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ANNALS OF THE NEW YORK ACADEMY OF SCIENCES Volume 757 EDITORIAL STAFF Erecutive Editor BILL BOLAND Managing Editor JUSTINE CULLINAN The New YorkAcademy of Sciences Associate Editor 2 East 63rd Street. MARION L. GARRY New York, New York 10021 THE NEW YORK ACADEMY.OF SCIENCES (Founded in 1817) BOARD OF GOVERNORS, July 1994-June 1995 JOSHUA LEDERBERG, Chairman of the Board HENRY M. GREENBERG. President MARTIN L. LEIBOWITZ, President-Elect Honorary Life Governor WILLIAM T. GOLDEN HENRY A. LICHSTEIN, Treasurer Governors-at-Large ELEANOR BAUM BARRY R. BLOOM D. ALLAN BROMLEY EDWARD COHEN SUSANNA CUNNINGRAM-RUNDLES ' BILL GREEN SANDRA PANEM RICHARD A. RIFKIND DOMINICK SALVATORE DAVID E. SHAW WILLIAM C. STEERE,.Ja. SHMUEL WINOGRAD CYRIL M. HARRIS, Past Chairman HELENE L. KAPLAN, General Counsel [ex officio] RODNEY W. NICHOLS, Chief Executive Officer [ex officio]

DIVERSITY OF INTERACTING - RECEPTORS

DIVERSITY OF INTERACTING RECEPTORS

i { ANNALS OF THE NEW YORK ACADEMY OF SCIENCES Volume 757 ~ > s. x ~ DIVERSITY OF INTERACTING RECEPTORS Edited by Leo G. Abood and Abel Lajtha , The New York Academy of Sciences New York, New York 1995

Copyright a 1995 by the New York Academy of Sciences. All rights reserved Under the provisions of the. United States Copyright Act of 1976, individual readers of the Annals are permitted to make fair use of them for teaching and research. Permission is granted to quote from the Annals provided that the customary acknowledgment is made of the source. Material in the Annals may be republished only by permission of the Academy. Address. _ inquiries to the Executive Editor at the New YorkAcademy of Sciences. Copying fees: For each copy of an article made beyond the free copying permitted under Section 107 or 108 of the 1976 Copyright Act, a fee should be paid through the Copyright.Clearance Center Inc., 222 Rosewood Drive, Danvers, MA 01923. For articles of more than 3 pages, the copying fee is $1.75. . ® The paper used in this publication meets the minimum requirements of the American National Standard for Information Sciences-Permanence of Paper for Printed Library Materials, ANSI Z39.48-1984. , Cover illustration: The cascade of effects caused by the release of a.neurotransmitter. , Library of Congress Cataloging-in-Publication Data Diversity of interacting receptors/edited by Leo G. Abood and Abel Laj tha. p. cm. -(Annals of the New. York Academy of Sciences, ISSN _ 0077-8923; v. 757) Papers presented at a conference entitled Functional Diversity.of - Interacting Receptors, held in Washington, D.C. on May 25-28, 1994. ISBN 0-89766-923-1 (cloth). - ISBN 0-89766-924-X (paper) 1. Neurotransmitter receptors-Congresses. 2. Cell receptors- -Congresses. I. Abood, Leo G. II. Lajtha, Abel. III. Series. Q11.N5 vol. 757 [QP364.7] 500 s-dc20 [591.1'88] 95-11515 CIP SP Printed in the United States ofAmenca ISBN 0-89766-923-1 (cloth) ISBN 0-89766-924-X (paper) ISSN 0077-8923

