product name Lafutidine
Description: Lafutidine (also known as FRG-8813), a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion. It is a second generation histamine H2 receptor antagonist having multimodal mechanism of action and used to treat gastrointestinal disorders. It is marketed in Japan and India.Lafutidine is used to treat gastric ulcers, duodenal ulcers, as well as wounds in the lining of the stomach associated with acute gastritis and acute exacerbation of chronic gastritis.
References: Nihon Yakurigaku Zasshi. 2001 Jun;117(6):377-86.; Wikipedia
431.55
Formula
C22H29N3O4S
CAS No.
118288-08-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 86 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: 13 mg/mL (30.1 mM)
Solubility (In vivo)
Synonyms
FRG-8813
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19427738
| In Vitro |
In vitro activity: Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.It is currently marketed in Japan (Stogar) China (Lemeiting) and India (Lafaxid). It not only suppresses gastric acid secretion, but also has cytoprotective properties by the virtue of its property to induce the collagen synthesis in the gastric mucosa. It has a novel mechanism of action in addition to blocking the H2 receptors, it decreases inflammation by modulating calcitonin gene-related peptide (CGRP) and vanilloid receptors. It is also found to stimulate mucin biosynthesis and promote the restitution of damaged mucosa. Lafutidine is absorbed in the small intestine, reaches gastric cells via the systemic circulation, and then directly and rapidly binds to gastric cell histamine H2 receptors, thereby inhibiting the stimulation of cAMP and a resultant decrease in acid production (antisecretory action). It causes a sustained increase in intracellular Ca2+ ion concentration in endothelial cells resulting in the release of Calcitonin Gene Related Peptide (CGRP), which causes acid suppression by decreasing the vagal tone. Lafutidine also increases plasma somatostatin levels which decreases secretion of gastrin from G cells. This decrease in gastrin causes inhibition of parietal cells, resulting in decrease in gastric acid secretion. Kinase Assay: Cell Assay: |
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| References | Nihon Yakurigaku Zasshi. 2001 Jun;117(6):377-86. |
