科研之友
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摘要
A series of aminoalkanolic derivatives of xanthone with high affinity for beta(1)-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 beta(2)- 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 beta(1)-adrenoceptors than compound MH-87, thus it suggests that blocking properties of beta(1)-adrenoceptors are involved in the observed antiarrhythmic effects. All studied compounds have revealed antagonistic potency for beta(2)-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.
- 出版日期2014-9-5
