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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 not true antihistamines.
H 1-receptor antagonists are competitive inhibitor of histamine receptor H 1 and are used to treat allergies. This group is often referred simply as antihistamines . Wikimedia Commons has media related to H1 receptor antagonists .
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
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 .
A histaminergic agent (or drug) is a chemical which functions to directly modulate the histamine system in the body or brain. Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines). Subdivisions of histamine antagonists include H 1 receptor antagonists, H 2 receptor antagonists, and H 3 receptor ...
Cyproheptadine is a very potent antihistamine or inverse agonist of the H 1 receptor. At higher concentrations, it also has anticholinergic , antiserotonergic , and antidopaminergic activities. Of the serotonin receptors , it is an especially potent antagonist of the 5-HT 2 receptors .
Brompheniramine works by acting as an antagonist of histamine H 1 receptors. It also functions as a moderately effective anticholinergic agent, and is likely an antimuscarinic agent [7] similar to other common antihistamines such as diphenhydramine. Brompheniramine is metabolised by cytochrome P450 isoenzymes in the liver. [7]
[medical citation needed] Loratadine is a long-acting antihistamine (H 1 histamine antagonist) that is less sedating than older substances of its type. [medical citation needed] In 2022, it was the 289th most commonly prescribed medication in the United States, with more than 500,000 prescriptions. [2] [3]
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