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Topics and Perspectives in Adenosine Research: Proceedings of the 3rd International Symposium on Adenosine, Munich, June 1986 PDF

641 Pages·1987·19.216 MB·English
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.T opics and Perspectives in Adenosine Research Proceedings of the 3rd International Symposium on Adenosine, Munich, June 1986 E. Gerlach B.F.Becker (Eds.) With 218 Figures and 64 Tables Springer-Verlag Berlin Heidelberg New York London Paris Tokyo Professor Dr. med. Eckehart Gerlach Dr. rer. nat. Bernhard Friedrich Becker Physiologisches Institut der UniversiHit Miinchen PettenkoferstraBe 12 8000 Miinchen 2 Federal Republic of Germany ISBN- 13 :978-3-642-45621-3 e-ISBN-13 :978-3-642-45619-0 DOl: 10.1007/978-3-642-45619-0 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, broadcasting, reproduction on microfilms or in other ways, and storage in data banks. Duplication of this pUblication or parts thereof is only permitted under the provisions of the German Copyright Law of September 9,1965, in its version of June 24, 1985, and a copyright fee must always be paid. Violations fall under the posecution act of the German Copyright Law. © Springer-Verlag Berlin Heidelberg 1987 Softcover reprint of the hardcover 1 st edition 1987 The use of general descriptive names, trade names, trade marks, etc. in this publication, even if the former are not especially identified, is not to be taken as a sign that such names, as under stood by the Trade Marks and Merchandise Marks Act, may accordingly be used freely by anyone. Product Liability: The publisher can give no guarantee for information about drug dosage and application thereof contained in this book. In every individual case the respective user must check its accuracy by consulting other pharmaceutical literature. Preface An "International Conference on Physiological and Regulatory Functions of Adenosine and Adenine Nucleotides" was held in Banff, Canada, in June 1978. Four years later, in June 1982, an "International Symposium on Adenosine" took place in Charlottesville, Virginia, USA. Both meetings revealed an increasing interest of scientists from numerous disciplines on biochemical, physiological and pathophysiological aspects of adenosine as a proposed mediator of various specified regulatory functions, both on the cellular and organ level. In view of the obvious continuity of adenosine research in well-established and newly emerging fields, a scientific committee was charged with organizing a further meeting to be held in Munich, Germany, in June 1986. Members of the committee were H. P. Baer, Canada, R. M. Berne, USA, and E. Gerlach, G. W. Kreutzberg and J. Schrader, FRG. It was the general intention that in this conference, purposely named "3rd International Symposium on Adenosine", emphasis should be placed on the presentation of shorter reports concerning both latest as well as controversial aspects and developments in as wide a scope of adenosine research as possible. Therefore, in addition to more than 50 presentations by invited speakers, over 120 posters were displayed. Coinciding with the symposium, abstracts of all contributions were published in Pfltigers Archiv - European Journal of Physiology [Vol. 407, Suppl. 