P2X and P2Y Receptors
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Additions and Deletions to the Drug Product List
Prescription and Over-the-Counter Drug Product List 40TH EDITION Cumulative Supplement Number 09 : September 2020 ADDITIONS/DELETIONS FOR PRESCRIPTION DRUG PRODUCT LIST ACETAMINOPHEN; BUTALBITAL; CAFFEINE TABLET;ORAL BUTALBITAL, ACETAMINOPHEN AND CAFFEINE >A> AA STRIDES PHARMA 325MG;50MG;40MG A 203647 001 Sep 21, 2020 Sep NEWA ACETAMINOPHEN; CODEINE PHOSPHATE SOLUTION;ORAL ACETAMINOPHEN AND CODEINE PHOSPHATE >D> AA WOCKHARDT BIO AG 120MG/5ML;12MG/5ML A 087006 001 Jul 22, 1981 Sep DISC >A> @ 120MG/5ML;12MG/5ML A 087006 001 Jul 22, 1981 Sep DISC TABLET;ORAL ACETAMINOPHEN AND CODEINE PHOSPHATE >A> AA NOSTRUM LABS INC 300MG;15MG A 088627 001 Mar 06, 1985 Sep CAHN >A> AA 300MG;30MG A 088628 001 Mar 06, 1985 Sep CAHN >A> AA ! 300MG;60MG A 088629 001 Mar 06, 1985 Sep CAHN >D> AA TEVA 300MG;15MG A 088627 001 Mar 06, 1985 Sep CAHN >D> AA 300MG;30MG A 088628 001 Mar 06, 1985 Sep CAHN >D> AA ! 300MG;60MG A 088629 001 Mar 06, 1985 Sep CAHN ACETAMINOPHEN; HYDROCODONE BITARTRATE TABLET;ORAL HYDROCODONE BITARTRATE AND ACETAMINOPHEN >A> @ CEROVENE INC 325MG;5MG A 211690 001 Feb 07, 2020 Sep CAHN >A> @ 325MG;7.5MG A 211690 002 Feb 07, 2020 Sep CAHN >A> @ 325MG;10MG A 211690 003 Feb 07, 2020 Sep CAHN >D> AA VINTAGE PHARMS 300MG;5MG A 090415 001 Jan 24, 2011 Sep DISC >A> @ 300MG;5MG A 090415 001 Jan 24, 2011 Sep DISC >D> AA 300MG;7.5MG A 090415 002 Jan 24, 2011 Sep DISC >A> @ 300MG;7.5MG A 090415 002 Jan 24, 2011 Sep DISC >D> AA 300MG;10MG A 090415 003 Jan 24, 2011 Sep DISC >A> @ 300MG;10MG A 090415 003 Jan 24, 2011 Sep DISC >D> @ XIROMED 325MG;5MG A 211690 -
P2Y6 Receptors Regulate CXCL10 Expression and Secretion in Mouse Intestinal Epithelial Cells
fphar-09-00149 February 26, 2018 Time: 17:57 # 1 ORIGINAL RESEARCH published: 28 February 2018 doi: 10.3389/fphar.2018.00149 P2Y6 Receptors Regulate CXCL10 Expression and Secretion in Mouse Intestinal Epithelial Cells Mabrouka Salem1,2, Alain Tremblay2, Julie Pelletier2, Bernard Robaye3 and Jean Sévigny1,2* 1 Département de Microbiologie-Infectiologie et d’Immunologie, Faculté de Médecine, Université Laval, Québec City, QC, Canada, 2 Centre de Recherche du CHU de Québec – Université Laval, Québec City, QC, Canada, 3 Institut de Recherche Interdisciplinaire en Biologie Humaine et Moléculaire, Université Libre de Bruxelles, Gosselies, Belgium In this study, we investigated the role of extracellular nucleotides in chemokine (KC, MIP- 2, MCP-1, and CXCL10) expression and secretion by murine primary intestinal epithelial cells (IECs) with a focus on P2Y6 receptors. qRT-PCR experiments showed that P2Y6 was the dominant nucleotide receptor expressed in mouse IEC. In addition, the P2Y6 Edited by: ligand UDP induced expression and secretion of CXCL10. For the other studies, we Kenneth A. Jacobson, −=− National Institutes of Health (NIH), took advantage of mice deficient in P2Y6 (P2ry6 ). Similar expression levels of P2Y1, −=− United States P2Y2, P2X2, P2X4, and A2A were detected in P2ry6 and WT IEC. Agonists of Reviewed by: TLR3 (poly(I:C)), TLR4 (LPS), P2Y1, and P2Y2 increased the expression and secretion Fernando Ochoa-Cortes, of CXCL10 more prominently in P2ry6−=− IEC than in WT IEC. CXCL10 expression Universidad Autónoma de San Luis −=− Potosí, Mexico and secretion induced by poly(I:C) in both P2ry6 and WT IEC were inhibited by Markus Neurath, general P2 antagonists (suramin and Reactive-Blue-2), by apyrase, and by specific Universitätsklinikum Erlangen, Germany antagonists of P2Y1, P2Y2, P2Y6 (only in WT), and P2X4. -
