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Antiarrhythmic activity of some xanthone derivatives with β1-adrenoceptor affinities in rats.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 2014 Sep 05; Vol. 738, pp. 14-21. Date of Electronic Publication: 2014 May 27. - Publication Year :
- 2014
-
Abstract
- A series of aminoalkanolic derivatives of xanthone with high affinity for β1-adrenoceptors was evaluated for antiarrhythmic activity in the model of ischemia-reperfusion in isolated hearts, as well as in barium chloride- and adrenaline-induced model of arrhythmia. In order to better understand biological activity of studied compounds, the influence on β2-adrenoceptors in guinea-pig trachea and vasorelaxant properties in rat aorta were evaluated. Furthermore, due to assessed antioxidant activity, some biochemical studies were also performed. All tested compounds showed prominent antiarrhythmic activity in the model of ventricular arrhythmias associated with coronary artery occlusion and reperfusion. In this experiment the most active was compound MH-97. Whereas, compound MH-82 was the most active in barium- and adrenaline-induced arrhythmia after i.v. or p.o. administration, respectively. These two compounds have higher affinity to β1-adrenoceptors than compound MH-87, thus it suggests that blocking properties of β1-adrenoceptors are involved in the observed antiarrhythmic effects. All studied compounds have revealed antagonistic potency for β2-adrenoceptors in tracheal smooth muscle, however weaker than that of propranolol. None of tested compounds demonstrated antioxidant effect. They also had weak calcium entry blocking activity. The results of this study suggest that new compounds with antiarrhythmic activity might be found in the group of xanthone derivatives.<br /> (Copyright © 2014 Elsevier B.V. All rights reserved.)
- Subjects :
- Animals
Anti-Arrhythmia Agents chemistry
Anti-Arrhythmia Agents therapeutic use
Antioxidants chemistry
Antioxidants therapeutic use
Arrhythmias, Cardiac drug therapy
Arrhythmias, Cardiac physiopathology
Atenolol pharmacology
Barium Compounds pharmacology
Chlorides pharmacology
Epinephrine adverse effects
Guinea Pigs
Heart drug effects
Heart physiopathology
Lipid Peroxidation drug effects
Male
Mice
Propranolol pharmacology
Protein Binding
Rats
Reperfusion Injury physiopathology
Trachea drug effects
Trachea physiology
Vasoconstriction drug effects
Vasodilation drug effects
Xanthones chemistry
Xanthones therapeutic use
Anti-Arrhythmia Agents metabolism
Anti-Arrhythmia Agents pharmacology
Antioxidants metabolism
Antioxidants pharmacology
Receptors, Adrenergic, beta-1 metabolism
Xanthones metabolism
Xanthones pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1879-0712
- Volume :
- 738
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 24876055
- Full Text :
- https://doi.org/10.1016/j.ejphar.2014.05.032