Perspectives in Receptor Research

Edited by

  • D. Giardinà
  • A. Piergentili
  • M. Pigini, Department of Chemical Sciences, University of Camerino, Via S. Agostino 1, 62032 Camerino, Italy

Series Editor:

  • H. Timmerman

This volume contains the results of an extremely intense exchange of information and opinions which took place during the five days of the symposium on which the book is based. A particular feature is the excellent reporting and debating of the most recent knowledge and discoveries of chemists, pharmacologists and biologists involved in studying receptors and their mechanisms of action. This exchange of opinions between the various lines of research will open the road to a deeper knowledge and understanding of the receptor as a biological target.
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Book information

  • Published: June 1996
  • Imprint: ELSEVIER
  • ISBN: 978-0-444-82204-8

Table of Contents

Preface. Medicinal chemistry: through a glass darkly. Mechanisms regulating G protein-coupled receptors. Introduction to muscarinic receptors. Structure-function analysis of muscatinic acetylcholine receptors. Muscarinic receptor subtypes - Search for selective agonists and antagonists. Perspectives in the design and application of dopamine receptor agonists. Serotoninreceptor complexity: relationships and roles. Design and synthesis of agonists and antagonists of the serotonin 5-HT4 receptor subtype. &agr;1-Adrenergic receptor subtypes and signal transduction. &agr;1 -Adrenoceptors: subtype- and organ-selectivity of differentagents. Molecular recognition in adenosine receptors. Chemical and pharmacological profile of selective adenosine receptor agonists. Partial agonists for adenosine receptors. New histamine H3 receptor ligands as pharmacological tools. Three-dimensional structure of G protein-coupled receptors: from speculations to facts. Ion channels as targets for drug design.Recent advances in potassium channel activators. Spinal glutamate receptors. GABAB receptor antagonists: new tools and potential new drugs. Thrombin inhibitors and thrombin receptor agonists/antagonists. Structure-activity relationships of non-peptide kappa-opioid analgesics: a perspective of the last 10 years. Selective nonpeptide ligands as probes to explore &dgr; opioid receptor architecture. The role of novel ligands in thebiological characterization of sigma receptors. Tetraamines as lead compounds for the design of neurotransmitter receptor ligands: focus on &agr;-adrenergic and muscarinic receptors recognition. Design and pharmacological characterization of selective P2- purinoceptor antagonists. Imidazoline receptors: an update. Discovery of highly selective imidazolinereceptor ligands. Synthesis and structure-activity relationship of new 1,5-benzodiazepine CCK-B antagonists. Author index. Subject index..