Histamine and its receptors.

Article Details

Citation

Parsons ME, Ganellin CR

Histamine and its receptors.

Br J Pharmacol. 2006 Jan;147 Suppl 1:S127-35.

PubMed ID
16402096 [ View in PubMed
]
Abstract

This article reviews the development of our knowledge of the actions of histamine which have taken place during the course of the 20th century. Histamine has been shown to have a key physiological role in the control of gastric acid secretion and a pathophysiological role in a range of allergic disorders. The synthesis of, and pharmacological studies on, selective agonists and antagonists has established the existence of four types of histamine receptor and histamine receptor antagonists have found very important therapeutic applications. Thus, in the 1940s, H(1)-receptor antagonists ('the antihistamines') yielded and still provide valuable treatment for allergic conditions such as hay fever and rhinitis. In the late 1970s and 1980s, H(2)-receptor antagonists (in the discovery of which the two authors were personally involved) revolutionised the treatment of peptic ulcer and other gastric acid-related diseases. The H(3)-receptor antagonists, although available since 1987, have been slower to find a therapeutic role. However, the discovery of nonimidazole derivatives such as brain-penetrating H(3) antagonists has provided drugs that are in early-phase clinical trials, possibly for application in obesity, and a variety of central nervous system disorders, such as memory, learning deficits and epilepsy. Finally, the most recently (1999) discovered H(4) receptor promises the potential to provide drugs acting on the immunological system with possible applications in asthma and inflammation.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
MepyramineHistamine H1 receptorProteinHumans
Yes
Antagonist
Details
Drug Interactions
DrugsInteraction
Arbutamine
Betahistine
The therapeutic efficacy of Arbutamine can be decreased when used in combination with Betahistine.
Arformoterol
Betahistine
The therapeutic efficacy of Arformoterol can be decreased when used in combination with Betahistine.
Celiprolol
Betahistine
The therapeutic efficacy of Celiprolol can be decreased when used in combination with Betahistine.
Clenbuterol
Betahistine
The therapeutic efficacy of Clenbuterol can be decreased when used in combination with Betahistine.
Dobutamine
Betahistine
The therapeutic efficacy of Dobutamine can be decreased when used in combination with Betahistine.