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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.
H 2 receptors are a type of histamine receptor found in many parts of the anatomy of humans and other animals. They are positively coupled to adenylate cyclase via G s alpha subunit . It is a potent stimulant of cAMP production, which leads to activation of protein kinase A . [ 5 ]
A histamine agonist is a drug which causes increased activity at one or more of the four histamine receptor subtypes. H 1 agonists promote wakefulness. [1] H 2: Betazole and Impromidine are examples of agonists used in diagnostics to increase histamine. H 3: Betahistine is a weak Histamine 1 agonist and a very strong antagonist of the Histamine ...
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]
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.
Loss of libido and erectile dysfunction can occur during treatment with histamine H 2 receptor antagonists such as cimetidine, ranitidine, and risperidone. [38] The injection of histamine into the corpus cavernosum in males with psychogenic impotence produces full or partial erections in 74% of them. [ 39 ]
Examples include histamine receptor agonists and histamine receptor antagonists (or antihistamines). Subdivisions of histamine antagonists include H 1 receptor antagonists , H 2 receptor antagonists , and H 3 receptor antagonists .
H 2-antihistamines, like H 1-antihistamines, exist as inverse agonists and neutral antagonists. They act on H 2 histamine receptors found mainly in the parietal cells of the gastric mucosa, which are part of the endogenous signaling pathway for gastric acid secretion.