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https://read.qxmd.com/read/30745807/platelet-reactivity-and-circulating-platelet-derived-microvesicles-are-differently-affected-by-p2y-12-receptor-antagonists
#1
Bernadeta Chyrchel, Anna Drożdż, Dorota Długosz, Ewa Ł Stępień, Andrzej Surdacki
Background : Platelet-derived microvesicles (PMVs), shed from platelet surface membranes, constitute the majority of circulating microvesicles and have been implicated in procoagulant, pro-inflammatory and pro-atherosclerotic effects. Our aim was to compare plasma PMVs numbers in relation to platelet reactivity during dual antiplatelet therapy (DAPT) with various P2Y12 adenosine diphosphate (ADP) receptor antagonists. Methods: In pre-discharge men treated with DAPT for an acute coronary syndrome, plasma PMVs were quantified by flow cytometry on the basis of CD62P (P-selectin) and CD42 (glycoprotein Ib) positivity, putative indices of PMVs release from activated and all platelets, respectively...
2019: International Journal of Medical Sciences
https://read.qxmd.com/read/30738371/high-and-low-on-treatment-platelet-reactivity-to-p2y-12-inhibitors-in-a-contemporary-cohort-of-acute-coronary-syndrome-patients-undergoing-percutaneous-coronary-intervention
#2
José Luis Ferreiro, David Vivas, Jesús María De La Hera, Ana Lucrecia Marcano, Leslie Marisol Lugo, Juan Carlos Gómez-Polo, Iria Silva, Antonio Tello-Montoliu, Francisco Marín, Inmaculada Roldán
INTRODUCTION: There is compelling evidence supporting the association between high on-treatment platelet reactivity (HPR) and low on-treatment platelet reactivity (LPR) to clopidogrel with atherothrombotic and bleeding events, respectively. However, it is uncertain if current cutoff values should be used in prasugrel- or ticagrelor-treated subjects. The objective of this analysis was to evaluate the pharmacodynamic (PD) efficacy of P2Y12 antagonists in a contemporary real-world population...
January 31, 2019: Thrombosis Research
https://read.qxmd.com/read/30734681/structure-activity-relationship-of-4-amino-2-thiopyrimidine-derivatives-as-platelet-aggregation-inhibitors
#3
Barbara Cacciari, Pamela Crepaldi, Chun Yan Cheng, Elena Bossi, Giampiero Spalluto, Stephanie Federico, Kenneth A Jacobson, Marco Cattaneo
BACKGROUND: Platelet aggregation plays a pathogenic role in the development of arterial thrombi, which are responsible for common diseases caused by thrombotic arterial occlusion, such as myocardial infarction and stroke. Much efforts is directed toward developing platelet aggregation inhibitors that act through several mechanisms: the main antiplatelet family of COX-inhibitors, phosphodiesterase inhibitors, and thrombin inhibitors. Recently, the important role in the platelet aggregation of adenosine diphosphate (ADP)-activated P2Y12 and P2Y1 receptors, G-protein coupled receptors of the P2 purinergic family, has emerged, and their inhibitors are explored as potential therapeutic antithrombotics...
February 8, 2019: Medicinal Chemistry
https://read.qxmd.com/read/30721767/purinergic-signaling-in-the-organ-of-corti-potential-therapeutic-targets-of-sensorineural-hearing-losses
#4
REVIEW
Eszter Berekméri, Judit Szepesy, László Köles, Tibor Zelles
Purinergic signaling is deeply involved in the development, functions and protective mechanisms of the cochlea. Release of ATP and activation of purinergic receptors on sensory and supporting/epithelial cells play a substantial role in cochlear (patho)physiology. Both the ionotropic P2X and the metabotropic P2Y receptors are widely distributed on the inner and outer hair cells as well as on the different supporting cells in the organ of Corti and on other epithelial cells in the scala media. Among others, they are implicated in the sensitivity adjustment of the receptor cells by a K+ shunt and can attenuate the cochlear amplification by modifying cochlear micromechanics acting on outer hair cells and supporting cells...
