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https://www.readbyqxmd.com/read/28645101/co-localization-of-endogenous-arf6-and-its-activator-efa6d-in-the-granular-convoluted-tubule-cells-of-mouse-submandibular-glands-under-normal-conditions-and-when-stimulated-by-isoproterenol-noradrenaline-and-carbachol
#1
Apussara Tachow, Wipawee Thoungseabyoun, Laorrat Phuapittayalert, Kanoktip Petcharat, Hiroyuki Sakagami, Hisatake Kondo, Wiphawi Hipkaeo
OBJECTIVE: This study proposed to investigate the localization at light and electron microscopic levels of Arf6 and its activator EFA6D in the mouse submandibular gland (SMG) under normal conditions and when stimulated by adrenergic or cholinergic agonists. MATERIALS AND METHODS: SMGs of male adult mice were utilized for immunoblotting and immuno-light and -electron microscopic analyses. Isoproterenol and noradrenalin were used as adrenergics, while carbachol was used for the cholinergic stimulant...
June 13, 2017: Archives of Oral Biology
https://www.readbyqxmd.com/read/28645087/ep2-receptor-agonist-ono-ae1-259-01-attenuates-pentylenetetrazole-and-pilocarpine-induced-seizures-but-causes-hippocampal-neurotoxicity
#2
Aline Carré Santos, Fernanda Rossatto Temp, Joseane Righes Marafiga, Micheli Mainardi Pillat, Amanda Titzel Hessel, Leandro Rodrigo Ribeiro, Lígia Gomes Miyazato, Mauro Schneider Oliveira, Carlos Fernando Mello
Epilepsy is a common and devastating neurological disease affecting more than 50 million people worldwide. Accumulating experimental and clinical evidence suggests that inflammatory pathways contribute to the development of seizures in various forms of epilepsy. In this context, while the activation of the PGE2 EP2 receptor causes early neuroprotective and late neurotoxic effects, the role of EP2 receptor in seizures remains unclear. We investigated whether the systemic administration of the highly selective EP2 agonist ONO-AE1-259-01 prevented acute pentylenetetrazole (PTZ)- and pilocarpine-induced seizures...
June 20, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28645054/computational-analysis-of-the-toxcast-estrogen-receptor-agonist-assays-to-predict-vitellogenin-induction-by-chemicals-in-male-fish
#3
David A Dreier, Nancy D Denslow, Christopher J Martyniuk
Endocrine disruptors, especially estrogen receptor (ER) agonists, have received considerable research attention. While there are several mechanistic endpoints for ER agonism in the Endocrine Disruptor Screening Program, there have been growing efforts to develop high-throughput screening assays and computational models to reduce testing cost, time, and animal use. For example, there are 16 ER agonist assays and an integrated computational model in ToxCast. In the present study, we examined the relationship between ToxCast ER agonist assays and model activity to male vitellogenin induction in the Fish-Short Term Reproduction Assay...
June 13, 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28645007/activation-of-the-pi3k-akt-pathway-promotes-neuroprotection-of-the-%C3%AE-opioid-receptor-agonist-against-cerebral-ischemia-reperfusion-injury-in-rat-models
#4
Mei-Rong Lv, Bin Li, Ming-Guang Wang, Fan-Guo Meng, Jian-Jun Yu, Feng Guo, Ye Li
The central objective was to identify the role of the PI3K-Akt activation pathway on the neuroprotection of δ-opioid receptor agonist (DADLE) against cerebral ischemia-reperfusion (I/R) injury in a rat model. Fifty-five male Sprague-Dawley (SD) rats were included to establish a middle cerebral artery occlusion (MCAO) model which were then divided into the sham, MCAO, LY294002 (MCAO+DADLE+LY294002 [inhibitor of PI3K-Akt pathway]), DADLE (MCAO+DADLE) and DMSO (MCAO+DADLE+DMSO [dimethyl sulphoxide]) groups. The cerebral infarction (CI) volume and nerve cell apoptosis was determined using TTC and TUNEL staining...
