Histamine receptors: specific ligands, receptor biochemistry, and signal transduction

Clin Allergy Immunol. 2002:17:27-64.


During the past few years, there has been a tremendous increase in our understanding of the histamine receptors. Important progress has been made in the development of H1-receptor agonists and the rationalization of H1-receptor-ligand interaction. The recent observation of constitutive H1- and H2-receptor activity has led to a reclassification of H1- and H2-antagonists. For the H3-receptor, a wide variety of selective and potent ligands are currently available and await clinical application. The recent cloning of the H3-receptor gene and the anticipated generation of transgenic mice will facilitate this development. Within the field of signal transduction, a previously unanticipated complexity has been unravelled. With the cloning of the H3-receptor gene, a similar complexity is to be expected.

Publication types

  • Review

MeSH terms

  • Animals
  • Arachidonic Acid / metabolism
  • Calcium Signaling
  • GTP-Binding Proteins / physiology
  • Humans
  • Models, Molecular
  • Nitric Oxide Synthase / metabolism
  • Receptors, Histamine / chemistry
  • Receptors, Histamine / genetics
  • Receptors, Histamine / physiology*
  • Signal Transduction*
  • Type C Phospholipases / metabolism


  • Receptors, Histamine
  • Arachidonic Acid
  • Nitric Oxide Synthase
  • Type C Phospholipases
  • GTP-Binding Proteins