Antihistamines

Abstract

The discovery of histamine, its physiological role and reversal of its pharmacological effects by antihistamines takes us on a journey through the origins of modern physiology and the rising understanding of pharmacology at the end of the 19th and the early part of the 20th centuries. This journey, which has been traced in the excellent historical review by Michael Emanuel [Clin Exp Allergy 1999;29:1-11], is populated by some of the greatest scientists of the era, including six Nobel laureates - Bovet, Dale, Ehrlich, Richet, Windaus and Black. In addition, it laid the basis of medicinal chemistry not only for antihistamines, but also for the discovery of a plethora of drugs still in use today.

The Ingenious Mast Cell: Contemporary insights into mast cell behavior and function

“…Mast cell mediators as targets of treatment MC-targeted treatments are primarily developed for chronic urticaria (CU), mastocytosis, and allergies, because of the critical role that MCs play in their pathogenesis 65,96 . The evolution of MC-targeted treatments started, more than 70 years ago, with the development of drugs that inhibit the effects of individual MC mediators, first histamine, followed by prostaglandins and leukotrienes 97 . Modern antihistamines that act on the histamine 1 receptor are superior to first generation ones in their binding affinity, specificity, and risk/benefit profiles.…”

New antihistamines – perspectives in the treatment of some allergic and inflammatory disorders

“…Many histamine H1 receptor antagonists are widely available over the counter and at low price. Although generally still referred to as H1R antagonists, so-called H1 antihistamines (rarely: H1R blockers) are not receptor antagonists, but are actually inverse agonists that reduce the constitutive activity of the receptor and compete with histamine [16, 35].…”

The ingenious mast cell: Contemporary insights into mast cell behavior and function

“…MC‐targeted treatments are primarily developed for chronic urticaria (CU), mastocytosis, and allergies, because of the critical role that MCs play in their pathogenesis 118,119 . The evolution of MC‐targeted treatments started, more than 70 years ago, with the development of drugs that inhibit the effects of individual MC mediators, first histamine, followed by prostaglandins and leukotrienes 120 . Modern antihistamines that act on the histamine 1 receptor are superior to first‐generation ones in their binding affinity, specificity, and risk/benefit profiles.…”