6264. Moprolol
Nomenclature
Description and references
β-Adrenergic blocker. Prepn: C. D. Lunsford et al., J. Am. Chem. Soc. 82, 1166 (1960); NL 301580 corresp to A. F. Crowther, L. H. Smith, US 3501769 (1965, 1970 both to ICI); A. F. Crowther et al., J. Med. Chem. 12, 638 (1969). Pharmacology: G. Croce et al., Arzneim.-Forsch. 20, 1074 (1970). Anti-anginal and hemodynamic effects: M. Radice et al., ibid. 28, 2160 (1978). Resolution of enantiomers: G. Ferrari, V. Vecchietti, EP 15418; eidem, US 4683245 (1980, 1987 both to Simes). Synthesis of (-)-form: K. Kan et al., Agric. Biol. Chem. 49, 207 (1985). Bioavailability of (-)-form in dog: A. Marzo, J. P. Desager, Curr. Ther. Res. 30, 442 (1981). Pharmacokinetics of racemate and (-)-form: C. Harvengt, J. P. Desager, Int. J. Clin. Pharmacol. Ther. Toxicol. 20, 57 (1982). Clinical comparison of antihypertensive activity of enantiomers: P. Ghirardi, F. Grosso, J. Cardiovasc. Pharmacol. 2, 471 (1980). Clinical studies of (-)-form in hypertension: G. Vrebos et al., Curr. Ther. Res. 29, 654 (1981); H. Hoeffkes, ibid. 30, 88 (1981).
Properties
Crystals from cyclohexane, mp 82-83°.Derivative
Hydrochloride.Nomenclature
Properties
Crystals, mp 110-112°.Derivative
l-Form.Nomenclature
Properties
Crystals from ethyl acetate, mp 78-80°. [α] -5.5 ±0.2° (c = 5.0 in ethanol).Derivative
l-Form hydrochloride.Nomenclature
Properties
Crystals from ethyl acetate/95% ethanol, mp 121-123°. [α]D25 -16.3° (c = 5.0 in ethanol).Therapeutic Category
Antihypertensive.
Keywords
β-Adrenergic Blocker; Antihypertensive; Aryloxypropanolamine Derivatives