1182. Betaxolol

Nomenclature

CAS number: 63659-18-7
1-[4-[2-(Cyclopropylmethoxy)ethyl]-phenoxy]-3-[(1-methylethyl)amino]-2-propanol; (±)-1-(isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol.
C18H29NO3; mol wt 307.43.
C 70.32%, H 9.51%, N 4.56%, O 15.61%.

Description and references

Cardioselective β1-adrenergic blocker. Prepn: P. M. J. Manoury et al., DE 2649605; eidem, US 4252984 (1977, 1981 both to Synthelabo). Blood concn and pharmacodynamic effects: S. J. Warrington et al., Br. J. Clin. Pharmacol. 10, 449 (1980). Pharmacokinetics: G. Bianchetti et al., Arzneim.-Forsch. 30, 1912 (1980). Cardiovascular effects in normal volunteers: P. J. Cadigan et al., Br. J. Clin. Pharmacol. 9, 569 (1980). Efficacy and pharmacokinetics: K. Balnave et al., ibid. 11, 171 (1981). Use in treatment of glaucoma: A. R. Berrospi, H. M. Leibowitz, Arch. Ophthalmol. 100, 943 (1982). Antihypertensive effect: M. Pathe et al., Therapie 37, 75 (1982). Book: Betaxolol and Other β1-Adrenoceptor Antagonists, P. L. Morselli et al., Eds. (Raven Press, New York, 1983) 385 pp.

Chemical structure

Properties

Crystals from petr ether, mp 70-72°.

Derivative

Hydrochloride.

Nomenclature

CAS number: 63659-19-8
SLD-212; SL-75.212; Betoptic (Alcon); Betoptima (Alcon); Kerlone (Synthelabo).
C18H29NO3.HCl; mol wt 343.89.
C 62.87%, H 8.79%, N 4.07%, O 13.96%, Cl 10.31%.

Properties

Crystals from acetone, mp 116°. LD50 in mice (mg/kg): 944 orally; 37 i.v. (Manoury).

Therapeutic Category

Antihypertensive; antiglaucoma.

Keywords

β-Adrenergic Blocker; Antiglaucoma; Antihypertensive; Aryloxypropanolamine Derivatives