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CORE Metadata, citation and similar papers at core.ac.uk Provided by Radboud Repository PDF hosted at the Radboud Repository of the Radboud University Nijmegen The following full text is a publisher's version. For additional information about this publication click this link. http://hdl.handle.net/2066/86683 Please be advised that this information was generated on 2017-12-06 and may be subject to change. OBSTETR GYNEC European Journal of Obstetrics & Gynecology ELSEV and Reproductive Biology 61 (1995) 171-173 Case report Critical limb ischemia after accidental subcutaneous infusion of sulprostone Yvonne W.C.M. de Koninga, Peter W. Plaisierb, I. Leng Tanc, Fred K. Lotgering*a aDepartment o f Obstetrics and Gynaecology, Erasmus University, School o f Medicine and Health Sciences, EUR EE 2283, P.O. Box 1738, 3000 DR Rotterdam, The Netherlands bDepartment o f General Surgery, Erasmus University, School o f Medicine and Health Sciences, EUR EE 2283, P.O. Box 1738, 3000 DR Rotterdam, The Netherlands cDepartment o f Radiology, Erasmus University, School o f Medicine and Health Sciences, EUR EE 2283, P.O. Box 1738, 3000 DR Rotterdam, The Netherlands Received 23 September 1994; accepted 20 January 1995 Abstract A 34-year-old patient was treated with constant intravenous infusion of sulprostone because of postpartum hemorrhage from a hypotonic uterus. The arm in which sulprostone had been infused was painful 23 h after infusion. A day later, the arm was found to be blueish, edematous and extremely painful as a result of arterial spasm. The vasospasm was probably caused by accidental subcutaneous infusion of sulprostone as a result of a displaced intravenous catheter. -
Structure-Based Discovery of Mpges-1 Inhibitors Suitable For
www.nature.com/scientificreports OPEN Structure-based discovery of mPGES-1 inhibitors suitable for preclinical testing in wild-type Received: 4 January 2018 Accepted: 9 March 2018 mice as a new generation of anti- Published: xx xx xxxx infammatory drugs Kai Ding1,2,3, Ziyuan Zhou1,2, Shurong Hou2, Yaxia Yuan1,2,4, Shuo Zhou1,2, Xirong Zheng2, Jianzhong Chen1,2, Charles Loftin2, Fang Zheng1,2 & Chang-Guo Zhan1,2,4 Human mPGES-1 is recognized as a promising target for next generation of anti-infammatory drugs without the side efects of currently available anti-infammatory drugs, and various inhibitors have been reported in the literature. However, none of the reported potent inhibitors of human mPGES-1 has shown to be also a potent inhibitor of mouse or rat mPGES-1, which prevents using the well-established mouse/rat models of infammation-related diseases for preclinical studies. Hence, despite of extensive eforts to design and discover various human mPGES-1 inhibitors, the promise of mPGES-1 as a target for the next generation of anti-infammatory drugs has never been demonstrated in any wild-type mouse/rat model using an mPGES-1 inhibitor. Here we report discovery of a novel type of selective mPGES-1 inhibitors potent for both human and mouse mPGES-1 enzymes through structure-based rational design. Based on in vivo studies using wild-type mice, the lead compound is indeed non-toxic, orally bioavailable, and more potent in decreasing the PGE2 (an infammatory marker) levels compared to the currently available drug celecoxib. This is the frst demonstration in wild-type mice that mPGES-1 is truly a promising target for the next generation of anti-infammatory drugs. -
Antiluteogenic Effects of Serial Prostaglandin F2α Administration in Mares
ANTILUTEOGENIC EFFECTS OF SERIAL PROSTAGLANDIN F2α ADMINISTRATION IN MARES Thesis Presented in partial fulfillment of the requirements for the Master of Science in the Graduate School of The Ohio State University Elizabeth Ann Coffman Graduate ProGram in Comparative and Veterinary Medicine The Ohio State University 2013 Thesis committee: Carlos R.F. Pinto PhD, MV, DACT; Dissertation Advisor Marco A. Coutinho da Silva PhD, MV, DACT; Academic Advisor Christopher Premanandan PhD, DVM, DACVP Copyright by Elizabeth Ann Coffman 2013 Abstract For breedinG manaGement and estrus synchronization, prostaGlandin F2α (PGF) is one of the most commonly utilized hormones to pharmacologically manipulate the equine estrous cycle. There is a general supposition a sinGle dose of PGF does not