9438. Tilisolol
Nomenclature
CAS number: 85136-71-6
4-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]-2-methyl-1(2H)-isoquinolinone; 4-[3-(tert-butylamino)-2-hydroxypropoxy]-N-methylisocarbostyril. C17H24N2O3; mol wt 304.38.
C 67.08%, H 7.95%, N 9.20%, O 15.77%.
Description and references
β-Adrenergic blocker. Prepn: H. Fukushima, Y. Suzuki, DE 2631080; eidem, US 4129565 (1977, 1978 both to Nisshin). Antiarrhythmic activity: K. Hashimoto et al., J. Pharmacol. Exp. Ther. 223, 801 (1982); and pharmacological profile: Y. Nakagawa et al., Arzneim.-Forsch. 34, 194 (1984). Receptor binding study: T. Nagatomo et al., Jpn. J. Pharmacol. 34, 249 (1984). Vasodilating activity in humans: T. Imaizumi et al., Arzneim.-Forsch. 38, 1342 (1988). HPLC determn in plasma: K. Yonezawa et al., J. Chromatogr. 339, 219 (1985). Toxicity data: S. Kawase et al., Oyo Yakuri 34, 499 (1987), C.A. 108, 161293m (1988).
Derivative
Hydrochloride.Nomenclature
CAS number: 62774-96-3
N-696; Selecal (Toyama). C17H24N2O3.HCl; mol wt 340.85.
C 59.90%, H 7.39%, N 8.22%, O 14.08%, Cl 10.40%.
Properties
White crystals from ethyl acetate, mp 203-205°. LD50 in male, female mice and rats (mg/kg): 1393, 1290, 145, 188 orally; 1219, 1245, 176, 169 s.c.; 578, 557, 39.5, 29.2 i.p.; 74.3, 104.7, 75.8, 38.1 i.v. (Kawase).Therapeutic Category
Antiarrhythmic; antihypertensive.
Keywords
β-Adrenergic Blocker; Antiarrhythmic; Antihypertensive; Aryloxypropanolamine Derivatives