ebrotidine
Ebrotidine is an H2 receptor antagonist with gastroprotective activity against ethanol-, aspirin- or stress-induced gastric mucosal damage. The antisecretory properties of ebrotidine are similar to those of ranitidine, and approximately 10-fold greater than those of cimetidine. Ebrotidine has anti-Helicobacter pylori activity via inhibition of the urease enzyme and the proteolytic and mucolytic activities of the bacterium. However, its activity is synergistic with a number of antibacterial agents. Ebrotidine counteracts the inhibitory effects of H. pylori lipopolysaccharides. Ebrotidine was withdrawn from the market due to risks of hepatotoxicity. — Wikipedia
Clinical trial activity
0 trials · 0 clinical orgs · 0 marketing orgs
Mechanism of action
- Histamine H2 receptorANTAGONIST
HRH2 antagonist
Ebrotidine is the first of a new generation of H2 receptor antagonists with gastroprotective activity. It stimulates epithelial cell proliferative activity and produces beneficial physicochemical changes in the gastric mucus that contribute to its gastro-protective action against ethanol-, aspirin- or stress-induced gastric mucosal damage. The antisecretory properties of ebrotidine are similar to those of ranitidine and approximately 10-fold greater than those of cimetidine. This drug exhibits anti-Helicobacter pylori activity that is synergistic with a number of antibacterial agents; it inhibits the urease enzyme and the proteolytic and mucolytic activities of H. pylori, and counteracts the inhibitory effects of H. pylori lipo-polysaccharide.
- UreaseINHIBITOR
ureB inhibitor
Ebrotidine is the first of a new generation of H2 receptor antagonists with gastroprotective activity. It stimulates epithelial cell proliferative activity and produces beneficial physicochemical changes in the gastric mucus that contribute to its gastro-protective action against ethanol-, aspirin- or stress-induced gastric mucosal damage. The antisecretory properties of ebrotidine are similar to those of ranitidine and approximately 10-fold greater than those of cimetidine. This drug exhibits anti-Helicobacter pylori activity that is synergistic with a number of antibacterial agents; it inhibits the urease enzyme and the proteolytic and mucolytic activities of H. pylori, and counteracts the inhibitory effects of H. pylori lipo-polysaccharide.
Chemistry & pharmacology
SMILES
NC(N)=Nc1nc(CSCCN/C=N/S(=O)(=O)c2ccc(Br)cc2)cs1- Mol. weight
- 477.44 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaEbrotidine ↗
- ChEMBLCHEMBL1742471 ↗
Also known as
- 4-bromo-n-(((2-(((-((diaminomethylene)amino)-4-thiazolyl)methyl)thio)ethyl)amino)methylene)benzenesulfonamide
- ebrodin
- ebrotidine
- ebrotidine
- ebrotidine
- ebrotidine
- ebrotidine
- ebrotidine
- fi-3542
- fi-3542
- fi-3542
- ulsanic