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MedChemExpressModel Acebutolol hydrochloride - 34381-68-5

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Acebutolol hydrochloride is an orally active β1 adrenergic receptor (β1AR) antagonist. Acebutolol hydrochloride is used in the treatment of hypertension, angina pectoris and cardiac arrhythmias[1][2][3].
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Acebutolol hydrochloride

MCE China:Acebutolol hydrochloride

Brand:MedChemExpress (MCE)

Cat. No.HY-17497A

CAS:34381-68-5

Purity:99.63%

Storage:4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Acebutolol hydrochloride is an orally active β1 adrenergic receptor (β1AR) antagonist. Acebutolol hydrochloride is used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.

In Vivo:Acebutolol is a beta blocker for the treatment of hypertension and arrhythmias. Acebutolol following single intravenous administration (10 mg/kg) to rat results in the plasma clearance of 61.9 mL/min/kg, the volume of distribution of 9.6 L/kg, and an elimination half-life of 1.8 hours. Acebutolol following single intravenous administration (50 mg/kg) to rat results in the plasma clearance of 46.5 mL/min/kg, the volume of distribution of 9.5 L/kg, and an elimination half-life of 2.3 hours[1]. Acebutolol (30 mg/kg) decreases cardiac output by 65% and 31% after 1 min and 10 min measurements, respectively, in Sprague-Dawley rats. Acebutolol (30 mg/kg) significantly reduces regional blood flow (RBF) in most organs either after 1 min or 10 min measurements when compare with the baseline values in Sprague-Dawley rats[3].

IC50 & Target:β1 adrenoceptor

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References:

[1]. Piquette-Miller, M. and F. Jamali, Pharmacokinetics and multiple peaking of acebutolol enantiomers in rats. Biopharm Drug Dispos, 1997. 18(6): p. 543-56.  [Content Brief]

[2]. Bristow MR, et al. Treatment of chronic heart failure with β-adrenergic receptor antagonists: a convergence of receptor pharmacology and clinical cardiology. Circ Res. 2011 Oct 28;109(10):1176-94.  [Content Brief]

[3]. Mostafavi, S., R. Lewanczuk, and R. Foster, Influence of acebutolol and metoprolol on cardiac output and regional blood flow in rats. Biopharm Drug Dispos, 2000. 21(4): p. 121-8.  [Content Brief]

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