Handbook of Experimental Pharmacology Volume 1041/ Editorial Board G.V.R. Born, London P. Cuatrecasas, Ann Arbor, MI H. Herken. Berlin Opioids I Contributors H. Akil, S. Archer, A. Beaumont, M. Blum, D. Bronstein, S.R. Childers A.D. Corbett, B.M. Cox, V. Dauge, R. Day, S. Dermer, J. Donnerer A.W. Duggan, R. Elde, S.M. Fleetwood-Walker, L.D. Fricker M.-C. Fournie-Zaluski, T.L. Gioannini, A. Goldstein, T. H6kfelt V. H6llt, J.W. Holaday, H. Khachaturian, N. Kley, C.M. Knapp H.W. Kosteriitz, N.M. Lee, F.M. Leslie, N. Levin, M.E. Lewis J.P. Loeffler, H.H. Loh, D. Lorang, J.R. Lundblad, A. Mansour A.H. Mulder, R.A. North, S.J. Paterson, D.E. Pellegrini-Giampietro J.E. Pintar, F. Porreca, P.S. Portoghese, J.L. Roberts, B.R. Roques J. Rossier, R.B. Rothman, M.K.H. Schafer, P.W. Schiller A.N.M. Schoffelmeer, R.E.M. Scott, E.J. Simon, A.P. Smith J.A.M. Smith, S. Spector, A. Tempel, H. Teschemacher, K.A. Trujillo E. Young, S.J. Watson, P.L. Wood, R.S. Zukin Editor: Albert Herz Section Editors: H. Akil and E.1. Simon Springer-Verlag Berlin Heidelberg New York London Paris Tokyo Hong Kong Barcelona Budapest Professor Dr.med. ALBERT HERZ Max-Planck-Institut fur Psychiatrie Abteilung Neuropharmakologie Am Klopferspitz 18 W-8033 Martinsried, FRG Section Editors Dr. med. HUDA AKIL Mental Health Research Institute School of Medicine University of Michigan 205 Zina Pitcher Ann Arbor, MI 48109, USA Dr. med. ERIC J. SIMON New York University Medical Center School of Medicine 550 First A venue New York, NY 10016, USA With 74 Figures and 52 Tables ISBN -13: 978-3-642-77462-1 e- ISBN -13: 978-3-642-77460-7 DOl: 10.1007/978-3-642-77460-7 Library of Congress Cataloging-in-Publication Data. Opioids I / contributors, H. Akil ... [et al.l; editor, Albert Herz; (H. Akil and EJ. Simon, section editors). p. cm. - (Handbook of experimental pharmacology; v. 104) Includes bibliographical references and index. ISBN-13:978-3-{i42-77462-1 l. Opioids. 2. Opioids - Receptors. I. Akil, H. (Huda) II. Herz, Albert, 1921- . III. Simon, Eric 1. IV. Title: Opioids l. V. Series. [DNLM: 1. Endorphins. 2. Receptors, Endorphin. WI HA51L v. 104 / QU 68 0603] QP905.H3 vol. 104 [RM328] 615' .1 s - dc20 [615' .78] DNLMIDLC for Library of Congress 92-2325 CIP 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, reuse of illustrations, recitation, broad­ casting, reproduction on microfilm or in any other way, and storage in data banks. Duplication of this publication or parts thereof is permitted only under 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. 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Typesetting: Best-set Typesetter Ltd., Hong Kong 27/3130 - 5 4 3 2 1 0 - Printed on acid-free paper List of Contributors AKIL, H., Mental Health Research Institute, School of Medicine, University of Michigan, 205 Zina Pitcher, Ann Arbor, MI 48109, USA ARCHER, S., Department of Chemistry, Cogswell Laboratory, Rensselaer Polytechnic Institute, Troy, NY 12180-3590, USA BEAUMONT, A., Departement de Chimie Organique, U 266 INSERM, UA 498 CNRS, UFR des Sciences Pharmaceutiques et Biologiques, 4, avenue de l'Observatoire, F-75006 Paris, France BLUM, M., The Fishberg Research Center in Neurobiology, Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029, USA BRONSTEIN, D., Laboratory of Molecular Integrative Neuroscience, National Institute of Environmental Health Sciences, Research Triangle, Park, NC 27709, USA CHILDERS, S.R., Department of Physiology and Pharmacology, Bowman Gray School of Medicine, Medical Center Boulevard, Winston-Salem, NC 27157-1083, USA CORBETT, A.D., Department of Biomedical Sciences, University of Aberdeen, Marischal College, Aberdeen AB9 lAS, Great Britain Cox, B.M., Department of Pharmacology, Uniformed Services University of the Health Sciences, 4301 lones Bridge Road, Bethesda, MD 20814- 4799, USA DAUGE, V., Departement de Chimie Organique, U 266 INSERM, UA 498 CNRS, UFR des Sciences Pharmaceutiques et Biologiques, 4, avenue de l'Observatoire, F-75006 Paris, France DAY, R., I.A. DeSeve Laboratory of Biochemical and Molecular Neuro­ endocrinology, Clinical Research Institute of Montreal, 110 Pine Avenue West, Montreal, Quebec, Canada H2W lR7 DERMER, S., The Fishberg Research Center in Neurobiology, Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029, USA VI List of Contributors