1, 1986]. This book, entitled "Topics and Perspectives in Adenosine Research", now enholds all papers presented at the 3rd International Symposium on Adenosine, together with the complete discussions following each talk. In order to make these proceedings available as early as possible, the manuscripts are published as submitted by the authors, except for copy-editing by the publishing company; standardization of abbreviations was not attempted. The transcripts of the oral discussions were edited where necessary. The chapters of the book are arranged according to the topics of the symposium; the sequence of contributions had to be modified only in a few cases. The editors are indebted to Dr. J. Wieczorek, Springer-Verlag, for his thoughtful cooperation in the publication of this book. We hope that these proceedings will help to update and to define the state of the art in major fields of adenosine research - at least for the year 1986 - and will be of value to a broader scientific community. Munich, February 1987 E. Gerlach and B. F. Becker Acknowledgements The "3rd International Symposium on Adenosine" was very generously sponso red by Pharma Schwarz GmbH, Monheim, FRG. Further support was kindly provided by Boehringer Mannheim GmbH, Mannheim, FRG, G6decke AG, Freiburg i. Br., FRG, Hoechst AG, Werk Albert, Wiesbaden, FRG, Paul-Martini-Stiftung, Mainz, FRG, Pfrimmer + Co., Pharmazeutische Werke, Erlangen, FRG, Sandoz AG, Niirnberg, FRG, Schering AG, Berlin, Dr. Willmar Schwabe, Karlsruhe, FRG, Springer-Verlag, Berlin Heidelberg, FRG, Dr. Karl Thomae GmbH, Biberach/Riss, FRG, Warner-Lambert Company, Ann Arbor, USA. Venue and splendid facilities for the meeting were obligingly made available by the Max-Planck-Institute, Martinsried, FRG. On behalf of the Scientific Committee, thanks are once again conferred to all the sponsoring institutions and companies as well as to Mr. M. Giicker, Pharma Schwarz GmbH, for his personal engagement, to Mrs. B. Kratzenberg for her excellent assistance in organisational matters, and to Mrs. K. Schaipp and Mrs. M. Bellstedt for their invaluable, conscientious secretarial help. E. Gerlach Table of Contents I. Adenosine Receptors and Nncleoside Transporter Agonist and Antagonist Radioligands and Photo affinity Labels for the Adenosine Al Receptor J. Linden, C. Q. Earl, A. Patel, R. H. Craig, and S. M. Daluge . . . . . 3 Functional Characterization of Al Adenosine Receptors by Photoaffinity Labeling M. J. Lohse, K-N. Klotz, and U. Schwabe .................. 15 Analogues of Adenosine, Theophylline, and Caffeine: Selective Interactions with Al and A2 Adenosine Receptors J. W. Daly, D. Ukena, and K A. Jacobson .................. 23 Structural Studies on Adenosine Ri Receptors from Rat Cerebral Cortex E. Perez-Reyes, S.-M. H. Yeung, R. L. Lasher, and D. M. F. Cooper . .. 37 Biochemical and Autoradiographic Approaches to the Characterization of Adenosine Receptors in Brain M. Reddington, S. P. Alexander, A. Erfurth, K S. Lee, and G. W. Kreutzberg 49 Adenosine Receptor Subtypes: Binding Studies R. F. Bruns, G. H. Lu, and T. A. Pugsley .................... 59 Central Sites of Adenosine Action and Their Interaction with Various Drugs P. J. Marangos, J. Deckert, and J.-c. Bisserbe ................. 74 Nucleoside Transport Inhibition In Vitro and In Vivo A. R. P. Paterson, E. S. Jakobs, C. Y. C. Ng, R. D. Odegard, and A. A. Adjei. 89 VIII Table of Contents Kinetic and Molecular Properties of Nucleoside Transporters in Animal Cells S. M. Jarvis .................................... 102 Drug Interactions with Nucleoside Transport Systems A. S. Clanachan, T. P. Heaton, and F. E. Parkinson ............. 118 II. Adenosine Formation, Metabolism and Transport Regulation and Function of 5'-Nucleotidases A. R. Collinson, K. J. Peuhkurinen, and J. M. Lowenstein ......... 133 Kinetics of Endothelial Cell Ectonucleotidases J. D. Pearson, and S. B. Coade ........ . . 145 Critical Evaluation of the Role of Ecto- and Cytosolic 5'-Nucleotidase in Adenosine Formation A. C. Newby, Y. Worku, and P. Meghji .................... 155 New Insights into the Mechanism of Myocardial Adenosine Formation A. Dendorfer, S. Lauk, A. Schaff, and S. Nees . . . . . . . . . . . . .. . 