Relationship of in vitro hydrolysis of 17 chloroacetylajmaline and 17 acetylajmaline in different animal species

M. Salmona, K. Lakszner, R. Fanelli, C. Saronio, R. Bianchi, E. Mussini

Research output: Contribution to journalArticle

Abstract

17 Chloroacetylajmaline and 17 acetylajmaline are reported to have in vivo antiarrhythmic activity and are metabolized by hydrolysis. Since the hydrolysis product, ajmaline, may be the actual antiarrhythmic agent, the hydrolysis of these derivatives by various tissues of the guinea pig, rat, and mouse was determined in vitro by a titrimetric method and compared to hydrolysis by α naphthylacetate. The heart is the most active tissue in the guinea pig for hydrolyzing 17 chloroacetylajmaline. The hydrolyzing activity is greater in the guinea pig than in rat or mouse heart, corresponding with the more significant pharmacological activity in the guinea pig. 17 Chloroacetylajmaline has a significantly lower K(m) value than 17 acetylajmaline, which is in agreement with the in vivo activity.

Original languageEnglish
Pages (from-to)1561-1563
Number of pages3
JournalJournal of Pharmaceutical Sciences
Volume64
Issue number9
DOIs
Publication statusPublished - 1975

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science

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