consistently induce luteolysis in the equine corpus luteum (CL) until at least five to six days after ovulation. This leads to the erroneous assumption that the early CL (before day five after ovulation) is refractory to the luteolytic effects of PGF. An experiment was desiGned to test the hypotheses that serial administration of PGF in early diestrus would induce a return to estrus similar to mares treated with a sinGle injection in mid diestrus, and fertility of the induced estrus for the two treatment groups would not differ. The specific objectives of the study were to evaluate the effects of early diestrus treatment by: 1) assessing the luteal function as reflected by hormone profile for concentration of plasma progesterone; 2) determininG the duration of interovulatory and treatment to ovulation intervals; 3) comparing of the number of pregnant mares at 14 days post- ovulation. The study consisted of a balanced crossover desiGn in which reproductively normal Quarter horse mares (n=10) were exposed to two treatments ii on consecutive reproductive cycles. -
Effect of Prostanoids on Human Platelet Function: an Overview
International Journal of Molecular Sciences Review Effect of Prostanoids on Human Platelet Function: An Overview Steffen Braune, Jan-Heiner Küpper and Friedrich Jung * Institute of Biotechnology, Molecular Cell Biology, Brandenburg University of Technology, 01968 Senftenberg, Germany; steff[email protected] (S.B.); [email protected] (J.-H.K.) * Correspondence: [email protected] Received: 23 October 2020; Accepted: 23 November 2020; Published: 27 November 2020 Abstract: Prostanoids are bioactive lipid mediators and take part in many physiological and pathophysiological processes in practically every organ, tissue and cell, including the vascular, renal, gastrointestinal and reproductive systems. In this review, we focus on their influence on platelets, which are key elements in thrombosis and hemostasis. The function of platelets is influenced by mediators in the blood and the vascular wall. Activated platelets aggregate and release bioactive substances, thereby activating further neighbored platelets, which finally can lead to the formation of thrombi. Prostanoids regulate the function of blood platelets by both activating or inhibiting and so are involved in hemostasis. Each prostanoid has a unique activity profile and, thus, a specific profile of action. This article reviews the effects of the following prostanoids: prostaglandin-D2 (PGD2), prostaglandin-E1, -E2 and E3 (PGE1, PGE2, PGE3), prostaglandin F2α (PGF2α), prostacyclin (PGI2) and thromboxane-A2 (TXA2) on platelet activation and aggregation via their respective receptors. Keywords: prostacyclin; thromboxane; prostaglandin; platelets 1. Introduction Hemostasis is a complex process that requires the interplay of multiple physiological pathways. Cellular and molecular mechanisms interact to stop bleedings of injured blood vessels or to seal denuded sub-endothelium with localized clot formation (Figure1). -
Medical Management of First-Trimester Induced Abortion and Miscarriage
PACE REVIEW Medical management of first-trimester induced abortion and miscarriage Shamim Amis Jonathon Evans-Jones MRCOG FKCOG urgical evacuation is the mainstay of treatment in the effects of bleeding per vaginum, diarrhoea and vomiting. In UK for first-trimester termination of pregnancy and a randomised trial, where 1 mg versus 0.5 mg of gemeprost Smiscarriage and, although a niinor procedure, it has an was compared, the complete abortion rate was similar for associated considerable morbidity and mortality.' Induced the two groups (98-100%), although the incidence of abortion in the UK is now a safe procedure but on a global adverse effects was significantly lower in the latter group.'O scale continues to be a major cause of maternal mortality.2 Misoprosto1 is a synthetic analogue of prostaglandin E, and Medical management would provide a safe and effective causes increased uterine contractility with a low incidence of alternative. Many women would prefer to be given the other unwanted effects." The main advantages over choice and avoid the risks associated with anaesthesia and gemeprost are that it does not require refngeration, is cheaper surgery.l Recent studies have confirmed high acceptability and can be administered orally or