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Pharmacology and physiology

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https://www.readbyqxmd.com/read/28108482/inhibition-of-prolyl-4-hydroxylase-decreases-muscle-fibrosis-following-chronic-rotator-cuff-tear
#1
J P Gumucio, M D Flood, A Bedi, H F Kramer, A J Russell, C L Mendias
OBJECTIVES: Rotator cuff tears are among the most frequent upper extremity injuries. Current treatment strategies do not address the poor quality of the muscle and tendon following chronic rotator cuff tears. Hypoxia-inducible factor-1 alpha (HIF-1α) is a transcription factor that activates many genes that are important in skeletal muscle regeneration. HIF-1α is inhibited under normal physiological conditions by the HIF prolyl 4-hydroxylases (PHDs). In this study, we used a pharmacological PHD inhibitor, GSK1120360A, to enhance the activity of HIF-1α following the repair of a chronic cuff tear, and measured muscle fibre contractility, fibrosis, gene expression, and enthesis mechanics...
January 2017: Bone & Joint Research
https://www.readbyqxmd.com/read/28108129/cardiovascular-impact-in-patients-undergoing-maintenance-hemodialysis-clinical-management-considerations
#2
REVIEW
Srisakul Chirakarnjanakorn, Sankar D Navaneethan, Gary S Francis, W H Wilson Tang
Patients undergoing maintenance hemodialysis develop both structural and functional cardiovascular abnormalities. Despite improvement of dialysis technology, cardiovascular mortality of this population remains high. The pathophysiological mechanisms of these changes are complex and not well understood. It has been postulated that several non-traditional, uremic-related risk factors, especially the long-term uremic state, which may affect the cardiovascular system. There are many cardiovascular changes that occur in chronic kidney disease including left ventricular hypertrophy, myocardial fibrosis, microvascular disease, accelerated atherosclerosis and arteriosclerosis...
January 4, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28107717/diclofenac-can-exhibit-estrogenic-modes-of-action-in-male-xenopus-laevis-and-affects-the-hypothalamus-pituitary-gonad-axis-and-mating-vocalizations
#3
Norah Johanna Efosa, Wibke Kleiner, Werner Kloas, Frauke Hoffmann
Diclofenac (DCF) is a non-steroidal analgesic and antiphlogistic. Due to its tremendous use, DCF can be found in the environment, especially in sewage, but also surface waters, ground and drinking water. Previous studies indicated that DCF can modulate the reproductive physiology of fish by altering the expression of important key enzymes of the hypothalamus-pituitary-gonad-axis (HPG-axis) and might act as an estrogenic endocrine disrupting chemical (EDC). Other studies, however, demonstrated that DCF does not exhibit any estrogenicity...
January 6, 2017: Chemosphere
https://www.readbyqxmd.com/read/28106668/primidone-inhibits-trpm3-and-attenuates-thermal-nociception-in-vivo
#4
Ute Krügel, Isabelle Straub, Holger Beckmann, Michael Schaefer
The melastatin-related transient receptor potential channel TRPM3 is a nonselective cation channel expressed in nociceptive neurons and activated by heat. Since TRPM3-deficient mice show inflammatory thermal hyperalgesia, pharmacological inhibition of TRPM3 may exert antinociceptive properties. Fluorometric Ca influx assays and a compound library containing approved or clinically tested drugs were used to identify TRPM3 inhibitors. Biophysical properties of channel inhibition were assessed using electrophysiological methods...
January 12, 2017: Pain
https://www.readbyqxmd.com/read/28105791/the-future-of-pleiotropic-therapy-in-heart-failure-lessons-from-the-benefits-of-exercise-training-on-endothelial-function
#5
REVIEW
Gilles W De Keulenaer, Vincent F M Segers, Faiez Zannad, Dirk L Brutsaert
A novel generation of drugs is introduced in the treatment of heart failure (HF). These drugs, including phosphodiesterase-5 inhibitors, guanylate cyclase stimulators and activators, share the feature that their action is either endothelial-mediated or substitutes for endothelial pathways, in particular the nitric oxide-cyclic guanosine monophosphate pathway, thereby influencing homeostatic balances in virtually each organ system in a pleiotropic fashion. Unfortunately, recent clinical trials with some of these drugs have shown disappointing results, at least in the setting of HF with a preserved ejection fraction...
