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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 ...
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.
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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Diphenhydramine is a potent antimuscarinic (a competitive antagonist of muscarinic acetylcholine receptors) and, as such, at high doses can cause anticholinergic syndrome. [69] The utility of diphenhydramine as an antiparkinson agent is the result of its blocking properties on the muscarinic acetylcholine receptors in the brain.
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. H1 receptors are linked to allergic responses, H2 to gastric acid regulation, H3 to neurotransmitter release modulation, and H4 to immune system function.
Hydroxyzine, sold under the brand names Atarax and Vistaril among others, is an antihistamine medication. [8] It is used in the treatment of itchiness, anxiety, insomnia, and nausea (including that due to motion sickness). [8]
Carbinoxamine is a histamine antagonist, specifically an H1-antagonist. The maleic acid salt of the levorotatory isomer is sold as the prescription drug rotoxamine. It was patented in 1947 and came into medical use in 1953. [1] It was first launched in the United States by the McNeil Corporation under the brand name Clistin. Carbinoxamine is ...