shibolet, Ehud Zigmond, Eli Zuckerman, Michal Carmiel-Haggai, Assy Nimer, Rawi Hazzan, Yaakov Maor, Yona Kitay-Cohen, Yonat Shemer, Zipi Kra-Oz, Lisita Schreiber, Ofer Peleg, Ella Mendelson, Orna Mor
BACKGROUND: Direct-acting antiviral (DAA) treatment regimens and response rates of patients with hepatitis C virus (HCV) genotype 1 (GT1) are currently considered subtype-dependent. Identification of clinically relevant resistance-associated substitutions (RASs) in the NS3 and NS5A proteins at baseline and in DAA failures, may also impact clinical decisions. METHODS: In a multicenter cohort study (n=308), NS3 or NS5B sequencing (n=248) was used to discriminate between GT1 subtypes...
January 9, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28067239/corrigendum-influenza-virus-mrna-trafficking-through-host-nuclear-speckles
#15
Amir Mor, Alexander White, Ke Zhang, Matthew Thompson, Matthew Esparza, Raquel Muñoz-Moreno, Kazunori Koide, Kristen W Lynch, Adolfo García-Sastre, Beatriz M A Fontoura
No abstract text is available yet for this article.
January 9, 2017: Nature Microbiology
https://www.readbyqxmd.com/read/28063910/racial-ethnic-differences-in-contraceptive-preferences-beliefs-and-self-efficacy-among-women-veterans
#16
Lisa S Callegari, Xinhua Zhao, Eleanor Bimla Schwarz, Elian Rosenfeld, Maria K Mor, Sonya Borrero
BACKGROUND: Significant racial/ethnic disparities in unintended pregnancy persist in the US, with the highest rates observed among low-income black and Hispanic women. Differences in contraceptive preferences, beliefs, and self-efficacy may be instrumental in understanding contraceptive behaviors that underlie higher rates of unintended pregnancy among racial/ethnic minorities. OBJECTIVES: Our objective was to understand how contraceptive preferences, beliefs and self-efficacy vary by race and ethnicity among women veterans...
January 4, 2017: American Journal of Obstetrics and Gynecology
https://www.readbyqxmd.com/read/28063353/rationally-designed-benzopyran-fused-isoxazolidines-and-derived-%C3%AE-2-3-3-amino-alcohols-as-potent-analgesics-synthesis-biological-evaluation-and-molecular-docking-analysis
#17
Gagandeep Singh, Gurjit Singh, Rajbir Bhatti, Vivek Gupta, Ajay Mahajan, Palwinder Singh, Mohan Paul Singh Ishar
Based on structure activity analysis of morphine related opiates, we have synthesized some novel benzopyran fused isoxazolidines (2a-e) and derived conformationally constrained β(2,3,3)-amino alcohols (3a-e), which were evaluated in vivo for their anti-nociceptive activity through acetic acid induced writhing test (peripheral) and formalin induced algesia (central). Results showed that, compound 2a possesses significant opioid agonist activity. Further, molecular docking analysis reveals that compound 2a binds to δ-opioid receptor (DOR) with comparatively better D-score than to μ (MOR) and κ (KOR) receptors...
December 28, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28054321/impact-of-clinicopathological-parameters-on-survival-after-multiorgan-resection-among-patients-with-t4-gastric-carcinoma-a-systematic-review-and-meta-analysis
#18
REVIEW
G Zu, T Zhang, W Li, Y Sun, X Zhang
BACKGROUND: The prognostic factors which can improve the overall survival (OS) of patients with T4 gastric carcinoma (GC) are still controversial: a meta-analysis was conducted to analyze the impact of clinicopathological parameters on survival after MOR among patients with T4 GC. METHODS: A systematic search was performed. Odd risks (ORs) of patients with T4 GC were used to calculate the relationship between clinicopathological parameters and OS. RESULTS: Nine studies involving 941 patients with T4 GC were identified...
January 4, 2017: Clinical & Translational Oncology
https://www.readbyqxmd.com/read/28054162/patients-age-rather-than-model-of-end-stage-liver-disease-score-predicts-survival-after-liver-transplantation
#19
Yaara Leibovici-Weissman, Eytan Mor, Moshe Leshno, Amir Shlomai
BACKGROUND: The model of end-stage liver disease (MELD) score is the standard tool for prioritizing patients awaiting liver transplantation. There is currently no definite high cutoff score reflecting disease severity that might exclude patients from transplantation. Furthermore, the age limit that used to disqualify patients from eligibility to transplantation was recently withdrawn in several countries. AIMS: The aims of this study were to assess the effects of MELD score and age at time of transplantation on patients' short- and long-term survival...
January 4, 2017: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/28051873/synergistically-improving-the-activity-antipoisonous-ability-and-long-term-stability-of-pt-to-methanol-oxidation-through-developing-favorable-graphene-based-supports
#20
Qiong Xue, Jin-Kuo Li, Zhi-Yong Yang
An interconnected framework of reduced graphene oxide/phenyl formaldehyde polymer composites was synthesized by a one-pot hydrothermal reaction followed by carbonizing under different conditions. Then, the obtained porous materials with varied surface properties were used to disperse ultrasmall Pt nanoparticles. The catalyst with the optimized support demonstrates superior achievements to methanol oxidation reaction (MOR): distinctive improved mass activity (MA) and specific activity at both forward peak position and at the potential range near the operation of fuel cells, best antipoisonous ability revealed by 17 times MA and 7 times the retaining rate of commercial Pt/C in chronoamperometric evaluations, and outstanding long-term stability verified by 3-4 times MA and the retaining rate of Pt/C in the accelerated duration tests...
January 18, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
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