P2Y Purinergic Receptors Regulate the Growth of Human Melanomas
Cancer Letters 224 (2005) 81–91 www.elsevier.com/locate/canlet P2Y purinergic receptors regulate the growth of human melanomas Nicholas Whitea,b, Mina Rytena, Elizabeth Claytonc, Peter Butlerb, Geoffrey Burnstocka,* aAutonomic Neuroscience Institute, Royal Free and University College Medical School, Rowland Hill Street, London NW3 2PF, UK bDepartment of Plastic and Reconstructive Surgery, Royal Free Hospital, Pond Street, London NW3 2QG, UK cRAFT Institute of Plastic Surgery, Mount Vernon Hospital, Northwood, Middlesex HA6 2RN, UK Received 3 October 2004; received in revised form 6 November 2004; accepted 9 November 2004 Abstract Adenosine 50-triphosphate is known to function as a potent extracellular messenger producing its effects via a distinct family of cell surface receptors. Different receptor subtypes have been shown to modulate different cellular functions such as proliferation, differentiation and apoptosis. We investigated the functional expression and proliferative action of metabotropic P2Y receptors in human melanoma tissue and cells. Expression of functional P2Y1, P2Y2 and P2Y6 receptor subtypes was established by reverse transcriptase polymerase chain reaction, immunohistochemistry and intracellular calcium measurements using a Fluorometric Imaging Plate Reader. Incubation of A375 melanoma cells with the P2Y1 receptor-selective agonist 2- methylthioadenosine-5-diphosphate caused a decrease in cell number which was dose-dependent, whereas incubation with the P2Y2 receptor agonist uridine triphosphate caused a dose-dependent increase in cell number. The action of extracellular nucleotides on P2Y receptors was shown to mediate the growth of melanomas and the P2Y1 receptor is a putative target for melanoma therapy. q 2004 Elsevier Ireland Ltd. All rights reserved. Keywords: Cancer; Melanoma; P2Y receptor; ATP 1. -
Lysophosphatidic Acid and Its Receptors: Pharmacology and Therapeutic Potential in Atherosclerosis and Vascular Disease
JPT-107404; No of Pages 13 Pharmacology & Therapeutics xxx (2019) xxx Contents lists available at ScienceDirect Pharmacology & Therapeutics journal homepage: www.elsevier.com/locate/pharmthera Lysophosphatidic acid and its receptors: pharmacology and therapeutic potential in atherosclerosis and vascular disease Ying Zhou a, Peter J. Little a,b, Hang T. Ta a,c, Suowen Xu d, Danielle Kamato a,b,⁎ a School of Pharmacy, University of Queensland, Pharmacy Australia Centre of Excellence, Woolloongabba, QLD 4102, Australia b Department of Pharmacy, Xinhua College of Sun Yat-sen University, Tianhe District, Guangzhou 510520, China c Australian Institute for Bioengineering and Nanotechnology, The University of Queensland, Brisbane, St Lucia, QLD 4072, Australia d Aab Cardiovascular Research Institute, Department of Medicine, University of Rochester School of Medicine and Dentistry, Rochester, NY 14642, USA article info abstract Available online xxxx Lysophosphatidic acid (LPA) is a collective name for a set of bioactive lipid species. Via six widely distributed G protein-coupled receptors (GPCRs), LPA elicits a plethora of biological responses, contributing to inflammation, Keywords: thrombosis and atherosclerosis. There have recently been considerable advances in GPCR