Lafutidine

Lafutidine Basic information
Description References
Product Name:Lafutidine
Synonyms:n-(4-(4-piperidinylmethyl)pyridyl-2-oxy)butenyl-2-(furfurylsulfinyl)acetamide;2-((Furan-2-ylMethyl)sulfinyl)-N-(4-((4-(piperidin-1-ylMethyl)pyridin-2-yl)oxy)but-2-en-1-yl)acetaMide;(Z)-2-((Furan-2-ylMethyl)sulfinyl)-N-(4-((3-(piperidin-1-ylMethyl)pyridin-2-yl)oxy)but-2-en-1-yl)acetaMide;Adefovir Dipivioxil;(Z)-2-((Furan-2-ylmethyl)sulfinyl)-N-(4-((3-(piperidin-1-ylmethyl)pyridin-2-yl)oxy)but-2-en-1-yl);(Z)-2-((Furan-2-ylmethyl)sulfinyl)-N-(4-((3-(piperidin-1-ylmethyl)pyridin-2-yl)oxy)but-2-en-1-;LAFUTIDINE(SUBJECTTOPATENTFREE);118288-08-07
CAS:118288-08-7
MF:C22H29N3O4S
MW:431.55
EINECS:601-513-8
Product Categories:Other APIs;Active Pharmaceutical Ingredients;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds
Mol File:118288-08-7.mol
Lafutidine Structure
Lafutidine Chemical Properties
Melting point 92.7-94.9°
Boiling point 704.2±60.0 °C(Predicted)
density 1.252±0.06 g/cm3(Predicted)
storage temp. Sealed in dry,Store in freezer, under -20°C
Water Solubility Insoluble in water
solubility DMF:5.0(Max Conc. mg/mL);11.59(Max Conc. mM)
DMSO:48.67(Max Conc. mg/mL);112.77(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:10):0.09(Max Conc. mg/mL);0.21(Max Conc. mM)
Ethanol:9.0(Max Conc. mg/mL);20.86(Max Conc. mM)


form powder to crystal
pka13.13±0.46(Predicted)
color White to Orange to Green
CAS DataBase Reference118288-08-7(CAS DataBase Reference)
Safety Information
Safety Statements 24/25
HS Code 29349990
MSDS Information
Lafutidine Usage And Synthesis
DescriptionLafutidine is a second generation of H2-receptor antagonist. H2-receptor antagonist can strongly inhibit gastric acid secretion compared with conventional drugs such as antacids. Unlike conventional H2-receptor antagonist, lafutidine inhibits gastric acid secretion during daytime as well as nighttime in clinical studies in humans. Lafutidine also has gastroprotective activity independent of its acid antisecretory efficacy, preventing noxious agent-induced gastric mucosal injury and accelerating the repair process following gastric mucosal damage. It also protects experimentally induced reflux esophagitis, indomethacin-induced intestinal, and dextran sulfate sodium-induced colonic inflammation.
Lafutidine is used for gastric and duodenal ulcers. It is also confirmed that lafutidine can be used as an empiric treatment and superior efficacy for primary care practice patients with dyspepsia.
References[1] Tomohiko Shimatani, Masaki Inoue, Tomoko Kuroiwa, Jing Xu, Masuo Nakamura, Susumu Tazuma, Kazuro Ikawa, Norifumi Morikawa (2006) Lafutidine, a Newly Developed Antiulcer Drug, Elevates Postprandial Intragastric pH and Increases Plasma Calcitonin Gene-Related Peptide and Somatostatin Concentrations in Humans: Comparisons with Famotidine, Digestive Diseases and Sciences, 51, 114-120
[2] Bhupesh Dewan, Nisha Philipose (2011) Lafutidine 10 mg versus Rabeprazole 20 mg in the Treatment of Patients with Heartburn-Dominant Uninvestigated Dyspepsia: A Randomized, Multicentric Trial, Gastroenterology Research and Practice, 2011, Article ID 640685
[3] https://www.drugs.com

DescriptionLafutidine is a histamine H2 receptor antagonist with gastroprotective activity. It inhibits histamine-induced cAMP production in CHO cells expressing human histamine H2 receptors when used at a concentration of 10 nM. Intragastric administration of lafutidine (3, 10, and 30 mg/kg) reduces hemorrhagic esophageal lesion size and gastric acid secretion in a rat model of pyloric ligation-induced reflux esophagitis. It prevents 5-fluorouracil-induced intestinal mucositis, diarrhea, and body weight loss in wild-type, but not Trpv1-/- or sensory deafferented, mice when administered at doses ranging from 3 to 30 mg/kg. Lafutidine (10 mg/kg) also reduces indomethacin-induced antral ulcer size in wild-type, but not chemically-deafferented, rats.
DescriptionLafutidine was launched in Japan for the treatment of gastritis, reflux oesophagitis and peptic ulcers. It can be prepared in eight steps from 4-(2-tetrahydropyranyloxy)-2(Z)-butenl- ol. Lafutidine is a potent and longer-acting H2 antagonist compared to other marketed compounds of its class such as cimetidine and famotidine. In contrast to other commercially available H2 antagonists, lafutidine also exerts a gastroprotective action probably via capsaicin-sensitive afferent nerves. It was clinically effective in the treatment of nonsteroidal antiinflammatory drug-induced ulcer in patients refractory to existing antiulcer agents.
OriginatorFujirebio (Japan)
UsesLafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion
Uses(Z)-2-((Furan-2-ylmethyl)sulfinyl)-n-(4-((3-(piperidin-1-ylmethyl)pyridin-2-yl)oxy)but-2-en-1-yl)acetamide is a Histaminic H2 receptor antagonists in ulcer disease. Also, it is a model compound used to investigate the binding mechanism between antiulcer drugs and human serum albumin (HSA).
UsesSecond generation histamine H2-receptor antagonist. Antiulcerative
DefinitionChEBI: Lafutidine is an organic molecular entity.
Brand nameStogar, Protecadin
2-CHLORO-4-(1-PIPERIDINYLMETHYL) PYRIDINE.OXALIC ACIDE(INTERMEDIATE FOR LAFUTIDINE) 2-(FURFURYLTHIO)ETHYLAMINE LACTITOL USP(CRM STANDARD) N-lactitol-S-(fluorophenacyl)cysteamine 4-Pyridinemethanamine,2-methoxy-(9CI) LACTITOL-OLIGOSACCHARIDE LACTITOL, [3H] Peracetylated lactitol,Lactitol nonaacetate N-(PYRIDIN-4-YLMETHYL)BUTAN-1-AMINE 4-[4-(Piperidinomethyl)pyridyl-2-oxy]-cis-2-butenamine LACTITOL MONOHYDRATE EPL(CRM STANDARD) 2(1H)-Pyridinone,4-(aminomethyl)-(9CI) p-Nitrophenyl 2-(Furfurylsulfinyl)acetate neuramin lactitol 2-((FURAN-2-YL)METHYLSULFINYL)-N-((Z)-4-HYDROXYBUT-2-ENYL)ACETAMIDE N-{4-[4-(PIPERIDINOMETHYL)PYRIDYL-2-OXY]-CIS-2-BUTENE}PHTHALIMIDE MALEIC ACID(INTERMEDIATE FOR LAFUTIDINE) 2-ALLYLOXYPYRIDINE (Z)-4-[(TETRAHYDRO-2H-PYRAN-2-YL)OXY]-2-BUTEN-1-OL (PREPARATION FOR LAFUTIDINE)

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