Handbook of Experimental Pharmacology Volume 147 Editorial Board G.Y.R. Born, London D. Ganten, Berlin H. Herken, Berlin K. Starke, Freiburg i. Br. P. Taylor, La Jolla, CA Springer-Verlag Berlin Heidelberg GmbH Pharmacology of Ionic Channel Function: Activators and Inhibitors Contributors s. Adachi-Akahane, l Barhanin, E.A. Barnard, IB. Bergsman, H. Betz, IM. Christie, M.-D. Drici, M. Endo, R.I Evans, G. Giebisch, T. Gonoi, M. Gordey, A.o. Grant, M.E. Grunwald, RJ. Harvey, s.c. Hebert, F. Hofmann, M. Iino, T. Ikemoto, K. Imoto, A. Inanobe, D.E. Jane, N. Klugbauer, Y. Kubo, Y. Kurachi, E. Latorre, M. Lazdunski, C. Legros, F. Lesage, M. Mishina, D.T. Monaghan, T. Nagao, c.G. Nichols, R.W. Olsen, o. Pongs, s. Seino, D.A. Skifter, E. Stefani, w. l Teulon, L. Toro, H.-W. Tse, R.W. Tsien, C. Vergara, Wang, D.B. Wheeler, IL. Yakel, K.-W. Yau, H. Zhong Editors: M. Endo, Y. Kurachi, and M. Mishina i Springer Professor MAKATO ENDO, M.D., Ph.D. Professor Dr. MASAYOSHI MISHINA Saitama Medical School University of Tokyo 38 Morohongo, Moroyama Department of Molecular Iruma-Gun Neurobiology and Pharmacology Saitama 350-0495 School of Medicine Japan Hongo 7-3-1, Bukyo-ku e-mail: [email protected] Tokyo 113-0033 Japan Professor Dr. YOSHIHISA KURACHI e-mail: [email protected] Osaka University Department of Pharmacology II Graduate School of Medicine and Faculty of Medicine 2-2 Yamada-oka, Suita Osaka 565-0871 Japan e-mail: [email protected] With 107 Figures and 25 Tables ISBN 978-3-642-63030-9 Library of Congress Cataloging·in-Publication Data Pharmacology of ionic channel function : activators and inhibitors / editors, M. Endo, Y. Kurachi, M. Mishina. p. cm - (Handbook of experimental pharmacology; v. 147) Inc1udes bibliographical references and index. ISBN 978-3-642-63030-9 ISBN 978-3-642-57083-4 (eBook) DOI 10.1007/978-3-642-57083-4 1. Ion channels. 2. Ion channels - Effect of drugs ono 1. Endo, Makoto, 1933- II. Kurachi, Yoshihisa. III. Mishina, M. (Masayoshi), 1947- . IV. Series. [DNLM: 1. Ion Channe1s - physiology. 2. Calcium Channel Blockers - pharmacology. 3. Cell Membrane - physiology. 4. Ion Channels - antagonists & inhibitors. 5. Membrane Potentials - physiology. QH 603.154 P536 2000] QP905.H3 voI. 147 [QH603.154] 615'.ls - dc21 [615'.7] 00-026585 This work is subject to copyright. All rights are reserved, whether the whole or part of the material is concerned, specifically the rights of translation, reprinting re-use of illustrations, recitation, broadcasting, reproduction on microfilms or in any other way, and storage in data banks. Duplication of this publication or parts thereof is permitted only under the provisions of the German Copyright Law of September 9, 1965, in its current version, and permission for use must always be obtained from Springer· Verlag. Violations are liable for Prosecution under the German Copyright Law. © Springer-Verlag Berlin Heidelberg 2000 Originally published by Springer-Verlag Berlin Heidelberg in 2000 Softcover reprint of the hardcover 1s t edition 2000 The use of general descriptive names, registered names, etc. in this publication does not imply, even in the absence of a specific statement, that such names are exempt from the relevant protective laws and regulations and free for general use. Product liability: The publishers cannot guarantee the accuracy of any information about dosage and applica tion contained in this book. In every individual case the user must check such information by consulting the relevant literature. Coverdesign: design & production GmbH, Heidelberg Typesetting: Best-set Typesetter Ud., Hong Kong SPIN: 10647765 27/3020-5432 1 0-printed on acid-free paper Preface Life did not come into existence until living organisms developed the ability to establish an internal ionic environment which was quite different from that of the external world. Not only is the intracellular ionic composition suitable for various cellular housekeeping reactions, but its difference from the extra cellular medium was ingeniously utilized by the cell for responding to stimuli given to the cell or to other changes in the environment. In the latter responses two major pathways are used: (1) alteration of the membrane potential that is formed by the difference in the ionic compositions across the boundary membrane combined with the different permeabilities of the membrane to each ion, and (2) alteration of the intracellular concentration of ions, particu larly of calcium ions, which is minute under normal conditions