DOCSLIB.ORG

Biomolecules) to Modify the Functions of Cells, Tissues, Physiological Systems and in Some Cases the Behaviour of Organisms

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Biomolecules) to Modify the Functions of Cells, Tissues, Physiological Systems and in Some Cases the Behaviour of Organisms L1&2: Introduction, ROA and absorption WHAT IS A DRUG? • A chemical entity of known structure, other than a nutrient/dietary supplement, which causes a biological effect in a living organism. • The defining feature of drugs is that they selectively interact with endogenous molecules (Biomolecules) to modify the functions of cells, tissues, physiological systems and in some cases the Behaviour of organisms. • Many drugs cannot Be used therapeutically Because the unwanted effects the drug produces outweigh its beneficial effects. • However, drugs used in the prevention or treatment of disease are often referred to as medicines, although that term refers to a preparation of one or more drug, alongside other substances (stabilisers, solvents, etc.), which is used therapeutically … i.e. to treat, cure, prevent or diagnose disease. WHAT IS A MEDICINE? • A preparation of one or more drug, alongside other suBstances (staBilisers, solvents, etc.), which is used therapeutically … i.e. to treat, cure, prevent or diagnose disease. • Note the difference Between a drug and a medicine … most drugs we’ll cover are components of medicines … but some “recreational drugs” clearly don’t fit the cure/treat/prevent/diagnose definition. Drugs classification: • Molecular Structure (catecholamines, tricyclics) • Mode of Action (acetylcholinesterase inhibitors, β-blockers) • Therapeutic Use (bronchodilators, antihypertensives) How are drugs named? • Drugs are named in three ways 1) chemical name 2) generic name 3) proprietary name (trade name) • Pharmacology- the science-orientated study of drug action • Toxicology- the study of adverse effects of chemicals on living organisms • Pharmacy- patient-orientated health service profession Two branches of pharmacology: 1. Pharmacodynamics: o What a drug does to the Body • Does the drug work? How well? • What is the dose-response relationship? • What is the molecular target? • How strongly does the drug Bind? • What is the mechanism of action? 2. Pharmacokinetics: o What the Body does o a drug • How is the drug administered? Why? • How much is bioavailaBle? • How much gets to the right place? • How long does it stay at the target site? • How much gets to the wrong place? • How does the drug leave the Body? ADME: • Absorption • DistriBution • MetaBolism • Excretion • ADME determines the concentration of the drug at the target site which effects the Onset, Intensity & Duration of the drug’s action • The concentration of a drug at its target site is very important it will be what determines its efficacy • However, to get to its target, a drug must first Be aBsorBed and then Be distriButed to the correct tissue -> These two processes contribute to drug DELIVERY -> While this is taking place, the body will be metabolising and excreting the drug, hence reducing its concentration in the body and hence at the target site • The latter two processes contribute to drug ELIMINATION/ • When you take a drug, it must first get into the systemic circulation (aBsorption) • Some may be metabolised even before getting there (e.g. by endothelial cells of the gut) and more will Be start to Be metaBolised and excreted as soon as it is absorbed • Meanwhile, some drug leaves the circulation and enters tissues no all the drug will enter the target tissues and this may be a cause for adverse effects but hopefully some gets to the target tissue and binds to the target molecules Administration and Absorption: • Absorption is the movement of drug from the site of administration to the systemic circulation (n.b. NOT to the site of action) • Before any drug can have an effect it must Be presented in a suitable form at an appropriate site of administration. For an action within the body, the drug must be absorbed from its site of administration and distributed via the blood to the tissue(s) where it acts. In general, drugs must cross Biological membranes to gain access to the blood and to their sites of action • Route of administration (ROA) plays a crucial role in absorption. o intra venous (I.V.) infusion - all drug reaches the systemic circulation the drug is “100% Bioavailable”! -> However, I.V. administration is unpleasant and requires supervised in- patient care hence not convenient for everyday use o All other routes of administration have <100% BioavailaBility But are much more convenient for patients! ROA: • Enteral (via GI tract)- Drugs must cross a tight Barrier composed of the epithelial cells of the gastrointestinal tract o Oral o Sublingual o Rectal • Parenteral: o I.V. o subcutaneous o intra muscular (I.M.) o inhalation o intranasal o topical o transdermal Oral drug administration: • Most common route – good for self-dosing, cost-effective to make, easy to dose • Most oral drugs are taken in taBlet form, although liquid/suspension form is more common