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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 several splice variants of H 3 present in various species. Though all of the receptors are 7-transmembrane g protein coupled receptors, H 1 and H 2 are quite different from H 3 and H 4 in their activities. H 1 causes an increase in PIP 2 hydrolysis, H2 stimulates gastric acid secretion, and H3 mediates feedback inhibition of histamine.
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. Due to its near complete metabolism by the liver immediately after leaving the gut, terfenadine normally is ...
Histamine release in the brain triggers secondary release of excitatory neurotransmitters such as glutamate and acetylcholine via stimulation of H 1 receptors in the cerebral cortex. Consequently, unlike the H 1-antihistamines which are sedating, H 3-antihistamines have stimulant and cognition-modulating effects.
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 ...
The gene sequence for H 3 receptors expresses only about 22% and 20% homology with both H 1 and H 2 receptors respectively. There is much interest in the histamine H 3 receptor as a potential therapeutic target because of its involvement in the neuronal mechanism behind many cognitive disorders and especially its location in the central nervous ...
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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.
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