ANNALS OF THE NEW YORK ACADEMY OF SCIENCES Volume 757 May 10, 1995 ` DIVERSITY OF INTERACTING RECEP.TORSa Editors and Conference Organizers LEO G. ABOOD AND ABEL LAJTHA CONTENTS Background and Overview of the Conference. By LEO G. ABOOD ..................... Part I. General Principles of Chemical Communication Molecular Organization of Receptors. Efficacy, Agonists, and Antagonists. By VICTOR J. HRUBY, HENRY L YAMAMURA, and FRANK PORRECA .......... 7 Determination of the Chemical Mechanism of Neurotransmitter Receptor- mediated Reactions by Rapid Chemical Kinetic Methods. By GEORGE P. HESS, LI NIU, and RAYMOND WIEBOLDT ....................................................... 23 . Ligands, Receptor Models, and Evolution. By VIC COCKCROFT, MARCELO ORTELLS, and GEORGE LUNT .................................................................:....... 40 Part II. Diversity- and Heterogeneity of Nicotinic Receptor Structure and Function. Nicotinic Receptor Function in the Mammalian Central Nervous System. By EDSON X. ALBUQUERQUE, EDNA F. R.' PEREIRA, NEWTON G. CASTRO, MANICKAVASAGOM ALKONDON, SIGRID REINHARDT, HANNSJORG SCHRODER, and ALFRED MAELICKE .............................................................. 48 Nicotinic Receptors and Cholinergic Neurotransmission in the Central Nervous System. By PAUL B. S. CLARKE ........................................................ 73 Neurochemical Evidence of Heterogeneity of Presynaptic and Somatodendritic Nicotinic Acetylcholine Receptors. By E. S. Vizi, H. SERSHEN, A. BALLA, A. MIKE, K. WINDISCH, ZS: JURi1NYi, and A. LA ITxA ...........................................................:.........................:.............. .... 84 Neuronal Nicotinic Receptor Subtypes. By JON LINDSTROm, ReNE ANAND, XIAO PENG, VOLODYMYR GERZANICH, FAN WANG, and YUEBING LI...:.... 1,00 Methods for Increasing the Expression Level of a Soluble Fusion Protein. Encoding a 62 Amino Acid Fragment of the a-Subunit of the Nicotinic Acetylcholine Receptor. By LISA N. GENTILE and EDWARD HAWROT:....... 117 °This volume contains papers presented at a conference entitled.Functional Diversity of Interacting Receptors, which was sponsored by the New York Academy of Sciences and held in Washington, D.C. on May 25-28, 1994.

Probing Ion Channels and Recognition Sites of Neuronal Nicotinic Cholinergic Receptors with Novel Nicotine Affinity and Other Ligands. By NICOLE LERNER-MARMAROSH, ANDREW S. KENDE, DAVID X. WANG, and LEO G. ABOOD ........... ....................................... ........................................ 120 Binding Sites for Neurotoxins and Cholinergic Ligands in Peripheral and Neuronal Nicotinic Receptors. Studies with Synthetic Receptor Sequences. By BIANCA M. CONTI-FINE, ALFRED MAELICKE, SIGRID REINI-IARDT-MAELICKE, VINCENT CHIAPPINELLI, and KATYA E. MCLaNE. 133 Diversity and Patterns of Regulation,of Nicotinic Receptor Subtypes. By RONALD J. LUxas ................................................:...................................... 153 Part III. Cholinergic Receptors, Subtypes, Function, and Regulation . Cholinergic Pathways and the Ascending Reticular Activating System of the Human Brain. By M-MARSEL MESULAM ....................................................... 169 Regulation_of Muscarinic Acetylcholine Receptor Expression and Function. By JACQUES C. MIGEON, PHYLLIS S. GOLDMAN, BETH A. HABECKER, and NEIL M. NATHANSON ...................................................................................... 180 Development of Selective Antisera for Muscarinic Cholinergic Receptor Subtypes. By BARRY B. WOLFE and ROBERT P. YASUDA ............................. 186 Studies on the Diversity of Muscarinic Receptors in the Autoregulation of Acetylcholine Release in the Rodent Cerebrum Using Furan Analogs of Muscarine. By B. V. RAMA SASTRY, O. S._TAYEB, and N. JAISWAL ............. . 194 •Phosphorylation of the Nicotinic Acetylcholine Receptor by Protein Tyrosine Kinases. By SHERIDAN L. SWOPE, ZHICAN Qu, and RICHARD L. HUGANIR. 197 S-Nitrosylation of m2 Muscarinic Receptor Thiols Disrupts Receptor-G- Protein Coupling. By ROBERT, S. ARONSTAM, DAN C. MARTIN, ROBERT L. DENNISON, and HEATHER G. COOLEY ...:....................................................... 215 Combined Administration of Agonist-Antagonist as a Method of Regulating Receptor Activation. By JED E. ROSE, EDWARD D. LEVIN, FREDERIQUE M. BEHM; ERIC C. WESTMAN, ROY M. STEIN, JAMES D. LANE, and GAIL V. RIPxA ...................................................................................:...............: ............ . 218 Preliminary Two-Dimensional [IH]NMR Characterization of the Complex Formed between an 18-Amino Acid Peptide Fragment of the a-Subunit of the Nicotinic Acetylcholine-Receptor and a-Bungarotoxin. By LISA N. GENTILE, VLADIMIR J. BASUS, Q[NG-LUO SHi, and EDWARD HAWROT...... 222 Part IV. Nicotinic Receptors and Interactions with Other Receptor Pathways Nicotine Effects on Presynaptic Receptor Interactions. By H. SERSHEN, E. TOTH, A. LAJTHA, and E. S. Vlzt ..:............................................................ 238 Acute and Chronic Nicotinic Interactions with Dopamine Systems and Working Memory Performance. By EDWARD D. LEVIN and JED E. ROSE.. 245

