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Title: Antiarrhythmic and hypotensive properties of new xanthone derivatives with adrenolytic activity
Abstract:
The aim of this work was to study antiarrhythmic and/or hypotensive properties of 17 new xanthone derivatives, to explain the mechanism of action of the most active compounds and also to investigate the relationship between structure and affinity for adrenoceptors, antiarrhythmic and/or antihypertensive activity. This work is a continuation of the research carried out for many years into chemical-pharmacological activity of xanthone derivatives. In the preliminary pharmacological studies, which included determination of affinity for α1-, α2-, β1-adrenoceptors, antiarrhythmic activity in the model of adrenaline-induced arrhythmia and hypotensive activity, six of the most active compounds were selected.Extended studies confirmed a high α1- or β1- adrenolytic activity (in vivo and in vitro tests), showed a prominent antiarrhythmic activity in arrhythmia induced by occlusion and reperfusion of coronary artery and for some compounds antiarrhythmic and hypotensive after p.o. administration. Pharmacological in vitro and in vivo studies showed a high correlation between the affinity for α1- and β1-adrenoceptors and antiarrhythmic activity in the model of adrenaline-induced arrhythmia and also for α1-adrenoceptors and hypotensive activity. The analysis of the structure-activity relationship showed that the highest pharmacological activity had compounds with a group of aminopropanol in p ; osition 4 of the xanthone core and compounds with 2-methoxyphenylpiperazine moiety.
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Last modified:
Mar 17, 2023
In our library since:
Mar 8, 2013
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64
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All available object's versions:
http://dl.cm-uj.krakow.pl:8080/publication/3465
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| Edition name | Date |
|---|---|
| ZB-116990 | Mar 17, 2023 |
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