Solification with Hydrobromic Acid as a Factor Defining the Antiarrhythmic Effect of Lappaconitine Derivatives

Author(s): T. G. Tolstikova, A. O. Bryzgalov, I. V. Sorokina, S. A. Osadchii, E. E. Shults, M. P. Dolgikh, M. V. Khvostov

Journal Name: Letters in Drug Design & Discovery

Volume 6 , Issue 7 , 2009


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Abstract:

Alkaloid lappaconitine (I) and its derivatives – N(20)-deethyllappaconitine (II) and 5-bromolappaconitine (III) in the base form and as salts - hydrochloride (I • HCl), hydrobromide (preparation allapinine) (I • HBr), hydrobromide (II • HBr), hydrobromide (III • HBr), succinate (I • Suc) were taken for research of pharmacology activity. Moreover, pharmacology activity was investigated for a clathrates of lappaconitine – the bases, hydrochloride and hydrobromide with glycyrrhizic acid (IV) (I-IV; I • HCl-IV; I • HBr-IV). It is shown that, neither the base nor the salts, with the exception for hydrobromide, possess antiarrhythmic action on any of the models. Among glycyrrhizic acid clathrates, only the clathrate with hydrobromide of lappaconitine (I • HBr-IV) has a high activity on the two models of arrhythmia.

Keywords: Antiarrhythmic agent, Lappaconitine compounds, Clathrate

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Article Details

VOLUME: 6
ISSUE: 7
Year: 2009
Page: [475 - 477]
Pages: 3
DOI: 10.2174/157018009789108312
Price: $65

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