170 Cardiac Myocyte and Coronary Endothelial Cell Adenosine Transport M. J. Rovetto, D. A. Ford, and A. Yassin ............. . . . 188 The Importance of the Transmethylation Pathway for Adenosine Metabolism in the Heart H. G. E. Lloyd, and J. Schrader .................. . ... 199 Uric Acid, the Major Catabolite of Cardiac Adenine Nucleotides and Adenosine, Originates in the Coronary Endothelium B. F. Becker, and E. Gerlach .......................... 209 Thermodynamic State of Cytosolic Adenylates in Guinea Pig Myocardium. Energy-Linked Adaptive Changes in Free Adenylates and Purine Nucleoside Release R. Bunger . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 223 Table of Contents IX III. Functions of Adenosine in Cells, Organs and Blood On Multiple Targets for Fat Cell Receptors C. Londos .................. . . .............. 239 The Renal and Epithelial Actions of Adenosine W. S. Spielman, L. J. Arend, and J. N. Forrest, Jr. .............. 249 Adenosine and Thermogenesis in Brown Adipose Tissue: Interaction with Beta and Alpha Adrenergic Responses R. J. Schimmel, M. E. Elliott, and L. McCarthy ............... 261 The Hormone-Modulatory Effects of Adenosine in Skeletal Muscle R. A. J. Challiss, B. Leighton, F. J. Lozeman, and E. A. Newsholme . 275 Effects of Adenosine on Human Neutrophil Function and Cyclic AMP , Content M. A. Iannone, T. P. Zimmerman, R. Reynolds-Vaughn, and G. Wolberg 286 A New Function for Adenosine: Protection of Vascular Endothelial Cells from Neutrophil-Mediated Injury B. N. Cronstein, R. I. Levin, J. Belanoff, G. Weissmann, and R. Hirschhorn. 299 Formation of Adenosine by Vascular Endothelium: a Homeostatic and Antithrombogenic Mechanism? E. Gerlach, B. F. Becker, and S. Nees ..................... 309 IV. Adenosine in the Heart and Vascular System Ionic Channels and Adenosine in Isolated Heart Cells G. Isenberg, E. Cerbai, and U. KlOckner ... 323 The Negative Chronotropic Effect of Adenosine in Sinus Node Cells G. A. West, W. Giles, and L. Belardinelli .......... . ... 336 Regulation of Atrioventricular Node Function by Adenosine L. Belardinelli, G. A. West, and S. H. F. Clemo ............... 344 X Table of Contents The Antiadrenergic Actions of Adenosine in the Heart J. G. Dobson, Jr., R. A. Fenton, and F. D. Romano .. . 356 Mechanism of the "Antiadrenergic" Effects of Adenosine on Myocardial Force of Contraction H. Scholz, M. Bohm, R. Briickner, J. Neumann, and W. Schmitz ..... 369 Further Evidence Against Adenosine-Catecholamine Antagonism In Vivo: Investigations with Treadmill Exercise in Dogs G. Raberger, G. Fischer, G. Krumpl, W. Schneider, and H. Stroifinig ... 383 Adenosine in the Local Regulation of Blood Flow: Some Controversies R. M. Berne, J. M. Gidday, H. E. Hill, R. R. Curnish, and R. Rubio .... 395 Adenosine in the Local Regulation of Blood Flow: Current Controversies H. V. Sparks, Jr., and M. W. Gorman . . . . . . . . . . . . . . . . . . .. 406 5'-Nucleotidase Inhibitors and the Myocardial Reactive Hyperemia and Adenosine Content S. Imai, M. Nakazawa, H. Imai, and H. Jin .................. 416 Estimates of Interstitial Adenosine in Isolated Rat Hearts from Surface Exudates During Rapid Pacing and EHNA Infusion L. J. Heller, and D. E. Mohrman ........................ 425 Intra-Arterial Adenosine Deaminase: a Tool for Assessing Physiological Functions of Adenosine R. A. Olsson ................................... 438 A Critique on the Use of Adenosine Deaminase to Test the Adenosine Hypothesis: Disregarded Implicit Assumptions R. Rubio, R. M. Knabb, S. W. Ely, and R. M. Berne . . . . . . . . . . . . . 445 Adenosine Receptors at the Coronary Endothelium: Functional Implications S. Nees, Ch. Des Rosiers, and M. Bock . . . . . . . . . . . . . . . . . . . . 454

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