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 Scijournal_title
Journal of pharmaceutical sciencesauthors
Salmona M,Lakszner K,Fanelli R,Saronio C,Bianchi R,Mussini Edoi
10.1002/jps.2600640933subject
Has Abstractpub_date
1975-09-01 00:00:00pages
1561-3issue
9eissn
0022-3549issn
1520-6017pii
S0022-3549(15)40406-Xjournal_volume
64pub_type
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