Perspectives in Drug Development and Clinical Pharmacology: The Discovery of Histamine H1 and H2 Antagonists

Clin Pharmacol Drug Dev. 2016 Jan;5(1):5-12. doi: 10.1002/cpdd.236.

Abstract

Knowledge about the history and development of therapeutic agents holds a central position in the education and training of pharmacists and pharmacologists. Students enjoy learning about the discovery of drugs, including details about the pioneer workers involved (apothecaries, organic chemists, pharmacologists, and physiologists) and the role played by serendipity. The treatment of people suffering from allergies and the development of drugs that block the actions of histamine at H1 and H2 receptors are the subject of this review. Pharmaceutical products that block H1 receptors are widely used as prophylactic treatment for seasonal allergies that plague millions of people worldwide. The development of H2 receptor antagonists revolutionized treatment of gastric hyperacidity, the principal cause of peptic ulcers. Antihistamine research has changed focus toward the development of drugs that block the action of histamine at H3 and H4 receptors and the therapeutic potential is gradually being appreciated.

Keywords: allergies; antihistamines; drug discovery; histamine antagonists; history; hyperacidity; ulcers.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Allergic Agents / pharmacology
  • Anti-Ulcer Agents / pharmacology
  • Drug Design*
  • Drug Discovery / methods
  • Histamine H1 Antagonists / pharmacology*
  • Histamine H2 Antagonists / pharmacology*
  • Humans
  • Hypersensitivity / drug therapy
  • Peptic Ulcer / drug therapy

Substances

  • Anti-Allergic Agents
  • Anti-Ulcer Agents
  • Histamine H1 Antagonists
  • Histamine H2 Antagonists