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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Veröffentlicht in:	Journal of medicinal chemistry 1980-06, Vol.23 (6), p.653-657
Hauptverfasser:	Ashton, Michael J, Chapman, Robert F, Loveless, Anthony H
Format:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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