Alzheimer Disease: Therapeutic Strategies PDF
Preview Alzheimer Disease: Therapeutic Strategies
ALZHEIMER DISEASE THERAPEUTIC STRATEGIES Advances in Alzheimer Disease Therapy Series Editors: Ezio Giacobini Robert Becker This series periodically brings up-to-date advances in basic and clinical sciences that are relevant to understanding the etiology, pathogenesis, diagnosis, and treatment of Alzheimer disease. Experts from the vari ous fields relevant to understanding Alzheimer disease report their new research findings and discuss the newest developments in possible Alzheimer disease therapies. Books in the Series Cholinergic Basis for Alzheimer Therapy Edited by Robert Becker and Ezio Giacobini ISBN 0-8176-3566-1 Alzheimer Disease: Therapeutic Strategies Edited by Ezio Giacobini and Robert Becker ISBN 0-8176-3757-5 ALZHEIMER DISEASE THERAPEUTIC STRATEGIES Ezio Giacobini Robert Becker Editors with the editorial assistance of Diana L. Smith & Joyce M. Barton Birkhiiuser Ezio Giacobini Robert E. Becker Chairman of Pharmacology Chairman of Psychiatry Southern Illinois University Southern Illinois University School of Medicine School of Medicine P.O. Box 19230 P.O. Box 19230 Springfield, IL 62794-9230 Springfield, IL 62794-9230 USA USA Library of Congress Cataloging-in-Publication Data Alzheimer disease: therapeutic strategies 1 Ezio Giacobini, Robert Becker, editors, with the editorial assistance of Diana L. Smith and Joyce M. Barton. p. cm. - (Advances in Alzheimer disease therapy) Includes bibliographical references and index. ISBN 978-1-4615-8151-2 ISBN 978-1-4615-8149-9 (eBook) DOI 10.1007/978-1-4615-8149-9 I. Alzheimer's disease-Chemotherapy. 2. Alzheimer's disease Pathophysiology. 3. Alzheimer's disease-Treatment. I. Giacobini, Ezio. II. Becker, Robert E. III. Series. [DNLM: I. Alzheimer's Disease-therapy. WM 220 A4755 1994] RC523.A39757 1994 616.8'31-dc20 DNLMlDLC for Library of Congress 94-34494 CIP Printed on acid-free paper. ~® Birkhiiuser a(J?) © 1994 Birkhauser Boston Softcover reprint of the hardcover 1s t edition 1994 Copyright is not claimed for works of U.S. Government employees. 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 prior permission of the copyright owner. The use of general descriptive names, trademarks, etc. in this publication even if the former are not especially identified, is not to be taken as a sign that such names, as understood by the Trade Marks and Merchandise Marks Act, may accordingly be used freely by anyone. While the advice and information in this book are believed to be true and accurate at the date of going to press, neither the authors nor the editors nor the publisher can accept any legal responsibil ity for any errors or omissions that may be made. The publisher makes no warranty, express or implied, with respect to the material contained herein. Permission to photocopy for internal or personal use, or the internal or personal use of specific clients, is granted by Birkhiiuser Boston for libraries and other users registered with the Copyright Clearance Center (Ccq, provided that the base fee of $6.00 per copy, plus $0.20 per page is paid directly to CCC, 222 Rosewood Drive, Danvers, MA 01923, U.S.A. Special requests should be addressed directly to Birkhiiuser Boston, 675 Massachusetts Avenue, Cambridge, MA 02139, U.S.A. ISBN 978-1-4615-8151-2 Camera-ready text prepared by the editors using WordPerfect 6.0 on an IBM PS2 987654321 CONTENTS Introductions Development of Drugs for Alzheimer Therapy: A Decade of Progress ... 1 Ezio Giacobini and Robert Becker Epidemiology of AD: Impact on the Treatment ................. 8 Luigi Amaducci and Laura Fratiglioni Part I. Neuropathologic and Genetic Basis of AD Treatment Neuropathological Bases of Alzheimer Disease, Implications for Treatment . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 17 Henryk M. Wisniewski and Jerzy Wegiel Amyloid Deposition as the Central Event in the Etiology and Pathogenesis of Alzheimer's Disease ............... 23 John Hardy and Karen Duff Role of Abnormal Phosphorylation of Tau in Neurofibrillary Degeneration: Implications for Alzheimer Therapy . . . . . . . . . . . . . . . 28 Khalid Iqbal and Inge Grundke-Iqbal Olfactory Bulb Involvement in AD: An Early Change? ............ 34 Robert G. Struble, Mona Ghobrial and Larry F. Hughes Alzheimer Disease-A Spirochetosis? . . . . . . . . . . . . . . . . . . . . . . . 