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
Letters in Drug Design & Discovery
Title: Solification with Hydrobromic Acid as a Factor Defining the Antiarrhythmic Effect of Lappaconitine Derivatives
Volume: 6 Issue: 7
Author(s): T. G. Tolstikova, A. O. Bryzgalov, I. V. Sorokina, S. A. Osadchii, E. E. Shults, M. P. Dolgikh and M. V. Khvostov
Affiliation:
Keywords: Antiarrhythmic agent, Lappaconitine compounds, Clathrate
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.
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Tolstikova G. T., Bryzgalov O. A., Sorokina V. I., Osadchii A. S., Shults E. E., Dolgikh P. M. and Khvostov V. M., Solification with Hydrobromic Acid as a Factor Defining the Antiarrhythmic Effect of Lappaconitine Derivatives, Letters in Drug Design & Discovery 2009; 6 (7) . https://dx.doi.org/10.2174/157018009789108312
DOI https://dx.doi.org/10.2174/157018009789108312 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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