research use only
Cat.No.S4010
| Related Targets | AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR |
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| Other Adrenergic Receptor Inhibitors | Zenidolol (ICI-118551) Hydrochloride L755507 Yohimbine HCl Atipamezole Higenamine hydrochloride Detomidine HCl Naftopidil Demethyl-Coclaurine Buflomedil HCl Fenoterol hydrobromide |
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In vitro |
DMSO
: 74 mg/mL
(198.44 mM)
Water : 74 mg/mL Ethanol : 74 mg/mL |
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In vivo |
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| Molecular Weight | 372.89 | Formula | C18H28N2O4.HCl |
Storage (From the date of receipt) | |
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| CAS No. | 34381-68-5 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | CCCC(=O)NC1=CC(=C(C=C1)OCC(CNC(C)C)O)C(=O)C.Cl | ||
| Features |
Acebutolol has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action.
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| Targets/IC50/Ki |
β-adrenergic receptor
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| In vitro |
Acebutolol inhibits NA uptake in rat brain P2 fractions with IC50 of 0.25 mM. 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. 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.
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| 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. 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.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| 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 |
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