February 2, 2019: Brain Research Bulletin
https://read.qxmd.com/read/30706780/insight-of-pain-modulation-nociceptors-sensitization-and-therapeutic-targets
#5
Amna Khan, Salman Khan, Yeong Shik Kim
Pain is a complex multidimensional concept that facilitates the initiation of the signaling cascade in response to any noxious stimuli. Action potential generation in the peripheral nociceptor terminal and its transmission through various types of nociceptors corresponding to mechanical, chemical or thermal stimuli leads to the activation of receptors and further neuronal processing produces sensation of pain. Numerous types of receptors are activated in pain sensation which varies in their signaling pathway...
January 30, 2019: Current Drug Targets
https://read.qxmd.com/read/30689196/a-targeted-mutation-disrupting-mitochondrial-complex-iv-function-in-primary-afferent-neurons-leads-to-pain-hypersensitivity-through-p2y-1-receptor-activation
#6
Rory Mitchell, Graham Campbell, Marta Mikolajczak, Katie McGill, Don Mahad, Sue M Fleetwood-Walker
As mitochondrial dysfunction is evident in neurodegenerative disorders that are accompanied by pain, we generated inducible mutant mice with disruption of mitochondrial respiratory chain complex IV, by COX10 deletion limited to sensory afferent neurons through the use of an Advillin Cre-reporter. COX10 deletion results in a selective energy-deficiency phenotype with minimal production of reactive oxygen species. Mutant mice showed reduced activity of mitochondrial respiratory chain complex IV in many sensory neurons, increased ADP/ATP ratios in dorsal root ganglia and dorsal spinal cord synaptoneurosomes, as well as impaired mitochondrial membrane potential, in these synaptoneurosome preparations...
January 28, 2019: Molecular Neurobiology
https://read.qxmd.com/read/30685502/switching-between-p2y-12-antagonists-from-bench-to-bedside
#7
REVIEW
Aleksandra Gasecka, Michał Konwerski, Justyna Pordzik, Aleksandra Soplińska, Krzysztof J Filipiak, Jolanta M Siller-Matula, Marek Postuła
Platelet P2Y12 receptors play a key role in platelet activation and thrombus formation. Accordingly, P2Y12 receptor antagonists are the cornerstone of secondary prevention of atherothrombotic events in patients undergoing percutaneous coronary intervention (PCI). The availability of different oral P2Y12 antagonists (clopidogrel, prasugrel, ticagrelor) along with the introduction of the first intravenous P2Y12 antagonist cangrelor offer an opportunity to individualize antiplatelet therapy according to the changing clinical setting...
January 24, 2019: Vascular Pharmacology
https://read.qxmd.com/read/30665144/studies-towards-the-development-of-a-pet-radiotracer-for-imaging-of-the-p2y-1-receptors-in-the-brain-synthesis-18-f-labeling-and-preliminary-biological-evaluation
#8
Rareş-Petru Moldovan, Barbara Wenzel, Rodrigo Teodoro, Wilma Neumann, Sladjana Dukic-Stefanovic, Werner Kraus, Peijing Rong, Winnie Deuther-Conrad, Evamarie Hey-Hawkins, Ute Krügel, Peter Brust
Purine nucleotides such as ATP and ADP are important extracellular signaling molecules in almost all tissues activating various subtypes of purinoreceptors. In the brain, the P2Y1 receptor (P2Y1 R) subtype mediates trophic functions like differentiation and proliferation, and modulates fast synaptic transmission, both suggested to be affected in diseases of the central nervous system. Research on P2Y1 R is limited because suitable brain-penetrating P2Y1 R-selective tracers are not yet available. Here, we describe the first efforts to develop an 18 F-labeled PET tracer based on the structure of the highly affine and selective, non-nucleotidic P2Y1 R allosteric modulator 1-(2-[2-(tert-butyl)phenoxy]pyridin-3-yl)-3-[4-(trifluoromethoxy)phenyl]urea (7)...