for young children. • Onset is rapid (10-20 min) But the drug must dissolve first • there is a huge capacity for absorption due to the large surface area of the small intestine • The small intestine is the major site for absorption from the GI tract by passive diffusion because of its huge surface area, which is about 200 m2, and thin membrane (one cell layer thick). In addition, the small intestine has a high blood flow relative to other areas of the GI tract. This helps to maintain the concentration gradient between drug in the lumen of the small intestine and drug in blood; hence the direction of diffusion is into the body (blood). • Most common But also most complicated: o Survive gastric acid. • e.g. Benzylpenicillin (penicillin G) hydrolysed By gastric acid and hence usually is given via IV route. Penicillin V (phenoxymethylpenicillin) is taken on an empty stomach • Some drugs have an “enteric coat” for protection. o Survive digestive enzymes. • e.g. insulin and other peptide drugs cannot Be given orally. o Co-exist with, or need to avoid, food. • e.g. tetracycline antiBiotics Bind to Ca2+ in food, Become insoluBle and are not absorbed • The presence of food also changes gastric emptying times o Cope with gut bacteria – metaBolism and metaBolites • e.g. simvastatin (anti-hypolipidemic drug) activity is altered by the presence of certain bacterial metabolites, which differ in different individuals. • e.g. sulphasalazine is cleaved into active anti-inflammatory component 5-ASA and sulphapyridine by colonic bacteria. • Drug formulation can have a major impact on absorption from the gut. If the drug is swallowed in solution, for example, its rate of absorption will be much quicker than if it were taken as a tablet. The tablet has to disintegrate to release solid particles of drug. The drug must then dissolve before absorption can occur. These processes take time; hence a drug that is already in solution will be aBsorBed more quickly than the same drug compacted into a solid tablet, so a drug in solution will have a faster onset of action than a drug in a tablet. • For drugs to be effective by the oral route, route they have to cross the epithelial lining of the gastrointestinal (GI) tract • The epithelial cells of the GI tract have tight junctions between them; hence to penetrate this layer of cells and to access the blood, drug molecules must pass through cell membranes -> This process is often referred to as transcellular diffusion. • The key structure of a cell membrane is the phospholipid bilayer. o This “fatty” layer forms a physical barrier to the entry of drugs into cells. o To penetrate this barrier drug molecules must be lipid soluble. o Lipid soluble drugs have an affinity for fat; they readily dissolve in fatty substances (such as phospholipids) and can diffuse through them -> Substances that do this are often called lipophilic. • Sometimes drugs are transported via carrier-mediated transport – however, for oral (and all enteral) routes, aBsorption is usually via transcellular diffusion ->This is via the process of diffusion • Lipophilic drugs penetrate cell membranes By passive diffusion o This is when molecules move from a region of high concentration to one of low concentration o Passive diffusion occurs Because of the random thermal motion of molecules and is described by Fick’s Law o This law states that the rate of diffusion is directly proportional to the concentration gradient across the memBrane; to the surface area of the memBrane and the lipid solubility of the molecule. o The rate of diffusion, however, is inversely proportional to the thickness of the memBrane(in this case we consider the “memBrane” to Be the Barrier, which may Be composed of one or more cell so actually, there are more than one plasma membranes involved). o Rate = (conc. gradient x area x lipid soluBility) / thickness of membrane o Fick’s law predicts the rate of diffusion will increase as the concentration gradient, membrane surface area and lipid solubility increase o By contrast, the rate of diffusion will decrease when the membrane thickness increases. Accordingly, rates of diffusion across a membrane one cell layer thick (e.g. small intestine) will be greater than when the membrane is several cell layers thick (e.g. skin) o Diffusion is an important mechanism for absorption of drugs from the GI tract and for absorption from other sites of drug administration such as the lung, skin and muscle. • P-glycoprotein is an ATP-powered drug-efflux pump which removes a wide range of substrates from the cell interior back into the gut lumen • Drug Bioavailability may Be reduced By activity of the ATP powered drug efflux pump, P-glycoprotein • This transporter is expressed By the epithelial cells of the small intestine and is embedded in the apical surface of these cells • It functions to pump a wide range to drug substrates out the cell and back into the gut lumen. Thus the permeaBility of the gut mucosa to its substrate drugs is reduced • Not all drugs are aBsorBed from the gut By passive diffusion o Some drugs are absorbed from the GI tract by carrier-mediated transport.
