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ID 41163
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Title Alternative
Pharmacological Studies on Dimethoxyisoquinolin Derivatives
Author
Kuroda, Akio
Jinzenji, Kei
Yamamoto, Takashi
Kondo, Kazuji
Shoda, Junzo
Abstract
Twelve members of a new series of 1-trialkylmethyl-1-6, 7-dimethoxy-3, 4-dihydroisoquinoline (D type) and eleven analogs of 1-trialkylmethyl-6, 7-dimethoxy isoquinoline (I type) were investigated for their pharmacological properties, with special reference to the toxicity and spasmolytic activity, comparing with papaverine. Along these isoquinoline, 1-methylisoquinoline, 6, 7-dimethoxyisoquinoline and their respective 3, 4-hydrogenated derivatives, were also examined for the elucidation of structure-activity relationship. All the compounds of D type produced a marked inhibitory action on the isolated rabbit intestine. The most potent members were n-tripropyl, ethyl-n-propyl-n-butyl and methyl-ethyl-n-butyl derivatives. Their spasmolytic actions on both barium and histamine contraction of the intestine exceeded those of papaverine, though the effect on acetylcholine spasm was slightly inferior. They were less toxic in mice than in the latter. The intestine inhibitory activity and toxicity of I Type compounds were both smaller than those of D type analogs. The differences between the two types seemed to be related to the solubility. Other smaller components of the papaverine structure, namely, the primitive isoquinoline derivatives were more toxic, but much less spasmolytic than papaverine. In mice toxic doses of all the compounds caused tremors, excitability and convulsions followed by a generalized central depression. Respiratory paralysis may be direct cause of death. Toxic symptoms were generally similar to those in frogs. The stimulant properties were increased by the saturation of the 3, 4-position on the isoquinoline nucleus.
Published Date
1959-09-20
Publication Title
岡山医学会雑誌
Publication Title Alternative
Journal of Okayama Medical Association
Volume
volume71
Issue
issue10-1
Publisher
岡山医学会
Publisher Alternative
Okayama Medical Association
Start Page
6223
End Page
6230
ISSN
0030-1558
NCID
AN00032489
Content Type
Journal Article
Official Url
https://www.jstage.jst.go.jp/article/joma1947/71/10-1/71_10-1_6223/_article/-char/ja/
Related Url
http://www.okayama-u.ac.jp/user/oma/
language
日本語
Copyright Holders
岡山医学会
File Version
publisher
Refereed
True
Eprints Journal Name
joma