January 7, 2019: European Journal of Medicinal Chemistry
https://read.qxmd.com/read/30640576/gpr17-receptor-modulators-and-their-therapeutic-implications-review-of-recent-patents
#9
Gabriella Marucci, Diego Dal Ben, Catia Lambertucci, Aleix Martí Navia, Andrea Spinaci, Rosaria Volpini, Michela Buccioni
The GPR17 receptor, phylogenetically related to both purinergic P2Y and CysLT receptors, is mainly expressed in the CNS and, in general, in organs that can typically undergo ischemic damage. This receptor is involved in various pathologies including stroke, brain and spinal cord trauma, multiple sclerosis and in all diseases characterized by neuronal and myelin dysfunction. Therefore, there is a strong needed to identify molecules capable of binding specifically to GPR17 receptors. Areas covered: The review provides a summary of patents, published between 2009 and 2018, on chemicals and biologics and their clinical use...
January 14, 2019: Expert Opinion on Therapeutic Patents
https://read.qxmd.com/read/30636506/-no-such-thing-as-a-free-lunch-personalized-p2y-12-inhibition-to-optimize-patient-outcomes
#10
EDITORIAL
Tim Kinnaird
See Article by Crimi et al.
January 22, 2019: Journal of the American Heart Association
https://read.qxmd.com/read/30624816/experimental-polycystic-ovarian-syndrome-is-associated-with-reduced-expression-and-function-of-p2y2-receptors-in-rat-theca-cells
#11
A R Campos-Contreras, A P Juárez-Mercado, A González-Gallardo, R Chávez-Genaro, E Garay, D L De Ita-Pérez, M Díaz-Muñoz, F G Vázquez-Cuevas
Extracellular purines through specific receptors have been recognized as new regulators of ovarian function. It is known that P2Y2 receptor activity induces theca cell proliferation, we hypothesized that purinergic signaling controls the changes related with hyperthecosis in polycystic ovarian syndrome (PCOS). The aim of this study was to analyze the expression of UTP-sensitive P2Y receptors and their role in theca cells (TC) proliferation in experimentally-induced PCOS (EI-PCOS). In primary cultures of TC from intact rats, all the transcripts of P2Y receptors were detected by PCR; in these cells UTP (10 μM) induced extracellular signal-regulated kinases (ERK) phosphorylation...
January 9, 2019: Molecular Reproduction and Development
https://read.qxmd.com/read/30623372/switching-of-oral-p2y-12-inhibitor-treatment-in-patients-with-acute-coronary-syndrome-prevalence-predictors-and-prognosis
#12
Luna Carrillo-Aleman, Francisco Marín, José M Rivera-Caravaca, Nuria Vicente-Ibarra, Elena Candela-Sanchez, Maria A Esteve-Pastor, Teresa Lozano, Miriam Sandín-Rollan, Vicente Pernias-Escrig, Manuel Macías, Miriam Quintana-Giner, Andrea Veliz, Esteban Orenes-Piñero, Juan G Martínez-Martínez, Juan M Ruiz-Nodar
BACKGROUND AND OBJECTIVE: Dual antiplatelet therapy is one of the main treatments in acute coronary syndrome (ACS). Switching antiplatelet agents may be necessary in some patients to improve efficacy or safety. The objective of this study was to determine the prevalence, predictors, and implications of clinical switching in patients during hospital admission and 1-year follow-up at discharge. METHODS: Observational, prospective, multicenter registry study in patients discharged following an admission for ACS and followed up for 1 year...
