Abstract
The current paper presents research results related to antiarrhythmic activity of halogen-containing derivatives of lappaconitine. Lappaconitine derivatives with iodine, chlorine or bromine substituting the anthranilate moiety at C-5` position were shown in vivo and in vitro to exhibit a more (Br, I) or less (Cl) pronounced antiarrhythmic activity in the models of calcium chloride- and adrenaline-induced arrhythmias as compared with the reference compound lappaconitine. The intensity of antiarrhythmic action depending on halogen substituent was found to be expressed by the following order: Cl < I < Br.
Keywords: Arrhythmia, lappaconitine, halogen-containing lappaconitine derivatives.
Cardiovascular & Hematological Agents in Medicinal Chemistry
Title:Lappaconitine: Influence of Halogen Substituent on the Antiarrhythmic Activity
Volume: 11 Issue: 3
Author(s): A. O. Bryzgalov, V. E. Romanov, T. G. Tolstikova and E. E. Shults
Affiliation:
Keywords: Arrhythmia, lappaconitine, halogen-containing lappaconitine derivatives.
Abstract: The current paper presents research results related to antiarrhythmic activity of halogen-containing derivatives of lappaconitine. Lappaconitine derivatives with iodine, chlorine or bromine substituting the anthranilate moiety at C-5` position were shown in vivo and in vitro to exhibit a more (Br, I) or less (Cl) pronounced antiarrhythmic activity in the models of calcium chloride- and adrenaline-induced arrhythmias as compared with the reference compound lappaconitine. The intensity of antiarrhythmic action depending on halogen substituent was found to be expressed by the following order: Cl < I < Br.
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Bryzgalov O. A., Romanov E. V., Tolstikova G. T. and Shults E. E., Lappaconitine: Influence of Halogen Substituent on the Antiarrhythmic Activity, Cardiovascular & Hematological Agents in Medicinal Chemistry 2013; 11 (3) . https://dx.doi.org/10.2174/18715257113119990083
DOI https://dx.doi.org/10.2174/18715257113119990083 |
Print ISSN 1871-5257 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6182 |
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