1873. Carvedilol

Nomenclature

CAS number: 72956-09-3
1-(9H-Carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol; BM-14190; DQ-2466; Coreg (GSK); Dilatrend (Roche); Dimitone (Erco); Eucardic (Roche); Kredex (GSK); Querto (Byk Gulden).
C24H26N2O4; mol wt 406.47.
C 70.92%, H 6.45%, N 6.89%, O 15.74%.

Description and references

Nonselective β-adrenergic blocker with α1-blocking activity. Prepn: F. Wiedemann et al., DE 2815926; eidem, US 4503067 (1979, 1985 both to Boehringer Mannheim). General pharmacological profile: M. Hirohashi et al., Arzneim.-Forsch. 40, 735 (1990). HPLC determn in biological fluids: K. Reiff, J. Chromatogr. 413, 355 (1987). Series of articles on clinical pharmacology and efficacy in hypertension: J. Cardiovasc. Pharmacol. 19, Suppl. 1, S1-S146 (1992). Clinical trial in chronic heart failure: M. Packer et al., N. Engl. J. Med. 334, 1349 (1996). Review: W. H. Frishman, ibid. 339, 1759-1765 (1998).

Chemical structure

Properties

Colorless crystals from ethyl acetate, mp 114-115°. Freely sol in DMSO; sol in methylene chloride, methanol; sparingly sol in ethanol, isopropanol; slightly sol in ethyl ether. Practically insol in water.

Therapeutic Category

Antihypertensive; in treatment of congestive heart failure.

Keywords

β-Adrenergic Blocker; Antihypertensive; Aryloxypropanolamine Derivatives