January 19, 2017: European Journal of Heart Failure
https://www.readbyqxmd.com/read/28105152/evaluation-by-quantitative-image-analysis-of-anticancer-drug-activity-on-multicellular-spheroids-grown-in-3d-matrices
#6
Aurélie Gomes, Adrien Russo, Guillaume Vidal, Elise Demange, Pauline Pannetier, Zied Souguir, Jean-Michel Lagarde, Bernard Ducommun, Valérie Lobjois
Pharmacological evaluation of anticancer drugs using 3D in vitro models provides invaluable information for predicting in vivo activity. Artificial matrices are currently available that scale up and increase the power of such 3D models. The aim of the present study was to propose an efficient and robust imaging and analysis pipeline to assess with quantitative parameters the efficacy of a particular cytotoxic drug. HCT116 colorectal adenocarcinoma tumor cell multispheres were grown in a 3D physiological hyaluronic acid matrix...
December 2016: Oncology Letters
https://www.readbyqxmd.com/read/28104407/metabotropic-glutamate-and-gaba-receptors-modulate-cellular-excitability-and-glutamatergic-transmission-in-chicken-cochlear-nucleus-angularis-neurons
#7
Wei Shi, Yong Lu
Neurons in the avian cochlear nucleus angularis (NA) receive glutamatergic input from the auditory nerve, and GABAergic input from the superior olivary nucleus. Physiologically heterogeneous, NA neurons perform multiple functions including encoding sound intensity information. Using in vitro whole-cell patch recordings from acute brain slices and immunohistochemistry staining, we investigated neuromodulation mediated by metabotropic glutamate and GABA receptors (mGluRs and GABABRs) in NA neurons. Based on their intrinsic firing patterns in response to somatic current injections, NA neurons were classified into one-spike (onset), damped, and tonic cells...
January 16, 2017: Hearing Research
https://www.readbyqxmd.com/read/28103441/enantio-specific-allosteric-modulation-of-cannabinoid-1-receptor
#8
Robert B Laprairie, Pushkar M Kulkarni, Jeffrey R Deschamps, Melanie E M Kelly, David R Janero, Maria G Cascio, Lesley A Stevenson, Roger G Pertwee, Terry Kenakin, Eileen M Denovan-Wright, Ganesh A Thakur
The cannabinoid 1 receptor (CB1R) is one of the most widely expressed metabotropic G protein-coupled receptors in brain, and its participation in various (patho)physiological processes has made CB1R activation a viable therapeutic modality. Adverse psychotropic effects limit the clinical utility of CB1R orthosteric agonists and have promoted the search for CB1R positive allosteric modulators (PAMs) with the promise of improved drug-like pharmacology and enhanced safety over typical CB1R agonists. In this study, we describe the synthesis and in vitro and ex vivo pharmacology of the novel allosteric CB1R modulator GAT211 (racemic) and its resolved enantiomers, GAT228 (R) and GAT229 (S)...
January 19, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28102910/arabidopsis-phosphoinositide-specific-phospholipase-c-4-negatively-regulates-seedling-salt-tolerance
#9
Keke Xia, Bo Wang, Jiewei Zhang, Yuan Li, Hailian Yang, Dongtao Ren
Previous physiological and pharmacological studies have suggested that the activity of phosphoinositide-specific phospholipase C (PI-PLC) plays an important role in regulating plant salt stress responses by altering the intracellular Ca(2+) concentration. However, the individual members of plant PLCs involved in this process need to be identified. Here, the function of AtPLC4 in the salt stress response of Arabidopsis seedlings was analyzed. plc4 mutant seedlings showed hyposensitivity to salt stress compared with Col-0 wild-type seedlings, and the salt hyposensitive phenotype could be complemented by the expression of native promoter-controlled AtPLC4...
January 19, 2017: Plant, Cell & Environment
https://www.readbyqxmd.com/read/28102470/neuronal-ryanodine-receptors-in-development-and-aging
#10
REVIEW
Nawaf Abu-Omar, Jogita Das, Vivian Szeto, Zhong-Ping Feng
Ryanodine receptors (RyRs) are intracellular calcium-release channels found on the endoplasmic reticulum of all cells. All three RyR isoforms, RyR1-3, are expressed in the brain, with RyR2 predominating. RyRs are localized within the soma, axons, dendritic spines, and presynaptic terminals of neurons. RyRs are highly expressed in the cerebellum, hippocampus, olfactory region, basal ganglia, and cerebral cortex. During the physiological processes of development and aging, the intracellular calcium homeostasis is largely regulated by RyRs...
January 19, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28100881/transporters-for-the-intestinal-absorption-of-cholesterol-vitamin-e-and-vitamin-k
#11
Yoshihide Yamanashi, Tappei Takada, Ryoya Kurauchi, Yusuke Tanaka, Toko Komine, Hiroshi Suzuki
Humans cannot synthesize fat-soluble vitamins such as vitamin E and vitamin K. For this reason, they must be obtained from the diet via intestinal absorption. As the deficiency or excess of these vitamins has been reported to cause several types of diseases and disorders in humans, the intestinal absorption of these nutrients must be properly regulated to ensure good health. However, the mechanism of their intestinal absorption remains poorly understood. Recent studies on cholesterol using genome-edited mice, genome-wide association approaches, gene mutation analyses, and the development of cholesterol absorption inhibitors have revealed that several membrane proteins play crucial roles in the intestinal absorption of cholesterol...
