| Identification | More | [Name]
Mosapride citrate | [CAS]
112885-42-4 | [Synonyms]
4-AMINO-5-CHLORO-2-ETHOXY-N-[[4-(4-FLUOROBENZYL)-2-MORPHOLINYL]METHYL]BENZAMIDE CITRATE DIHYDRATE
MOSAPRIDE CITRATE
MOSAPRIDE CITRATE DIHYDRATE
(+-)-4-amino-5-chloro-2-ethoxy-n-((4-(4-fluorobenzyl)-2-morpholinyl)methyl)b
as4370
benzamide,4-amino-5-chloro-2-ethoxy-n-((4-((4-fluorophenyl)methyl)-2-morpholin
enzamidecitrate
yl)methyl)-,2-hydroxy-1,2,3-propanetricarboxylate(1:1)
4-Amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]-2-morpholinyl]methyl]-benzamide 2-hydroxy-1,2,3-propanetricarboxylate
Gasmotin | [EINECS(EC#)]
601-211-6 | [Molecular Formula]
C27H37ClFN3O12 | [MDL Number]
MFCD00874415 | [Molecular Weight]
650.05 | [MOL File]
112885-42-4.mol |
| Hazard Information | Back Directory | [Description]
Mosapride is an agonist of the serotonin (5-HT) receptor subtype 5-HT4 (Ki = 69.9 nM).1,2 It is selective for 5-HT4 over 5-HT1, 5-HT2, dopamine D2, and α1- and α2-adrenergic receptors but acts as a partial antagonist at 5-HT3 (Ki = 1,189 nM).1,2 It induces relaxation of precontracted rat esophageal thoracic muscularis mucosa preparations and enhances electrically evoked contractions in isolated guinea pig ileum (EC50s = 208.4 and 73.2 nM, respectively).3 Mosapride (0.5 and 1 mg/kg, i.v.) increases antral and duodenal, but not ileal or colonic, motility in conscious dogs.1 It also increases gastric emptying in rats when administered at doses ranging from 0.03 to 30 mg/kg. | [Uses]
A selective SR-4 activator and a SR-3 inhibitor | [Uses]
As a selective SR-4 activator and a SR-3 inhibitor, Mosapride(Mosapride citrate) is a gastroprokinetic agent that acts as a selective 5HT4 agonist which accelerates gastric emptying and is used for the treatment of acid reflux, irritable bowel syndrome and functional dyspepsia.
| [Biological Activity]
5-HT 4 receptor agonist and 5-HT 3 receptor antagonist. Displays no activity at D 2 , α 1 , α 2 , 5-HT 1 and 5-HT 2 receptors. Gastroprokinetic agent; increases gastric emptying in rats and stimulates gastric motor actvity in conscious dogs. | [storage]
room temperature (desiccate) |
| Safety Data | Back Directory | [Toxicity]
LD50 in male, female mice, rats (mg/kg): >3000, >3000, >3000, 1905 orally; >1000, 914, >1000, >1000 i.p.; all species >1000 s.c.; in male, female dogs (mg/kg): both >400 orally (Yatera) |
|
|