signaling especially Lysophosphatidic acid recognition of the extended role for GPCR transactivation of tyrosine and serine/threonine kinase growth factor G-protein coupled receptors receptors. This review covers LPA signaling pathways in the light of new information. The use of transgenic and Atherosclerosis gene knockout animals, gene manipulated cells, pharmacological LPA receptor agonists and antagonists have Gproteins fi β-arrestins provided many insights into the biological signi cance of LPA and individual LPA receptors in the progression Transactivation of atherosclerosis and vascular diseases. -
P2Y Purinergic Receptors, Endothelial Dysfunction, and Cardiovascular Diseases
International Journal of Molecular Sciences Review P2Y Purinergic Receptors, Endothelial Dysfunction, and Cardiovascular Diseases Derek Strassheim 1, Alexander Verin 2, Robert Batori 2 , Hala Nijmeh 3, Nana Burns 1, Anita Kovacs-Kasa 2, Nagavedi S. Umapathy 4, Janavi Kotamarthi 5, Yash S. Gokhale 5, Vijaya Karoor 1, Kurt R. Stenmark 1,3 and Evgenia Gerasimovskaya 1,3,* 1 The Department of Medicine Cardiovascular and Pulmonary Research Laboratory, University of Colorado Denver, Aurora, CO 80045, USA; [email protected] (D.S.); [email protected] (N.B.); [email protected] (V.K.); [email protected] (K.R.S.) 2 Vascular Biology Center, Augusta University, Augusta, GA 30912, USA; [email protected] (A.V.); [email protected] (R.B.); [email protected] (A.K.-K.) 3 The Department of Pediatrics, Division of Critical Care Medicine, University of Colorado Denver, Aurora, CO 80045, USA; [email protected] 4 Center for Blood Disorders, Augusta University, Augusta, GA 30912, USA; [email protected] 5 The Department of BioMedical Engineering, University of Wisconsin, Madison, WI 53706, USA; [email protected] (J.K.); [email protected] (Y.S.G.) * Correspondence: [email protected]; Tel.: +1-303-724-5614 Received: 25 August 2020; Accepted: 15 September 2020; Published: 18 September 2020 Abstract: Purinergic G-protein-coupled receptors are ancient and the most abundant group of G-protein-coupled receptors (GPCRs). The wide distribution of purinergic receptors in the cardiovascular system, together with the expression of multiple receptor subtypes in endothelial cells (ECs) and other vascular cells demonstrates the physiological importance of the purinergic signaling system in the regulation of the cardiovascular system. -
A Comparative Study of Molecular Structure, Pka, Lipophilicity, Solubility, Absorption and Polar Surface Area of Some Antiplatelet Drugs
International Journal of Molecular Sciences Article A Comparative Study of Molecular Structure, pKa, Lipophilicity, Solubility, Absorption and Polar Surface Area of Some Antiplatelet Drugs Milan Remko 1,*, Anna Remková 2 and Ria Broer 3 1 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University in Bratislava, Odbojarov 10, SK-832 32 Bratislava, Slovakia 2 Department of Internal Medicine, Faculty of Medicine, Slovak Medical University, Limbová 12, SK–833 03 Bratislava, Slovakia; [email protected] 3 Department of Theoretical Chemistry, Zernike Institute for Advanced Materials, University of Groningen, Nijenborgh 4, 9747 AG Groningen, The Netherlands; [email protected] * Correspondence: [email protected]; Tel.: +421-2-5011-7291 Academic Editor: Michael Henein Received: 18 February 2016; Accepted: 11 March 2016; Published: 19 March 2016 Abstract: Theoretical chemistry methods have been used to study the molecular