and, therefore, easily altered. In both cases, ion channels in the boundary membrane play the key role, by changing the ionic permeability and by allowing ionic transport down the electrochemical potential gradient as a result of the permeability change. Since ion channels are thus vitally important in living organisms, they developed various kinds of ion channels, some of which, for example, are highly selective for a particular ion but others are rather nonselective. All the ion channels have special gating mechanisms of their own which are suitable for playing the given physiological role. The alteration of the functions of these ion channels by drugs or chemical agents, therefore, undoubtedly constitutes a very important field of pharmacology. Studies on ion channels have made great advances since the late 1980s, especially using molecular biology tech niques. Many books have been published on ion channels, but we felt that we still need a comprehensive book which focuses on activatiors and inhibitors of ion channels. This book is meant to fulfill that need. Although some of the important ion channels, such as chloride channels or mechanically activated channels, have unfortunately not been included in this book, the editors of this volume believe that this book is still fairly comprehensive and very useful. We hope that the readers will agree that the authors have done an excellent job and that they will enjoy reading this stimulating volume. Spring 2000 MAKoTo ENDO Saitama, Japan List of Contributors ADACHI-AKAHANE, S., Laboratory of Pharmacology and Toxicology, Graduate School of Pharmaceutical Sciences, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan e-mail: [email protected] BARHANIN, 1., Institut de Pharmacologie Moleculaire et Cellulaire, CNRS-UPR 411, 660 Route des Lucioles, Sophia Antipolis, F-06560 Valbonne, France e-mail: [email protected] BARNARD, E.A., Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge CB2 1QJ, United Kingdom e-mail: [email protected] BERGSMAN, 1.B., Department of Molecular and Cellular Physiology, Beckman Center BI05, Stanford University School of Medicine, Stanford, CA 94305-5345, USA BETZ, H., Max-Planck-Institut fUr Hirnforschung, Abteilung Neurochemie, Deutschordenstr. 46, D-60528 Frankfurt am Main, Germany e-mail: [email protected] CHRISTIE, 1.M., Department of Pharmacology, University of Nebraska Medical Center, 600 S. 42nd Street, Box 986260, Omaha, NE 68198-6260, USA DRICI, M.-D., Institut de Pharmacologie Moleculaire et Cellulaire, CNRS-UPR 411,660 Route des Lucioles, Sophia Antipolis, F-06560 Valbonne, France ENDO, M., Saitama Medical School, 38 Morohongo, Moroyama, lruma-Gun, Saitama 350-0495, Japan e-mail: [email protected] VIII List of Contributors EVANS, R.J., Department of Cell Physiology and Pharmacology, University of Leicester, Medical Sciences Building, University Road, Leicester LE1 9HN, United Kingdom e-mail: [email protected] GIEBISCH, G., Department of Cellular and Molecular Physiology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520-8026, USA e-mail: [email protected] GONOI, T., Research Center for Pathogenic Fungi and Microbial Toxicoses, Chiba University, 1-8-1, Inohana Chuo-ku, Chiba, Japan 260-8673, Japan e-mail: [email protected] GORDEY, M., Department of Molecular and Medical Pharmacology, UCLA School of Medicine, 23-120 CHS, Box 951735, Los Angeles, CA 90024-1735, USA GRANT. A.o., Cardiovascular Division, Department of Medicine, Duke University Medical Center, Durham, NC 27710-3504, USA e-mail: [email protected] GRUNWALD, M.E., Department of Molecular and Cell Biology, University of California at Berkeley, Berkeley, CA 94720, USA HARVEY, R.J., Department of Pharmacology, The School of Pharmacy, 29-39 Brunswick Square, London WC1 N1AX, United Kingdom HEBERT, S.c., Department of Cellular and Molecular Physiology, Yale University, School of Medicine, 333 Cedar Street, New Haven, CT 06520-8026, USA HOFMANN, F., Institut fUr Pharmakologie und Toxikologie, Technische Universitat Mtinchen, Biedersteiner Str. 29, D-80802 Mtinchen, Germany e-mail: [email protected] IINO, M., Department of Pharmacology, Graduate School of Medicine, The University of Tokyo; CREST, Japan Science and Technology Corporation, Bunkyo-ku, Tokyo 113-0033, Japan e-mail: [email protected] IKEMOTO, T., Department of Pharmacology, Saitama Medical School, 38 Morohongo, Moroyama, Iruma-Gun, Saitama 350-0495, Japan List of Contributors IX IMOTO, K., National Institute for Physiological Sciences, Department