Acylthioxanthenes: agents which selectively reduce decerebrate rigidity in the cat

A series of 2-acylthioxanthene-delta 9 (gamma)-propylamines was synthesized, and their effect of reducing the intercollicular decerebrate rigidity in the cat was evaluated. The compound exhibiting the greatest separation between the dosage that reduced rigidity and that which caused sedation was (Z)...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1980-06, Vol.23 (6), p.653-657
Main Authors: Ashton, Michael J, Chapman, Robert F, Loveless, Anthony H
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Cats
Decerebrate State - physiopathology
Infusions, Parenteral
Isomerism
Mice
Motor Activity - drug effects
Structure-Activity Relationship
Thioxanthenes - administration & dosage
Thioxanthenes - chemical synthesis
Thioxanthenes - pharmacology
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Summary:A series of 2-acylthioxanthene-delta 9 (gamma)-propylamines was synthesized, and their effect of reducing the intercollicular decerebrate rigidity in the cat was evaluated. The compound exhibiting the greatest separation between the dosage that reduced rigidity and that which caused sedation was (Z)-2-propionyl-9-[3-(dimethylamino)propylidene]thioxanthene. The separation of Z and E isomers was monitored by 1H NMR spectroscopy, using an europium shift reagent.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00180a014