A non-selective β-adrenergic receptor antagonist (Kds = 1.78

Carvedilol – 250 mg

Brand:
Cayman
CAS:
72956-09-3
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Carvedilol is a non-selective antagonist of the β-adrenergic receptor (β-AR; Kds = 1.78, 0.4, and 5.01 nM for β1-, β2-, and β3-ARs, respectively).{25151} It also binds to α1-, but not α2-, adrenergic receptors (Kis = 0.81 and 3,400 nM, respectively).{25150} Carvedilol reverses increases in heart rate induced by the β1-AR agonist isoproterenol (Item No. 15592) in isolated guinea pig atria (Kb = 0.8 nM) and induces relaxation of isolated precontracted guinea pig trachea (Kb = 1.3 nM).{43226} It prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia with an ED50 value of 0.25 mg/kg.{25150} Carvedilol also inhibits the contractile response to the α1-AR agonist norepinephrine in isolated rabbit aorta (Kb = 11 nM).{43226} 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.{43227} Carvedilol also activates cardioprotective signaling through β-arrestin and ERK1/2 activation.{25152,25153,23372} Formulations containing carvedilol have been used in the treatment of congestive heart failure and hypertension.  

 

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Description

A non-selective β-adrenergic receptor antagonist (Kds = 1.78, 0.4, and 5.01 nM for β1-, β2-, and β3-ARs, respectively); also binds to α1-, but not α2-, adrenergic receptors (Kis = 0.81 and 3,400 nM, respectively); reverses increases in heart rate induced by isoproterenol in isolated guinea pig atria (Kb = 0.8 nM); induces relaxation of isolated precontracted guinea pig trachea (Kb = 1.3 nM); prevents epinephrine-induced premature ventricular beats in a rat model of arrhythmia (IC50 = 0.25 mg/kg); inhibits the contractile response to norepinephrine in isolated rabbit aorta (Kb = 11 nM); decreases systolic blood pressure and heart rate in rat models of hypertension at 3-30 mg/kg

Formal name: 1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol

Synonyms:  BM 14190

Molecular weight: 406.5

CAS: 72956-09-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cardiovascular System|Vasculature|Vasodilation

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