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https://www.readbyqxmd.com/read/29141109/hepatic-ppar%C3%AE-mediates-the-major-metabolic-effects-of-wy-14643
#1
Guolin Li, Chad N Brocker, Cen Xie, Tingting Yan, Audrey Noguchi, Kristopher W Krausz, Rong Xiang, Frank J Gonzalez
BACKGROUND AND AIM: Peroxisome proliferator-activated receptor alpha (PPARα) is a molecular target of various fibrate drugs clinically used to lower serum lipids. However, the tissue-specific functions of PPARα remain to be elucidated. This study aimed to explore the tissue-specific functions of PPARα in response to Wy-14643. METHODS: A hepatocyte-specific Ppara knockout mouse line was used to explore the impact of hepatic PPARα activity on the systemic response to treatment with the potent PPARα agonist Wy-14643...
November 15, 2017: Journal of Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/29140951/platelet-aggregation-after-blunt-trauma-is-associated-with-the-acute-respiratory-distress-syndrome-and-altered-by-cigarette-smoke-exposure
#2
Farzad Moazed, Carolyn Hendrickson, Mary Nelson, Amanda Conroy, Mitchell J Cohen, Carolyn S Calfee
BACKGROUND: The risk of the acute respiratory distress syndrome (ARDS) is increased in passive and active smokers after blunt trauma. However, the mechanisms responsible, including the role of platelet aggregation, for this association are unknown. METHODS: We analyzed 215 patients with severe blunt trauma from a prospective observational cohort at a Level 1 trauma center between 2010 - 2015. Subjects underwent impedance-based platelet aggregometry in response to platelet agonists arachidonic acid (ASPI), adenosine diphosphate (ADP), collagen (COL) and thrombin receptor activating peptide-6 (TRAP)...
November 14, 2017: Journal of Trauma and Acute Care Surgery
https://www.readbyqxmd.com/read/29140922/fingolimod-reduces-neuropathic-pain-behaviors-in-a-mouse-model-of-multiple-sclerosis-by-a-sphingosine-1-phosphate-receptor-1-dependent-inhibition-of-central-sensitization-in-the-dorsal-horn
#3
Suzanne Doolen, Tommaso Iannitti, Benjamin C Shaw, Carolyn M Grachen, Renee R Donahue, Bradley K Taylor
Multiple sclerosis (MS) is an autoimmune-inflammatory neurodegenerative disease that is often accompanied by a debilitating neuropathic pain. Disease-modifying agents slow the progression of MS and prevent relapses, yet it remains unclear if they yield analgesia. We explored the analgesic potential of fingolimod (FTY720), an agonist/functional antagonist at the sphingosine-1-phosphate receptor 1 (S1PR1), because it reduces hyperalgesia in models of peripheral inflammatory and neuropathic pain. We used a myelin oligodendrocyte glycoprotein 35-55 (MOG35-55) mouse model of experimental autoimmune encephalomyelitis (EAE), modified to avoid frank paralysis and thus allow for assessment of withdrawal behaviors to somatosensory stimuli...
November 13, 2017: Pain
https://www.readbyqxmd.com/read/29140832/platelet-function-changes-in-a-time-dependent-manner-following-traumatic-brain-injury-in-a-murine-model
#4
Grace E Martin, Brent Xia, Young Kim, Mark D Johnson, Rosalie Veile, Lou Ann Friend, Amy T Makley, Charles C Caldwell, Michael D Goodman
Traumatic brain injury (TBI) results in systemic changes in coagulation and inflammation that contribute to post-traumatic morbidity and mortality. The potential interaction of platelets and pro-inflammatory cytokines in the modulation of coagulation, microthrombosis, and venous thromboembolic events after moderate TBI (TBI) has not been determined. Using a murine model, we hypothesized 1) that the degree of platelet-induced coagulation varies depending on the platelet aggregation agonist 2) platelet-induced coagulation changes in a time-dependent manner following TBI, and 3) changes in platelet-induced coagulation are mirrored by changes in the levels of circulating pro-inflammatory cytokines...
