Chapter 21. Histamine H1 Blockers: From Relative Failures to Blockbusters within Series of Analogues

  1. Dr. János Fischer2,
  2. Prof. Dr. C. Robin Ganellin3
  1. Henk Timmerman

Published Online: 22 MAY 2006

DOI: 10.1002/3527608001.ch21

Book Title

Analogue-based Drug Discovery

Analogue-based Drug Discovery

Additional Information

How to Cite

Timmerman, H. (2006) Histamine H1 Blockers: From Relative Failures to Blockbusters within Series of Analogues, in Analogue-based Drug Discovery (eds J. Fischer and C. R. Ganellin), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, FRG. doi: 10.1002/3527608001.ch21

Editor Information

  1. 2

    Gedeon Richter Ltd., P.O. Box 27, H-1475 Budapest 10, Hungary

  2. 3

    University College London, Department of Chemistry, 20 Gordon Street, London WC1H OAJ, UK

Author Information

  1. Vrije Universiteit, Department of Pharmacochemistry, De Boelelaan 1083, 1081 HV Amsterdam, The Netherlands

Publication History

  1. Published Online: 22 MAY 2006
  2. Published Print: 20 JAN 2006

ISBN Information

Print ISBN: 9783527312573

Online ISBN: 9783527608003

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CHAPTER TOOLS

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Keywords:

  • analogue-based drug discovery;
  • histamine H1 blockers;
  • first antihistamines;
  • diphenhydramine;
  • new antihistamines;
  • inverse agonism

Summary

This chapter contains sections titled:

  • Introduction

  • The First Antihistamines

  • Diphenhydramine as a Skeleton for Antihistamines

    • The Diaryl Group

    • The Linker

    • The Basic Group

    • The Analogue Principle

    • The Analogue Principle in Perspective

  • The New Antihistamines

  • Antihistamines for Which the Analogue Principle Does not Seem to Work

  • Inverse Agonism

  • A Further Generation of Antihistamines?

  • Conclusions

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