1866. Carteolol

Nomenclature

CAS number: 51781-06-7
5-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]-3,4-dihydro-2(1H)-quinolinone; 5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydrocarbostyril.
C16H24N2O3; mol wt 292.37.
C 65.73%, H 8.27%, N 9.58%, O 16.42%.

Description and references

β-Adrenergic blocker. Prepn: K. Nakagawa et al., DE 2302027; Y. Tamura et al., US 3910924 (1973, 1975 both to Otsuka); K. Nakagawa, J. Med. Chem. 17, 529 (1974). Pharmacological evaluation in rats: S. Morita et al., Biochem. Pharmacol. 25, 1836 (1976). HPLC determn in plasma and urine: S. Y. Chu, J. Pharm. Sci. 67, 1623 (1978). In vitro study: S. Chiba, Arzneim.-Forsch. 29, 895 (1979). Carcinogenicity study: M. Kurosomi et al., Farmaco Ed. Prat. 34, 202 (1979). Series of articles on pharmacology, toxicology and clinical studies: Arzneim.-Forsch. 33, 277-345 (1983). Acute toxicity data: W. Lang, ibid. 290. Review of clinical experience in glaucoma and ocular hypertension: P. Chrisp, E. M. Sorkin, Drugs Aging 2, 58-77 (1992).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 51781-21-6
Abbott 43326; OPC-1085; Arteoptic (Novartis); Carteol (Otsuka); Endak (Madaus); Mikelan (Otsuka); Ocupress (Novartis); Teoptic (Novartis).
C16H24N2O3.HCl; mol wt 328.83.
C 58.44%, H 7.66%, N 8.52%, O 14.60%, Cl 10.78%.

Properties

Crystals from ethanol, mp 278°. LD50 in male mice, rats (mg/kg): 810, 1380 orally; 54.5, 158 i.v.; 380, 400 i.p. (Lang).

Therapeutic Category

Antihypertensive; antianginal; antiarrhythmic; antiglaucoma.

Keywords

β-Adrenergic Blocker; Antianginal; Antiarrhythmic; Antiglaucoma; Antihypertensive; Aryloxypropanolamine Derivatives