November 14, 2017: Shock
https://www.readbyqxmd.com/read/29139561/the-novel-potent-and-highly-selective-5-ht4-receptor-agonist-yh12852-significantly-improves-both-upper-and-lower-gastrointestinal-motility
#5
Eun Jeong Jeong, Soo Yong Chung, Han Na Hong, Se-Woong Oh, Jae Young Sim
BACKGROUND AND PURPOSE: 5-HT4 receptor agonists have been shown to be effective to treat various gastrointestinal tract disorders. However, a lack of selectivity against off-targets has been a limiting factor. EXPERIMENTAL APPROACH: The binding affinity and selectivity of YH12852 for human 5-HT4(a) receptor in CHO-K1 cells were evaluated using radioligand binding assays, and agonistic activity was assessed using a beta-lactamase reporter system. Contractile activity and propulsive motility were measured in isolated guinea pig distal colon...
November 15, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29139105/preoperative-medical-therapy-before-surgery-for-uterine-fibroids
#6
REVIEW
Anne Lethaby, Lucian Puscasiu, Beverley Vollenhoven
BACKGROUND: Uterine fibroids occur in up to 40% of women aged over 35 years. Some are asymptomatic, but up to 50% cause symptoms that warrant therapy. Symptoms include anaemia caused by heavy menstrual bleeding, pelvic pain, dysmenorrhoea, infertility and low quality of life. Surgery is the first choice of treatment. In recent years, medical therapies have been used before surgery to improve intraoperative and postoperative outcomes. However, such therapies tend to be expensive.Fibroid growth is stimulated by oestrogen...
November 15, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29138877/%C3%AE-9-tetrahydrocannabinol-like-discriminative-stimulus-effects-of-five-novel-synthetic-cannabinoids-in-rats
#7
Michael B Gatch, Michael J Forster
RATIONALE AND OBJECTIVES: Novel synthetic cannabinoid compounds continue to appear in the market advertised as legal alternatives to marijuana and the older synthetic cannabinoid compounds which are now controlled substances. Most of these newer compounds have been found to act at CB1 receptors, so the purpose of this study was to study the abuse liability of these compounds. METHODS: Five of these compounds (BB-22, FUB-PB-22, 5F-AMB, NM2201, and MAB-CHMINACA) were tested for their ability to produce discriminative stimulus effects similar to Δ(9)-tetrahydrocannabinol (Δ(9)-THC) in rats...
November 14, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/29138822/fucoidan-inhibits-ca2-responses-induced-by-a-wide-spectrum-of-agonists-for-g%C3%A2-protein%C3%A2-coupled-receptors
#8
Hong Wu, Shuibo Gao, Min Fu, Takashi Sakurai, Susumu Terakawa
Fucoidan, a sulfated polysaccharide extracted from brown seaweed, has been used in traditional Chinese herbal medicine to treat thyroid tumors for many years. Although a number of its cellular effects have been investigated, the role of fucoidan in molecular signaling, particularly in Ca2+ signaling, remains largely unknown. In the present study, the effects of fucoidan on Ca2+ responses in HeLa cells, human umbilical vein endothelial cells and astrocytes were investigated using a wide range of receptor agonists...
November 13, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29138819/beneficial-effect-of-resveratrol-on-%C3%AE-%C3%A2-naphthyl-isothiocyanate%C3%A2-induced-cholestasis-via-regulation-of-the-fxr-pathway
#9
Lili Ding, Binfeng Zhang, Jinmei Li, Li Yang, Zhengtao Wang
Cholestasis is defined as a functional impairment of bile secretion which results in the accumulation of bile acids (BAs) and other toxic molecules in the blood and liver, however, there are very few effective therapies for cholestasis. The farnesoid X receptor (FXR), as a nuclear receptor for BAs, is important in the regulation of BA levels in enterohepatic circulation. It has previously been demonstrated that activation of the FXR pathway may be a useful strategy with which to treat cholestasis. Resveratrol, one of the important ingredients from grape skins and Chinese medicine Polygonum cuspidatum, resulted in FXR‑activated effects in vitro and exhibited a protective effect against α‑naphthylisothiocyanate (ANIT)‑induced cholestasis through FXR regulation in vivo...
November 14, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29138795/hesperidin-induces-apoptosis-and-g0-g1-arrest-in-human-non-small-cell-lung-cancer-a549-cells
#10
Rongmu Xia, Xin Sheng, Xianlin Xu, Chunbo Yu, Hongling Lu
Lung cancer has high incidence and mortality rates worldwide. In the present study, the mechanisms by which hesperidin decreases the viability and induces the apoptosis of human non-small cell lung cancer (NSCLC) A549 cells were investigated. Initially, MTT and flow cytometric assays were performed to evaluate the effects of hesperidin on the viability and apoptosis of A549 cells and human normal lung epithelial BEAS-2B cells. The results revealed that hesperidin has no negative effects on the human normal lung epithelial BEAS-2B cells and the viability of cells treated with various concentrations of hesperidin was inhibited in a time- and dose-dependent manner compared with the control groups...
