Histamine H4 receptor antagonists: the new antihistamines?

Abstract

Antihistamines (histamine H1 receptor antagonists) are a mainstay treatment for atopic allergy, yet they are only partially effective in relieving the symptoms of the disease. They also have very limited value for the treatment of asthma, despite the well-characterized bronchoconstrictory effects of histamine. The recent discovery of a fourth histamine receptor (H4), and the realization that it is exclusively expressed on hematopoietic cell types that are most implicated in the development and symptomatology of allergy and asthma, suggests that pharmacological targeting of the H4 receptor, either alone or in combination with H1 receptor antagonists, may prove useful for treating both allergy and asthma. Here we review the known biology associated with the H4 receptor, as well the effects of a highly selective H1 receptor antagonist.

• Authors: Wai-Ping Fung-Leung, Robin L Thurmond, Ping Ling, Lars Karlsson
• Journal: Current opinion in investigational drugs (London, England : 2000) (Curr Opin Investig Drugs) Vol. 5 Issue 11 Pg. 1174-83 (Nov 2004) ISSN: 1472-4472 [Print] England
• PMID: 15573868 (Publication Type: Journal Article, Review)

Chemical References

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

Topics

• Animals
• Eosinophils (physiology)
• Histamine (metabolism)
• Histamine Antagonists (pharmacology)
• Humans
• Ligands
• Mast Cells (physiology)
• Receptors, G-Protein-Coupled (antagonists & inhibitors, physiology)
• Receptors, Histamine (physiology)
• Receptors, Histamine H4