The future antihistamines: histamine H3 and H4 receptor ligands

Adv Exp Med Biol. 2010;709:125-40. doi: 10.1007/978-1-4419-8056-4_12.


The field of histamine research has progressed far from a century ago when the first biological functions of histamine were identified. It is now known that histamine function is mediated by four histamine receptors, which belong to the G-protein-coupled receptor family. While antihistamines that target the first two receptors have enjoyed clinical and commercial success, efforts to find new antihistamines against the histamine H3 and H4 receptors are still in the early stages. Here we will review the therapeutic potential of targeting these new histamine receptors.

Publication types

  • Review

MeSH terms

  • Animals
  • Disease
  • Drug Therapy
  • Histamine / metabolism
  • Histamine Antagonists / metabolism*
  • Histamine Antagonists / therapeutic use
  • Humans
  • Receptors, G-Protein-Coupled / metabolism*
  • Receptors, Histamine / metabolism*
  • Receptors, Histamine H3 / metabolism*
  • Receptors, Histamine H4


  • HRH4 protein, human
  • Histamine Antagonists
  • Receptors, G-Protein-Coupled
  • Receptors, Histamine
  • Receptors, Histamine H3
  • Receptors, Histamine H4
  • Histamine