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The H 1 receptor is a histamine receptor belonging to the family of rhodopsin-like G-protein-coupled receptors. This receptor is activated by the biogenic amine histamine . It is expressed in smooth muscles , on vascular endothelial cells , in the heart, and in the central nervous system .
The K i values for the H 1 receptor are approximately 6 nM for cetirizine, 3 nM for levocetirizine, and 100 nM for dextrocetirizine, indicating that the levorotatory enantiomer is the main active form. [3] Cetirizine has 600-fold or greater selectivity for the H 1 receptor over a wide variety of other sites, including muscarinic acetylcholine ...
H 1 receptor H1 Receptors: These receptors are primarily located on smooth muscle cells, endothelial cells, and neurons. Activation of H1 receptors mediates various responses, including smooth muscle contraction (leading to bronchoconstriction, intestinal cramping), increased vascular permeability (resulting in edema ), and stimulation of ...
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.g., itching, runny nose, and
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H 1 antagonists, also called H 1 blockers, are a class of medications that block the action of histamine at the H 1 receptor, helping to relieve allergic reactions. Agents where the main therapeutic effect is mediated by negative modulation of histamine receptors are termed antihistamines ; other agents may have antihistaminergic action but are ...
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It is classified as a second-generation antihistamine and works by blocking histamine H 1-receptors. [6] [3] Levocetirizine was approved for medical use in the United States in 2007, [3] and is available as a generic medication. [4] In 2022, it was the 152nd most commonly prescribed medication in the United States, with more than 3 million ...