9038. Talinolol

Nomenclature

CAS number: 57460-41-0
N-Cyclohexyl-N′-[4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]phenyl]urea; 1-(4-cyclohexylureidophenoxy)-2-hydroxy-3-tert-butylaminopropane; (±)-1-[p-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-3-cyclohexylurea; 02-115; Cordanum (AWD).
C20H33N3O3; mol wt 363.49.
C 66.09%, H 9.15%, N 11.56%, O 13.20%.

Description and references

Selective β1-adrenergic blocker structurally related to practolol, q.v. Prepn: R. Eckardt et al., DE 2153024 (1972 to Arzneimittelwerke VEB), C.A. 77, 61639b (1972); idem et al., Pharmazie 30, 633 (1975). Series of articles on pharmacology, toxicology: ibid. 638-683. Acute toxicity: K. Femmer et al., ibid. 642. Clinical pharmacokinetics and bioavailability: B. Trausch et al., Biopharm. Drug Dispos. 16, 403 (1995). Review of clinical experience: I. Assmann, Curr. Med. Res. Opin. 13, 325-342 (1995).

Chemical structure

Properties

Cryst from isopropanol, mp 142-144°. LD50 in rats, mice (mg/kg): 1180, 593 orally; 54.3, 74.7 i.p.; 29.7, 25.0 i.v. (Femmer).

Therapeutic Category

Antihypertensive; antiarrhythmic.

Keywords

β-Adrenergic Blocker; Antiarrhythmic; Antihypertensive; Aryloxypropanolamine Derivatives