Details
Stereochemistry | RACEMIC |
Molecular Formula | C22H29N3O4S |
Molecular Weight | 431.548 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[O-][S+](CC(=O)NC\C=C/COC1=NC=CC(CN2CCCCC2)=C1)CC3=CC=CO3
InChI
InChIKey=KMZQAVXSMUKBPD-DJWKRKHSSA-N
InChI=1S/C22H29N3O4S/c26-21(18-30(27)17-20-7-6-14-28-20)23-9-2-5-13-29-22-15-19(8-10-24-22)16-25-11-3-1-4-12-25/h2,5-8,10,14-15H,1,3-4,9,11-13,16-18H2,(H,23,26)/b5-2-
DescriptionSources: http://www.ncbi.nlm.nih.gov/pubmed/11436515Curator's Comment: description was created based on several sources, including
http://www.zuventus.co.in/doctor_wise_products_selected.aspx?Medi_Id=39
Sources: http://www.ncbi.nlm.nih.gov/pubmed/11436515
Curator's Comment: description was created based on several sources, including
http://www.zuventus.co.in/doctor_wise_products_selected.aspx?Medi_Id=39
Lafutidine is a novel histamine H2 antagonist with gastroprotective activity. Lafutidine exhibited potent and long-lasting H2 antagonism and prolonged antisecretion. In addition, lafutidine showed a gastroprotective effect against noxious agents-induced gastric mucosal damage through capsaicin-sensitive afferent nerves. Lafutidine showed antiulcer activities against acute ulcer models, prevented gastric ulcer relapse of acetic ulcer. Adverse events observed during clinical trials included constipation, diarrhea, drug rash, nausea, vomiting and dizziness.It also activates calcitonin gene-related peptide, resulting in the stimulation of nitric oxide (NO) and regulation of gastric mucosal blood flow, increases somatostatin levels also resulting in less gastric acid secretion, causes the stomach lining to generate more mucin, inhibits neutrophil activation thus preventing injury from inflammation, and blocks the attachment of Helicobacter pylori to gastric cells
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL1941 Sources: http://www.ncbi.nlm.nih.gov/pubmed/11786663 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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[A case of paclitaxel-induced peripheral neuropathy successfully treated by H2-blocker, lafutidine]. | 2009 Sep |
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Protective effect of lafutidine, a histamine H2 receptor antagonist, against loxoprofen-induced small intestinal lesions in rats. | 2010 May |
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Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. | 2011 Jul 14 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/25532503
20 mg
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/12577045
lafutidine, 86.64 +/- 9.52 pg/mL pretreatment of gastric mucosal before water-immersion restraint stress caused a significant increase in serum calcitonin gene-related peptide concentration
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C29702
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WHO-ATC |
A02BA08
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WHO-VATC |
QA02BA08
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DB12770
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5282136
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7173
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1537
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CHEMBL1742461
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C076948
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206449-93-6
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SUB08388MIG
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C79117
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LAFUTIDINE
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49S4O7ADLC
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ACTIVE MOIETY