CARVEDILOL-D5

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.

Chemical Properties

White Solid

Uses

Carvedilol-d5 is the labelled analog of Carvedilol, a nonselective β-adrenergic blocker with α1-blocking activity. Carvedilol is an antihypertensive used in the treatment of congestive heart failure.

Uses

Labeled Carvedilol, intended for use as an internal standard for the quantification of Carvedilol by GC- or LC-mass spectrometry.

References

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[3] M TANAKA. Studies on the antihypertensive properties of carvedilol, a compound with beta-blocking and vasodilating effects.[J]. Journal of Cardiovascular Pharmacology, 1987, 10 Suppl 11: S52-7.
[4] JAMES W WISLER. A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2007, 104 42: 16657-16662. DOI: 10.1073/pnas.0707936104
[5] ISLAM A.A.E.-H. IBRAHIM  Hitoshi K. β-Arrestin-Mediated Signaling Improves the Efficacy of Therapeutics[J]. Journal of pharmacological sciences, 2012, 118 4: Pages 408-412. DOI: 10.1254/jphs.11r10cp
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