January 17, 2017: Journal of Atherosclerosis and Thrombosis
https://www.readbyqxmd.com/read/28100828/an-integrated-modelling-framework-for-neural-circuits-with-multiple-neuromodulators
#12
Alok Joshi, Vahab Youssofzadeh, Vinith Vemana, T M McGinnity, Girijesh Prasad, KongFatt Wong-Lin
Neuromodulators are endogenous neurochemicals that regulate biophysical and biochemical processes, which control brain function and behaviour, and are often the targets of neuropharmacological drugs. Neuromodulator effects are generally complex partly owing to the involvement of broad innervation, co-release of neuromodulators, complex intra- and extrasynaptic mechanism, existence of multiple receptor subtypes and high interconnectivity within the brain. In this work, we propose an efficient yet sufficiently realistic computational neural modelling framework to study some of these complex behaviours...
January 2017: Journal of the Royal Society, Interface
https://www.readbyqxmd.com/read/28100277/stress-echo-2020-the-international-stress-echo-study-in-ischemic-and-non-ischemic-heart-disease
#13
Eugenio Picano, Quirino Ciampi, Rodolfo Citro, Antonello D'Andrea, Maria Chiara Scali, Lauro Cortigiani, Iacopo Olivotto, Fabio Mori, Maurizio Galderisi, Marco Fabio Costantino, Lorenza Pratali, Giovanni Di Salvo, Eduardo Bossone, Francesco Ferrara, Luna Gargani, Fausto Rigo, Nicola Gaibazzi, Giuseppe Limongelli, Giuseppe Pacileo, Maria Grazia Andreassi, Bruno Pinamonti, Laura Massa, Marco A R Torres, Marcelo H Miglioranza, Clarissa Borguezan Daros, José Luis de Castro E Silva Pretto, Branko Beleslin, Ana Djordjevic-Dikic, Albert Varga, Attila Palinkas, Gergely Agoston, Dario Gregori, Paolo Trambaiolo, Sergio Severino, Ayana Arystan, Marco Paterni, Clara Carpeggiani, Paolo Colonna
BACKGROUND: Stress echocardiography (SE) has an established role in evidence-based guidelines, but recently its breadth and variety of applications have extended well beyond coronary artery disease (CAD). We lack a prospective research study of SE applications, in and beyond CAD, also considering a variety of signs in addition to regional wall motion abnormalities. METHODS: In a prospective, multicenter, international, observational study design, > 100 certified high-volume SE labs (initially from Italy, Brazil, Hungary, and Serbia) will be networked with an organized system of clinical, laboratory and imaging data collection at the time of physical or pharmacological SE, with structured follow-up information...
January 18, 2017: Cardiovascular Ultrasound
https://www.readbyqxmd.com/read/28099880/modifications-of-inhibitory-transmission-onto-pyramidal-neurons-by-postnatal-exposure-to-mk-801-effects-of-enriched-environment
#14
Amir Shojaei, Afsaneh Kamali Anaraki, Javad Mirnajafi-Zadeh, Nafiseh Atapour
Early enriched environment (EE) prevents several deficits associated with postnatal MK-801 [N-Methyl-D-Aspartate (NMDA) receptor antagonist] treatment such as cognitive and locomotor deficits. We sought physiological correlates to such changes by looking at inhibitory synaptic inputs onto pyramidal cells in a prefrontal cortex slice preparation. Pharmacologically isolated γ-amino-butyric acid A (GABAA) receptor-mediated currents were measured using whole-cell patch clamp recordings. Wistar rats were raised in standard or EE from birth up to the time of experiments and were injected with saline or MK-801 (1mg/kg) on postnatal days (P) 6-10...
January 15, 2017: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28098152/human-farnesyl-pyrophosphate-synthase-is-allosterically-inhibited-by-its-own-product
#15
Jaeok Park, Michal Zielinski, Alexandr Magder, Youla S Tsantrizos, Albert M Berghuis
Farnesyl pyrophosphate synthase (FPPS) is an enzyme of the mevalonate pathway and a well-established therapeutic target. Recent research has focused around a newly identified druggable pocket near the enzyme's active site. Pharmacological exploitation of this pocket is deemed promising; however, its natural biological function, if any, is yet unknown. Here we report that the product of FPPS, farnesyl pyrophosphate (FPP), can bind to this pocket and lock the enzyme in an inactive state. The Kd for this binding is 5-6 μM, within a catalytically relevant range...
