Home Neuronal Signaling Adrenergic Receptor antagonist Acebutolol HCl For research use only.

Acebutolol HCl

Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.

Acebutolol HCl Chemical Structure

Acebutolol HCl Chemical Structure

CAS No. 34381-68-5

Purity & Quality Control

Acebutolol HCl Related Products

Signaling Pathway

Adrenergic Receptor Signaling Pathways

Adrenergic Receptor Signaling Pathway

Biological Activity

Description Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
Features Acebutolol has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action.
Targets
β-adrenergic receptor [1]
In vitro
In vitro Acebutolol inhibits NA uptake in rat brain P2 fractions with IC50 of 0.25 mM. [1] Acebutolol produces a concentration-dependent inhibition of 125I-labeled CYP binding to human fat cell membranes and are able to completely displace all specifically bound radioligand. Acebutolol totally inhibits lipolytic activity initiated by 1 μM isoproterenol. Acebutolol is a cardioselective antagonist possessing low lipid solubility. [2] Acebutolol, which does not bind to LDL, shows a stronger inhibiting effect on the intracellular accumulation of cholesterol esters in J774 macrophages than alprenolol and oxprenolol which bind to LDL. [3]
In Vivo
In vivo 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. [4] 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. [5]
Animal Research Animal Models Sprague–Dawley rats
Dosages 10 mg/kg
Administration Intravenously
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01514019 Completed
Healthy
In-Jin Jang MD PhD|Oita University|Seoul National University Hospital|Kyushu University
 January 2012 Phase 4

Chemical Information & Solubility

Molecular Weight 372.89 Formula

C18H28N2O4.HCl

 
CAS No. 34381-68-5 SDF Download Acebutolol HCl SDF
Smiles CCCC(=O)NC1=CC(=C(C=C1)OCC(CNC(C)C)O)C(=O)C.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (198.44 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 74 mg/mL

Ethanol : 74 mg/mL


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In vivo
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