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Pharmacological evaluation of natural product analogues. I. Preliminary pharmacological evaluation of O‐methylgortschakoine and O‐methylpetaline
Author(s) -
AlAzizi M. M.,
ElOlemy M. M.,
AlHarbi M. M.
Publication year - 1992
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.2650060412
Subject(s) - papaverine , muscle relaxant , blocking (statistics) , pharmacology , chemistry , neuromuscular blocking agents , muscle relaxation , natural product , smooth muscle , medicine , stereochemistry , anesthesia , statistics , mathematics
The synthesis of O‐methylgortschakoine and O‐methylpetaline was achieved through an unambiguous route. Pharmacological testing of O‐methylgortschakoine in comparison to papaverine and 7,8‐dimethoxy‐N‐methyltetrahydroisoquinoline, indicated that it possesses hypotensive, neuromuscular blocking and smooth muscle relaxant activities. 7,8‐Dimethoxy‐N‐methyltetrahydroisoquinoline showed only nonspecific smooth muscle relaxation in our testing system. The 1‐( p ‐methoxybenzyl)‐substituent of O‐methylgortschakoine appears to be required for this hypotensive and neuromuscular blocking effect. The quaternary analogue O‐melthylpetaline was found to possess a more potent neuromuscular blocking activity.