Part V.'Aminergic Receptor Heterogeneity, Regulation, and Interactions Structural and Functional Diversity of f3-Adrenergic Receptors. By A: D. STROSBERG .................................................................................................... ... , 253 Inverse Regulation of Hepatic a16- and i3Z-Adrenergic Receptors. Cellular Mechanisms and Physiological Implications. By GEORGE KUNOS, EDWARD J. N. ISHAC, BIN GAO, and Liu JIANG ........ .................................... 261 Induced Hibernation by a2-Adrenoceptor Agonists. By N. ERIC NAFTCHI....... 272 Effect of HypothermialAnesthesia Induced by a2-Adrenoceptor Agonist on Monoamine Turnover and Neurotensin Concentrations in the Rat Brain. ByN. ERIC NAFTCHI, HENRY SERSHEN, AUDREY HASHIM, and GARTH B I S S ET T .................................................................................................... ......... 2 75 Novel Dopamine Receptor Subtypes as Targets for Antipsychotic Drugs..By PIERRE SOKOLOFF, JORGE DIAZ, DANIEL LEVESQUE,.CATHERINE PILON, . VIOLETTA DIMITRIADOU, NATHALIE GRIFFON, CLAAS H. LAMMERS, MARIE-PASCALE MARTRES, and JEAN-CHARLES SCHWARTZ ....................... 278 Denervation, Hyperinnervation, and Interactive Regulation of Dopamine and Serotonin Receptors. By TOMAS A. READER, FATIHA RAD.rA, KAREN M. DEWAR, and LAURENT DESCARRIES ......................................... ....... ............... 293 Aspartame Does Not Affect Aminergic and Glutamatergic Receptor Kinetics - in Rat Brain. By M. A. REILLY and A. LA.tTHA ............................................. 311 Molecular and Functional Diversity of Histamine Receptor Subtypes. By JEAN-MICHEL ARRANG, GUILLAUME DRUTEL, MONIQUE GARBARG, MARTIAL RUAT, ELISABETH: TRAIFFORT, and JEAN-CHARLES SCHWARTZ. 314 Part VI. Opioid Receptor Subtypes and Modulation Recent Studies on a µ-Opioid Receptor Purified from Bovine Striatum. By ERIC J. SIMON ...........................................................................:................. 324 i Correlating the Pharmacology and Molecular Biology of Opioid Receptors. Cloning and Antisense Mapping a Kappa3-related Opiate Receptor. By G. W. PASTERNAK,-Y-X. PAN, and J. CHENG .:............................................... 332 Characterization of Opioid Receptor Types and Subtypes.with New Ligands. By ANNA BoRSODt and GEZA TOTH ............................................................... 339 Opiate Receptor Changes after Chronic Exposure to Agonists and Antagonists. By. JAMES E. ZADINA, ABBA J. KASTIN, LAURA M. ° - HARRISON, LIN-JUN GE, and SULIE L. CHANG .............................................. 353 In rivo Interactions between Opioid and Adrenergic Receptors for Peripheral Sympathetic Functional Regulation. By HERMAN M: RHEE and DONG H. PARK .........................:............................................................... 362 Part VIII. Peptidergic Receptor Interactions . Receptor-Receptor Interactions and Their Relevance for Receptor Diversity. Focus on Neuropeptide(Dopamine Interactions. By K: FuxE, X: M. Li, S. TANGANELLI, P. HEDLUND, W. T. O'CONNOR, L. FERRARO, U. UNGERSTEDT, and L. F. AGNATI ............................................. ......... ........... 65 Anatomy and Mechanisms of Neurotensin-Dopamine Interactions in the Central Nervous System. By PHILIP D. LAMBERT, ROBIN GROSS, CHARLES B. NEMEROFF, and CLINTON D. KILTS ................................. :.......... 377