41 Judit Miklossy Part II. Therapeutical Strategies to Arrest Production and Processing of Amyloid Beta Amyloid (Afj) as a Therapeutic Target in Alzheimer's Disease .... 49 Ivan Lieberburg Regulation of APP Processing by First Messengers .............. 54 Roger M. Nitsch, John H. Growdon, Steven A. Farber, Meihua Deng and Richard J. Wurtman vi Contents In Vitro Production of Amyloid (J-Protein: A Route to the Mechanism and Treatment of Alzheimer's Disease ............... 62 Dennis J. Selkoe Apolipoprotein E and Alzheimer's Disease: Therapeutic Implications . ... 65 Warren J. Strittmatter, David Y. Huang, Ann Saunders, Donald Schmechel, Margaret Pericak-Vance, Allen D. Roses, Karl H. Weisgraber and Michel Goedert Apolipoprotein E4 and Cholinergic Dysfunction in Alzheimer's Disease ................................ 72 Judes Poirier, Isabelle Aubert, Philippe Bertrand, Remi Quirion, Serge Gauthier and Josephine Nalbantoglu m. Part The Cholinergic System of Human Brain Butyrylcholinesterase in Alzheimer's Disease .................. 79 M.-Marsel Mesulam Modulating Cholinergic Neurotransmission Through Transgenic Overexpression of Human Cholinesterases . . . . . . . . . . . . . . . . . . . . 84 Hermona Soreq, Rachel Beeri, Shlomo Seidman, Rina Timberg, Yael Loewenstein, Meira Sternfeld, Christian Andres and Moshe Shani Structure-Function Relationships in the Binding of Reversible Inhibitors in the Active-Site Gorge of Acetylcholinesterase .......... 88 I. Silman, M. Harel, J. Eichler, J.L. Sussman, A. Anselmet and J. Massoulie Cholinergic Changes and Synaptic Alterations in Alzheimer's Disease . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 93 Steven T. DeKosky, Scot D. Styren and Mark E. O'Malley Part IV. Cholinesterase Inhibitors in AD Treatment Introduction to Cholinesterase Inhibitors Used in Alzheimer's Disease Therapy .......................... 99 Vinod Kumar Contents vii A Pharmacodynamic Strategy to Optimize the Clinical Response to Eptastigmine (MF-20J) ............................... 103 Bruno P. Imbimbo and Paolo E. Lucchelli Eptastigmine (MF-20J). A Double-Blind, Placebo-Controlled, Clinical Trial in Alzheimer Disease Patients . . . . . . . . . . . . . . . . . . 108 Nicola Canal, Massimo Franceschi and the Italian Eptastigmine Investigators Cognition Improvement by Oral Hupenine A: A Novel Acetylcholinesterase Inhibitor ..................... 113 Xi Can Tang, Zhi Qi Xiong, Bo Chu Qian, Zhi Fang Zhou and Ci Lu Zhang In Vitro and In Vivo Effects of a Dual Inhibitor of Acetylcholinesterase and Muscarinic Receptors, CI-JOO2 .......... 120 Mark R. Emmerling, Vlad E. Gregor, Roy D. Schwarz, Jeff D. Scholten, Michael J. Callahan, Chitase Lee, Catherine J. Moore, Charlotte Raby, William J. Lipinski, Juan Jaen and Robert E. Davis Effects of Novel Cholinesterase Inhibitors Based on the Mechanism of Enzyme Inhibition ...................... 125 Albert Enz, Dieter Meier and Rene Spiegel Biochemistry, Pharmacokinetics and Pharmacodynamics of MDL 73,745: A Potent and Selective Inhibitor of Acetylcholinesterase . .......... 131 Jean-Marie Homsperger, Jean-Noel Collard, Daniel Schirlin, James Dow, Jean-Georges Heydt and Bertrand Dulery Clinical Experience with MDL 73,745; Pharmacokinetics, Pharmacodynamics, and Clinical Tolerance in Normal Volunteers .... 137 Margo M. Schleman, Stephen S. Songer, 010 J. Szylleyko, Randall D. Seifert and Neal R. Cutler Galanthamine in Alzheimer's Disease . ..................... 140 Helmut Kewitz, Gordon Wilcock and Bonnie Davis Tacrine: An Overview of Efficacy in Two Parallel Group Studies . .... 145 Stephen I. Gracon and Margaret J. Knapp Clinical Update of Velnacrine Research 150 Klaudius Siegfried and Rich Civil viii Contents Second and Third Generation Cholinesterase Inhibitors: From Preclinical Studies to Clinical Efficacy ................. 155 Ezio Giacobini and Gabriel Cuadra Second and Third Generation Cholinesterase Inhibitors: Clinical Aspects ................................... 172 Robert E. Becker, Pamela Moriearty, Rita Surbeck, Latha Unni, Andrew Varney and Sandra K. Vicari Part V. Nicotinic Agonists as Drugs for AD Treatment Nicotinic Receptors in Human Brain ...................... 181 Hannsjorg SchrOder, Andrea Wevers, Christina Birtsch, Mona Ghobrial, Ezio Giacobini and Alfred Maelicke Development of Nicotinic Agonists for the Treatment of Alzheimer's Disease ............................... 