Title: Mosapride
CAS Registry Number: 112885-41-3
CAS Name: 4-Amino-5-chloro-2-ethoxy-N-[[4-[(4-fluorophenyl)methyl]-2-morpholinyl]methyl]benzamide
Additional Names: (±)-4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]methyl]benzamide
Molecular Formula: C21H25ClFN3O3
Molecular Weight: 421.89
Percent Composition: C 59.78%, H 5.97%, Cl 8.40%, F 4.50%, N 9.96%, O 11.38%
Literature References: Selective 5-HT4 receptor agonist. Prepn: T. Kon et al., EP 243959; eidem, US 4870074 (1987, 1989 both to Dainippon); S. Kato et al., J. Med. Chem. 34, 616 (1991). Pharmacology: N. Yoshida et al., Arch. Int. Pharmacodyn. Ther. 300, 51 (1989). Series of articles on pharmacokinetics: Arzneim.-Forsch. 43, 859-872 (1993); on pharmacology and metabolism: ibid. 1083-1108. HPLC determn in plasma: I. Yokoyama et al., J. Pharm. Biomed. Anal. 15, 1527 (1997). Clinical evaluation in gastro-esphageal reflux disease: M. Ruth et al., Aliment. Pharmacol. Ther. 12, 35 (1998). Toxicity study: S. Yatera et al., Jpn. Pharmacol. Ther. 21, 21 (1993).
Properties: Crystals from ethanol, mp 151-153°.
Melting point: mp 151-153°
Derivative Type: Citrate
CAS Registry Number: 112885-42-4
Manufacturers' Codes: AS-4370
Trademarks: Gasmotin (Dainippon)
Molecular Formula: C21H25ClFN3O3.C6H8O7
Molecular Weight: 614.02
Percent Composition: C 52.81%, H 5.42%, Cl 5.77%, F 3.09%, N 6.84%, O 26.06%
Properties: Crystals from ethanol, mp 143-145°. 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).
Melting point: mp 143-145°
Toxicity data: 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)
Therap-Cat: Gastroprokinetic.
Keywords: Gastroprokinetic. |