Mosapride citrate
as4370 · Gasmotin · enzamidecitrate · AS-4370 citrate · TAK-370 citrate · MOSAPRIDE CITRATE · Mosapride citrate,>99% · Mosapride Citrate (TAK-370
Identifikatoren & physikalische Daten
| CAS No. | 112885-42-4 |
|---|---|
| Summenformel | C27H33ClFN3O10 |
| Durchschnittliche Molmasse | 614 g/mol |
| Monoisotopische Masse | 613,18385016 g/mol |
| SMILES | CCOc1cc(N)c(Cl)cc1C(=O)NCC1CN(Cc2ccc(F)cc2)CCO1.O=C(O)CC(O)(CC(=O)O)C(=O)O |
| InChIKey | HUZTYZBFZKRPFG-UHFFFAOYSA-N |
| PubChem CID | 119583 |
| ChEMBL | CHEMBL1733174 |
| EC No. | 601-211-6 |
| DTXSID | DTXSID7046207 |
Chemische & physikalische Eigenschaften
| Polarare Oberfläche (TPSA) | 209 |
|---|---|
| H-Brücken-Donoren | 6 |
| H-Brücken-Akzeptoren | 13 |
| Frei drehbare Bindungen | 12 |
| Schwere Atome | 42 |
| Formalladung | 0 |
| Komplexität | 749 |
| Schmelzpunkt | 143-145° |
| Lagerbedingungen | Inert atmosphere,2-8°C |
| Löslichkeit | DMSO (Slightly), Ethanol (Slightly, Sonicated) |
| Aggregatzustand | Solid |
| Farbe | White to Off-White |
| Stabilität | 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 Datenbank | 112885-42-4(CAS DataBase Reference) |
Sicherheit & Vorschriften
| GHS-Einstufung | WarningH361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]P203, P280, P318, P405, and P501 (click each P-code to see the statement)The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory. |
|---|---|
| Hazard Classes and Categories | Repr. 2 (100%) |
| Toxizität | 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) |
Anwendungen & Verwendung
Beschreibung
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.
Verwenden
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.