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In common use, the term "antihistamine" refers only to H 1-antihistamines. Virtually all H 1-antihistamines function as inverse agonists at the histamine H 1-receptor, as opposed to neutral antagonists, as was previously believed. [1] [2] [3]
Itching, sneezing, and inflammatory responses are suppressed by antihistamines that act on H1-receptors. [2] [8] In 2014, antihistamines such as desloratadine were found to be effective to complement standardized treatment of acne due to their anti-inflammatory properties and their ability to suppress sebum production. [9] [10]
The histamine receptors are a class of G protein–coupled receptors which bind histamine as their primary endogenous ligand. [1] [2] Histamine receptors are proteins that bind with histamine, a neurotransmitter involved in various physiological processes. There are four main types: H1, H2, H3, and H4.
Histamine H 1 receptors are activated by endogenous histamine, which is released by neurons that have their cell bodies in the tuberomammillary nucleus of the hypothalamus. The histaminergic neurons of the tuberomammillary nucleus become active during the 'wake' cycle, firing at approximately 2 Hz; during slow wave sleep , this firing rate ...
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.
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 .