References of 5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1H-quinolin-2-one
Title: Carteolol
CAS Registry Number: 51781-06-7
CAS Name: 5-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]-3,4-dihydro-2(1
H)-quinolinone
Synonyms: 5-[3-(
tert-butylamino)-2-hydroxypropoxy]-3,4-dihydrocarbostyril
Molecular Formula: C16H24N2O3
Molecular Weight: 292.37
Percent Composition: C 65.73%, H 8.27%, N 9.58%, O 16.42%
Literature References: b-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).
Derivative Type: Hydrochloride
CAS Registry Number: 51781-21-6
Manufacturers' Codes: Abbott 43326; OPC-1085
Trademarks: Arteoptic (Novartis); Carteol (Otsuka); Endak (Madaus); Mikelan (Otsuka); Ocupress (Novartis); Teoptic (Novartis)
Molecular Formula: C16H24N2O3.HCl
Molecular Weight: 328.83
Percent Composition: 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).
Melting point: mp 278°
Toxicity data: LD50 in male mice, rats (mg/kg): 810, 1380 orally; 54.5, 158 i.v.; 380, 400 i.p. (Lang)
Therap-Cat: Antihypertensive; antianginal; antiarrhythmic; antiglaucoma.
Keywords: ?Adrenergic Blocker; Antianginal; Antiarrhythmic; Antiglaucoma; Antihypertensive; Aryloxypropanolamine Derivatives.