Load more

Recommended publications
  • Principle of Pharmacodynamics
    Principle of pharmacodynamics Dr. M. Emamghoreishi Full Professor Department of Pharmacology Medical School Shiraz University of Medical Sciences Email:[email protected] Reference: Basic & Clinical Pharmacology: Bertrum G. Katzung and Anthony J. Treveror, 13th edition, 2015, chapter 20, p. 336-351 Learning Objectives: At the end of sessions, students should be able to: 1. Define pharmacology and explain its importance for a clinician. 2. Define ―drug receptor‖. 3. Explain the nature of drug receptors. 4. Describe other sites of drug actions. 5. Explain the drug-receptor interaction. 6. Define the terms ―affinity‖, ―intrinsic activity‖ and ―Kd‖. 7. Explain the terms ―agonist‖ and ―antagonist‖ and their different types. 8. Explain chemical and physiological antagonists. 9. Explain the differences in drug responsiveness. 10. Explain tolerance, tachyphylaxis, and overshoot. 11. Define different dose-response curves. 12. Explain the information that can be obtained from a graded dose-response curve. 13. Describe the potency and efficacy of drugs. 14. Explain shift of dose-response curves in the presence of competitive and irreversible antagonists and its importance in clinical application of antagonists. 15. Explain the information that can be obtained from a quantal dose-response curve. 16. Define the terms ED50, TD50, LD50, therapeutic index and certain safety factor. What is Pharmacology?It is defined as the study of drugs (substances used to prevent, diagnose, and treat disease). Pharmacology is the science that deals with the interactions betweena drug and the bodyor living systems. The interactions between a drug and the body are conveniently divided into two classes. The actions of the drug on the body are termed pharmacodynamicprocesses.These properties determine the group in which the drug is classified, and they play the major role in deciding whether that group is appropriate therapy for a particular symptom or disease.
    [Show full text]
  • Opioid Receptorsreceptors
    OPIOIDOPIOID RECEPTORSRECEPTORS defined or “classical” types of opioid receptor µ,dk and . Alistair Corbett, Sandy McKnight and Graeme Genes encoding for these receptors have been cloned.5, Henderson 6,7,8 More recently, cDNA encoding an “orphan” receptor Dr Alistair Corbett is Lecturer in the School of was identified which has a high degree of homology to Biological and Biomedical Sciences, Glasgow the “classical” opioid receptors; on structural grounds Caledonian University, Cowcaddens Road, this receptor is an opioid receptor and has been named Glasgow G4 0BA, UK. ORL (opioid receptor-like).9 As would be predicted from 1 Dr Sandy McKnight is Associate Director, Parke- their known abilities to couple through pertussis toxin- Davis Neuroscience Research Centre, sensitive G-proteins, all of the cloned opioid receptors Cambridge University Forvie Site, Robinson possess the same general structure of an extracellular Way, Cambridge CB2 2QB, UK. N-terminal region, seven transmembrane domains and Professor Graeme Henderson is Professor of intracellular C-terminal tail structure. There is Pharmacology and Head of Department, pharmacological evidence for subtypes of each Department of Pharmacology, School of Medical receptor and other types of novel, less well- Sciences, University of Bristol, University Walk, characterised opioid receptors,eliz , , , , have also been Bristol BS8 1TD, UK. postulated. Thes -receptor, however, is no longer regarded as an opioid receptor. Introduction Receptor Subtypes Preparations of the opium poppy papaver somniferum m-Receptor subtypes have been used for many hundreds of years to relieve The MOR-1 gene, encoding for one form of them - pain. In 1803, Sertürner isolated a crystalline sample of receptor, shows approximately 50-70% homology to the main constituent alkaloid, morphine, which was later shown to be almost entirely responsible for the the genes encoding for thedk -(DOR-1), -(KOR-1) and orphan (ORL ) receptors.