June 20, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28644987/thiophene-thiazole-benzene-replacement-on-guanidine-derivatives-targeting-%C3%AE-2-adrenoceptors
#5
Aoife Flood, Cristina Trujillo, Goar Sanchez-Sanz, Brendan Kelly, Carolina Muguruza, Luis F Callado, Isabel Rozas
Searching for improved antagonists of α2-adrenoceptors, a thorough theoretical study comparing the aromaticity of phenyl-, pyridinyl-, thiophenyl- and thiazolylguanidinium derivatives has been carried out [at M06-2X/6-311++G(p,d) computational level] confirming that thiophene and thiazole will be good 'ring equivalents' to benzene in these guanidinium systems. Based on these results, a small but chemically diverse library of guanidine derivatives (15 thiophenes and 2 thiazoles) were synthesised to explore the effect that the bioisosteric change has on affinity and activity at α2-adrenoceptors in comparison with our previously studied phenyl derivatives...
June 6, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28644617/dynamic-covalent-chemistry-of-carbon-dioxide-opportunities-to-address-environmental-issues
#6
Jean Septavaux, Geoffroy Germain, Julien Leclaire
Extraction and purification of basic chemicals from complex mixtures has been a persistent issue throughout the development of the chemical sciences. The chemical industry and academic research have grown over the centuries by following a deconstruction-reconstruction approach, reminiscent of the metabolism process. Chemists have designed and optimized extraction, purification, and transformation processes of molecules from natural deposits (fossil fuels, biomass, ores), in order to reassemble them into complex adducts...
June 23, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28644608/targeting-cpg-adjuvant-to-lymph-node-via-dextran-conjugate-enhances-anti-tumor-immunotherapy
#7
Weidong Zhang, Myunggi An, Jingchao Xi, Haipeng Liu
Nucleic acids based adjuvants recognized by Toll-like receptors (TLR) are potent immune system stimulants that can augment the anti-tumor immune responses in an antigen-specific manner. However, their clinical uses as vaccine adjuvants are limited primarily due to lack of accumulation in the lymph nodes, the anatomic sites where the immune responses are initiated. Here, we showed that chemical conjugation of type B CpG DNA, a TLR9 agonist to dextran polymer dramatically enhanced CpG's lymph node accumulation in mice...
June 23, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28644418/new-mt%C3%A2-melatonin-receptor-selective-ligands-agonists-and-partial-agonists
#8
Jean A Boutin, Anne Bonnaud, Chantal Brasseur, Olivier Bruno, Nolwenn Lepretre, Peter Oosting, Sophie Coumailleau, Philippe Delagrange, Olivier Nosjean, Céline Legros
The search for melatonin receptor agonists and antagonists specific towards one of the receptor subtypes will extend our understanding of the role of this system in relaying circadian information to the body. A series of compounds derived from a hit compound discovered in a screening process led to powerful agonists specific for one of the isoform of the melatonin receptor namely, MT₂. The compounds are based on a poorly explored skeleton in the molecular pharmacology of melatonin. By changing the steric hindrance of one substituent (i...
June 23, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28644104/the-association-between-blood-eosinophil-count-and-benralizumab-efficacy-for-patients-with-severe-uncontrolled-asthma-subanalyses-of-the-phase-iii-sirocco-and-calima-studies
#9
Mitchell Goldman, Ian Hirsch, James G Zangrilli, Paul Newbold, Xiao Xu
OBJECTIVE: Benralizumab, an anti-eosinophilic monoclonal antibody, in combination with high-dosage inhaled corticosteroids and long-acting β2-agonists (ICS/LABA) significantly reduced asthma exacerbations, improved lung function, and reduced symptoms for patients with severe, uncontrolled asthma with blood eosinophil counts ≥300 cells/µL in the Phase III SIROCCO and CALIMA studies. To understand the efficacy and safety of benralizumab for patients with eosinophil-driven disease with blood eosinophil counts lower than 300 cells/µL, we evaluated the effect of applying an eosinophil cutoff of ≥150 cells/µL...
June 23, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28644012/sigma-2-receptor-tmem97-agonists-produce-long-lasting-anti-neuropathic-pain-effects-in-mice
#10
James J Sahn, Galo L Mejia, Pradipta R Ray, Stephen F Martin, Theodore John Price
Neuropathic pain is an important medical problem with few effective treatments. The sigma 1 receptor (σ1R) is a potential target for neuropathic pain therapeutics, and antagonists for this receptor are effective in preclinical models and are currently in phase II clinical trials. Relatively little is known about the σ2R, which has recently been identified as transmembrane protein 97 (Tmem97). We generated a series of σ1R and σ2R/Tmem97 agonists and antagonists and tested them for efficacy in the mouse spared nerve injury (SNI) model...
