Histamine H4 Receptor Antagonists

In a mouse model of allergic contact dermatitis, an H4 receptor antagonist produced encouraging results.

The histamine receptors H1 and H2 (antagonized by H1 antihistamines, such as diphenhydramine, and by H2 antihistamines, such as cimetidine) are well known. Investigators recently discovered additional, unique histamine receptors H3 and H4. H3 receptors reside mostly on neurons, so antagonists to these receptors could treat cognitive impairment, schizophrenia, sleep/wake disorders, epilepsy, and neuropathic pain. H4 receptors reside mostly on hemopoietic cells, and thus their antagonists might treat inflammatory diseases and pruritus. Blockade of H4 receptors obstructs histamine-induced chemotaxis of eosinophils and mast cells. A potential H4 antagonist drug is currently being tested in a phase II clinical trial.

In a recent study in mice wit…

Reviewing Author

Mark V. Dahl, MD

Disclosures

Consultant / Advisory board Ulthera, Inc.; AuBio LifeSciences, LLC; Paris Therapeutics

Equity Elorac, Inc.; Makucell, Inc.; Paris Therapeutics

Editorial boards UpToDate

Leadership positions in professional societiesNational Rosacea Society (Chairman, Medical Board)