    [Show full text]
  • The Importance of Serotonergic and Adrenergic Receptors for the Induction and Expression of One-Trial Cocaine-Induced Behavioral Sensitization" (2016)
    California State University, San Bernardino CSUSB ScholarWorks Electronic Theses, Projects, and Dissertations Office of aduateGr Studies 12-2016 THE IMPORTANCE OF SEROTONERGIC AND ADRENERGIC RECEPTORS FOR THE INDUCTION AND EXPRESSION OF ONE- TRIAL COCAINE-INDUCED BEHAVIORAL SENSITIZATION Krista N. Rudberg California State University - San Bernardino Follow this and additional works at: https://scholarworks.lib.csusb.edu/etd Part of the Biological Psychology Commons, and the Pharmacology Commons Recommended Citation Rudberg, Krista N., "THE IMPORTANCE OF SEROTONERGIC AND ADRENERGIC RECEPTORS FOR THE INDUCTION AND EXPRESSION OF ONE-TRIAL COCAINE-INDUCED BEHAVIORAL SENSITIZATION" (2016). Electronic Theses, Projects, and Dissertations. 420. https://scholarworks.lib.csusb.edu/etd/420 This Thesis is brought to you for free and open access by the Office of aduateGr Studies at CSUSB ScholarWorks. It has been accepted for inclusion in Electronic Theses, Projects, and Dissertations by an authorized administrator of CSUSB ScholarWorks. For more information, please contact [email protected]. THE IMPORTANCE OF SEROTONERGIC AND ADRENERGIC RECEPTORS FOR THE INDUCTION AND EXPRESSION OF ONE-TRIAL COCAINE- INDUCED BEHAVIORAL SENSITIZATION A Thesis Presented to the Faculty of California State University, San Bernardino In Partial Fulfillment of the Requirements for the Degree Master of Arts in General/Experimental Psychology by Krista Nicole Rudberg December 2016 THE IMPORTANCE OF SEROTONERGIC AND ADRENERGIC RECEPTORS FOR THE INDUCTION AND EXPRESSION OF ONE-TRIAL COCAINE- INDUCED BEHAVIORAL SENSITIZATION A Thesis Presented to the Faculty of California State University, San Bernardino by Krista Nicole Rudberg December 2016 Approved by: Sanders McDougall, Committee Chair, Psychology Cynthia Crawford, Committee Member Matthew Riggs, Committee Member © 2016 Krista Nicole Rudberg ABSTRACT Addiction is a complex process in which behavioral sensitization may be an important component.
    [Show full text]
  • A1-Blocker Therapy in the Nineties: Focus on the Disease
    Prostate Cancer and Prostatic Diseases (1999) 2 Suppl 4, S9±S15 ß 1999 Stockton Press All rights reserved 1365±7852/99 $15.00 http://www.stockton-press.co.uk/pcan a1-Blocker therapy in the nineties: focus on the disease KHoÈfner1* 1Department of Urology, Hannover Medical School, Hannover, Germany Therapy for benign prostatic hyperplasia has evolved rapidly over the last decade, with the introduction in the early 1990s of new agents such as a1-blockers and 5a-reductase inhibitors. The major advantage of a1-blockers over 5a- reductase inhibitors is their rapid onset of action. Maximum ¯ow rate is improved after ®rst administration and optimal symptom relief is usually reached within 2 ± 3 months. In addition, a1-blockers are effective regardless of prostate size and they provide a similar degree of symptom relief in patients with or without bladder outlet obstruction. The main adverse events with the a1- blockers relate to their effects on the cardiovascular system (postural hypoten- sion) and central penetration (asthenia, somnolence). Newer uroselective a1- blockers, such as alfuzosin and tamsulosin, have a better safety pro®le and, as such, do not require initial dose titration. Alfuzosin has also been shown in a six- month study to signi®cantly reduce both residual urine and the incidence of acute urinary retention (AUR) compared with placebo. In addition, alfuzosin is effective in improving the success rate of a trial without catheter in patients with AUR. Keywords: benign prostatic hyperplasia; prostate; a1-blockers; 5a-reductase inhibitors; acute urinary retention; LUTS Management of BPH adrenoceptors. Medical management of BPH suddenly exploded at the beginning of the 1990s with the introduc- Therapy for benign prostatic hyperplasia (BPH) has tion of selective a1-blockers and 5a-reductase inhibitors.
