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

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 alpha-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 Km value than 17-acetylajmaline, which is in agreement with the in vivo activity.

journal_name

J Pharm Sci

authors

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

doi

10.1002/jps.2600640933

subject

Has Abstract

pub_date

1975-09-01 00:00:00

pages

1561-3

issue

9

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)40406-X

journal_volume

64

pub_type

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