of Information Physiology, Myodaiji, Okazaki 444-8585, Japan e-mail: [email protected] INANOBE, A., Department of Pharmacology II, Graduate School of Medicine and Faculty of Medicine, Osaka University, 2-2 Yamada-oka, Suita, Osaka 565-0871, Japan JANE, D.E., Department of Pharmacology, University of Bristol, Bristol, BS8 lTD United Kingdom e-mail: [email protected] KLUGBAUER, N., Institut fUr Pharmakologie und Toxikologie, Technische Universitat Munchen, Biedersteiner Str. 29, D-80802 Munchen, Germany KUBO, Y, Department of Systems Physiology, Tokyo Medical and Dental University, Graduate School of Medicine and Dentistry, Yushima 1-5-45, Bunkyo-ku, Tokyo 113-8519, Japan e-mail: [email protected] KURACHI, Y, Department of Pharmacology II, Graduate School of Medicine and Faculty of Medicine, Osaka University, 2-2 Yamada-oka, Suita, Osaka 565-0871, Japan e-mail: [email protected] LATORRE, E., Avenida Arturo Prat 514, Casilla 1469, Valdivia, Chile e-mail: [email protected] LAZDUNSKI, M., Institut de Pharmacologie Moleculaire et Cellulaire, CNRS UPR 411, 660 Route des Lucioles, Sophia Antipolis, F.06560 Valbonne, France e-mail: [email protected] LEGROS, c., Institut fUr Neurale Signalverarbeitung, ZMNH, Martinistr. 52, D-20246 Hamburg, Germany LESAGE, F., Institut de Pharmacologie Moleculaire et Cellulaire, CNRS-UPR 411,660 Route des Lucioles, Sophia Antipolis, F.06560 Valbonne, France MISHINA, M., Department of Molecular Neurobiology and Pharmacology, University of Tokyo, School of Medicine, Hongo 7-3-1, Tokyo 113-0033, Japan e-mail: [email protected] x List of Contributors MONAGHAN, D.T., Department of Pharmacology, Box 986260, University of Nebraska Medical Center, Omaha, NE 68198-6260, USA e-mail: [email protected] NAGAO, T., Laboratory of Pharmacology and Toxicology, Graduate School of Pharmaceutical Sciences, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan NICHOLS, CG., Department of Cell Biology and Physiology, Washington University School of Medicine, 660 South Euclid Ave., St. Louis, MO 63110, USA e-mail: [email protected] OLSEN, R.W., Department of Molecular and Medical Pharmacology, UCLA School of Medicine, 23-120 CHS, Box 951735, Los Angeles, CA 90024-1735, USA e-mail: [email protected] PONGS, 0., Institut fUr Neurale Signalverarbeitung, ZMNH, Martinistr. 52, D-20246 Hamburg, Germany e-mail: [email protected] SEINO, S., Department of Molecular Medicine, Chiba University Graduate School of Medicine, 1-8-1, Inohana, Chuo-ku, Chiba 260-8673, Japan e-mail: [email protected] SKIFTER, D.A., Department of Pharmacology, University of Nebraska Medical Center, 600 S. 42nd Street, Box 986260, Omaha, NE 68198-6260, USA STEFANI, E., Facultad de Ciencias, Universidad de Chile, Centro de Estudios Cientificos de Santiago, Av. Presidente Emizuriz #3132, Casilla 16443, Santiago 9, Chile, and Departments of Anesthesiology, Physiology and Brain Research Institute, University of California, Los Angeles, CA, USA TEULON, J., INSERM U-426, Faculte de Medecine Xavier Bichat, B.P. 416, 16 rue Henri Huchard, F-75870 Paris cedex, France e-mail: [email protected] TORO, L., Departments of Anesthesiology, Physiology and Brain Research Institute, University of California, Los Angeles, CA, USA TSE, H.-W., Department of Pharmacology, University of Bristol, Bristol, United Kingdom List of Contributors XI TSIEN, RW., Department of Molecular and Cellular Physiology, Beckman Center BI05, Stanford University School of Medicine, Stanford, CA 94305-5345, USA e-mail: rwtsien@lelandostanfordoedu VERGARA, C, Facultad de Ciencias, Universidad de Chile, Centro de Estudios Cientificos de Santiago, Avo Presidente Emizuriz #3132, Casilla 16443, Santiago 9, Chile WANG, w., Department of Pharmacology, New York Medical College, New York, NY, USA WHEELER, DoB., Department of Molecular and Cellular Physiology, Beckman Center BI05, Stanford University School of Medicine, Stanford, CA 94305-5345, USA YAKEL, IL., Laboratory of Signal Transduction, National Institute of Environmental Health Sciences, National Institutes of Health, F2-08, p.o. Box 12233, 111 ToW. Alexander Drive, Research Triangle Park, NC 27709, USA e-mail: yakel@niehsonihogov YAU, K.-Wo, Department of Neuroscience and Ophthalmology, 9th Floor, Preclinical Teaching Building, Johns Hopkins University School of Medicine, 725 North Wolfe Street, Baltimore, MD 21205-2185, USA e-mail: [email protected] ZHONG, H., Department of Johns Hopkins University School of Medicine, 725 North Wolfe Street, Baltimore, MD 21205-2185, USA