    [Show full text]
  • Anew Drug Design Strategy in the Liht of Molecular Hybridization Concept
    www.ijcrt.org © 2020 IJCRT | Volume 8, Issue 12 December 2020 | ISSN: 2320-2882 “Drug Design strategy and chemical process maximization in the light of Molecular Hybridization Concept.” Subhasis Basu, Ph D Registration No: VB 1198 of 2018-2019. Department Of Chemistry, Visva-Bharati University A Draft Thesis is submitted for the partial fulfilment of PhD in Chemistry Thesis/Degree proceeding. DECLARATION I Certify that a. The Work contained in this thesis is original and has been done by me under the guidance of my supervisor. b. The work has not been submitted to any other Institute for any degree or diploma. c. I have followed the guidelines provided by the Institute in preparing the thesis. d. I have conformed to the norms and guidelines given in the Ethical Code of Conduct of the Institute. e. Whenever I have used materials (data, theoretical analysis, figures and text) from other sources, I have given due credit to them by citing them in the text of the thesis and giving their details in the references. Further, I have taken permission from the copyright owners of the sources, whenever necessary. IJCRT2012039 International Journal of Creative Research Thoughts (IJCRT) www.ijcrt.org 284 www.ijcrt.org © 2020 IJCRT | Volume 8, Issue 12 December 2020 | ISSN: 2320-2882 f. Whenever I have quoted written materials from other sources I have put them under quotation marks and given due credit to the sources by citing them and giving required details in the references. (Subhasis Basu) ACKNOWLEDGEMENT This preface is to extend an appreciation to all those individuals who with their generous co- operation guided us in every aspect to make this design and drawing successful.
    [Show full text]
  • International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification
    0031-6997/03/5504-597–606$7.00 PHARMACOLOGICAL REVIEWS Vol. 55, No. 4 Copyright © 2003 by The American Society for Pharmacology and Experimental Therapeutics 30404/1114803 Pharmacol Rev 55:597–606, 2003 Printed in U.S.A International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology RICHARD R. NEUBIG, MICHAEL SPEDDING, TERRY KENAKIN, AND ARTHUR CHRISTOPOULOS Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Institute de Recherches Internationales Servier, Neuilly sur Seine, France (M.S.); Systems Research, GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina (T.K.); and Department of Pharmacology, University of Melbourne, Parkville, Australia (A.C.) Abstract ............................................................................... 597 I. Introduction............................................................................ 597 II. Working definition of a receptor .......................................................... 598 III. Use of drugs in definition of receptors or of signaling pathways ............................. 598 A. The expression of amount of drug: concentration and dose ............................... 598 1. Concentration..................................................................... 598 2. Dose. ............................................................................ 598 B. General terms used to describe drug action ...........................................
    [Show full text]
  • International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology
    0031-6997/03/5504-597–606$7.00 PHARMACOLOGICAL REVIEWS Vol. 55, No. 4 Copyright © 2003 by The American Society for Pharmacology and Experimental Therapeutics 30404/1114803 Pharmacol Rev 55:597–606, 2003 Printed in U.S.A International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology RICHARD R. NEUBIG, MICHAEL SPEDDING, TERRY KENAKIN, AND ARTHUR CHRISTOPOULOS Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Institute de Recherches Internationales Servier, Neuilly sur Seine, France (M.S.); Systems Research, GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina (T.K.); and Department of Pharmacology, University of Melbourne, Parkville, Australia (A.C.) Abstract ............................................................................... 597 I. Introduction............................................................................ 597 II. Working definition of a receptor .......................................................... 598 III. Use of drugs in definition of receptors or of signaling pathways ............................. 598 A. The expression of amount of drug: concentration and dose ............................... 598 Downloaded from 1. Concentration..................................................................... 598 2. Dose. ............................................................................ 598 B. General terms used to describe drug action ...........................................
