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Table 2 H2 Receptor Antagonists

From: The Role of Antihistamines in the Treatment of Vasomotor Rhinitis

Receptor

H2

Signal conduction through

Gs

Location of receptors

Widely expressed including: Mucosa of stomach, cardiac tissue, uterus, smooth muscle vascular bed, epithelium of mucosa of nose, submucosal glands in nose, central nervous system, immune cells

Chromosome location

5q35.3

Signal conduction induces

Increase in cyclic AMP, activation of adenyl cyclase

Antagonists (reverse agonists)

Burimamide, cimetidine, dimaprit, famotidine, nizatidine, ranitidine, and others (it should be noted that a number of different H1 antagonists also show affinity for the H2 receptor

Activities

Increased gastric acid secretion; increases vascular permeability producing a fall in blood pressure, flush, headache, and reflex tachycardia; stimulate mucus production in the lungs; direct chronotropic effect on atrium and inotropic action on ventricle; relaxation of esophageal sphincter; stimulation of suppressor T-cells; decrease in neutrophil and basophil chemotaxis and activation; proliferation of lymphocytes; activity of NK cells

Nasal symptoms produced

Antagonism of the H2 receptor could potentially reduce the effect of histamine on nasal airway swelling, producing nasal decongestion