January 18, 2017: Nature Communications
https://www.readbyqxmd.com/read/28096356/active-mlkl-triggers-the-nlrp3-inflammasome-in-a-cell-intrinsic-manner
#16
Stephanie A Conos, Kaiwen W Chen, Dominic De Nardo, Hideki Hara, Lachlan Whitehead, Gabriel Núñez, Seth L Masters, James M Murphy, Kate Schroder, David L Vaux, Kate E Lawlor, Lisa M Lindqvist, James E Vince
Necroptosis is a physiological cell suicide mechanism initiated by receptor-interacting protein kinase-3 (RIPK3) phosphorylation of mixed-lineage kinase domain-like protein (MLKL), which results in disruption of the plasma membrane. Necroptotic cell lysis, and resultant release of proinflammatory mediators, is thought to cause inflammation in necroptotic disease models. However, we previously showed that MLKL signaling can also promote inflammation by activating the nucleotide-binding oligomerization domain (NOD)-like receptor protein 3 (NLRP3) inflammasome to recruit the adaptor protein apoptosis-associated speck-like protein containing a caspase activation and recruitment domain (ASC) and trigger caspase-1 processing of the proinflammatory cytokine IL-1β...
January 17, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28096255/sheppheartcabg-trial-comprehensive-early-rehabilitation-after-coronary-artery-bypass-grafting-a-protocol-for-a-randomised-clinical-trial
#17
Ida Elisabeth Højskov, Philip Moons, Niels Viggo Hansen, Søren La Cour, Peter Skov Olsen, Christian Gluud, Per Winkel, Jane Lindschou, Lau Caspar Thygesen, Ingrid Egerod, Selina Kikkenborg Berg
INTRODUCTION: Patients undergoing coronary artery bypass graft surgery often experience a range of symptoms. Studies indicate that non-pharmacological interventions such as exercise training and psychoeducation have a positive physiological and psychological effect in early outpatient rehabilitation. The SheppHeartCABG trial will investigate the effect of early comprehensive rehabilitation in early phase rehabilitation versus usual care. The aim of this paper is to present the protocol for the SheppHeartCABG trial...
January 17, 2017: BMJ Open
https://www.readbyqxmd.com/read/28095860/mouse-models-of-atherosclerosis-a-historical-perspective-and-recent-advances
#18
REVIEW
Yee Ting Lee, Hiu Yu Lin, Yin Wah Fiona Chan, Ka Hou Christien Li, Olivia Tsz Ling To, Bryan P Yan, Tong Liu, Guangping Li, Wing Tak Wong, Wendy Keung, Gary Tse
Atherosclerosis represents a significant cause of morbidity and mortality in both the developed and developing countries. Animal models of atherosclerosis have served as valuable tools for providing insights on its aetiology, pathophysiology and complications. They can be used for invasive interrogation of physiological function and provide a platform for testing the efficacy and safety of different pharmacological therapies. Compared to studies using human subjects, animal models have the advantages of being easier to manage, with controllable diet and environmental risk factors...
January 17, 2017: Lipids in Health and Disease
https://www.readbyqxmd.com/read/28095752/isolation-and-identification-of-a-humantrpv1-activating-compound-from-soy-sauce
#19
Mayu Oshida, Yasunori Matsuura, Shinnosuke Hotta, Jun Watanabe, Yoshinobu Mogi, Tatsuo Watanabe
Transient receptor potential vanilloid 1 (TRPV1) was identified as a receptor of capsaicin, which is a pungent ingredient in hot red peppers. Due to its relevance for nociception, a physiological and pharmacological study of TRPV1 has also been developed. Therefore, it is important to enrich scientific knowledge regarding the TRPV1 activating or inhibiting compounds. In this study, we fractionated soy sauce based on the human TRPV1 (hTRPV1) activity using column chromatography and purified 5-(9H-pyrido[3,4-b]indol-1-yl)-2-furanmethanol (perlolyrine) as an hTRPV1-activating compound...
January 18, 2017: Bioscience, Biotechnology, and Biochemistry
https://www.readbyqxmd.com/read/28095616/using-xenopus-to-understand-human-disease-and-developmental-disorders
#20
REVIEW
Amy Sater, Sally A Moody
Model animals are crucial to biomedical research. Among the commonly used model animals, the amphibian, Xenopus, has had tremendous impact because of its unique experimental advantages, cost effectiveness, and close evolutionary relationship with mammals as a tetrapod. Over the past 50 years the use of Xenopus has made possible many fundamental contributions to biomedicine, and it is a cornerstone of research in cell biology, developmental biology, evolutionary biology, immunology, molecular biology, neurobiology, and physiology...
January 17, 2017: Genesis: the Journal of Genetics and Development
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