January 8, 2019: Clinical Drug Investigation
https://read.qxmd.com/read/30600215/common-p2y-13-polymorphisms-are-associated-with-plasma-inhibitory-factor-1-and-lipoprotein-a-concentrations-heart-rate-and-body-fat-mass-the-genes-study
#13
Céline Verdier, Jean-Bernard Ruidavets, Annelise Genoux, Guillaume Combes, Vanina Bongard, Dorota Taraszkiewicz, Michel Galinier, Meyer Elbaz, Jean Ferrières, Laurent O Martinez, Bertrand Perret
BACKGROUND: The P2Y13 purinergic receptor regulates hepatic high-density lipoprotein uptake and biliary sterol secretion; it acts downstream of the membrane ecto-F1-adenosine triphosphatase, which generates extracellular adenosine diphosphate that selectively activates P2Y13 , resulting in high-density lipoprotein endocytosis. Previous studies have shown that the serum concentration of the F1-adenosine triphosphatase inhibitor inhibitory factor 1 is negatively associated with cardiovascular risk...
December 29, 2018: Archives of Cardiovascular Diseases
https://read.qxmd.com/read/30599217/natural-compounds-acting-at-p2-receptors-alleviate-peripheral-neuropathy
#14
REVIEW
Lifang Zou, Yingxin Gong, Shuangmei Liu, Shangdong Liang
Neuropathic pain is generally resistant to currently available treatments, and it is often a consequence of nerve injury due to surgery, diabetes or infection. Myocardial ischemic nociceptive signaling increases the sympathoexcitatory reflex to aggravate myocardial injury. Elucidation of the pathogenetic factors might provide a target for optimal treatment. Abundant evidence in the literature suggests that P2X and P2Y receptors play important roles in signal transmission. Traditional Chinese medicines, such as emodin, puerarin and resveratrol, antagonize nociceptive transmission mediated by purinergic 2 (P2) receptors in primary afferent neurons...
December 29, 2018: Brain Research Bulletin
https://read.qxmd.com/read/30593879/p2-receptor-interaction-and-signalling-cascades-in-neuroprotection
#15
REVIEW
Mª Teresa Miras-Portugal, Mª José Queipo, Juan Carlos Gil-Redondo, Felipe Ortega, Rosa Gómez-Villafuertes, Javier Gualix, Esmerilda G Delicado, Raquel Pérez-Sen
Nucleotides can contribute to the survival of different glial and neuronal models at the nervous system via activation of purinergic P2X and P2Y receptors. Their activation counteracts different proapoptotic events, such as excitotoxicity, mitochondrial impairment, oxidative stress and DNA damage, which concur to elicit cell loss in different processes of neurodegeneration and brain injury. Thus, it is frequent to find that different neuroprotective mediators converge in the activation of the same intracellular survival pathways to protect cells from death...
December 26, 2018: Brain Research Bulletin
https://read.qxmd.com/read/30582977/microglia-and-the-purinergic-signaling-system
#16
REVIEW
Stefano Calovi, Paula Mut-Arbona, Beáta Sperlágh
Microglia are the main resident immune-competent cell type of the central nervous system (CNS); these cells are highly sensitive to subtle changes in the chemical environment of the brain. Microglia are activated during diverse conditions, such as apoptosis, trauma, inflammation, and infection. The specific activities of microglia result from the confluence of environmental stimuli and the cellular state. It is likely that several signaling systems with different biological functions operate in competition and/or synergy, thus regulating similar microglial behaviors...