    [Show full text]
  • Comparative Exploration of the Structure–Activity Space of Cloned A-Like Octopamine Receptors from a Marine and a Terrestrial Arthropod S
    Supplemental material to this article can be found at: http://molpharm.aspetjournals.org/content/suppl/2017/06/29/mol.117.108456.DC1 1521-0111/92/3/297–309$25.00 https://doi.org/10.1124/mol.117.108456 MOLECULAR PHARMACOLOGY Mol Pharmacol 92:297–309, September 2017 Copyright ª 2017 by The American Society for Pharmacology and Experimental Therapeutics Comparative Exploration of the Structure–Activity Space of Cloned a-Like Octopamine Receptors from a Marine and a Terrestrial Arthropod s Dhwanil A. Dalwadi and John A. Schetz Department of Pharmacology and Neuroscience (D.A.D., J.A.S.), Graduate School of Biomedical Sciences, Institute for Healthy Aging, Center for Neuroscience Discovery, and Department of Medical Education (J.A.S.), Texas College of Osteopathic Medicine, University of North Texas Health Science Center, Fort Worth, Texas Received January 23, 2017; accepted June 26, 2017 Downloaded from ABSTRACT The a-like octopamine receptors (OctR) are believed to be the different mechanisms of action. For instance, significant differ- evolutionary precursor to the vertebrate a2-adrenergic receptors ences in the efficacy for some agonists were observed, includ- (a2-ARs) based upon sequence similarity and the ability to ing that vertebrate biogenic amines structurally related to interact with norepinephrine and a number of compounds that octopamine acted as superagonists at the DmOctR but partial molpharm.aspetjournals.org bind with high affinity to a2-ARs. Barnacles and fruit flies are agonists at the BiOctR, and the two species diverged in their 3 two prominent model marine and terrestrial representatives of sensitivities to the a2-AR antagonist [ H]rauwolscine.
    [Show full text]
  • Progress in Medicinal Chemistry 3 5
    Progress in MedUicinal Chemistry 35 This Page intentionally left blank Progress in Medicinal Chemistry 3 5 Editors: G.P. ELLIS,D.SC., PH.D., F.R.S.C. Department of Chemistry University of Wales P.0. Box 912, Card18 CFI 3 TB United Kitigdom D.K. LUSCOMBE, B.PHARM., PH.D., F.I.BIOL., F.R.PHARM.S Welsh School of Pharmacy University of Wales P.0. Box 13, Cardig CFI 3XF United Kingdom and A.W. OXFORD, M.A., D.PHIL. Consultant in Medicinal Cheniistry P. 0. Box 151 Royston SG8 5 YQ United Kingdom 1998 ELSEVIER AMSTERDAM LAUSANNE- NEW YORK *OXFORD*SHANNON*SINCAPORE -TOKYO Elsevier Science BV P.O. Box 21 1 1000 AE Amsterdam The Netherlands Library of Congress Cataloging in Publication Data: Please refer to card number 62-2712 for this series. ISBN 0-444-82909-1 ISBN Series 0-7204-7400-0 0 1998 Elsevier Science BV. All rights reserved No part of this publication may be reproduced, stored in a retrieval system or transmitted in any form or by any means, electronic, mechanical, photocopying, recording or otherwise without the prior written permission of the Publisher, Elsevier Science B.V., Copyright and Permissions Department, P.O. Box 521, 1000 AM Amsterdam, The Netherlands. No responsibility is assumed by the Publisher for any injury and/or damage to persons or property as a matter of products liability, negligence or otherwise, or from any use or operation of any methods, products, instructions or ideas contained in the material herein. Because of rapid advances in the medical sciences, the Publisher recommends that independent verification of diagnoses and drug dosages should be made.
    [Show full text]
  • International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology
    0031-6997/03/5504-597–606$7.00 PHARMACOLOGICAL REVIEWS Vol. 55, No. 4 Copyright © 2003 by The American Society for Pharmacology and Experimental Therapeutics 30404/1114803 Pharmacol Rev 55:597–606, 2003 Printed in U.S.A International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology RICHARD R. NEUBIG, MICHAEL SPEDDING, TERRY KENAKIN, AND ARTHUR CHRISTOPOULOS Department of Pharmacology, University of Michigan, Ann Arbor, Michigan (R.R.N.); Institute de Recherches Internationales Servier, Neuilly sur Seine, France (M.S.); Systems Research, GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina (T.K.); and Department of Pharmacology, University of Melbourne, Parkville, Australia (A.C.) Abstract ............................................................................... 597 I. Introduction............................................................................ 597 II. Working definition of a receptor .......................................................... 598 III. Use of drugs in definition of receptors or of signaling pathways ............................. 598 A. The expression of amount of drug: concentration and dose ............................... 598 Downloaded from 1. Concentration..................................................................... 598 2. Dose. ............................................................................ 598 B. General terms used to describe drug action ...........................................
