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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 .
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 ...
Clinically, H 1-antihistamines are used to treat allergic reactions and mast cell-related disorders. Sedation is a common side effect of H 1-antihistamines that readily cross the blood–brain barrier; some of these drugs, such as diphenhydramine and doxylamine, may therefore be used to treat insomnia.
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 .
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 ...
H 1 agonists promote wakefulness. [1] H 2: Betazole and Impromidine are examples of agonists used in diagnostics to increase histamine. H 3: Betahistine is a weak Histamine 1 agonist and a very strong antagonist of the Histamine 3 autoreceptor. Antagonizing H 3 increases histaminergic tone.
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.
An H 3 receptor antagonist is a type of antihistaminic drug used to block the action of histamine at H 3 receptors.. Unlike the H 1 and H 2 receptors which have primarily peripheral actions, but cause sedation if they are blocked in the brain, H 3 receptors are primarily found in the brain and are inhibitory autoreceptors located on histaminergic nerve terminals, which modulate the release of ...
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