Carvedilol is a beta- and alpha1-adrenoreceptor blocker for the treatment of hypertension and congestive heart failure (CHF). The drug is metabolized by CYP2D6 (to 4'-OH and 5'-OH), CYP2C9 (to O-desmethyl), CYP1A2 (to 8-OH). It is also oxidized to 1-OH carvedilol, but the enzyme involved is not yet clear. These metabolites are useful markers for studying and monitoring the activities of cytochrome metabolizing enzymes. M4 metabolite (4'-OH), but not M2 or M5, is most likely to contribute to total beta-adrenoceptor blocking activity due to its higher potency.
Synonyms: 5'-Hydroxy carvedilol; 3-[2-[[3-(9H-Carbazol-4-yloxy)-2-hydroxypropyl]amino]ethoxy]-4-methoxyphenol; 5'-Hydroxyphenyl carvedilol; 5'-Hydroxyphenyl carvedilol; 5'-Hydroxyphenylcarvedilol; 5'-OH carvedilol; 5-Hydroxycarvedilol; 5OHC; BM-140830; Carvedilol metabolite M5
Molecular Formula: C24H26N2O5
Molecular Weight: 422.47
Linear Structural Formula: C24H26N2O5
Purity: >=95% (HPLC)
Storage: 2-8C