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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.
The histamine receptors are a class of G protein–coupled receptors which bind histamine as their primary endogenous ligand. [1] [2] Histamine receptors are proteins that bind with histamine, a neurotransmitter involved in various physiological processes. There are four main types: H1, H2, H3, and H4.
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 often explored as a potential cause for diseases related to hyper-responsiveness of the immune system. In patients with asthma, abnormal histamine receptor activation in the lungs is associated with bronchospasm, airway obstruction, and production of excess mucus. Mutations in histamine degradation are more common in patients with ...
Nizatidine is a histamine H 2 receptor antagonist that inhibits stomach acid production, and is commonly used in the treatment of peptic ulcer disease and gastroesophageal reflux disease. [2] It was patented in 1980 and approved for medical use in 1988. [3] [4] It was developed by Eli Lilly.
Amthamine is a histamine agonist selective for the H 2 subtype. [1] It has been used in vitro and in vivo to study gastric secretion , [ 2 ] as well as other functions of the H 2 receptor. [ 3 ] [ 4 ] [ 5 ]
Burimamide is an antagonist at the H 2 and H 3 histamine receptors.At physiological pH, it is largely inactive as an H 2 antagonist, [1] but its H 3 affinity is 100x higher. It is a thiourea derivative.
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 an ...