June 23, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28643469/atra-signaling-regulates-the-expression-of-col9a1-through-bmp2-wnt4-runx1-pathway-in-antler-chondrocytes
#11
Hong-Liang Zhang, Bin Guo, Zhan-Qing Yang, Cui-Cui Duan, Shuang Geng, Kai Wang, Hai-Fan Yu, Zhan-Peng Yue
Although all-trans retinoic acid (ATRA) is involved in the regulation of cartilage growth and development, its regulatory mechanisms remain unknown. Here, we showed that ATRA could induce the expression of COL9A1 in antler chondrocytes. Silencing of cellular retinoic acid binding protein 2 (CRABP2) could impede the ATRA-induced upregulation of COL9A1, whereas overexpression of CRABP2 presented the opposite effect. RARα agonist Am80 induced the expression of COL9A1, whereas treatment with RARα antagonist Ro 41-5253 or RXRα small-interfering RNA (siRNA) caused an obvious blockage of ATRA on COL9A1...
June 22, 2017: Journal of Experimental Zoology. Part B, Molecular and Developmental Evolution
https://www.readbyqxmd.com/read/28643468/eltrombopag-use-in-a-patient-with-wiskott-aldrich-syndrome
#12
Maria Gabelli, Antonio Marzollo, Lucia Dora Notarangelo, Giuseppe Basso, Maria Caterina Putti
Wiskott-Aldrich syndrome (WAS) is an inherited X-linked disorder characterized by microthrombocytopenia, immunodeficiency, and eczema. Hematopoietic stem cell transplantation (HSCT) is the treatment of choice. Eltrombopag, a thrombopoietin receptor agonist, may be useful to prevent bleeding while awaiting HSCT. We present a case of a male with WAS, profound thrombocytopenia, and bleeding diathesis successfully managed with eltrombopag before HSCT. Eltrombopag was given for 32 weeks obtaining a stable platelet count without any platelet transfusion...
June 23, 2017: Pediatric Blood & Cancer
https://www.readbyqxmd.com/read/28643293/-why-is-a-combination-of-basal-insulin-with-a-glp-1-receptor-agonist-useful-in-many-patients-with-type-2-diabetes
#13
Michael Nauck, Birgit Wilhelm
BACKGROUND: In 2015, the combination of basal insulin and GLP-1 receptor agonist (RA) was incorporated into the guideline recommendations for type 2 diabetes as an option for the last escalation step. The two antidiabetics to be injected subcutaneously are complementary regarding their respective main effects and limitations. Basal insulin is predominantly active between meals and in the fasting state, whereas the main action of GLP-1 RA consists in preventing an excessive postprandial blood glucose increase...
June 2017: MMW Fortschritte der Medizin
https://www.readbyqxmd.com/read/28643183/dopaminergic-therapies-for-non-motor-symptoms-in-parkinson-s-disease
#14
REVIEW
Eva Schaeffer, Daniela Berg
Apart from the typical motor symptoms, Parkinson's disease is characterized by a wide range of different non-motor symptoms, which are highly prevalent in all stages of the disease and have an incisive influence on quality of life. Moreover, their treatment continues to be challenging. In this review, we critically summarize the evidence for the impact of dopaminergic therapies on non-motor symptoms in Parkinson's disease. We performed a PubMed search to identify relevant clinical studies that investigated the response of non-motor symptoms to dopaminergic therapy...
June 22, 2017: CNS Drugs
https://www.readbyqxmd.com/read/28643088/potential-therapeutic-applications-of-human-anti-m%C3%A3-llerian-hormone-amh-analogues-in-reproductive-medicine
#15
REVIEW
Vitaly A Kushnir, David B Seifer, David H Barad, Aritro Sen, Norbert Gleicher
Members of the transforming growth factor-beta (TGF-beta) superfamily are key regulators of various physiological processes. Anti-Müllerian hormone (AMH) which is also commonly known as Müllerian-inhibiting substance (MIS) is a member of the TGF-beta superfamily and an important regulator of reproductive organ differentiation and ovarian follicular development. While AMH has been used for diagnostic purposes as a biomarker for over 15 years, new potential therapeutic applications of recombinant human AMH analogues are now emerging as pharmacologic agents in reproductive medicine...
