Title: Ketanserin
CAS Registry Number: 74050-98-9
CAS Name: 3-[2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl]-2,4[1H,3H]-quinazolinedione
Manufacturers' Codes: R-41468
Trademarks: Ketensin (Janssen); Serefrex (Janssen); Taseron (Janssen)
Molecular Formula: C22H22FN3O3
Molecular Weight: 395.43
Percent Composition: C 66.82%, H 5.61%, F 4.80%, N 10.63%, O 12.14%
Literature References: Specific serotonin (5HT2)-receptor antagonist. Prepn: J. Vandenbeck et al., EP 13612; eidem, US 4335127 (1980, 1982 both to Janssen). X-ray structure: O. M. Peeters et al., Cryst. Struct. Commun. 11, 375 (1982). Receptor binding profile: J. E. Leysen et al., Life Sci. 28, 1015 (1981). Pharmacology: J. M. Van Neuten et al., J. Pharmacol. Exp. Ther. 218, 217 (1981). HPLC determn in plasma: A. T. Kacprowicz et al., J. Chromatogr. 272, 417 (1983). Clinical efficacy in intermittent claudication: J. De Cree et al., Lancet 2, 775 (1984); in Raynaud's phenomenon: J. R. Seibold, A. H. M. Jageneau, Arthritis Rheum. 27, 139 (1984); in hypertension: A. Amery et al., J. Cardiovasc. Pharmacol. 6, 182 (1984). Series of articles on pharmacology and clinical studies: ibid. 7, Suppl. 7, S1-S182 (1985); on pharmacokinetics and metabolism: Arzneim.-Forsch. 38, 775-800 (1988). Review of pharmacology and clinical efficacy in hypertension and vascular disease: R. N. Brogden, E. M. Sorkin, Drugs 40, 903-949 (1990).
Properties: Crystals from 4-methyl-2-pentanone, mp 227-235°. Soly (g/100 ml): 0.001 in water; 0.038 in ethanol; 2.34 in DMF. pKa 7.5.
Melting point: mp 227-235°
pKa: pKa 7.5
Derivative Type: Tartrate
CAS Registry Number: 83846-83-7
Manufacturers' Codes: R-49945
Trademarks: Ket (Irbi); Perketan (Inverni); Serepress (Formenti); Sufrexal (Janssen)
Molecular Formula: C22H22FN3O3.C4H6O6
Molecular Weight: 545.51
Percent Composition: C 57.25%, H 5.17%, F 3.48%, N 7.70%, O 26.40%
Therap-Cat: Antihypertensive.
Keywords: Antihypertensive; Serotonin Receptor Antagonist. |