DONNERER, J., Department of Experimental and Clinical Pharmacology, University of Graz, A-801O Graz, Austria DUGGAN, A.W., Department of Preclinical Veterinary Sciences, Royal (Dick) School of Veterinary Studies, University of Edinburgh, Summerhall, Edinburgh EH9 1QH, Great Britain ELDE, R., University of Minnesota, Department of Cell Biology and Neuroanatomy, 321 Church Street SE, Minneapolis, MN 55455, USA FLEETWOOD-WALKER, S.M., Department of Preclinical Veterinary Sciences, Royal (Dick) School of Veterinary Studies, University of Edinburgh, Summerhall, Edinburgh EH9 1QH, Great Britain FRICKER, L.D., Department of Molecular Pharmacology, Albert Einstein College of Medicine, 1300 Morris Park Avenue, Bronx, NY 10461, USA FOURNIE-ZALUSKI, M.-C., Departement de Chimie Organique, U 266 INSERM, UA 498 CNRS, UFR des Sciences Pharmaceutiques et Biologiques, 4, avenue de l'Observatoire, F-75006 Paris, France GIOANNINI, T.L., Department of Psychiatry, New York University Medical Center, 550 First Avenue, New York, NY 10016, and Baruch College, CUNY, New York, NY 10010, USA GOLDSTEIN, AVRAM, Stanford University, 735 Dolores, Stanford, CA 94305, USA HOKFELT, T., Karolinska Institute, Department of Histology and Neuro­ biology, P.O. Box 60 400, S-104 01 Stockholm, Sweden HOLLT, V., Physiologisches Institut, Universitat Munchen, PettenkoferstraBe 12, W-8000 Munchen, FRG HOLADAY, J.W., Medicis Corporation, 100 East 42nd Street, 15th Floor, New York, NY 10017, USA KHACHATURIAN, H., Molecular and Cellular Neuroscience Research Branch, National Institute of Mental Health, Room llC-05, Parklawn Building, Rockville, MD 20857, USA KLEY, N., Molecular Neurooncology Laboratory, Massachusetts General Hospital, Harvard Medical School, 149 13th Street, Charlestown, MA 02129-9142, USA KNAPP, C.M., Department of Pharmacy, Veterans Admin. Hospital, 130 W. Kingsbridge Road, Bronx, NY 10468, USA KOSTERLITZ, H.W., Unit for Research on Addictive Drugs, Marischal College, University of Aberdeen, Aberdeen AB9 lAS, Great Britain List of Contributors VII LEE, N.M., Department of Pharmacology, University of Minnesota Twin Cities, Medical School, 3-249 Millard Hall, 435 Delaware Street, S.E., Minneapolis, MN 55455, USA LESLIE, F.M., Department of Pharmacology, California College of Medicine, University of California, Irvine, CA 92717, USA LEVIN, N., The Fishberg Research Center in Neurobiology, Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029, USA LEWIS, M.E., Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380, USA LOEFFLER, J.P., Laboratoire de Physiologie Generale, IPCB, 21, rue Rene Descartes, F-67100 Strasbourg Cedex, France LOH, H.H., Department of Pharmacology, University of Minnesota Twin Cities, Medical School, 3-249 Millard Hall, 435 Delaware Street, S.E., Minneapolis, MN 55455, USA LORANG, D., The Fishberg Research Center in Neurobiology, Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029, USA LUNDBLAD, J.R., The Fishberg Research Center in Neurobiology, Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029, USA MANSOUR, A., Mental Health Research Institute, University of Michigan, 205 Zina Pitcher Place, Ann Arbor, MI 48109-0720, USA MULDER, A.H., Department of Pharmacology, Free University Medical Faculty, Van der Boechorststraat 7, NL-1081 BT Amsterdam, The Netherlands NORTH, R.A., Vollum Institute, Oregon Health Sciences University, 3181 SW Sam Jackson Park Road, Portland, OR 97201, USA PATERSON, S.J., U.M.D.S., Guy's and St. Thomas's Medical and Dental School, Department of Pharmacology, Lambeth Palace Road, London SE1 7EH, Great Britain PELLEGRINI-GIAMPIETRO, D.E., Department of Neuroscience, Albert Einstein College of Medicine, 1300 Morris Park Avenue, Bronx, NY 10461-1988, USA PINTAR, J.E., Department of Anatomy and Cell Biology, Columbia College of Physicians and Surgeons, 630 W. 168th Street, New York, NY 10032, USA VIII List of Contributors PORRECA, F., Department of Pharmacology, College of Medicine, University of Arizona, Tucson, AZ 85724, USA PORTOGHESE, P.S., Department of Medicinal Chemistry, College of Phar­ macy, University of Minnesota, 308 Harvard Street, S.E., Minneapolis, MN 55455, USA ROBERTS, J.L., The Fishberg Research Center in Neurobiology, Mount Sinai School of Medicine, One Gustave L. Levy Place, New York, NY 10029, USA ROQuEs,