Milestones in the biology and pharmacology of H1-receptor antagonists.

Daniele Bovet's pioneering discovery that a series of compounds possessing anti-histamine activity reduced the symptoms of anaphylaxis provided the proof that histamine plays a pivotal role as a mediator of allergic reactions. Basophils and mast cells are the major sources of histamine in man and they are thus one of the primary effector cells of allergic inflammation. Some H1-receptor antagonists possess a variety of antiinflammatory activity to H1 antagonism in vitro and in vivo. This promising area should be explored further and much remains to be done in the evaluation of the immunomodulatory effects of anti-histamines.