properties of antiplatelet agents (ticlopidine, clopidogrel, prasugrel, elinogrel, ticagrelor and cangrelor) and several thiol-containing active metabolites. The geometries and energies of most stable conformers of these drugs have been computed at the Becke3LYP/6-311++G(d,p) level of density functional theory. Computed dissociation constants show that the active metabolites of prodrugs (ticlopidine, clopidogrel and prasugrel) and drugs elinogrel and cangrelor are completely ionized at pH 7.4. Both ticagrelor and its active metabolite are present at pH = 7.4 in neutral undissociated form. The thienopyridine prodrugs ticlopidine, clopidogrel and prasugrel are lipophilic and insoluble in water. Their lipophilicity is very high (about 2.5–3.5 logP values). The polar surface area, with regard to the structurally-heterogeneous character of these antiplatelet drugs, is from very large interval of values of 3–255 Å2. -
NIH Public Access Author Manuscript Neuron Glia Biol
NIH Public Access Author Manuscript Neuron Glia Biol. Author manuscript; available in PMC 2006 May 1. NIH-PA Author ManuscriptPublished NIH-PA Author Manuscript in final edited NIH-PA Author Manuscript form as: Neuron Glia Biol. 2006 May ; 2(2): 125±138. Purinergic receptors activating rapid intracellular Ca2+ increases in microglia Alan R. Light1, Ying Wu2, Ronald W. Hughen1, and Peter B. Guthrie3 1 Department of Anesthesiology, University of Utah, Salt Lake City, UT, USA 2 Oral Biology Program, School of Dentistry, University of North Carolina at Chapel Hill, Chapel Hill, NC 27510, USA 3 Scientific Review Administrator, Center for Scientific Review, National Institutes of Health, 6701 Rockledge Drive, Room 4142 Msc 7850, Bethesda, MD 20892-7850, USA Abstract We provide both molecular and pharmacological evidence that the metabotropic, purinergic, P2Y6, P2Y12 and P2Y13 receptors and the ionotropic P2X4 receptor contribute strongly to the rapid calcium response caused by ATP and its analogues in mouse microglia. Real-time PCR demonstrates that the most prevalent P2 receptor in microglia is P2Y6 followed, in order, by P2X4, P2Y12, and P2X7 = P2Y13. Only very small quantities of mRNA for P2Y1, P2Y2, P2Y4, P2Y14, P2X3 and P2X5 were found. Dose-response curves of the rapid calcium response gave a potency order of: 2MeSADP>ADP=UDP=IDP=UTP>ATP>BzATP, whereas A2P4 had little effect. Pertussis toxin partially blocked responses to 2MeSADP, ADP and UDP. The P2X4 antagonist suramin, but not PPADS, significantly blocked responses to ATP. These data indicate that P2Y6, P2Y12, P2Y13 and P2X receptors mediate much of the rapid calcium responses and shape changes in microglia to low concentrations of ATP, presumably at least partly because ATP is rapidly hydrolyzed to ADP. -
Regulation and Relevance for Chronic Lung Diseases
View metadata, citation and similar papers at core.ac.uk brought to you by CORE provided by Springer - Publisher Connector Purinergic Signalling (2006) 2:399–408 DOI 10.1007/s11302-006-9001-7 ORIGINAL ARTICLE E-NTPDases in human airways: Regulation and relevance for chronic lung diseases Lauranell H. Burch & Maryse Picher Received: 11 January 2005 /Accepted: 21 December 2005 / Published online: 30 May 2006 # Springer Science + Business Media B.V. 2006 Abstract Chronic obstructive lung diseases are char- are characterized by higher rates of nucleotide elimi- acterized by the inability to prevent bacterial infection nation, azide-sensitive E-NTPDase