Title: Indenolol
CAS Registry Number: 60607-68-3
CAS Name: 1-[1H-Inden-4(or 7)-yloxy]-3-[(1-methylethyl)amino]-2-propanol
Additional Names: (±)-1-[inden-4(or 7)-yloxy]-3-(isopropylamino)-2-propanol
Manufacturers' Codes: YB-2; Sch-28316Z
Molecular Formula: C15H21NO2
Molecular Weight: 247.33
Percent Composition: C 72.84%, H 8.56%, N 5.66%, O 12.94%
Literature References: Non-selective b-adrenergic blocker. Prepn: M. Murakami et al., DE 1955229; eidem, US 4045482 (1970, 1977 both to Yamanouchi); K. Murase et al., Yakugaku Zasshi 92, 1358 (1972), C.A. 78, 71723 (1973). Indenolol is a tautomeric mixture of the 7- and 4-indenyloxy isomers in a 2:1 ratio, respectively. Unambiguous synthesis of the two isomers: eidem, Chem. Pharm. Bull. 24, 552 (1976). b-Blocking and cardiovascular properties: T. Takenaka, S. Tachikawa, Arzneim.-Forsch. 22, 1864 (1972). General pharmacology: M. Takeda et al., Oyo Yakuri 7, 469 (1973), C.A. 80, 44015 (1974). Comparative pharmacological study with other b-blockers: W. Bartsch et al., Arzneim.-Forsch. 27, 1022 (1977). Dose-response studies: F. E. Okupa et al., Clin. Pharmacol. Ther. 29, 434 (1981). Pharmacokinetics: R. Sega et al., J. Clin. Pharmacol. 25, 337 (1985). Clinical evaluation in hypertension: B. Trimarco et al., ibid. 328; L. Poggesi et al., Clin. Pharmacol. Ther. 41, 344 (1987).
Properties: Crystals from n-hexane/ether, mp 88-89°.
Melting point: mp 88-89°
Derivative Type: Hydrochloride
CAS Registry Number: 81789-85-7
Trademarks: Pulsan (Yamanouchi); Securpres (Poli)
Molecular Formula: C15H21NO2.HCl
Molecular Weight: 283.79
Percent Composition: C 63.48%, H 7.81%, N 4.94%, O 11.28%, Cl 12.49%
Properties: Crystals from ethanol/ether, mp 147-148°. LD50 in mice: 26 mg/kg i.v. (Bartsch).
Melting point: mp 147-148°
Toxicity data: LD50 in mice: 26 mg/kg i.v. (Bartsch)
Therap-Cat: Antihypertensive, antiarrhythmic, antianginal.
Keywords: ?Adrenergic Blocker; Antianginal; Antiarrhythmic; Antihypertensive; Aryloxypropanolamine Derivatives. |