vaginally. One gemeprost rates, showing that 8496% of women would choose pessary costs &22, whereas the equivalent dose of misoprostol medical treatment for a subsequent abortion." is just over The uterotonic properties are enkanced if women are pretreated with rmfepristone, reflecting the effect BACKGROUND of antiprogesterones in increasing sensitivity to prostaglandins. The drugs used for medically induced abortion in the UK When misoprostol is used in combination with mifepristone, include an antiprogesterone,mifepristone, and several prost- the vaginal route has been shown to be superior to the onl aglandin analogues, including gemeprost and misoprostol. -
Misoprostol Induces Relaxation of Human Corpus Cavernosum Smooth Muscle: Comparison to Prostaglandin E1
International Journal of Impotence Research (2000) 12, 107±110 ß 2000 Macmillan Publishers Ltd All rights reserved 0955-9930/00 $15.00 www.nature.com/ijir Misoprostol induces relaxation of human corpus cavernosum smooth muscle: comparison to prostaglandin E1 RB Moreland1, NN Kim1, A Nehra2, BG Parulkar3 and A Traish1,4* 1Department of Urology, Boston University School of Medicine, Boston, MA 02118, USA; 2Department of Urology, Mayo Clinic and Foundation, Rochester, MN 55905, USA; 3Department of Urology, University of Massachusetts Medical Center, Worcester, MA 01604, USA; and 4Department of Biochemistry, Boston University School of Medicine, Boston, MA 02118, USA Prostaglandin E1 (PGE1) relaxes trabecular smooth muscle by interacting with speci®c G-protein coupled receptors on human corpus cavernosum smooth muscle and increasing intracellular synthesis of cAMP. Misoprostol (CytotecTM), is an oral prostaglandin E analogue. The purpose of this study was to compare the functional activity of misoprostol with PGE1 in human corpus cavernosum and cultured human corpus cavernosum smooth muscle cells. Misoprostol, misoprostol free acid or PGE1 induced dose-dependent relaxations in strips of human corpus cavernosum. At concentrations greater than 1076 M, tissue recontraction was observed with all three agents. This was abrogated by pretreatment with the thromboxane A2 receptor antagonist SQ29,548. From these observations, we conclude that misoprostol is activated by human corpus cavernosum in situ and relaxes phenylephrine-precontrated tissue -
The EP2 Receptor Is the Predominant Prostanoid Receptor in the Human
110 BritishJournalofOphthalmology 1993; 77: 110-114 The EP2 receptor is the predominant prostanoid receptor in the human ciliary muscle Br J Ophthalmol: first published as 10.1136/bjo.77.2.110 on 1 February 1993. Downloaded from Toshihiko Matsuo, Max S Cynader Abstract IP prostanoid receptors, respectively. The EP Prostaglandins canreduce intraocularpressure receptor can be further classified into three by increasing uveoscleral outflow. We have subtypes, called EPI, EP2, and EP3 previously demonstrated that the human receptors.'89 The framework of the receptor ciliary muscle was a zone of concentration for classification has been supported in part, by binding sites (receptors) for prostaglandin F2a cloning and expression of cDNA for a human and for prostaglandin E2. Here, we try to thromboxane A2 receptor.20 elucidate the types of prostanoid receptors in It is important to know the types ofprostanoid the ciliary muscle using competitive ligand receptors located on the human ciliary muscle in binding studies in human eye sections and order to understand its role in uveoscleral out- computer assisted autoradiographic densito- flow, and to design new drugs with more potency metry. Saturation binding curves showed that and fewer adverse effects. In this study we tried the human ciliary muscle had a large number of to elucidate the type(s) of prostanoid receptors binding sites with a high affinity for prosta- located on the human ciliary muscle by glandin E2 compared with prostaglandin D2 combining receptor autoradiography with and F2,. The binding oftritiated prostaglandin competitive binding studies with various ligands E2 and F2a in the ciliary muscle was displaced on human eye sections. -
Evidence Review D
