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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.
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.
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.
Cimetidine, sold under the brand name Tagamet among others, is a histamine H 2 receptor antagonist that inhibits stomach acid production. [1] [9] [10] It is mainly used in the treatment of heartburn and peptic ulcers.
All of these drugs inhibit the gastric H,K-ATPase by covalent binding, so the duration of their effect is longer than expected from their levels in the blood. [ 76 ] Targeting the terminal step in acid production, as well as the irreversible nature of the inhibition, results in a class of medications that are significantly more effective than H ...
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]
Histamine has two basic centres, namely the aliphatic amino group and whichever nitrogen atom of the imidazole ring does not already have a proton. Under physiological conditions, the aliphatic amino group (having a pK a around 9.4) will be protonated, whereas the second nitrogen of the imidazole ring (pK a ≈ 5.8) will not be protonated. [11]
Hyoscyamine (also known as daturine or duboisine) is a naturally occurring tropane alkaloid and plant toxin. It is a secondary metabolite found in certain plants of the family Solanaceae, including henbane, mandrake, angel's trumpets, jimsonweed, the sorcerers' tree, and Atropa belladonna (deadly nightshade).