activities and ex- and a gradual loss of lung function caused by recurrent pression. This review integrates the biphasic regulation inflammatory responses. In the past decade, numerous of airway E-NTPDases with the function of purine studies have demonstrated the importance of nucleo- signaling in lung diseases. During acute insults, a tide-mediated bacterial clearance. Their interaction transient reduction in E-NTPDase activities may be with P2 receptors on airway epithelia provides a rapid beneficial to stimulate ATP-mediated bacterial clear- Fon-and-off_ signal stimulating mucus secretion, cilia ance. In chronic lung diseases, elevating E-NTPDase beating activity and surface hydration. On the other activities may represent an attempt to prevent P2 hand, abnormally high ATP levels resulting from receptor desensitization and nucleotide-mediated lung damaged epithelia and bacterial lysis may cause lung damage. edema and exacerbate inflammatory responses. Air- way ATP concentrations are regulated by ecto nucle- Keywords apyrase . bacterial clearance . CD39 . oside triphosphate diphosphohydrolases (E-NTPDases) chronic obstructive lung diseases . -
PHARMACEUTICAL APPENDIX to the TARIFF SCHEDULE 2 Table 1
Harmonized Tariff Schedule of the United States (2020) Revision 19 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2020) Revision 19 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names INN which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service CAS registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. -
Health and Social Outcomes Associated with High-Risk Alcohol Use
Manitoba Centre for Health Policy Health and Social Outcomes Associated with High-Risk Alcohol Use Summer 2018 Nathan C Nickel, MPH, PhD Jeff Valdivia, MNRM, CAPM Deepa Singal, PhD James Bolton, MD Christine Leong, PharmD Susan Burchill, BMus Leonard MacWilliam, MSc, MNRM Geoffrey Konrad, MD Randy Walld, BSc, BComm (Hons) Okechukwu Ekuma, MSc Greg Finlayson, PhD Leanne Rajotte, BComm (Hons) Heather Prior, MSc Josh Nepon, MD Michael Paille, BHSc This report is produced and published by the Manitoba Centre for Health Policy (MCHP). It is also available in PDF format on our website at: http://mchp-appserv.cpe.umanitoba.ca/deliverablesList.html Information concerning this report or any other report produced by MCHP can be obtained by contacting: Manitoba Centre for Health Policy Rady Faculty of Health Sciences Max Rady College of Medicine, University of Manitoba 4th Floor, Room 408 727 McDermot Avenue Winnipeg, Manitoba, Canada R3E 3P5 Email: [email protected] Phone: (204) 789-3819 Fax: (204) 789-3910 How to cite this report: Nathan C Nickel, James Bolton, Leonard MacWilliam, Okechukwu Ekuma, Heather Prior, Jeff Valdivia, Christine Leong, Geoffrey Konrad, Greg Finlayson, Josh Nepon, Deepa Singal, Susan Burchill, Randy Walld, Leanne Rajotte, Michael Paille. Health and Social Outcomes Associated with High-Risk Alcohol Use. Winnipeg, MB. Manitoba Centre for Health Policy, Summer 2018. Legal Deposit: Manitoba Legislative Library National Library of Canada ISBN 978-1-896489-90-2 ©Manitoba Health This report may be reproduced, in whole or in part, provided the source is cited. 1st printing (Summer 2018) This report was prepared at the request of Manitoba Health, Seniors and Active Living (MHSAL), a department within the Government of Manitoba, as part of the contract between the University of Manitoba and MHSAL. -