National Institute for Health and Care Excellence Draft for consultation Intrapartum care for women with existing medical conditions or obstetric complications and their babies [D] Evidence reviews for asthma NICE guideline <TBC at publication> Evidence reviews for women at high risk of adverse outcomes for themselves and/or their baby because of existing maternal medical conditions September 2018 Draft for consultation Developed by the National Guideline Alliance hosted by the Royal College of Obstetricians and Gynaecologists DRAFT FOR CONSULTATION Disclaimer The recommendations in this guideline represent the view of NICE, arrived at after careful consideration of the evidence available. When exercising their judgement, professionals are expected to take this guideline fully into account, alongside the individual needs, preferences and values of their patients or service users. The recommendations in this guideline are not mandatory and the guideline does not override the responsibility of healthcare professionals to make decisions appropriate to the circumstances of the individual patient, in consultation with the patient and/or their carer or guardian. Local commissioners and/or providers have a responsibility to enable the guideline to be applied when individual health professionals and their patients or service users wish to use it. They should do so in the context of local and national priorities for funding and developing services, and in light of their duties to have due regard to the need to eliminate unlawful discrimination, to advance equality of opportunity and to reduce health inequalities. Nothing in this guideline should be interpreted in a way that would be inconsistent with compliance with those duties. NICE guidelines cover health and care in England. -
The Roles of Prostaglandin F2 in Regulating the Expression of Matrix Metalloproteinase-12 Via an Insulin Growth Factor-2-Dependent Mechanism in Sheared Chondrocytes
Signal Transduction and Targeted Therapy www.nature.com/sigtrans ARTICLE OPEN The roles of prostaglandin F2 in regulating the expression of matrix metalloproteinase-12 via an insulin growth factor-2-dependent mechanism in sheared chondrocytes Pei-Pei Guan1, Wei-Yan Ding1 and Pu Wang 1 Osteoarthritis (OA) was recently identified as being regulated by the induction of cyclooxygenase-2 (COX-2) in response to high 12,14 fluid shear stress. Although the metabolic products of COX-2, including prostaglandin (PG)E2, 15-deoxy-Δ -PGJ2 (15d-PGJ2), and PGF2α, have been reported to be effective in regulating the occurrence and development of OA by activating matrix metalloproteinases (MMPs), the roles of PGF2α in OA are largely overlooked. Thus, we showed that high fluid shear stress induced the mRNA expression of MMP-12 via cyclic (c)AMP- and PGF2α-dependent signaling pathways. Specifically, we found that high fluid shear stress (20 dyn/cm2) significantly increased the expression of MMP-12 at 6 h ( > fivefold), which then slightly decreased until 48 h ( > threefold). In addition, shear stress enhanced the rapid synthesis of PGE2 and PGF2α, which generated synergistic effects on the expression of MMP-12 via EP2/EP3-, PGF2α receptor (FPR)-, cAMP- and insulin growth factor-2 (IGF-2)-dependent phosphatidylinositide 3-kinase (PI3-K)/protein kinase B (AKT), c-Jun N-terminal kinase (JNK)/c-Jun, and nuclear factor kappa-light- chain-enhancer of activated B cells (NF-κB)-activating pathways. Prolonged shear stress induced the synthesis of 15d-PGJ2, which is responsible for suppressing the high levels of MMP-12 at 48 h. -
The in Vitro Effect of Prostaglandin E2 and F2α on the Chemerin System In
International Journal of Molecular Sciences Article The In Vitro Effect of Prostaglandin E2 and F2α on the Chemerin System in the Porcine Endometrium during Gestation , Kamil Dobrzyn * y, Marta Kiezun y , Ewa Zaobidna, Katarzyna Kisielewska, Edyta Rytelewska, Marlena Gudelska, Grzegorz Kopij, Kinga Bors, Karolina Szymanska, Barbara Kaminska, Tadeusz Kaminski and Nina Smolinska * Department of Animal Anatomy and Physiology, Faculty of Biology and Biotechnology, University of Warmia and Mazury in Olsztyn, Oczapowskiego 1A, 10-719 Olsztyn-Kortowo, Poland; [email protected] (M.K.); [email protected] (E.Z.); [email protected] (K.K.); [email protected] (E.R.); [email protected] (M.G.); [email protected] (G.K.); [email protected] (K.B.); [email protected] (K.S.); [email protected] (B.K.); [email protected] (T.K.) * Correspondence: [email protected] (K.D.); [email protected] (N.S.) These authors