Lappaconitine: Influence of Halogen Substituent on the Antiarrhythmic Activity
Cardiovascular & Hematological Agents in Medicinal Chemistry,
A. O. Bryzgalov, V. E. Romanov, T. G. Tolstikova and E. E. ShultsAffiliation:
Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Sciences, 9 Prosp. Akad. Lavrent`eva, 630090 Novosibirsk, Russian Federation.
AbstractThe 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.
Arrhythmia, lappaconitine, halogen-containing lappaconitine derivatives.
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