NIH Public Access Author Manuscript J Med Chem
NIH Public Access Author Manuscript J Med Chem. Author manuscript; available in PMC 2012 June 23. NIH-PA Author ManuscriptPublished NIH-PA Author Manuscript in final edited NIH-PA Author Manuscript form as: J Med Chem. 2011 June 23; 54(12): 4018±4033. doi:10.1021/jm101591j. Pyrimidine Nucleotides with 4-Alkyloxyimino and Terminal Tetraphosphate δ-Ester Modifications as Selective Agonists of the P2Y4 Receptor Hiroshi Maruokaa, M.P. Suresh Jayasekaraa, Matthew O. Barrettb, Derek A. Franklinb, Sonia de Castroa, Nathaniel Kima, Stefano Costanzic, T. Kendall Hardenb, and Kenneth A. Jacobsona,* aMolecular Recognition Section, Laboratory of Bioorganic Chemistry, NIDDK, National Institutes of Health, Bethesda, Maryland 20892-0810 bDepartment of Pharmacology, University of North Carolina, School of Medicine, Chapel Hill, North Carolina 27599-7365 cLaboratory of Biological Modeling, NIDDK, National Institutes of Health, Bethesda, Maryland 20892 Abstract P2Y2 and P2Y4 receptors are G protein-coupled receptors, activated by UTP and dinucleoside tetraphosphates, which are difficult to distinguish pharmacologically for lack of potent and selective ligands. We varied structurally phosphate and uracil moieties in analogues of pyrimidine nucleoside 5′-triphosphates and 5′-tetraphosphate esters. P2Y4 receptor potency in phospholipase C stimulation in transfected 1321N1 human astrocytoma cells was enhanced in N4- alkyloxycytidine derivatives. OH groups on a terminal δ-glucose phosphoester of uridine 5′- tetraphosphate were inverted or substituted with H or F to probe H-bonding effects. N4- 4 (Phenylpropoxy)-CTP 16 (MRS4062), Up4-[1]3′-deoxy-3′-fluoroglucose 34 (MRS2927) and N - (phenylethoxy)-CTP 15 exhibit ≥10-fold selectivity for human P2Y4 over P2Y2 and P2Y6 receptors (EC50 values 23, 62 and 73 nM, respectively). -
Mechanisms for the Regulation of Pro-Death
MECHANISMS FOR THE REGULATION OF PRO-DEATH GLYCERALDEHYDE-3-PHOSPHATE DEHYDROGENASE NUCLEAR ACCUMULATION IN RETINAL MÜLLER CELLS UNDER HIGH GLUCOSE CONDITIONS By E. CHEPCHUMBA KOECH YEGO Submitted in partial fulfillment of the requirements For the degree of Doctor of Philosophy Dissertation Advisor: Susanne Mohr, PhD Department of Physiology and Biophysics CASE WESTERN RESERVE UNIVERSITY May, 2010 2 CASE WESTERN RESERVE UNIVERSITY SCHOOL OF GRADUATE STUDIES We hereby approve the thesis/dissertation of ____E Chepchumba Koech Yego______________________ candidate for the _____Doctor of Philosophy (PhD)________degree *. (signed) _____Corey Smith _________ (chair of the committee) __________Cathleen Carlin__________ ______________ __________Joseph LaManna_______ ____________ __________Carole Liedtke _______________________ __________Andrea Romani_________________________ __________Michael Simonson _ _ ________ Susanne Mohr _________ (date) _____March 11th, 2010______________ *We also certify that written approval has been obtained for any proprietary material contained therein. 3 Dedication This dissertation is dedicated to my grandparents Mark Tireito *, Dinah Tireito *, Asbel Cheruiyot, Hannah Cheruiyot*, and John Korir. *Deceased 4 TABLE OF CONTENTS Dedication .......................................................................................... 3 List of Figures ..................................................................................... 8 List of Tables ...................................................................................