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Fexofenadine, sold under the brand name Allegra among others, [10] is an antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever and urticaria. [ 11 ] Therapeutically, fexofenadine is a selective peripheral H 1 blocker .
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.
Terfenadine acts as a peripherally-selective antihistamine, or antagonist of the histamine H 1 receptor. [3] It is a prodrug, generally completely metabolized to the active form fexofenadine in the liver by the enzyme cytochrome P450 3A4.
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.
Upon study of records in mouse studies associated with 40 common medications ranging from antibiotics, antihistamines, aspirin, and hydrocortisone, that for subjects with melanoma and lung cancers, fexofenadine, one of three medications, along with loratadine, and cetirizine, that target histamine receptor H1 (HRH1), demonstrated significantly ...
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There are four main types: H1, H2, H3, and H4. H1 receptors are linked to allergic responses, H2 to gastric acid regulation, H3 to neurotransmitter release modulation, and H4 to immune system function. There are four known histamine receptors: H 1 receptor H1 Receptors: These receptors are primarily located on smooth muscle cells, endothelial ...
Bilastine binds to guinea-pig cerebellar histamine H1-receptors (Ki=44 nM) and to human recombinant histamine H1-receptors (Ki=64 nM) with an affinity comparable to that of astemizole and diphenhydramine, and superior than that of cetirizine by three-fold and fexofenadine by five-fold (Corcóstegui). In different murine models, bilastine by ...