Distribution of Neuropeptide Receptors. New Views of Peptidergic Neurotransmission Made Possible by Antibodies to Opioid Receptors. By ROBERT ELDE, ULF ARVIDSSON, MAUREEN RIEDL, LUCY VULCHANOVA, JANG-HERN LEE, ROBERT DADO, ALBERT NAKANO, SUMITA CHAKRABARTI, Xu ZHANG; HORACE H. LOH, PING Y. LAw, TOMAS- HOKFELT, and MARTIN WESSENDORF .................................................:.........: 390 Localization of the Peptide Binding Domain of the NK 1 Tachykinin Receptor Using Photoreactive Analogues of Substance P. By N. D. BOYD, R. KAGE,.J. J. DuMAS, S. C. SILBERMAN, J. E. KRAUSE, and S. E. LEEMAN ...............................................................................:.................... ........ 405 Effects of Peptide YY on CCK/CCKAntagonist Interactions in Cerulein- induced Pancreatic Injury. By JOSEPH M. TITO, MAREK RUDNICKI, DIANE C. ROBINSON, WILLIAM B. GUINEY, THOMAS E. ADRIAN, and MICHAEL S. GOLD .............................................:...................................................... :......:.... 410 Aglyco Pathology of Viral_Receptors in Dementias. By:S. BOGOCH and E. S. BoGOCH .................................................................................................... ........ 413 Part VIII. Excitatory Amino Acid Receptor Modulation and Pathology Excitatory Amino Acid Metabotropic Receptor Subtypes and Calcium Regulation. By 1V1AX RECASENS 8nd MICHEL VIGNES.:................................. 418, Polyamines as Endogenous Modulators of the N-Methyl-D-Aspartate Receptor. By EDYTHE D. LONDON and ALEXEY MUKHIN ........:................... 430. Effects of Systematically Administered Polyamines on Imipramine. Immobility Action in Rats. By K. SzczAwirtsKA and D. CENA.fEK-MUSIAL. 437 Glutamate Receptor Modulation of [3H]GABA Release and Intracellular Calcium in Chick Retina Cells. By ARSELIO P. CARVALHO,.ILDETE L. FERREIRA, ANA L. CARVALHO, and CARLOS B. DUARTE ............................. .. 439 . Characterization of Voltage-Sensitive Ca2+ Channels Activated by Presynaptic Glutamate Receptor Stimulation in Hippocampus..By C. M. CARVALHO, J. O. MALVA, C. B. DUARTE, and A. P. CARVALHO ................. 457 Roles of Metabotropic Glutamate Receptors in Brain Plasticity and Pathology: By STEPHAN MILLER, J. PATRICK KESSLAK, CARMELO ROMANO, and CARL W. COTMAN ................................................................... 460. Role of Glutamate and Glutamate Receptors in Memory Function and Alzheimer's Disease. By FRODE FoNNUM, TROND MYHRER, RAGNHILD E. PAULSEN, KATRINE WANGEN, and ANNE RITA OKSENGARD ....................... 475 Pharmacological Augmentation of NMDA Receptor Function for Treatment of Schizophrenia. By ILANA ZYLBERMAN, DANIEL C. JAVITT, and STEPHEN R. ZUKIN .......................................................................................... 487 Excitatory Amino.Acid Receptors and Their Role in Epilepsy and Cerebral Ischemia: By BRIAN S. MELDRUM ............. ...................................................... 492 Part IX. GABA Receptor Heterogeneity Structure and Distribution of Multiple GABAA Receptor Subunits with Special Reference to the Cerebellum. By W. WISDEN ..................................... 506 Cerebral GABAA and GABAe Receptors. Structure and Function. By HIROSHI NAKAYASU, HIROSHI KIMURA, and KINYA KURIYAMA ................. 516