Celiprolol
Title: Celiprolol
CAS Registry Number: 56980-93-9
CAS Name: N¢-[3-Acetyl-4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]phenyl]-N,N-diethylurea
Additional Names: N-[3-acetyl-4-(3¢-tert-butylamino-2¢-hydroxy)propoxy]phenyl-N¢-diethylurea
Manufacturers' Codes: ST-1396
Molecular Formula: C20H33N3O4
Molecular Weight: 379.49
Percent Composition: C 63.30%, H 8.76%, N 11.07%, O 16.86%
Literature References: Cardioselective b1-adrenergic blocker. Prepn: BE 823411; G. Zölss et al., US 4034009 (1975, 1977 both to Chemie Linz). Hemodynamic effects: J. Bonelli et al., Wien. Klin. Wochenschr. 90, 350 (1978); H. Pittner, Arch. Pharmacol. 311, Suppl., 180 (1980). Series of articles on determn in biological material, pharmacology, toxicology, clinical studies: Arzneim.-Forsch. 33, 1-79 (1983). Toxicity: W. Wendtlandt, H. Pittner, ibid. 41. Symposium on pharmacology, clinical efficacy and comparison with other b-blockers: J. Cardiovasc. Pharmacol. 8, Suppl. 4, S1-S152 (1986). Comprehensive description: D. J. Mazzo et al., Anal. Profiles Drug Subs. 20, 237-301 (1991).
Properties: Crystals, mp 110-112°.
Melting point: mp 110-112°
 
Derivative Type: Hydrochloride
CAS Registry Number: 57470-78-7
Trademarks: Celectol (Sanofi-Aventis); Corliprol (Pharmacia & Upjohn); Selectol (Pharmacia)
Molecular Formula: C20H33N3O4.HCl
Molecular Weight: 415.95
Percent Composition: C 57.75%, H 8.24%, N 10.10%, O 15.39%, Cl 8.52%
Properties: White, odorless crystals, mp 197-200° (dec). Soly at ~25°C (g/100 ml): water 15.1, methanol 18.2, ethanol 1.61, chloroform 0.42. uv max (water): 231, 324 nm (E1% 652, 57); (0.01N HCl): 231, 324 nm (E1% 660, 60); (0.01N NaOH): 231, 324 nm (E1% 640, 60); (methanol): 232, 329 nm (E1% 775, 58). LD50 in male mice, rats (mg/kg): 56.2, 68.3 i.v.; 1834, 3826 orally (Wendtlandt, Pittner).
Melting point: mp 197-200° (dec)
Absorption maximum: uv max (water): 231, 324 nm (E1% 652, 57); (0.01N HCl): 231, 324 nm (E1% 660, 60); (0.01N NaOH): 231, 324 nm (E1% 640, 60); (methanol): 232, 329 nm (E1% 775, 58)
Toxicity data: LD50 in male mice, rats (mg/kg): 56.2, 68.3 i.v.; 1834, 3826 orally (Wendtlandt, Pittner)
 
Therap-Cat: Antihypertensive, antianginal.
Keywords: ?Adrenergic Blocker; Antianginal; Antihypertensive; Aryloxypropanolamine Derivatives.

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