November 9, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29138555/the-efficacy-of-extrafine-beclomethasone-dipropionate-formoterol-fumarate-in-copd-patients-who-are-not-frequent-exacerbators-a-post-hoc-analysis-of-the-forward-study
#11
Dave Singh, Stefano Vezzoli, Stefano Petruzzelli, Alberto Papi
The GOLD 2017 strategy document recommends that the pharmacological management of COPD patients be based on the risk of future exacerbations and the severity of symptoms. A threshold of two moderate exacerbations or one hospitalization is used to define high-risk patients. The FORWARD study was a randomized, double-blind, parallel-group trial that compared 48 weeks' treatment with extrafine beclomethasone dipropionate plus formoterol fumarate (BDP-FF) versus FF in severe COPD patients with a history of one or more exacerbations in the previous year...
2017: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/29138547/efficacy-of-tiotropium-and-indacaterol-monotherapy-and-their-combination-on-dynamic-lung-hyperinflation-in-copd-a-random-open-label-crossover-study
#12
Keisaku Fujimoto, Haruna Yamazaki, Midori Ura, Yoshiaki Kitaguchi
Background and objective: The difference in efficacy of long-acting muscarinic antagonists (LAMAs) and long-acting β2-agonists (LABAs) for dynamic lung hyperinflation (DLH) in COPD is unclear. The purpose of this study was to elucidate the difference in efficacy of LAMA and LABA alone and the combination thereof for DLH. Subjects and methods: Thirty stable patients were enrolled and randomly divided into two groups following baseline measurements. One group was treated with 5 μg tiotropium (Respimat inhaler) for 4 weeks following a 4-week treatment with 150 μg indacaterol, while the other group was treated with indacaterol for 4 weeks following a 4-week treatment with tiotropium...
2017: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/29138471/%C3%AE-subunits-in-gabaa-receptors-are-dispensable-for-gaba-and-diazepam-action
#13
Nisa Wongsamitkul, Maria C Maldifassi, Xenia Simeone, Roland Baur, Margot Ernst, Erwin Sigel
The major isoform of the GABAA receptor is α1β2γ2. The binding sites for the agonist GABA are located at the β2+/α1- subunit interfaces and the modulatory site for benzodiazepines at α1+/γ2-. In the absence of α1 subunits, a receptor was formed that was gated by GABA and modulated by diazepam similarly. This indicates that alternative subunits can take over the role of the α1 subunits. Point mutations were introduced in β2 or γ2 subunits at positions homologous to α1- benzodiazepine binding and GABA binding positions, respectively...
November 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29138105/adrenergic-receptor-agonists-modulation-of-dopaminergic-and-non-dopaminergic-neurons-in-the-ventral-tegmental-area
#14
Kamil Pradel, Tomasz Blasiak, Wojciech B Solecki
The ventral tegmental area (VTA) neuronal population consists of dopaminergic (DAergic) and non-DAergic neurons (mainly GABAergic), the activity of which is intertwined with VTA behavioural functions. Both DAergic and GABAergic neurons in the VTA have been shown to express adrenergic receptors (ARs) and respond to AR stimulation. The aim of the present study was to demonstrate the effects of selective AR agonists on DAergic and non-DAergic neuronal activity in the central and lateral parts of the VTA using in vivo electrophysiological recording combined with microiontophoretic drug application in anaesthetized rats...
November 11, 2017: Neuroscience
https://www.readbyqxmd.com/read/29138055/merkel-cells-sense-cooling-with-trpm8-channels
#15
Valentine Bouvier, Yann Roudaut, Nancy Osorio, Jean-Marc Aimonetti, Edith Ribot-Ciscar, Virginie Penalba, Thierry Merrot, Nicolas Lebonvallet, Christelle Le Gall-Ianotto, Laurent Misery, Patrick Delmas, Marcel Crest
In the skin, Merkel cells (MCs) connect with keratinocytes and Aβ nerve fibers to form a touch receptor which functions as a slow adapting mechanoreceptor (SA1 receptor). In human and mouse MCs, we observed an increased concentration of intracellular Ca(2+) ions in response to cold temperature and transient receptor potential melastatine 8 (TRPM8) ion channel agonists. A reduction in the response to cooling and TRPM8 agonists occurred following addition of TRPM8 antagonists, as well as in TRPM8 knockout mice...
