Title: Dolasetron
CAS Registry Number: 115956-12-2
CAS Name: 1H-Indole-3-carboxylic acid (2a,6a,8a,9ab)-octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl ester
Additional Names: endo-hexahydro-8-(3-indolylcarbonyloxy)-2,6-methano-2H-quinolizin-3(4H)-one
Manufacturers' Codes: MDL-73147
Molecular Formula: C19H20N2O3
Molecular Weight: 324.37
Percent Composition: C 70.35%, H 6.21%, N 8.64%, O 14.80%
Literature References: Bridged pseudopelletierine derivative; specific serotonin (5HT3) receptor antagonist. Prepn: M. W. Gittos, EP 266730; idem et al., US 4906755 (1988, 1990 both to Merrell Dow). Binding study: P. H. Boeijinga et al., Eur. J. Pharmacol. 219, 9 (1992). Pharmacology: R. C. Miller et al., Drug Dev. Res. 28, 87 (1993). Clinical pharmacokinetics: H. Boxenbaum et al., Biopharm. Drug Dispos. 13, 693 (1992); eidem, ibid. 14, 131 (1993). GC-MS and LC determn in plasma: T. A. Gillespie et al., J. Pharm. Biomed. Anal. 11, 955 (1993). Clinical trial in emetogenic chemotherapy: A. A. Fauser et al., Eur. J. Cancer 32A, 1523 (1996); for prevention of postoperative nausea: S. G. Graczyk et al., Anesth. Analg. 84, 325 (1997).
Derivative Type: Methanesulfonate
CAS Registry Number: 115956-13-3
Additional Names: Dolasetron mesylate
Manufacturers' Codes: MDL-73147EF
Trademarks: Anzemet (Aventis)
Molecular Formula: C19H20N2O3.CH3SO3H
Molecular Weight: 420.48
Percent Composition: C 57.13%, H 5.75%, N 6.66%, O 22.83%, S 7.63%
Properties: Crystalline solid, mp 278°.
Melting point: mp 278°
Therap-Cat: Antiemetic.
Keywords: Antiemetic; Antimigraine; Serotonin Receptor Antagonist. |