contributed equally to this work. y Received: 21 May 2020; Accepted: 21 July 2020; Published: 23 July 2020 Abstract: Chemerin belongs to the group of adipocyte-derived hormones known as adipokines, which are responsible mainly for the control of energy homeostasis. Adipokine exerts its influence through three receptors: Chemokine-like receptor 1 (CMKLR1), G protein-coupled receptor 1 (GPR1), and C-C motif chemokine receptor-like 2 (CCRL2). A growing body of evidence indicates that chemerin participates in the regulation of the female reproductive system. According to the literature, the expression of chemerin and its receptors in reproductive structures depends on the local hormonal milieu. -
Application for Inclusion on WHO Model List of Essential Medicines
20th Expert Committee on the Selection and Use of Essential Medicines Geneva, 2015 PROPOSAL FOR THE INCLUSION OF MISOPROSTOL IN THE WHO MODEL LIST OF ESSENTIAL MEDICINES Submitted on behalf of: Gynuity Health Projects, NY, USA Dina Abbas, MPH Jill Durocher Beverly Winikoff, MD,MPH Program Associate Senior Program Associate President [email protected] [email protected] [email protected] Gynuity Health Projects 15 East 26th Street, Suite 801 New York, NY 10010 Tel: (1) 212-448-1230 Fax: (1) 212-448-1260 Table of Contents 1. Summary Statement of the proposal for inclusion, change or deletion ..................................3 2. Name of the focal point in WHO submitting or supporting the application ..........................5 3. Name of organization(s) consulted and/or supporting the application ...................................5 4. International Nonproprietary Name (INN, generic name) of the medicine............................5 5. Formulation proposed for inclusion; including adult and pediatric (if appropriate) ...............5 6. International availability – sources, of possible manufacturers and trade names ...................5 7. Whether listing is requested as an individual medicine or as an example of a therapeutic group ..........................................................................................................................................6 8. Information support the public health relevance ...................................................................6 8.1 Disease Burden ..................................................................................................................6 -
Binding and Signaling Differences Between Prostaglandin E1 and E2 Mediated By
Binding and Signaling Differences between Prostaglandin E1 and E2 Mediated by Prostaglandin E Subtype Receptors A Dissertation Presentation to The Department of Pharmacological and Pharmaceutical Sciences University of Houston In Partial Fulfillment of The Requirement for the Degree Doctor of Philosophy By Annirudha Jaikaran Chillar August 2010 i BINDING AND SIGNALING DIFFERENCES BETWEEN PROSTAGLANDIN E1 AND E2 MEDIATED BY PROSTAGLANDIN E SUBTYPE RECEPTORS A dissertation for the degree Doctor of Philosophy By Annirudha Jaikaran Chillar Approved by Dissertation Committee: _____________________________________ Dr. Ke‐He Ruan, MD, Ph.D. Professor of Medicinal Chemistry & Pharmacology Director of the Center for Experimental Therapeutics and Pharmacoinformatics ,PPS _____________________________________ Dr. Diana Chow Ph.D, Committee Member, Professor of Pharmaceutics, Director, Institute for Drug Education and Research _____________________________________ Dr. Xiaolian Gao, Ph.D, Committee Member Professor, Department of Biology and Biochemistry _____________________________________ Dr. Louis Williams, Ph.D, Committee Member Associate Professor of Medicinal Chemistry, PPS __________________________________ Dr. Joydip Das, Ph.D, Committee Member Assistant Professor of Medicinal Chemistry, PPS _____________________________________ Dr. F. Lamar Pritchard, Dean College of Pharmacy August 2010 ii ACKNOWLEDGEMENTS I would like to thank Dr. Ke‐He Ruan for being my advisor and giving me the freedom to think freely. I would also like to thank my committee member Dr. Chow for being the most loving faculty and giving me support when I needed it the most. I would also like to thank my committee member Dr. Williams for being there as a wonderful ear and shoulder on which I could relentlessly cry on. I would also like to thank my committee member Dr.