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Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons. [5] Its various actions are mediated by histamine receptors H 1, H 2, H 3 and H 4. The histamine receptor H 2 belongs to the rhodopsin-like family of G protein-coupled receptors.
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 2-antihistamines bind to histamine H 2 receptors in the upper gastrointestinal tract, primarily in the stomach. Antihistamines that target the histamine H 2-receptor are used to treat gastric acid conditions (e.g., peptic ulcers and acid reflux). Other antihistamines also target H 3 receptors and H 4 receptors.
The histamine receptors are a class of G protein–coupled receptors which bind histamine as their primary endogenous ligand. [1] [2] Histamine is a neurotransmitter involved in various physiological processes. There are four main types of histamine receptors: H1, H2, H3, and H4.
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.
Ranitidine is an H 2 histamine receptor antagonist that works by blocking histamine, thus decreasing the amount of acid released by cells of the stomach. [12] Ranitidine was discovered in England in 1976 and came into commercial use in 1981. [26] It is on the World Health Organization's List of Essential Medicines.
In addition, subjective sleepiness correlated well with the brain H 1 receptor occupancy. [45] PET studies with antihistamines have found that brain H 1 receptor occupancy of more than 50% is associated with a high prevalence of somnolence and cognitive decline, whereas brain H 1 receptor occupancy of less than 20% is considered to be non ...
Cimetidine was the prototypical histamine H 2 receptor antagonist from which the later members of the class were developed. Cimetidine was the culmination of a project at Smith, Kline and French (SK&F) Laboratories in Welwyn Garden City (now part of GlaxoSmithKline ) by James W. Black , C. Robin Ganellin , and others to develop a histamine ...
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