June 22, 2017: Journal of Assisted Reproduction and Genetics
https://www.readbyqxmd.com/read/28642887/dynamic-regulation-of-serum-aryl-hydrocarbon-receptor-agonists-in-ms
#16
Veit Rothhammer, Davis M Borucki, Maria Isabel Garcia Sanchez, Maria Antonietta Mazzola, Christopher C Hemond, Keren Regev, Anu Paul, Pia Kivisäkk, Rohit Bakshi, Guillermo Izquierdo, Howard L Weiner, Francisco J Quintana
OBJECTIVE: Several factors influence the clinical course of autoimmune inflammatory diseases such as MS and inflammatory bowel disease. Only recently, the complex interaction between the gut microbiome, dietary factors, and metabolism has started to be appreciated with regard to its potential to modulate acute and chronic inflammation. One of the molecular sensors that mediates the effects of these environmental signals on the immune response is the aryl hydrocarbon receptor (AHR), a ligand-activated transcription factor with key functions in immune cells...
July 2017: Neurology® Neuroimmunology & Neuroinflammation
https://www.readbyqxmd.com/read/28642766/high-throughput-screening-method-for-identifying-potential-agonists-and-antagonists-of-arabidopsis-thaliana-cytokinin-receptor-cre1-ahk4
#17
Pavel Klimeš, Dušan Turek, Pavel Mazura, Lucia Gallová, Lukáš Spíchal, Břetislav Brzobohatý
The CRE1/AHK4 cytokinin receptor is an important component of plants' hormone signaling systems, and compounds that can alter its activity have potential utility for studying the receptor's functions and/or developing new plant growth regulators. A high throughput method was developed for screening compounds with agonist or antagonist properties toward the CRE1/AHK4 cytokinin receptor in a single experiment using the Nanodrop II liquid handling system and 384-well plates. Potential ligands are screened directly, using a reporter system in which receptor signaling activity triggers expression of β-galactosidase in Escherichia coli...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28642642/access-to-and-payment-for-office-based-buprenorphine-treatment-in-ohio
#18
Theodore V Parran, Joseph Z Muller, Elina Chernyak, Chris Adelman, Christina M Delos Reyes, Douglas Rowland, Mykola Kolganov
IMPORTANCE: Office-based opiate agonist therapy has dramatically expanded access to medication-assisted treatment over the past decade but has also led to increased buprenorphine diversion. OBJECTIVE: Our study sought to characterize physicians who participate in office-based therapy (OBT) to assess patient access to OBT in Ohio 10 years after its introduction. DESIGN/SETTING/PARTICIPANTS: Cross-sectional telephone survey of Drug Addiction Treatment Act-waivered physicians in Ohio listed by the Center for Substance Abuse Treatment (CSAT)...
2017: Substance Abuse: Research and Treatment
https://www.readbyqxmd.com/read/28642485/sphingosine-1-phosphate-treatment-can-ameliorate-microvascular-leakage-caused-by-combined-alcohol-intoxication-and-hemorrhagic-shock
#19
Travis M Doggett, Natascha G Alves, Sarah Y Yuan, Jerome W Breslin
Fluid resuscitation following hemorrhagic shock is often problematic, with development of prolonged hypotension and edema. In addition, many trauma patients are also intoxicated, which generally worsens outcomes. We directly investigated how alcohol intoxication impacts hemorrhagic shock and resuscitation-induced microvascular leakage using a rat model with intravital microscopic imaging. We also tested the hypothesis that an endothelial barrier-protective bioactive lipid, sphingosine-1-phosphate (S1P), could ameliorate the microvascular leakage following alcohol intoxication plus hemorrhagic shock and resuscitation...
June 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28642153/characterization-of-the-differential-coregulator-binding-signatures-of-the-retinoic-acid-receptor-subtypes-upon-ant-agonist-action
#20
Ignacio Miro Estruch, Diana Melchers, René Houtman, Laura H J de Haan, John P Groten, Jochem Louisse, Ivonne M C M Rietjens
Retinoic Acid Receptor alpha (RARα/NR1B1), Retinoic Acid Receptor beta (RARβ/NR1B2) and Retinoic Acid Receptor gamma (RARγ/NR1B3) are transcription factors regulating gene expression in response to retinoids. Within the RAR genomic pathways, binding of RARs to coregulators is a key intermediate regulatory phase. However, ligand-dependent interactions between the wide variety of coregulators that may be present in a cell and the different RAR subtypes are largely unknown. The aim of this study is to characterize the coregulator binding profiles of RARs in the presence of the pan-agonist all-trans-Retinoic Acid (AtRA); the subtype-selective agonists Am80 (RARα), CD2314 (RARβ) and BMS961 (RARγ); and the antagonist Ro415253...
June 19, 2017: Biochimica et Biophysica Acta
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