    [Show full text]
  • Drug-Gut Microbiota Interactions: Implications for Neuropharmacology Author(S) Walsh, Jacinta; Griffin, Brendan T.; Clarke, Gerard; Hyland, Niall P
    UCC Library and UCC researchers have made this item openly available. Please let us know how this has helped you. Thanks! Title Drug-gut microbiota interactions: implications for neuropharmacology Author(s) Walsh, Jacinta; Griffin, Brendan T.; Clarke, Gerard; Hyland, Niall P. Publication date 2018-05-21 Original citation Walsh, J., Griffin, B. T., Clarke, G. and Hyland, N. P. (2018) 'Drug-gut microbiota interactions: implications for neuropharmacology', British Journal of Pharmacology. doi:10.1111/bph.14366 Type of publication Article (peer-reviewed) Link to publisher's http://dx.doi.org/10.1111/bph.14366 version Access to the full text of the published version may require a subscription. Rights © 2018, British Pharmacological Society. All rights reserved. Published by John Wiley & Sons Ltd. This is the peer reviewed version of the following article: Walsh, J., Griffin, B. T., Clarke, G. and Hyland, N. P. (2018) 'Drug-gut microbiota interactions: implications for neuropharmacology', British Journal of Pharmacology. doi:10.1111/bph.14366, which has been published in final form at https://doi.org/10.1111/bph.14366. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Self-Archiving. Embargo information Access to this article is restricted until 12 months after publication by request of the publisher. Embargo lift date 2019-05-21 Item downloaded http://hdl.handle.net/10468/6243 from Downloaded on 2021-10-02T02:32:36Z Drug-Gut Microbiota Interactions: Implications for Neuropharmacology Walsh, Jacinta 1,4, Griffin, Brendan T. 2,4, Clarke, Gerard 3,4*, Hyland, Niall P. 1,4 1 Department of Pharmacology and Therapeutics, University College Cork, 2 School of Pharmacy, University College Cork, 3 Department of Psychiatry and Neurobehavioural Science, University College Cork, 4 APC Microbiome Ireland, University College Cork.
    [Show full text]
  • 5-HT2A Receptors in the Central Nervous System the Receptors
    The Receptors Bruno P. Guiard Giuseppe Di Giovanni Editors 5-HT2A Receptors in the Central Nervous System The Receptors Volume 32 Series Editor Giuseppe Di Giovanni Department of Physiology & Biochemistry Faculty of Medicine and Surgery University of Malta Msida, Malta The Receptors book Series, founded in the 1980’s, is a broad-based and well- respected series on all aspects of receptor neurophysiology. The series presents published volumes that comprehensively review neural receptors for a specific hormone or neurotransmitter by invited leading specialists. Particular attention is paid to in-depth studies of receptors’ role in health and neuropathological processes. Recent volumes in the series cover chemical, physical, modeling, biological, pharmacological, anatomical aspects and drug discovery regarding different receptors. All books in this series have, with a rigorous editing, a strong reference value and provide essential up-to-date resources for neuroscience researchers, lecturers, students and pharmaceutical research. More information about this series at http://www.springer.com/series/7668 Bruno P. Guiard • Giuseppe Di Giovanni Editors 5-HT2A Receptors in the Central Nervous System Editors Bruno P. Guiard Giuseppe Di Giovanni Faculté de Pharmacie Department of Physiology Université Paris Sud and Biochemistry Université Paris-Saclay University of Malta Chatenay-Malabry, France Msida MSD, Malta Centre de Recherches sur la Cognition Animale (CRCA) Centre de Biologie Intégrative (CBI) Université de Toulouse; CNRS, UPS Toulouse, France The Receptors ISBN 978-3-319-70472-2 ISBN 978-3-319-70474-6 (eBook) https://doi.org/10.1007/978-3-319-70474-6 Library of Congress Control Number: 2017964095 © Springer International Publishing AG 2018 This work is subject to copyright.
    [Show full text]