CARVEDILOL-D5

Properties

Safety Information

Description

Carvedilol-d₅ is intended for use as an internal standard for the quantification of carvedilol by GC- or LC-MS. Carvedilol is a non-selective antagonist of the β-adrenergic receptor (β-AR; K_ds = 1.78, 0.4, and 5.01 nM for β₁-, β₂-, and β₃-ARs, respectively). It also binds to α₁-, but not α₂-, adrenergic receptors (K_is = 0.81 and 3,400 nM, respectively). Carvedilol reverses increases in heart rate induced by the β₁-AR agonist isoproterenol in isolated guinea pig atria (K_b = 0.8 nM) and induces relaxation of isolated precontracted guinea pig trachea (K_b = 1.3 nM). It prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia with an ED₅₀ value of 0.25 mg/kg. Carvedilol also inhibits the contractile response to the α₁-AR agonist norepinephrine in isolated rabbit aorta (K_b = 11 nM). It decreases systolic blood pressure and heart rate in rat models of hypertension, including spontaneously hypertensive, renal hypertensive, and deoxycorticosterone acetate-treated rats when administered at doses ranging from 3 to 30 mg/kg. Carvedilol also activates cardioprotective signaling through β-arrestin and ERK1/2 activation. Formulations containing carvedilol have been used in the treatment of congestive heart failure and hypertension.