product name Acebutolol HCl
Description: Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias. 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.
References: J Lipid Res. 1988 May;29(5):587-601; Biopharm Drug Dispos. 1997 Aug;18(6):543-56.
372.89
Formula
C18H28N2O4.HCl
CAS No.
34381-68-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 75 mg/mL (201.1 mM)
Water:
Ethanol: 75 mg/mL (201.1 mM)
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397859
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | Sprague–Dawley rats |
| Formulation & Dosage | Dissolved in saline; 10 mg/kg; i.v. injection |
| References | J Lipid Res. 1988 May;29(5):587-601; Biopharm Drug Dispos. 1997 Aug;18(6):543-56. |
Related Posts
product name Acebutolol HCl
Description: Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias. 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.
References: J Lipid Res. 1988 May;29(5):587-601; Biopharm Drug Dispos. 1997 Aug;18(6):543-56.
372.89
Formula
C18H28N2O4.HCl
CAS No.
34381-68-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 75 mg/mL (201.1 mM)
Water:
Ethanol: 75 mg/mL (201.1 mM)
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19397859
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | Sprague–Dawley rats |
| Formulation & Dosage | Dissolved in saline; 10 mg/kg; i.v. injection |
| References | J Lipid Res. 1988 May;29(5):587-601; Biopharm Drug Dispos. 1997 Aug;18(6):543-56. |