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Antihistamines are drugs which treat allergic rhinitis and other allergies. The two largest classes of antihistamines are H 1 -antihistamines and H 2 -antihistamines. H 1 -antihistamines work by binding to histamine H 1 receptors in mast cells, smooth muscle, and endothelium in the body as well as in the tuberomammillary nucleus in the brain. Antihistamines that target the histamine H 1 -receptor are used to treat allergic reactions in the nose e. In addition, they may be used to treat insomnia, motion sickness, or vertigo caused by problems with the inner ear. H 2 -antihistamines bind to histamine H 2 receptors in the upper gastrointestinal tract, primarily in the stomach. Antihistamines that target the histamine H 2 -receptor are used to treat gastric acid conditions e. Histamine receptors exhibit constitutive activity, so antihistamines can function as either a neutral receptor antagonist or an inverse agonist at histamine receptors. Histamine produces increased vascular permeability, causing fluid to escape from capillaries into tissues, which leads to the classic symptoms of an allergic reaction — a runny nose and watery eyes.

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