Title: Alpiropride
CAS Registry Number: 81982-32-3
CAS Name: 4-Amino-2-methoxy-5-[(methylamino)sulfonyl]-N-[[1-(2-propenyl)-2-pyrrolidinyl]methyl]benzamide
Additional Names: (±)-N-[(1-allyl-2-pyrrolidinyl)methyl]-4-amino-5-(methylsulfamoyl)-o-anisamide; N-(1-allyl-2-pyrrolidinylmethyl)-2-methoxy-4-amino-5-methylsulfamoylbenzamide
Manufacturers' Codes: RIV-2093
Trademarks: Rivistel (Delagrange)
Molecular Formula: C17H26N4O4S
Molecular Weight: 382.48
Percent Composition: C 53.38%, H 6.85%, N 14.65%, O 16.73%, S 8.38%
Literature References: Dopamine D2-receptor antagonist structurally similar to sulpiride, q.v. Prepn: J. Perrot, M. Thominet, EP 47207; eidem, US 4550179 (1982, 1985 both to Soc. d'Etudes Sci. Ind. l'Ile-de-France). Dopamine receptor binding study: P. Sokoloff et al., Arch. Pharmacol. 327, 221 (1984). HPLC determn in plasma and urine: F. Bressolle et al., J. Chromatogr. 343, 443 (1985). Pharmacokinetics and metabolism in humans: F. Bressolle et al., J. Pharm. Clin. 4, 261 (1985). Preliminary study in experimentally induced migraine: A. Bès et al., Int. J. Clin. Pharmacol. Res. 6, 189 (1986).
Properties: Crystals from absolute ethanol, mp 168.5-169°. LD50 in male mice (mg/kg): 44 i.v.; 184 i.p.; 204 s.c.; 3600 orally (Perrot, Thominet, 1985).
Melting point: mp 168.5-169°
Toxicity data: LD50 in male mice (mg/kg): 44 i.v.; 184 i.p.; 204 s.c.; 3600 orally (Perrot, Thominet, 1985)
Therap-Cat: Antimigraine.
Keywords: Antimigraine. |