December 21, 2018: Neuroscience
https://read.qxmd.com/read/30560202/short-term-outcome-following-acute-phase-switch-among-p2y-12-inhibitors-in-patients-presenting-with-acute-coronary-syndrome-treated-with-pci-a-systematic-review-and-meta-analysis-including-22-500-patients-from-14-studies
#17
Enrico Cerrato, Matteo Bianco, Akshay Bagai, Leonardo De Luca, Simone Biscaglia, Alessia Luciano, Paola Destefanis, Giorgio Quadri, Ilaria Meynet, Carol Gravinese, Alessandra Chinaglia, Shaun G Goodman, Roberto Pozzi, Gianluca Campo, Ferdinando Varbella
Introduction: The efficacy and safety of switching P2Y12 receptor antagonists in patients admitted for acute coronary syndrome (ACS) remain unclear. We assessed the short-term clinical outcomes (in-hospital and within 30 days) of switching P2Y12 inhibitor (P2Y12 I) drugs versus maintaining the same regimen by performing a comprehensive review and meta-analysis of available data. Methods: MEDLINE/PubMed/SCOPUS/Cochrane databases were screened for studies regarding switching of P2Y12 I in patients with ACS that reported 30 days follow-up...
March 2019: IJC Heart & Vasculature
https://read.qxmd.com/read/30544633/altered-purinergic-receptor-sensitivity-in-type-2-diabetes-associated-endothelial-dysfunction-and-up%C3%A2-a-mediated-vascular-contraction
#18
Ali Mahdi, Tong Jiao, Yahor Tratsiakovich, Jiangning Yang, Claes-Göran Östenson, John Pernow, Zhichao Zhou
Purinergic signaling may be altered in diabetes accounting for endothelial dysfunction. Uridine adenosine tetraphosphate (Up₄A), a novel dinucleotide substance, regulates vascular function via both purinergic P1 and P2 receptors (PR). Up₄A enhances vascular contraction in isolated arteries of diabetic rats likely through P2R. However, the precise involvement of PRs in endothelial dysfunction and the vasoconstrictor response to Up₄A in diabetes has not been fully elucidated. We tested whether inhibition of PRs improved endothelial function and attenuated Up₄A-mediated vascular contraction using both aortas and mesenteric arteries of type 2 diabetic (T2D) Goto Kakizaki (GK) rats vs...
December 7, 2018: International Journal of Molecular Sciences
https://read.qxmd.com/read/30542266/astroglial-ca-2-dependent-hyperexcitability-requires-p2y-1-purinergic-receptors-and-pannexin-1-channel-activation-in-a-chronic-model-of-epilepsy
#19
Mario Wellmann, Carla Álvarez-Ferradas, Carola J Maturana, Juan C Sáez, Christian Bonansco
Astrocytes from the hippocampus of chronic epileptic rats exhibit an abnormal pattern of intracellular calcium oscillations, characterized by an augmented frequency of long lasting spontaneous Ca2+ transients, which are sensitive to purinergic receptor antagonists but resistant to tetrodotoxin. The above suggests that alterations in astroglial Ca2+ -dependent excitability observed in the epileptic tissue could arise from changes in astrocyte-to-astrocyte signaling, which is mainly mediated by purines in physiological and pathological conditions...
2018: Frontiers in Cellular Neuroscience
https://read.qxmd.com/read/30526214/new-insights-in-purinergic-therapy-novel-antagonists-for-uridine-5-triphosphate-activated-p2y-receptors-from-brazilian-flora
#20
Natiele Carla da Silva Ferreira, Rômulo José Soares-Bezerra, Rebeca Ferreira Couto da Silveira, Clayton Menezes da Silva, Carla Santos de Oliveira, Andrea Surrage Calheiros, Tânia Maria Alves, Carlos Leomar Zani, Luiz Anastacio Alves
P2Y2 and P2Y4 receptors are physiologically activated by uridine 5'-triphosphate (UTP) and are widely expressed in many cell types in humans. P2Y2 plays an important role in inflammation and proliferation of tumor cells, which could be attenuated with the use of antagonists. However, little is known about the physiological functions related to P2Y4, due to the lack of selective ligands for these receptors. This can be solved through the search for novel compounds with antagonistic activity. The aim of this study was to discover new potential antagonist candidates for P2Y2 and P2Y4 receptors from natural products...
December 8, 2018: Journal of Medicinal Food
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