November 11, 2017: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/29137986/long-range-stress-transmission-guides-endothelial-gap-formation
#16
C Corey Hardin, Joyjit Chattoraj, Greeshma Manomohan, Jader Colombo, Trong Nguyen, Dhananjay Tambe, Jeffrey J Fredberg, Konstantin Birukov, James P Butler, Emanuela Del Gado, Ramaswamy Krishnan
In endothelial gap formation, local tractions exerted by the cell upon its basal adhesions are thought to exceed balancing tensile stresses exerted across the cell-cell junction, thus causing the junction to rupture. To test this idea, we mapped evolving tractions, intercellular stresses, and corresponding growth of paracellular gaps in response to agonist challenge. Contrary to expectation, we found little to no relationship between local tensile stresses and gap formation. Instead, we discovered that intercellular stresses were aligned into striking multi-cellular domains punctuated by defects in stress alignment...
November 11, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29137945/the-effects-of-local-microinjection-of-selective-dopamine-d1-and-d2-receptor-agonists-and-antagonists-into-the-dorsal-raphe-nucleus-on-sleep-and-wakefulness-in-the-rat
#17
Jaime M Monti, Héctor Jantos
The effects of the dopamine (DA) D1 and D2 receptor agonists SKF38393, bromocriptine and quinpirole, respectively, on spontaneous sleep were analyzed in adult rats prepared for chronic sleep recordings. Local administration of the DAergic agonists into the dorsal raphe nucleus (DRN) during the light phase of the light-dark cycle induced a significant reduction of rapid-eye movement sleep (REMS) and the number of REM periods. Additionally, bromocriptine and quinpirole significantly increased wakefulness (W)...
November 11, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/29137557/the-impact-of-a-state-medicaid-peer-review-authorization-program-on-pediatric-use-of-antipsychotic-medications
#18
Dinci Pennap, Mehmet Burcu, Daniel J Safer, Julie Magno Zito
OBJECTIVE: This cross-sectional study assessed the impact of a peer-review program on the prevalence of pediatric antipsychotic use among Medicaid-insured youths in a Mid-Atlantic state. METHODS: Medicaid claims (2010-2014) were assessed among continuously enrolled youths in the 12 months before and after implementation of peer review. The study identified children ages zero to four preimplementation (N=118,815) and postimplementation (N=121,431), ages five to nine preimplementation (N=98,681) and postimplementation (N=107,872), and ages 10 to 17 preimplementation (N=154,696) and postimplementation (N=161,370)...
November 15, 2017: Psychiatric Services: a Journal of the American Psychiatric Association
https://www.readbyqxmd.com/read/29137494/trh-receptor-mobility-in-the-plasma-membrane-is-strongly-affected-by-agonist-binding-and-by-interaction-with-some-cognate-signaling-proteins
#19
Radka Moravcova, Barbora Melkes, Jiri Novotny
OBJECTIVES: Extensive research has been dedicated to elucidating the mechanisms of signal transduction through different G protein-coupled receptors (GPCRs). However, relatively little is known about the regulation of receptor movement within the cell membrane upon ligand binding. In this study we focused our attention on the thyrotropin-releasing hormone (TRH) receptor that typically couples to Gq/11 proteins. METHODS: We monitored receptor diffusion in the plasma membrane of HEK293 cells stably expressing yellow fluorescent protein (YFP)-tagged TRH receptor (TRHR-YFP) by fluorescence recovery after photobleaching (FRAP)...
November 14, 2017: Journal of Receptor and Signal Transduction Research
https://www.readbyqxmd.com/read/29137489/androgen-deprivation-therapy-for-the-treatment-of-prostate-cancer-a-focus-on-pharmacokinetics
#20
Charles F Polotti, Christopher J Kim, Nadiya Chuchvara, Alyssa B Polotti, Eric A Singer, Sammy Elsamra
Medical therapy has undergone many changes as our understanding of prostate cancer cell biology has improved. Androgen deprivation therapy (ADT) remains the mainstay of therapy for metastatic disease. Metastatic castrate-resistant prostate cancer (CRPC) is an important concern since we are unable to stop progression with currently available agents. Areas covered: Pharmacologic ADT is the most commonly used treatment for metastatic prostate cancer. Multiple agents are available for both first-line and second-line use: antiandrogens, estrogens, luteinizing hormone-releasing hormone agonists/antagonists, and CYP17 inhibitors...
November 15, 2017: Expert Opinion on Drug Metabolism & Toxicology
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