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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.
Cimetidine was the prototypical histamine H 2 receptor antagonist from which later drugs were developed. Cimetidine was the culmination of a project at Smith, Kline & French (SK&F; now GlaxoSmithKline) by James W. Black, C. Robin Ganellin, and others to develop a histamine receptor antagonist that would suppress stomach acid secretion.
Doxepin is a highly potent antihistamine, with this being its strongest activity. [49] [53] [57] [8] In fact, doxepin has been said to be the most or one of the most potent H 1 receptor antagonists available, with one study finding an in vitro K i of 0.17 nM. [37]
Betahistine is a strong antagonist at histamine H 3 receptors and a weak agonist at histamine H 1 receptors. [1] Betahistine has two mechanisms of action. Primarily, it is a weak agonist at histamine H 1 receptors located on blood vessels in the inner ear. This gives rise to local vasodilatation and increased permeability, which helps to ...
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 .
Allegra Gelcaps, a type 1 histamine blocker, work best for skin symptoms, according to Dr. Chaudry. These fast-acting capsules are said to offer 24-hour non-drowsy relief and start working within ...
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.
Therapeutically, fexofenadine is a selective peripheral H 1 blocker. It is classified as a second-generation antihistamine because it is less able to pass the blood–brain barrier and cause sedation, compared to first-generation antihistamines. [12] [13] It was patented in 1979 and came into medical use in 1996. [14]
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