186 Patrick M. Lippiello, William S. Caldwell, Michael J. Marks and Allan C. Collins The Role of Nicotinic Systems in the Cognitive Disorder of Alzheimer's Disease . ................................ 191 Paul A. Newhouse, Alexandra Potter, June Corwin and Robert Lenox ABT-418: A Novel Cholinergic Channel Activator (ChCA) for the Potential Treatment of Alzheimer's Disease . ............. 196 Stephen P. Americ, James P. Sullivan, Michael W. Decker, Jorge D. Brioni, Clark A. Briggs, Diana Donnelly-Roberts, Kennan C. Marsh, A. David Rodrigues, David S. Garvey, Michael Williams and Jerry J. Buccafusco Nicotine, Catecholamines and Cognitive Enhancement ........... 201 Jeffrey A. Gray, Grigory A. Grigoryan, Chuly Lee, Stephen N. Mitchell and Helen Hodges The Subunit Specific Effects of Novel Anabaseine-Derived Nicotinic Agents . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 206 Roger L. Papke, Christopher M. de Fiebre, William Kem and Edwin M. Meyer Serotonin Depletion Decreases Therapeutic Effect of THA and Nicotine ................................. 212 Paavo J. Riekkinen, Jr., Minna K. Riekkinen and Jouni S. Sirvio Contents ix Part VI. Muscarinic Agonists: Preclinical and Clinical Approaches Selective Signaling Via Novel Muscarinic Agonists: Implications for Alzheimer'S Disease Treatments and Clinical Update ................................ 219 Abraham Fisher, Eliahu Heldman, David Gurwitz, Rachel Haring, Yishai Karton, Haim Meshulam, Zippora Pittel, Daniele Marciano, Itzhak Marcovitch, Rachel Brandeis, Terese A. Treves, Ruth Verchovsky, Sonia Klimowsky and Amos D. Korczyn Selective Muscarinic Agonists for Alzheimer Disease Treatment . . . . . . 224 Roy D. Schwarz, Michael J. Callahan, Robert E. Davis, Juan C. Jaen, William Lipinski, Charlotte Raby, Carolyn J. Spencer and Haile Teele Xanomeline: An Efficacious and Specific MI Receptor Agonist-Preclinical Update ........................... 229 Harlan E. Shannon, Frank P. Bymaster, David O. Calligaro, Beverley Greenwood, Charles H. Mitch, John S. Ward, Per Sauerberg, Preben Olesen, Malcolm Sheardown, Michael D.B. Swedberg and Peter D. Suzdak Xanomeline, A Specific MI Agonist: Early Clinical Studies. . . . . . . . . 234 N.C. Bodick, A.F. DeLong, P.L. Bonate, T. Gillespie, D.P. Henry, J.H. Satterwhite, R.A. Lucas, J. Heaton, G.V. Carter, L. Farde, N.R. Cutler, J.J. Sramek, R.D. Seifert, J.J. Conrad and T.S. Wardle CI-979/RU 35926: A Novel Muscarinic Agonist for the Treatment of Alzheimer'S Disease ........................ 239 Toni M. Hoover Part Vll. Drugs to Enhance Acetylcholine Synthesis and Release Choline Metabolism, Membrane Phospholipids, and Alzheimer's Disease . ............................. 247 Steven A. Farber, Barbara E. Slack, Enrico DeMicheli, Richard J. Wurtman, Roger M. Nitsch, John H. Growdon, Bruce M. Cohen, Andrew L. Stoll and Perry F. Renshaw x Contents Neurotransmitter Release Enhancement as a Possible Therapy for Neurodegenerative Diseases: Update on Linopirdine (DUP996) ..... 252 Robert Zaczek, Robert J. Chorvat, Richard A. Earl and S. William Tam Part vm. Nootropic Drugs in AD Treatment Nootropic Drugs: The Gap Between Preclinical and Clinical Results . .. 259 Giancarlo Pepeu, Maria Grazia Giovannini, neana Marconcini Pepeu and Luciano Bartolini Nootropic Drugs in Allheimer Disease Treatment. New Pharmacological Strategies . . . . . . . . . . . . . . . . . . . . . . . . . 265 Tatiana A. Voronina Therapeutic Efficacy of Nootropic Drugs in Alzheimer's Disease and Age Related Cognitive Dysfunction ............... 270 Julian A. Gray, Jennifer A. Nagel, Roman Amrein, Giorgio Marini and Umberto Senin Part IX. Neurotrophins, Growth Factors, and Neuroprotection in the Treatment or Alzheimer's Disease Toward the Repair of Cortical Synapses in Alzheimer's Disease . . . . . . 277 A. Claudio Cuello Gangliosides in Allheimer's Disease: Experimental and Clinical Data ......................... 284 Lars Svennerholm and Gino Toffano Part X. Excitatory Amino Acids, Ca + + Cellular Homeostasis, Nitric Oxide, and AD Treatment Excitatory Transmitter Neurotoxicity and Allheimer's Disease . . . . . . . 293 John W. Olney and Nuri B. Farber Free Intracellular Calcium in Aging and Allheimer's Disease ....... 299 Walter Muller, Anne Eckert, Henrike Hartmann and Hans Forstl Nitric Oxide Synthase in a Lesion Model of Alzheimer'S Disease ..... 304 Kiminobu Sugaya and Michael McKinney
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