Principles and Methods in Receptor Binding

1. Front Matter

   Pages i-viii

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2. Ligand Binding Data Analysis: Theoretical and Practical Aspects

   • Peter J. Munson

   Pages 1-12

3. Radioligand Binding Assays

   • S. J. Enna

   Pages 13-33

4. Binding Ligands to Receptors: Additional Comments

   • Alexander Levitzki

   Pages 35-39

5. Basic Concepts to Analyze Binding Data Using Personal Computers: The “RECEPT” program

   • Fabio Benfenati, Vincenzo Guardabasso

   Pages 41-63

6. The Muscarinic Receptors

   • Giancarlo Pepeu, Ileana Marconcini Pepeu

   Pages 65-77

7. The β-Adrenergic Receptors and Their Mode of Interaction with Adenylate Cyclase

   • Alexander Levitzki

   Pages 79-91

8. Biochemical Pharmacology of Dopamine Receptors

   • M. Memo, E. Carboni, H. Uzumaki, S. Govoni, M. O. Carruba, M. Trabucchi et al.

   Pages 93-111

9. Benzodiazepine Receptor Ligands with Positive and Negative Efficacy

   • Claus Braestrup, Mogens Nielsen, Tage Honoré

   Pages 113-125

10. Synapses with Multiple Chemical Signals: New Models and Perspectives in Drug Development

    • Erminio Costa

    Pages 127-154

11. Steroid Hormone Receptors

    • Paolo Marchetti, Gigliola Sica, Clara Natoli, Maria Assunta Spina, Stefano Iacobelli

    Pages 155-159

12. Steroid Hormone Receptors in Endocrine-Related Tumors

    • Paolo Marchetti, Giovanni Scambia, Gigliola Sica, Vittoria Natoli, Stefano Iacobelli

    Pages 161-193

13. The Role of Phospholipids in Receptor Binding in the Nervous System

    • Michael Giesing

    Pages 195-213

14. Incorporation of Receptors into Planar Lipid Bilayers: Ionic Transport Properties

    • Franco Gambale, Cesare Usai, Mauro Robello, Carla Marchetti

    Pages 215-231

15. Structure-Function Relations for Cell Surface Receptors and Adenylate Cyclase: Studies Using Target Size Analysis of Radiation Inactivation

    • Werner Schlegel

    Pages 233-253

16. Back Matter

    Pages 255-267

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One of the major advances in the understanding of the mechanism of action of hormones, neurotransmitters and drugs had arisen from the hypothesis that the physiological or pharmacological responses are trig­ gered by their interaction with specific cell compo­ nents, termed receptors. However, the presence of receptors has been inferred from indirect data, and only recently has it been possible to study the kinetics of the interaction between drug and receptors directly, through the so called "binding technique. " This NATO-ASI on "Principles and Methods in Receptor Binding" was devoted mainly to the following aspects of the study of receptors: the principles underlying the use of the binding technique; the mathematical models necessary to interpret binding data; the application of binding methods to specific receptors; and, finally, a few selected examples of coupling between receptors and physiological re­ sponses. In the chapters of this book, special interest is devoted to the analysis of the simplest models for the interaction of receptors with their ligands (either hormones or neurotransmitters or drugs). The graphical techniques used to analyze the data from binding exper iments are extensively discussed, together with the statistics that have to be used in binding analysis. Moreover, the basic concepts to analyze binding data using a personal computer are presented. v vi PREFACE The factors which should be considered when setting up a binding assay (such as choice of ligand and incubation conditions, preparation of tissue, termina­ tion of incubation) are discussed.

• Institute of Pharmacology and Pharacognosy, University of Urbino, Urbino, Italy

  F. Cattabeni

• Institute of Pharmacology and Pharmacognosy, University of Milan, Milan, Italy

  S. Nicosia

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