Title: Bisoprolol
CAS Registry Number: 66722-44-9
CAS Name: 1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol
Additional Names: (±)-1-[[a-(2-isopropoxyethoxy)-p-tolyl]oxy]-3-(isopropylamino)-2-propanol; (±)-1-[p-(2-isopropoxyethoxymethyl)phenoxy]-3-(isopropylamino)-2-propanol
Manufacturers' Codes: EMD-33512
Molecular Formula: C18H31NO4
Molecular Weight: 325.44
Percent Composition: C 66.43%, H 9.60%, N 4.30%, O 19.66%
Literature References: Cardioselective b1-adrenergic blocker. Prepn: BE 859425; R. Jonas et al., US 4258062 (1978, 1981 both to E. Merck). Clinical pharmacology: A. E. Tattersfield et al., Br. J. Clin. Pharmacol. 18, 343 (1984); P. Dorow, U. Tönnesmann, Eur. J. Clin. Pharmacol. 27, 135 (1984). Binding study of (-)-form: A. J. Kaumann, H. Lemoine, Arch. Pharmacol. 331, 27 (1985). HPLC determn of enantiomers in plasma and urine: T. Suzuki et al., J. Chromatogr. 619, 267 (1993). Clinical evaluation in angina: R. S. Kohli et al., Eur. Heart J. 6, 845 (1985); in hypertension: F. R. Bühler et al., J. Cardiovasc. Pharmacol. 8, Suppl. 11, S122 (1986). Review of pharmacokinetics: J. Grevel et al., Clin. Pharmacokinet. 17, 53-63 (1989); of clinical efficacy in combination with hydrochlorothiazide: P. K. Zachariah et al., Clin. Ther. 15, 779-787 (1993). Clinical trial in chronic heart failure: CIBIS-II Investigators, Lancet 353, 9 (1999).
Derivative Type: Hemifumarate
CAS Registry Number: 104344-23-2
Trademarks: Concor (Merck KGaA); Detensiel (Merck-Cl¢enot); Emconcor (Merck KGaA); Emcor (Merck KGaA); Euradal (Lacer); Isoten (Lederle); Monocor (Am. Cyanamid); Soprol (Lederle); Zebeta (Lederle)
Molecular Formula: C18H31NO4.½C4H4O4
Molecular Weight: 383.48
Percent Composition: C 62.64%, H 8.67%, N 3.65%, O 25.03%
Properties: Crystals, mp 100°. Sol in ethanol.
Melting point: mp 100°
Derivative Type: Mixture with hydrochlorothiazide
Trademarks: Ziac (Am. Cyanamid)
Therap-Cat: Antihypertensive.
Keywords: ?Adrenergic Blocker; Antihypertensive; Aryloxypropanolamine Derivatives. |