- Mosapride citrate
-
-
2026-07-01
- CAS:112885-42-4
- Min. Order: 1KG
- Purity: 99.9%
- Supply Ability: 500kg/month
- Mosapride citrate
-
-
2026-06-30
- CAS:112885-42-4
- Min. Order: 1kg
- Purity: 98%
- Supply Ability: 1000kgs
- Mosapride citrate
-
-
2026-06-30
- CAS:112885-42-4
- Min. Order: 1kg
- Purity: 98%
- Supply Ability: 10000kgS
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| | Mosapride citrate Basic information |
| Product Name: | Mosapride citrate | | Synonyms: | 4-AMINO-5-CHLORO-2-ETHOXY-N-[[4-(4-FLUOROBENZYL)-2-MORPHOLINYL]METHYL]BENZAMIDE CITRATE DIHYDRATE;4-Amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]-2-morpholinyl]methyl]-benzamide 2-hydroxy-1,2,3-propanetricarboxylate;Gasmotin;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]benzamidecitrate;4-amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl]benzamide;4-azanyl-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]morpholin-2-yl]methyl]benzamide | | CAS: | 112885-42-4 | | MF: | C27H33ClFN3O10 | | MW: | 614.02 | | EINECS: | 601-211-6 | | Product Categories: | Inhibitors;APIS;API;TAK-370, AS-4370, Gasmotin;Gastroprokinetic Agent | | Mol File: | 112885-42-4.mol |  |
| | Mosapride citrate Chemical Properties |
| Melting point | 143-145° | | storage temp. | Inert atmosphere,2-8°C | | solubility | DMSO (Slightly), Ethanol (Slightly, Sonicated) | | form | Solid | | color | White to Off-White | | Stability: | Hygroscopic | | InChIKey | HUZTYZBFZKRPFG-UHFFFAOYSA-N | | SMILES | C(O)(C(=O)O)(CC(=O)O)CC(=O)O.C(C1C=C(Cl)C(N)=CC=1OCC)(=O)NCC1OCCN(CC2C=CC(F)=CC=2)C1 | | CAS DataBase Reference | 112885-42-4(CAS DataBase Reference) |
| 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) |
| | Mosapride citrate Usage And Synthesis |
| Description | Mosapride is an agonist of the serotonin (5-HT) receptor subtype 5-HT4 (Ki = 69.9 nM). 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). 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). Mosapride (0.5 and 1 mg/kg, i.v.) increases antral and duodenal, but not ileal or colonic, motility in conscious dogs. It also increases gastric emptying in rats when administered at doses ranging from 0.03 to 30 mg/kg. | | 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. | | Uses | Mosapride Citrate is a selective SR-4 activator and a SR-3 inhibitor. | | 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. | | Synthesis | GENERAL STEPS: To a suspension of 1.3 g (2.5 mmol) of 4-amino-5-chloro-2-ethoxy-N-((4-(4-fluorobenzyl)morpholin-2-yl)methyl)benzamide (Compound VIII) and 3 mL of water was added 12 mL of 117% aqueous hydrochloric acid. The resulting solution was stirred at 40°C for 3 hours, cooled to 10°C and 38 mL of 4M aqueous sodium hydroxide solution was added dropwise. The precipitated mosapride base (Compound IX) was filtered and washed twice with water to give 1.05 g (100%) of Compound IX.1.01 g of the above obtained Compound IX was warmed to boiling with 25 mL of 10% aqueous citric acid solution with stirring, cooled to 0°C, the precipitated product was filtered, and washed twice with water to give 1.34 g (86%) of 4-amino-5-chloro-2-ethanol oxy-N-((4-(4-fluorobenzyl)morpholin-2-yl)methyl)benzamide 2-hydroxypropane-1,2,3-tricarboxylate. Melting point: 110-113°C. | | storage | room temperature (desiccate) | | References | [1] Patent: WO2003/106440, 2003, A2. Location in patent: Page 10 |
| | Mosapride citrate Preparation Products And Raw materials |
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