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Ball-and-stick model of cimetidine, the prototypical H 2 receptor antagonist. H 2 antagonists, sometimes referred to as H2RAs [1] and also called H 2 blockers, are a class of medications that block the action of histamine at the histamine H 2 receptors of the parietal cells in the stomach. This decreases the production of stomach acid.
H2 antagonists (H2 blockers) are used to reduce stomach acid production and treat conditions like gastroesophageal reflux disease (GERD) and peptic ulcers. [ 3 ] H 3 receptor H3 Receptors: These receptors are predominantly located in the central nervous system (CNS), particularly in regions associated with neurotransmitter release and modulation.
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.
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 -histamine receptor blockers should be taken 2 hours after taking itraconazole a or ketoconazole a to avoid a significant decrease in their absorption. H 2 -histamine receptor blockers can counteract the effects of pentagastrin a and histamine a on gastric acid-forming function, so use H 2 blockers within 24 hours prior to the test ...
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 ...
Like other H 2 receptor antagonists, lafutidine acts by preventing the secretion of gastric acid. [3] It also activates calcitonin gene-related peptide, resulting in the stimulation of nitric oxide (NO) and regulation of gastric mucosal blood flow, increases somatostatin levels also resulting in less gastric acid secretion, causes the stomach lining to generate more mucin, inhibits neutrophil ...
[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 ...