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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.
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.
H 2 receptor H2 Receptors: Found mainly in the stomach lining (parietal cells), H2 receptors regulate gastric acid secretion by stimulating the production of hydrochloric acid. H2 antagonists (H2 blockers) are used to reduce stomach acid production and treat conditions like gastroesophageal reflux disease (GERD) and peptic ulcers. [3]
[4] [5] Normally, histamine binds to the H 1 receptor and heightens the receptor's activity; the receptor antagonists work by binding to the receptor and blocking the activation of the receptor by histamine; by comparison, the inverse agonists bind to the receptor and both block the binding of histamine, and reduce its constitutive activity, an ...
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 ...
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.
The H 2 receptor antagonists are a class of drugs used to block the action of histamine on parietal cells in the stomach, decreasing the production of acid by these cells. H 2 antagonists are used in the treatment of dyspepsia, although they have been surpassed in popularity by the more effective [1] proton pump inhibitors.
Famotidine, sold under the brand name Pepcid among others, is a histamine H 2 receptor antagonist medication that decreases stomach acid production. [4] It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellison syndrome. [4] It is taken by mouth or by injection into a vein. [4] It begins working within ...