The basics of histamine biology

Abstract

Objective: To review the evolution of our understanding of the basics of histamine biology as it pertains to the treatment of allergic rhinitis.

Data sources: Review articles and original research were retrieved from MEDLINE, OVID, PubMed (1950 to November 2009), personal files of articles, and bibliographies of located articles that addressed the topic of interest.

Study selection: Key articles were selected that, taken together, provide a history of scientific insight into histamine biology and receptors and mechanism of action of antihistamines. Publications included reviews, treatment guidelines, and clinical studies (primarily randomized controlled trials) of both children and adults.

Results: The seminal work on histamine was published in 1910, but histamine was not identified as a mediator of anaphylactic reactions until 1932. Research later showed that histamine is a major mediator responsible for the symptoms of allergic rhinitis, with its activities mediated through 4 G protein-coupled receptors. Most of histamine's effects are exerted through the H₁ receptor, but some effects are through the H₂ and H₃ receptors, and possibly also through the H₄ receptor.

Conclusions: We hope that the progress made in understanding the mechanism of action of the histamine response will lead to better targeted treatment options.